Patent(s) and the Corresponding Patented Drug(s) |
Top |
World Intellectual Property Organization (WIPO) |
Patent ID |
WO2015069110 |
Title |
Multiple D2 A(Nta)Gonists/H3 Antagonists for Treatment of Cns-Related Disorders. |
Abstract |
The present invention relates to compounds compound according to Formula (III); and pharmaceutically acceptable salts, hydrates and solvates thereof. These compounds have D2receptor antagonist/(partial) agonist effects and H3antagonistic effects, pharmaceutical compositions thereof, and methods of using them for application in the prophylaxis or treatment of CNS disorders. |
Applicant(s) |
Aapa Bv |
Representative Drug(s) |
D0RP1J |
Drug Info
|
IC50 = 0.33 nM |
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[1] |
2
|
D0SO4O
|
Drug Info
|
IC50 = 2.6 nM
|
[1] |
3
|
D05KKZ
|
Drug Info
|
IC50 = 3 nM
|
[1] |
4
|
D0N8CU
|
Drug Info
|
IC50 = 5 nM
|
[1] |
5
|
D0BZ0N
|
Drug Info
|
IC50 = 63 nM
|
[1] |
6
|
D0D5AH
|
Drug Info
|
IC50 = 513 nM
|
[1] |
Patent ID |
WO2014013469 |
Title |
Carbamate/Urea Derivatives. |
Abstract |
The invention relates to compound of the formula (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it. |
Applicant(s) |
Novartis Ag |
Representative Drug(s) |
D0KP0I |
Drug Info
|
Ki < 10 nM |
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[1] |
2
|
D0R0GY
|
Drug Info
|
Ki < 10 nM
|
[1] |
Patent ID |
WO2013107336 |
Title |
Therapeutic Uses. |
Abstract |
This invention relates to novel therapeutic uses for compounds which are inverse agonists of the H3 receptor. In particular this invention relates to therapeutic use of these compounds in the treatment of Multiple Sclerosis. |
Applicant(s) |
Glaxosmithkline Intellectual Property Development Limited |
Representative Drug(s) |
D0RV0O |
Drug Info
|
pKi(hH3R,native) = 9.92; pKi(rH3R,native) = 9.44 |
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[1] |
2
|
D0TE2D
|
Drug Info
|
ED50 = 25 nM
|
[1] |
3
|
D0EP0M
|
Drug Info
|
ED50 = 31 nM; pKi >= 9
|
[1] |
Patent ID |
WO2013050987 |
Title |
Carbamate/ Urea Derivatives Containing Piperidin and Piperazin Rings As H3 Receptor Inhibitors. |
Abstract |
The invention relates to compound of the formula I (I) or a salt thereof, wherein the substituents are as defined in the specification; to its preparation and to medicaments comprising it for traeting diseases connected to tehinhibition of H3 receptor. |
Applicant(s) |
Novartis Ag |
Representative Drug(s) |
D01EHZ |
Drug Info
|
Ki < 10 nM |
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[1] |
2
|
D01IJA
|
Drug Info
|
Ki < 10 nM
|
[1] |
3
|
D0FJ3N
|
Drug Info
|
Ki < 10 nM
|
[1] |
4
|
D0H7OC
|
Drug Info
|
Ki < 10 nM
|
[1] |
5
|
D0KP0I
|
Drug Info
|
Ki < 10 nM
|
[1] |
6
|
D0R0GY
|
Drug Info
|
Ki < 10 nM
|
[1] |
7
|
D0TM4R
|
Drug Info
|
Ki < 10 nM
|
[1] |
Patent ID |
WO2014030170 |
Title |
Acrylamide Compounds As Histamine H3 Receptor Ligands. |
Abstract |
The present invention relates to novel acrylamide compounds of formula (I), and their pharmaceutically acceptable salts and process of their preparation. (The chemical formula should be inserted here.) The compounds of formula (I) are useful in the treatment of various disorders that related to Histamine H3 receptors. |
Applicant(s) |
Suven Life Sciences Limited |
Representative Drug(s) |
D08EYN |
Drug Info
|
Ki = 1.32 nM |
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[1] |
2
|
D03EHI
|
Drug Info
|
Ki = 3.43 nM
|
[1] |
3
|
D0DS9D
|
Drug Info
|
Ki = 77.18 nM
|
[1] |
4
|
D0K9MH
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2013076590 |
