| Patent(s) and the Corresponding Patented Drug(s) |
Top |
| World Intellectual Property Organization (WIPO) |
| Patent ID |
WO2014184327 |
| Title |
Novel (Cyano-Dimethyl-Methyl)-Isoxazoles and -[1,3,4]Thiadiazoles. |
| Abstract |
This invention relates to novel (Cyano-dimethyl-methyl)-isoxazolesand -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions. |
| Applicant(s) |
Boehringer Ingelheim International Gmbh |
| Representative Drug(s) |
D0X5ZS |
Drug Info
|
EC50 = 0.27 nM |
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[1] |
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2
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D0LN9D
|
Drug Info
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EC50 = 0.36 nM
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[1] |
| Patent ID |
WO2014097188 |
| Title |
Compounds of 2,3-Dihydro-4H-1,3-Benzoxazine-4-One, Method for Preparing Them and Pharmaceutical form Comprising Them. |
| Abstract |
The present invention concerns new compounds of 2,3-dihydro-4H-1,3- benzoxazine-4-one, a method for preparing the said compounds, a pharmaceutical form that contains the said compounds, and their use. In particular, the present invention concerns new compounds of 2,3-dihydro-4H-1,3-benzoxazine-4-one having a selective agonist action for the type 2 cannabinoid receptor (CB2), and their use in the treatment of pathologies associated with non-activation of this receptor, particularly chronic pain. |
| Applicant(s) |
C4T Scarl |
| Representative Drug(s) |
D01PUS |
Drug Info
|
EC50 = 110 nM |
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[1] |
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2
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D0OE0D
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Drug Info
|
EC50 = 190 nM
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[1] |
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3
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D00TIB
|
Drug Info
|
EC50 = 290 nM
|
[1] |
| Patent ID |
WO2014062965 |
| Title |
2-Cycloalkyl Resorcinol Cannabinergic Ligands. |
| Abstract |
The present invention relates to novel 2-cycloalkyl resorcinol compounds; to pharmaceutical compositions comprising the compounds; and to methods of preparing the compounds and uses thereof. The disclosed compounds can bind to and modulate the cannabinoid receptors and thus, they are specific ligands for these receptors. The invented compounds, when administered in a therapeutically effective amount to an individual or animal, results in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response may be useful to treat a number of physiological conditions. |
| Applicant(s) |
Northeastern University |
| Representative Drug(s) |
D0H0XC |
Drug Info
|
Ki = 0.8 nM |
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[1] |
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2
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D05CEL
|
Drug Info
|
Ki = 3 nM
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[1] |
| Patent ID |
WO2014039042 |
| Title |
Novel Cannabinergic Compounds and Uses Thereof. |
| Abstract |
Disclosed are compounds and compositions that modulate cannabinoid receptors, methods of modulating cannabinoid receptors, and methods of treating various disorders related to the modulation of cannabinoid receptors. This disclosure is directed to methods of treating cannabinoid dependence, neuropathy, inflammation, glaucoma, a neurodegenerative disorder, a motor function disorder, a gastrointestinal disorder, hypothermia, emesis, loss of appetite, or anorexia associated with AIDS. |
| Applicant(s) |
Northeastern University |
| Representative Drug(s) |
D09GJQ |
Drug Info
|
Ki = 0.5 nM |
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[1] |
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2
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D02TOI
|
Drug Info
|
Ki = 4.3 nM
|
[1] |
| Patent ID |
WO2013041859 |
| Title |
Cannabinoid-2-Receptor Agonists. |
| Abstract |
The present invention relates to cannabinnoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions). |
| Applicant(s) |
Isis Innovation Limited |
| Representative Drug(s) |
D0E6YT |
Drug Info
|
EC50 = 14 to 19 nM |
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[1] |
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2
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D07ULI
|
Drug Info
|
EC50 = 95 nM
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[1] |
| Patent ID |
WO2013005168 |
| Title |
Cannabinoid Receptor Modulators. |
| Abstract |
Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I). |
| Applicant(s) |
Lupin Limited |
| Representative Drug(s) |
D0D1TS |
Drug Info
|
EC50 < 10 nM |
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[1] |
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2
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D0TC7X
