Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T11754 Target Info
Target Name Fatty acid amide hydrolase (FAAH)
Synonyms Oleamidehydrolase; Anandamide amidohydrolase
Target Type Successful Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017087863
Title Pyrazole Compounds and Methods of Making and Using Same.
Abstract Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0S2JF Drug Info IC50 = 1000 to 10000 nM Click to Show More [1]
2 D0YM0G Drug Info IC50 = 1000 to 10000 nM [1]
Patent ID WO2016014975
Title Urea/Carbamates Faah Magl or Dual Faah/Magl Inhibitors and Uses Thereof.
Abstract Disclosed are compounds that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.
Applicant(s) Northeastern University
Representative Drug(s) D00IPI Drug Info IC50 = 0.01 to 0.1 nM Click to Show More [1]
2 D02ZUW Drug Info IC50 = 0.01 to 0.1 nM [1]
3 D09RGE Drug Info IC50 = 0.01 to 0.1 nM [1]
4 D08SMT Drug Info IC50 = 10 to 100 nM [1]
Patent ID WO2015179559
Title Pyrazole Compounds and Methods of Making and Using Same.
Abstract Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0LL0X Drug Info IC50 > 1000 nM Click to Show More [1]
2 D0O9DS Drug Info IC50 > 1000 nM [1]
3 D0X9GC Drug Info IC50 > 1000 nM [1]
Patent ID WO2012145737
Title Fatty Acid Amide Hydrolase Inhibitors for Treating Pain.
Abstract Compounds of Formula 1 are described herein. These compounds may be administered to a patient for treatment of suffering from pain or other FAAH mediated conditions.
Applicant(s) Allergan, Inc
Representative Drug(s) D0HZ7J Drug Info IC50 = 20 nM Click to Show More [2]
2 D05FQX Drug Info IC50 = 180 nM [2]
Patent ID WO2010141809
Title Aryl-Substituted Heterocyclic Urea Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D05MKN Drug Info IC50 = 3 nM Click to Show More [2]
2 D0J1KT Drug Info IC50 = 5 nM [2]
3 D0X7MV Drug Info IC50 = 50 nM [2]
Patent ID WO2010135360
Title Isoxazolines As Inhibitors of Fatty Acid Amide Hydrolase.
Abstract The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D0OI8P Drug Info Ki < 100 nM Click to Show More [2]
2 D0Q6GP Drug Info Ki < 100 nM [2]
3 D0R3JK Drug Info Ki < 100 nM [2]
4 D0X8VL Drug Info Ki < 100 nM [2]
Patent ID WO2010118155
Title Inhibitors of Fatty Acid Amide Hydrolase.
Abstract Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating FAAH-mediated disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D05HJF Drug Info Ki < 10 nM Click to Show More [2]
2 D07JMG Drug Info Ki < 10 nM [2]
Patent ID WO2009126691
Title Inhibitors of Fatty Acid Amide Hydrolase.
Abstract The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D0P3MU Drug Info Ki < 10 nM Click to Show More [2]
2 D0PU2A Drug Info Ki < 10 nM [2]
Patent ID WO2010007966
Title Azole Compound.
Applicant(s) Astellas Pharma Inc
Representative Drug(s) D00RKV Drug Info IC50human FAAH in a bladder-derived cell line (HTB-9) = 0.047 nM Click to Show More [2]
2 D0W9GL Drug Info IC50human FAAH in a bladder-derived cell line (HTB-9) = 0.077 nM [2]
Patent ID WO2012106569
Title Alpha-Ketoheterocycles and Methods of Making and Using.
Abstract Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.
Applicant(s) The Scripps Research Institute
Representative Drug(s) D0V1VT Drug Info Ki = 4 nM Click to Show More [2]
2 D03MCC Drug Info N.A. [2]
3 D0LZ8I Drug Info N.A. [2]
Patent ID WO2010141817
Title Heteroaryl-Substituted Spirocyclic Diamine Urea Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D09VEY Drug Info N.A. Click to Show More [2]
2 D0GI7I Drug Info N.A. [2]
Patent ID WO2010074588
Title Pharmaceutical Compounds.
Abstract The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
Applicant(s) Bial Portela & Ca Sa
Representative Drug(s) D02JER Drug Info N.A. Click to Show More [2]
2 D0U0QQ Drug Info N.A. [2]
Patent ID WO2010068453
Title Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D04USU Drug Info N.A. Click to Show More [2]
2 D0LB8Y Drug Info N.A. [2]
Patent ID WO2010068452
Title Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D04USU Drug Info N.A. Click to Show More [2]
2 D0LB8Y Drug Info N.A. [2]
Patent ID WO2010005572
Title Alpha-Keto Heterocycles As Faah Inhibitors.