Title |
Benzothiazine Compounds As H3 Receptor Ligands. |
Abstract |
The present invention provides benzothiazine derivative of formula (I), useful in the treatment of CNS disorders including cognitive disorders, ADHD, narcolepsy, pain, dementias, schizophrenia as well as obesity and sleep disorders. Pharmacological profile of these compounds includes high affinity binding with H3 receptor along with favourable selectivity profile for other aminergic receptors. The present invention also includes 'their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions. |
Applicant(s) |
Oxygen Healthcare Research Pvt. Ltd |
Representative Drug(s) |
D04DUF |
Drug Info
|
pKi = 5.4 |
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[1] |
2
|
D0D8LP
|
Drug Info
|
pKi = 8.96
|
[1] |
3
|
D0ZC7W
|
Drug Info
|
pKi = 9.4
|
[1] |
4
|
D0W3RA
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2013027001 |
Title |
Compounds and Their Use To Treat Histamine H3 Related Disorders. |
Abstract |
The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, m, n, p, q, Q1, Q2, Q3, Q4, Q5, Q6, X1, X2, X3, X4, A1 and L1, are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. |
Applicant(s) |
Takeda Pharmaceutical Company Limited |
Representative Drug(s) |
D09QCB |
Drug Info
|
IC50 <= 10 nM |
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[1] |
2
|
D09STY
|
Drug Info
|
IC50 <= 10 nM
|
[1] |
3
|
D09AQZ
|
Drug Info
|
IC50 <= 100 nM
|
[1] |
4
|
D0A8VU
|
Drug Info
|
IC50 >= 150 nM
|
[1] |
5
|
D0CE7X
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2014136075 |
Title |
H3 Antagonists Containing Phenoxypiperidine Core Structure. |
Abstract |
The present invention relates to new histamine H 3(H 3) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/ or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H 3receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor. |
Applicant(s) |
Richter Gedeon Nyrt |
Representative Drug(s) |
D0A2ZO |
Drug Info
|
N.A. |
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[1] |
2
|
D0QV0P
|
Drug Info
|
N.A.
|
[1] |
Patent ID |
WO2016027275 |
Title |
Process for Large Scale Production of N-[4-(1- Cyclobutyl Piperidin-4-Yloxy) Phenyl]-2-(Morpholin-4-Yl) Acet Amide Dihydrochloride. |
Abstract |
The present, invention relates to a process for large scale production of N- [4-(1-Cyclobutyl piperidin-4-yloxy) phenyl] -2-(morpholin-4-yl) acetamide dihydrochloride of formula (I). |
Applicant(s) |
Suven Life Sciences Limited |
Patent ID |
WO2014159776 |
Title |
Solid State forms of 6-[4-[3-(R)-2-Methylpyrrolidine-1-Yl)-Propoxy]Phenyl]2H-Pyridazine-3-One Hydrochloride. |
Abstract |
Solid state forms of the compound 6-[ 4- 13 -((R )- 2-mefhy lpyrrolidine-1 - yl )-propoxy | phenyl ] 2H-pyridazine-3-one hydrochloride (Compound 1), processes for preparing the solid state forms, an. |
Applicant(s) |
Cephalon, Inc |
Representative Drug(s) |
D0GB3P |
Drug Info
|
Ki = 2 nM |
[1] |
Patent ID |
WO2014110103 |
Title |
Biphenyl-Ethyl-Pyrrolidine Derivatives As Histamine H3 Receptor Modulators for The Treatment of Cognitive Disorders. |
Abstract |
The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor (Ia). Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders. |
Applicant(s) |
Arena Pharmaceuticals, Inc |
Representative Drug(s) |
D0AX9N |
Drug Info
|
IC50 <= 35000 nM |
[1] |
Patent ID |
WO2014028322 |
Title |
Modulators of The Histamine H3 Receptor and The Treatment of Disorders Related Thereto. |
Abstract |
The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders. |