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Drug Info
|
EC50 < 10 nM
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[1] |
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3
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D0ZM1H
|
Drug Info
|
EC50 < 10 nM
|
[1] |
| Patent ID |
WO2012090179 |
| Title |
Isoquinoline Derivatives As Cannabinoid Receptor Modulators. |
| Abstract |
Compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I). |
| Applicant(s) |
Lupin Limited |
| Representative Drug(s) |
D0D1TS |
Drug Info
|
EC50 < 10 nM |
Click to Show More |
[1] |
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2
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D0TC7X
|
Drug Info
|
EC50 < 10 nM
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[1] |
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3
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D0ZM1H
|
Drug Info
|
EC50 < 10 nM
|
[1] |
| Patent ID |
WO2012090177 |
| Title |
Cannabinoid Receptor Modulators. |
| Abstract |
Compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I). |
| Applicant(s) |
Lupin Limited |
| Representative Drug(s) |
D0D1TS |
Drug Info
|
EC50 < 10 nM |
Click to Show More |
[1] |
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2
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D0TC7X
|
Drug Info
|
EC50 < 10 nM
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[1] |
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3
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D0ZM1H
|
Drug Info
|
EC50 < 10 nM
|
[1] |
| Patent ID |
WO2014134127 |
| Title |
Cannabinergic Nitrate Esters and Related Analogs. |
| Abstract |
The present technology relates to novel cannabinergic nitrate esters and related analogs, process of preparation, pharmaceutical compositions and their methods of use as medicaments, pharmacological tools and/or biomarkers. The novel cannabinergic nitrate ester compounds provide medicaments useful in treating a variety of diseases and medical disorders. |
| Applicant(s) |
Northeastern University |
| Representative Drug(s) |
D09WPA |
Drug Info
|
N.A. |
Click to Show More |
[1] |
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2
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D0RZ4M
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Drug Info
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N.A.
|
[1] |
| Patent ID |
WO2013025984 |
| Title |
Cannabinoid Receptor Treatments. |
| Abstract |
The present invention includes methods and compositions for treating a transplant recipient by administration of a CB2 receptor agonist either alone or in combination with one or more active pharmaceutical ingredients to block the rejection of foreign tissue and prolong grafted organs, tissues and cells. |
| Applicant(s) |
Temple University |
| Representative Drug(s) |
D0YZ8I |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2012012307 |
| Title |
Sulfonyl Compounds Which Modulate The Cb2 Receptor. |
| Abstract |
Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. |
| Applicant(s) |
Boehringer Ingelheim International Gmbh |
| Representative Drug(s) |
D0EX1T |
Drug Info
|
N.A. |
Click to Show More |
[1] |
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2
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D0O2TY
|
Drug Info
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N.A.
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[1] |
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3
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D0Q9TO
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
WO2016005419 |
| Title |
4-Oxo-1,4-Dihydroquinoline-3-Carboxamide As Selective Ligand for Cannabinoid Receptor 2 for Diagnosis and Therapy. |
| Abstract |
The present invention is directed to new compounds of formula (I) selectively binding the cannabinoid 2 receptor. In addition, the invention relates to the use of said compounds for determining cannabinoid receptor 2 (CB2)-selective receptor localization and density, preferably in the central nervous system (CNS), the peripheral nervous system (PNS), heart, liver, gastrointestinal tract, spleen, pancreas, kidney, testis, ovary and/or the prostate. Moreover, the invention pertains to the use of said compounds in the diagnosis, prophylaxis and/or therapy of CB2 receptor-related diseases. |
| Applicant(s) |
Eth Zuerich |
| Patent ID |
WO2014086805 |
| Title |
Pyridine-2-Amides Useful As Cb2 Agonists. |
| Abstract |
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 agonist and can be used as an active ingredient in a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0W9PY |
Drug Info
|
EC50 = 0.6 nM |
[1] |
| Patent ID |
WO2014013117 |
| Title |
Chromenopyrazole Diones As Cannabinoid Quinone Derivatives Having Anti-Tumour Activity. |
| Abstract |