Abstract The invention provides a series of -alphaketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.
Applicant(s) The Scripps Research Institute
Representative Drug(s) D0UD4X Drug Info N.A. Click to Show More [2]
2 D0WJ0T Drug Info N.A. [2]
Patent ID WO2009117444
Title Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase for Modulation of Cannabinoid Receptors.
Abstract Disclosed are compounds and compositions that inhibit the action of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGL), methods of inhibiting FAAH and MGL, methods of modulating cannabinoid receptors, and methods of treating various disorders related to modulation of cannabinoid receptors.
Applicant(s) Northeastern University
Representative Drug(s) D09AAB Drug Info N.A. Click to Show More [2]
2 D0RZ5O Drug Info N.A. [2]
Patent ID WO2012088469
Title Faah Inhibitors.
Abstract The present disclosure relates to compounds useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. Compounds of the invention are described in Table 1.
Applicant(s) Ironwood Pharmaceuticals, Inc
Representative Drug(s) D00PFD Drug Info IC50 = 4 nM [2]
Patent ID WO2011139951
Title Modulators of Fatty Acid Amide Hydrolase.
Abstract 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). A method of synthesizing 4- (2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4- chloro-pyridin-3-yl)-amide is also disclosed.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0IA7Z Drug Info IC50 = 75 nM [2]
Patent ID WO2011071996
Title Faah Inhibitors.
Abstract The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders.
Applicant(s) Ironwood Pharmaceuticals, Inc
Representative Drug(s) D00PFD Drug Info IC50 = 4 nM [2]
Patent ID WO2011022348
Title Ethylene Diamine Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0M1ND Drug Info IC50 = 20 nM [2]
Patent ID WO2010118159
Title Inhibitors of Fatty Acid Amide Hydrolase.
Abstract Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, R4, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating an FAAH-mediated disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D0H8LZ Drug Info Ki < 100 nM [2]
Patent ID WO2010058318
Title 1-Oxa-8-Azaspiro [4, 5 ] Decane- 8 -Carboxamide Compounds As Faah Inhibitors.
Abstract Provided herein are 1-oxa-8-azaspiro[4.5]decane-8-carboxamide compounds of formula I wherein Ar1, Ar2, R1, R2, R3 and R4 are as defined herein and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
Applicant(s) Pfizer Inc
Representative Drug(s) D0DD7K Drug Info kinact/Ki = 30800 M-1s-1 [2]
Patent ID WO2010049841
Title 7-Azaspiro [3.5] Nonane-7-Carboxamide Compounds As Modulators of Fatty Acid Amide Hydrolase.
Abstract Provided herein are 7-azaspiro[3.5]nonane-7-carboxamide compounds and the pharmaceutically acceptable salts of such compounds useful in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, conditions including including acute pain, chronic pain, neuropathic pain, nociceptive pain, inflammatory pain, cancer and cancer pain, fibromyalgia, rheumatoid arthritis, inflammatory bowel disease, lupus, diabetes, allergic asthma, vascular inflammation, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
Applicant(s) Pfizer Inc
Representative Drug(s) D0XQ4B Drug Info kinact/Ki = 21700 M-1s-1 [2]
Patent ID WO2010039186
Title Benzoxazoles Useful As Faah Modulators and Uses Thereof.
Abstract Compounds are disclosed that have formula I: wherein X, R1, R2, R3, R4 and n are as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, anxiety, depression, inflammation, cognitive disorders, weight and eating disorders, Parkinson's disease, Alzheimer's disease, spasticity, addiction, glaucoma, and others.
Applicant(s) Renovis, Inc
Representative Drug(s) D05RQF Drug Info IC50 = 1.3 nM [2]
Patent ID WO2009127949
Title 4- [3- (Aryloxy) Benzylidene] -3-Methyl Piperidine Aryl Carboxamide Compounds Useful As Faah Inhibitors.
Abstract The present invention relates to compounds of Formula (I), wherein Ar is optionally substituted phenyl or heteroaryl and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
Applicant(s) Pfizer Inc
Representative Drug(s) D0K2WP Drug Info kinact/Ki = 40000 M-1s-1 [2]
Patent ID WO2009127948
Title 4- [3- (Aryloxy) Benzylidene] -3-Methyl Piperidine 5-Membered Aryl Carboxamide Compounds Useful As Faah Inhibitors.
Abstract The present invention relates to compounds of Formula (I), wherein Ar is a 5-membered heteroaryl moiety and X, Y and Z are independently N or CH; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity.
Applicant(s) Pfizer Inc
Representative Drug(s) D07MIY Drug Info kinact/Ki = 40000 M-1s-1 [2]
Patent ID WO2009127944
Title Ether Benzylidene Piperidine Aryl Carboxamide Compounds Useful As Faah Inhibitors.