Applicant(s) |
Arena Pharmaceuticals, Inc |
Representative Drug(s) |
D02SKQ |
Drug Info
|
IC50 <= 7 nM |
[1] |
Patent ID |
WO2013150150 |
Title |
An H3 Receptor Antagonist for Use In The Treatment of Alzheimer'S Disease. |
Abstract |
This disclosure relates to methods of using 2-(cyclohexylmethyl)-N-{2-[(2S)-1- methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide in a disease modifying therapy of Alzheimer's disease, other tauopathies and related neurodegenerative diseases. |
Applicant(s) |
Sanofi |
Representative Drug(s) |
D0F8PG |
Drug Info
|
Ki = 0.06 nM |
[1] |
Patent ID |
WO2013027073 |
Title |
Histamine H3 Antagonist Steroidal Carboxamides. |
Abstract |
The present invention relates to new histamine-3 (H3) receptor subtype preferring ligands of formula (I) (as defined in the claims) and/or geometric isomers and/or stereoisomers and/or diastereoisomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions comprising such compounds and the use of these compounds in methods for treating or preventing of conditions which require modulation of histamine-3 (H3) receptors. The invention also provides a method for manufacturing medicaments useful in the treatment or prevention of such conditions. |
Applicant(s) |
Richter Gedeon Nyrt |
Representative Drug(s) |
D0V2WE |
Drug Info
|
Ki < 10 nM |
[1] |
Patent ID |
WO2010151611 |
Title |
Novel Fumarate Salts of A Histamine H3 Receptor Antagonist. |
Abstract |
The disclosure relates to fumarate salts of 2-(cyclohexylmethyl)-N-{2-[(2S)-1-methylpyrrolidin-2-yl]ethyl}-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide, to pharmaceutical compositions thereof, processes for making the same, and methods of use thereof. |
Applicant(s) |
Sanofi |
Representative Drug(s) |
D0F8PG |
Drug Info
|
Ki = 0.06 nM |
[1] |
Patent ID |
WO2008013838 |
Title |
Pyridizinone Derivatives. |
Abstract |
The present invention provides compounds of formula (I*): their use as H3 inhibitors, processes for their preparation, and pharmaceutical compositions thereof. |
Applicant(s) |
Cephalon, Inc |
Representative Drug(s) |
D0GB3P |
Drug Info
|
Ki = 2 nM |
[1] |
Patent ID |
WO2005118547 |
Title |
Tetrahydroisoquinoline Sulfonamide Derivatives, The Preparation Thereof, and The Use of The Same In Therapeutics. |
Abstract |
The invention relates to a compound of formula (I) wherein n can represent a value between 1 and 6; -(C)n- represents a C1-6 alkylidene group, optionally substituted by between 1 and 4 substituents; R1 represents a hydrogen atom, or a C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl or C3-6 cycloalkyl group optionally substituted by between 1 and 4 substituents; and B represents NR3R4, R3 and R4 independently representing a C1-6 alkyl group or a hydrogen atom, or together representing a C1-6 alkylidene group, a C2-8 alkenylidene group, a C1-3 alkylidene-O-C1-3 alkylidene group, or a C1-3 alkylidene-N(R5)-C1-3 alkylidene group wherein R5 represents a hydrogen atom, or a C1-3 alkyl or C1-6 alkylcarbonyl group, said C1-3 alkyl and C1-6 alkylcarbonyl groups being substitutable, or an aminocycle which is linked by a carbon to the group -NR1-(C)n-, such as aziridine, azetidine, pyrrolidine, piperidine or morpholine, the groups R3, R4, the aminocycle, and the nitrogen atom being optionally substituted. The invention can be applied to therapeutics. |
Applicant(s) |
Sanofi-Aventis |
Representative Drug(s) |
D0F8PG |
Drug Info
|
Ki = 0.06 nM |
[1] |
Patent ID |
WO2005014571 |
Title |