The invention relates to a compound of general formula (I) or a tautomer, pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1 is independently selected from hydrogen or C1-C18 alkyl; R2 is independently selected from hydrogen, C1-C18 alkyl or C5-C18 aryl; and R3 is independently selected from hydrogen or C1-C5 alkyl. The invention also relates to the use of said compound of formula (I) for treating cancer or a malignant tumor, such as a blastoma, carcinoma, glioma, leukemia, lymphoma and melanoma, and to a method for treating said cancer or tumour, comprising the administration of a therapeutically effective quantity of the compound of formula (I). Consequently, the invention further relates to a pharmaceutical composition comprising a therapeutically effective quantity of a compound of general formula (I) and at least one pharmaceutically acceptable excipient. In addition, the invention relates to the method for producing said compound of general formula (I) by means of oxidation with [bis(trifluoroacetoxy)iode]benzene of the corresponding precursor phenolic derivative. |
| Applicant(s) |
Consejo Superior De Investigaciones Cient |
| Representative Drug(s) |
D07BFP |
Drug Info
|
IC50 = 15000 nM |
[1] |
| Patent ID |
WO2013087643 |
| Title |
1,3,5 -Triazine-2-Amine Derivatives, Preparation Thereof and Diagnostic and Therapeutic Use Thereof. |
| Abstract |
The present invention relates to compounds corresponding to formula (I) in which: - R1 represents a substituted phenyl; - R2 represents: - a substituted phenyl; - a heteroaromatic group, the said group being unsubstituted or substituted one or more times; - R3 represents a group Alk; - R4 represents a hydrogen atom or a (C1-C4)alkyl; - R5 represents a hydrogen atom, a (C3-C6)cycloalkyl or a (C1-C4)alkyl-O-Alk; - or alternatively R4 and R5, together with the nitrogen atom to which they are attached, constitute a heterocyclic radical chosen from: azetidin-1-yl, pyrrolidin-1-yl, piperid-1-yl, morpholin-4-yl; - R6 represents a group -COOAlk, a group -CONH 2 or a group -NHSO 2 Alk; - Alk represents a (C1-C4)alkyl, which is unsubstituted or substituted one or more times with a halogen atom; in the form of the base or of an acid-addition salt. Preparation process and diagnostic and therapeutic use. |
| Applicant(s) |
Sanofi |
| Representative Drug(s) |
D0HG0F |
Drug Info
|
IC50 = 0.4 nM |
[1] |
| Patent ID |
WO2012116276 |
| Title |
Crystalline forms and Processes for The Preparation of Condensed Azacycles ( Cannabinoid Receptor Modulators). |
| Abstract |
The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)- 1a,2,5.5a-tetrahydro- 1 H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)- 1 - hydroxymcthyl-2.2-dimcthyl-propyl)-amidc (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in t treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough; leukemia; lymphoma; CNS rumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis; and Parkinson's disease. |
| Applicant(s) |
Arena Pharmaceuticals, Inc |
| Representative Drug(s) |
D0SR5L |
Drug Info
|
EC50 = 5.4 nM |
[1] |
| Patent ID |
WO2014005968 |
| Title |
Novel Adamantyl Derivatives As Cannabinoid Receptor 2 Agonists. |
| Abstract |
The invention relates to a compound of formula (I), wherein i.a. A1is -CH2- or -C(O)-; one of R1 and R2 is hydrogen and the other one is -A2 -C(O)-R3; A2 is NH- or absent; and R3 is (A), (B) or (C) The compounds are preferential agonists of the cannabinoid receptor 2 (CB2) and can be used as medicaments for the treatment of pain, inflammation, ischemia, etc. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D0T9OL |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2013060751 |
| Title |
Novel Pyrazine Derivatives. |
| Abstract |
The invention relates to a compound of formula (I), wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Representative Drug(s) |
D08XES |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2012098090 |
| Title |
Cb2 Agonists for The Treatment and Prevention of Endometriosis. |
| Abstract |
The application relates to the treatment and prevention of endometriosis using pharmaceuticals comprising CB2 agonists. |
| Applicant(s) |
Bayer Intellectual Property Gmbh |
| Representative Drug(s) |
D03YAA |
Drug Info
|
N.A. |
[1] |
| Patent ID |
WO2015189523 |
| Title |
Derivatives of 2H-Pyrazolo[4,3-C]Quinolin-3(5H)-One and Use Thereof. |
| Abstract |
The invention relates to compounds of formula (I) or the pharmaceutically acceptable solvates thereof, as well as to the use thereof as a drug. |
| Applicant(s) |
Univ Lille Ii Droit & Sante |
| Patent ID |
WO2015150440 |
| Title |
Pyridine-2-Amides Useful As Cb2 Agonists. |
| Abstract |
The invention relates to a compound of formula (I) wherein A and R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2015150438 |
| Title |
5,6-Disubstituted Pyridine-2-Carboxamides As Cannabinoid Receptor Agonists. |
| Abstract |