Abstract The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
Applicant(s) Pfizer Inc
Representative Drug(s) D02ZPG Drug Info kinact/Ki = 40000 M-1s-1 [2]
Patent ID WO2009109743
Title Azetidine Derivatives.
Abstract Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.
Applicant(s) Vernalis (R & D) Ltd
Representative Drug(s) D0BN7S Drug Info IC50 = 38 nM [2]
Patent ID WO2009105220
Title Aryl-Hydroxyethylamino-Pyrimidines and Triazines As Modulators of Fatty Acid Amide Hydrolase.
Abstract Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D01THA Drug Info IC50 = 1 nM [2]
Patent ID WO2009011904
Title Compounds Useful As Faah Modulators and Uses Thereof.
Abstract Compounds are disclosed that have formula (I): where A, B, L1, X, W, Y, R1, R3, and nlare as defined herein. The compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, anxiety, depression, inflammation, cognitive disorders, weight and eating disorders, Parkinson's disease, Alzheimer's disease, spasticity, addiction, glaucoma, and others.
Applicant(s) Renovis, Inc
Representative Drug(s) D05KXF Drug Info IC50 < 100 nM [2]
Patent ID WO2015003002
Title Pyrrolo-Pyrrole Carbamate and Related organic Compounds, Pharmaceutical Compositions, and Medical Uses Thereof.
Abstract The invention provides pyrrolo-pyrrole carbamate and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., solid tumor cancer, obesity, Down's syndrome, Alzheimer's disease, or pain, in a patient. The octahydropyrrolo pyrrole carbamates could be derived from hexafluoroisopropanol, ,-disuccinimide and such. The activity of carbamates in MAGL, FAAH, and ABHD6 assays are also described.
Applicant(s) Abide Therapeutics, Inc
Representative Drug(s) D0GT0I Drug Info N.A. [1]
Patent ID WO2014004676
Title Use of Faah Inhibitors As Neuroprotective Agents In The Cns.
Abstract The present disclosure relates to methods of using a fatty acid amide hydrolase (FAAH) inhibitor of Formula I alone or in combination with one or more additional therapeutic agents for the treatment or prevention of neuronal injury or neurodegeneration in a patient in need thereof.
Applicant(s) Ironwood Pharmaceuticals, Inc
Representative Drug(s) D04VYE Drug Info N.A. [2]
Patent ID WO2012015704
Title Peripherally Restricted Faah Inhibitors.
Abstract Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R1 is a polar group. In some embodiments, R1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R2 and R3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.
Applicant(s) The Regents of the University of California
Representative Drug(s) D0LR7Z Drug Info N.A. [2]
Patent ID WO2011140164
Title Aza-Indole Derivatives Useful As Modulators of Faah.
Abstract The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D05IZN Drug Info N.A. [2]
Patent ID WO2011126960
Title Oxazole Derivatives Useful As Modulators of Faah.
Abstract The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D0P2AB Drug Info N.A. [2]
Patent ID WO2011097233
Title Fatty Acid Amide Hydrolase Inhibitors.
Abstract The present invention provides fatty acid amide hydrolase inhibitors, solid forms thereof, compositions thereof, and methods of making and using the same.
Applicant(s) Infinity Pharmaceuticals, Inc
Representative Drug(s) D02LJQ Drug Info N.A. [2]
Patent ID WO2011085216
Title Use of Faah Inhibitors for Treating Parkinson'S Disease and Restless Legs Syndrome.
Abstract The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.
Applicant(s) Ironwood Pharmaceuticals, Inc
Representative Drug(s) D04VYE Drug Info N.A. [2]
Patent ID WO2010105930
Title Carbamate Derivatives In Particular for The Treatment of Neurological Disorders.
Abstract The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.
Applicant(s) Sigma-Tau Industrie Farmaceutiche Riunite Spa
Representative Drug(s) D0KE8U Drug Info N.A. [2]
Patent ID WO2010101724
Title Imidazole Derivatives Useful As Modulators of Faah and As Faah Imaging Agents.
Abstract The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D05LBM Drug Info N.A. [2]
Patent ID WO2009152025
Title Imidazole Derivatives Useful As Inhibitors of Faah.
Abstract The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D00ZGG Drug Info N.A. [2]
Patent ID WO2009151991
Title Pyrazole Derivatives Useful As Inhibitors of Faah.
Abstract The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease.
Applicant(s) Merck Sharp & Dohme Corp
Representative Drug(s) D09SWG Drug Info N.A. [2]
Patent ID WO2009109504
Title Enol Carbamate Derivatives As Modulators of Fatty Acid Amide Hydrolase.
Abstract The invention provides novel enol carbamate derivatives of formula (I) for inhibiting Fatty Acid Amide Hydrolase (FAAH), compositions that include such compounds as well as methods of treating diseases of energy metabolism, central nervous system disorders, cardiovascular and respiratory disorders, retinopathy, cancer, gastrointestinal and liver disorders and/or musculoskeletal disorders. The compounds of the present invention proved particularly efficacious in animal models of anxiety and pain.
Applicant(s) Sigma-Tau Industrie Farmaceutiche Riunite Spa
Representative Drug(s) D07VNW Drug Info N.A. [2]
Patent ID WO2009084970
Title 5-O-Substituted 3-N-Phenyl-1,3,4-Oxadiazolones for Medical Use.
Abstract The present invention relates to compounds having a 5-O-substituted 3-N-phenyl-1,3,4-oxadiazolone structural unit which have unexpectedly high level of inhibition of FAAH (fatty acid amide hydrolase). (I).
Applicant(s) Bial-Portela & Ca., Sa
Representative Drug(s) D0B7CW Drug Info N.A. [2]
Patent ID WO2006054652
Title Amide Compound.
Abstract An FAAH inhibitor; and a preventive/therapeutic agent for cerebrovascular disorders and a preventive/therapeutic agent for sleep disorders which each contains the inhibitor. The FAAH inhibitor is a compound represented by the formula (I0): (wherein Z represents oxygen or sulfur; R1 represents optionally substituted aryl or an optionally substituted heterocyclic group; R1a represents hydrogen, an optionally substituted hydrocarbon group, hydroxy, etc.; R2 represents optionally substituted piperidine-1,4-diyl or optionally substituted piperazine-1,4-diyl; R3 represents an optionally substituted group formed by removing two hydrogen atoms from a 5-membered aromatic heterocycle having 1-3 heteroatoms selected among nitrogen, oxygen, and sulfur, or represents -CO-, etc.; and R4 represents an optionally substituted hydrocarbon group or optionally substituted heterocyclic group) or a salt of the compound.
Applicant(s) Takeda Pharmaceutical Company Limited
Representative Drug(s) D08JES Drug Info N.A. [2]
Patent ID WO2010151160
Title O-Substituted 3-N-Heteroaryl-1,3,4-Oxadiazolones for Medical Use.
Abstract The present invention relates to compound of formula (I), wherein A represents a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, which is optionally substituted, and to a stereoisomer, pharmaceutically acceptable salt or ester, or prodrug thereof.
Applicant(s) Bial Portela & Ca Sa
Patent ID WO2010074587
Title 5-O-Substituted 3-N-Aryl-1,3,4-Oxadiazolones for Medical Use.
Abstract The present invention relates to a compound of formula (I), wherein A represents an optionally substituted phenyl or a 5- or 6-membered heteroaromatic ring system containing up to 4 heteroatoms selected from O, S and N, B represents a single bond, O, S or NR1, wherein R1 is selected from hydrogen or a C1-C6-alkyl group; L represents a linker; C represents an amino moiety; n represents 0 or 1; m represents 0, 1, 2, 3, 4, 5 or 6; X represents O or S; and Y represents hydrogen or an optionally substituted carbon moiety; and to stereoisomers, pharmaceutically acceptable salts or esters, or prodrugs thereof. The compounds of the invention are potent FAAH inhibitors.
Applicant(s) Bial-Portela & Ca., Sa
Patent ID WO2008063300
Title Boronic Acids and Esters As Inhibitors of Fatty Acid Amide Hydrolase.
Abstract The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
Applicant(s) Infinity Pharmaceuticals, Inc
United States Patent and Trademark Office (USPTO)
Patent ID US2009062294
Title Heteroaryl-Substituted Urea Modulators of Fatty Acid Amide Hydrolase.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D04USU Drug Info N.A. Click to Show More [2]
2 D0LB8Y Drug Info N.A. [2]
Patent ID US20100292266
Title Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase.
Applicant(s) Apodaca Richard et al
Representative Drug(s) D0Z5MJ Drug Info IC50 = 2 nM [2]
Patent ID US20090111778
Title 2-Keto-Oxazoles As Modulators of Fatty Acid Amide Hydrolase.
Applicant(s) Janssen Pharmaceutica Nv
Representative Drug(s) D0IK9V Drug Info IC50 = 0.4 nM [2]
References  Top
REF 1 A patent review of Monoacylglycerol Lipase (MAGL) inhibitors (2013-2017).Expert Opin Ther Pat. 2017 Dec;27(12):1341-1351.
REF 2 Fatty acid amide hydrolase inhibitors: a patent review (2009-2014).Expert Opin Ther Pat. 2015;25(11):1247-66.

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