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) are agonists of the Cannabinoid Receptor 2 and are therefore useful in the treatment of various diseases such as pain, atherosclerosis, inflammation etc. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2015140377 |
| Title |
Novel Chromene Quinones for Modulating Cannabinoid Receptors Cb2Having Antitumor Activity. |
| Abstract |
The present invention provides new cannabinoids derived from the chromenepyrazole-ortho-quinone represented by Formula (I), to pharmaceutical compositions containing said compounds, and to the use thereof as modulators of the cannabinoid receptor CB2, which are especially useful for treating cancer and malignant tumors. |
| Applicant(s) |
Consejo Superior Investigacion |
| Patent ID |
WO2015074137 |
| Title |
Compositions and Methods for Treatment of Ocular Inflammation and Pain. |
| Abstract |
The disclosure provides methods of treatment of ocular inflammation or neuropathic pain in a subject in need thereof, comprising administering to the subject in need thereof a CB2 target agent, a cannabimimetic agent (such as a non-psychotropic cannabimimetic agent) or a combination thereof. The agent is optionally a cannabinoid, such as a non-psychotropic cannabinoid or a synthetic cannabinoid. In certain embodiments, the non-psychotropic phytocannabinoid is gama-caryophyllene or cannabidiol [CBD] and the synthetic cannabinoid is HU-433, HU-308, or a modified CBD such as CBD-DMH. The disclosure also provides ocular pharmaceutical compositions containing the CB2 target agents or cannabimimetic agents such as non-psychotropic cannabimimetic agents described herein. |
| Applicant(s) |
Mary Lynch et al |
| Patent ID |
WO2014154612 |
| Title |
Novel Pyridine Derivatives. |
| Abstract |
The invention relates to a compound of formula (I); wherein A and R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2014086807 |
| Title |
Novel Pyrazine Derivatives As Cb2 Receptor Agonists. |
| Abstract |
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) is a CB2 receptor agonist for use in the treatment of several disorders, such as pain, atherosclerosis and glaucoma. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2014086806 |
| Title |
Pyridine-2-Amides Useful As Cb2 Agonists. |
| Abstract |
The invention relates to CB2 agonists of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2014086705 |
| Title |
Novel Pyridine Derivatives. |
| Abstract |
The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2014008567 |
| Title |
Modified Peptide, Cb Receptor Ligand, Kit, In Vitro Process for Evaluating Cb Receptor Bonds, Uses, Pharmaceutical Composition for Modulating Cb Receptor Activity. |
| Abstract |
The present invention discloses new, non-natural and modified peptides that act as ligands for cannabinoid receptors (CB), especially CB1 and/or CB2, and are useful as modulators of the activity of the latter; also described are a kit and an in vitro process for evaluating CB receptor bonds, uses and a pharmaceutical composition for modulating CB receptor activity. The invention covers the non-natural peptide of SEQ. ID. No: 1 and peptides having at least 70% similarity therewith, including, as particularly useful embodiments of the invention, the non-natural peptides of SEQ. ID. No: 2, SEQ. ID. No: 3, SEQ. ID. No: 4, SEQ. ID. No: 5 and SEQ. ID. No: 6. |
| Applicant(s) |
Proteimax Biotecnologia Ltda |
| Patent ID |
WO2012168350 |
| Title |
Pyridin- 2 -Amides Useful As Cb2 Agonists. |
| Abstract |
The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| Patent ID |
WO2008040649 |
| Title |
Pyrazine-2-Carboxamide Derivatives As Cb2 Receptor Modulators. |
| Abstract |
The present invention relates to compounds of the formula (I) wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB2 receptors. |
| Applicant(s) |
F. Hoffmann-La Roche Ag |
| United States Patent and Trademark Office (USPTO) |
| Patent ID |
US2013172388 |
| Title |
Novel Cb2 Inverse Agonists and Therapeutic Potential for Multiple Myeloma and Osteoporosis Bone Diseases. |
| Representative Drug(s) |
D0WJ3F |
Drug Info
|
Ki = 0.5 nM |
Click to Show More |
[1] |
|
2
|
D0FA2L
|
Drug Info
|
Ki = 19 nM
|
[1] |
|
3
|
D07IHT
|
Drug Info
|
Ki = 64 nM
|
[1] |
| Patent ID |
US2013143874 |
| Title |
Fused Ring Pyridine Compound. |
| Representative Drug(s) |
D03YWY |
Drug Info
|
N.A. |
Click to Show More |
[1] |
|
2
|
D0CR0Y
|
Drug Info
|
N.A.
|
[1] |
|
3
|
D0XG7K
|
Drug Info
|
N.A.
|
[1] |
| Patent ID |
US20130209483 |
| Title |
Cannabidinoid Derivatives As Therapeutic Agents. |
| Patent ID |
US2012039804 |
| Title |
Novel Tricyclic Modulators of Cannabinoid Receptors. |
| Representative Drug(s) |
D0GQ8W |
Drug Info
|
N.A. |
[1] |
| Patent ID |
US20120122917 |
| Title |
Method for Treatment of Hiv and Diseases of Immune Dysregulation. |
| European Patent Office (EPO) |
| Patent ID |
EP2966062 |
| Title |
Preparation of 4-Oxo-1,4-Dihydroquinoline-3-Carboxamides As Selective Ligands for Cannabinoid Receptor 2 for Diagnosis and Therapy. |