Substituted Piperidines As Histamine H3 Receptor Ligands. |
Abstract |
The present invention relates to novel piperidine ether derivatives having affinity for the histamine H3 receptor, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. |
Applicant(s) |
GLAXO GROUP LIMITED BAILEY, James, Matthew BRUTON, Gordon HUXLEY, Anthony MILNER, Peter, Henry ORLEK, Barry, Sidney |
Representative Drug(s) |
D0EP0M |
Drug Info
|
ED50 = 31 nM; pKi >= 9 |
[1] |
Patent ID |
WO2004056369 |
Title |
Benzo ...D!Azepine Derivatives for The Treatment of Neurological Disorders. |
Abstract |
The present invention relates to benzazepine derivatives of formula ( I ) wherein: R1 represents -C3-7 cycloalkyl optionally substituted by C1-3 alkyl; having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. |
Applicant(s) |
Glaxo Group Limited |
Representative Drug(s) |
D0RV0O |
Drug Info
|
pKi(hH3R,native) = 9.92; pKi(rH3R,native) = 9.44 |
[1] |
Patent ID |
WO2014147353 |
Title |
Use of 4-{3-[Cis-Hexahydrocyclopenta[C]Pyrrole-2(1H)-Yl]Propoxy}Benzamide for Treating Neuropathic Pain. |
Abstract |
The invention relates to the use of 4-{3-[cis-hexahydrocyclopenta[C]pyrrole-2(1H)-yl]propoxy}benzamide of formula (I): or of the acid or base addition salts thereof, which is pharmaceutically acceptable for treating neuropathic pain as well as cognitive disorders, depression and anxiety associated with said pains. |
Applicant(s) |
Les Laboratoires Servier |
Representative Drug(s) |
D0B2NV |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2012168657 |
Title |
Process for Synthesis and Crystalline form of 4-{3-[Cis-Hexahydrocyclopenta[C]Pyrrol-2(1H)-Yl]Propoxy}Benzamide Hydrochloride. |
Abstract |
Industrial process for synthesis and crystalline form I of the compound of formula (I): and the crystalline form I of the associated free base. Medicaments. |
Applicant(s) |
Les Laboratoires Servier |
Representative Drug(s) |
D0B2NV |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2012150412 |
Title |
Novel Combination of 4-(3-[Cis-Hexahydrocyclopenta[C]Pyrrol-2(1H)-Yl]Propoxy)Benzamide and An Acetylcholinesterase Inhibitor, and Pharmaceutical Compositions Containing Same. |
Abstract |
The invention relates to a combination of the 4-(3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy)benzamide of formula (I), or of one of the addition salts thereof, with a pharmaceutically acceptable acid or base and an acetylcholinesterase inhibitor. The invention can be used in the field of drugs. |
Applicant(s) |
Les Laboratoires Servier |
Representative Drug(s) |
D0B2NV |
Drug Info
|
N.A. |
[1] |
Patent ID |
WO2005089747 |
Title |
Novel Azabicyclic Derivatives, Preparation Method Thereof and Pharmaceutical Compositions Containing Same. |
Abstract |
The invention relates to compounds having general formula (I), the enantiomers and diastereoisomers thereof, as well as their addition salts with one or more acids or one or more pharmaceutically-acceptable bases. The inventive compounds are of particular interest for their interaction with central histaminergic systems. |
Applicant(s) |
Les Laboratoires Servier |
Representative Drug(s) |
D0B2NV |
Drug Info
|
N.A. |
[1] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US20160237052 |
Title |
Histamine H3 Receptor Antagonists. |
Representative Drug(s) |
D0VX6P |
Drug Info
|
Ki = 20 nM |
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[1] |
2
|
D0FA3G
|
Drug Info
|
Ki = 155 nM
|
[1] |
Patent ID |
US20130040940 |
Title |
Mercaptoamidine Derivatives and Methods of Use. |
Representative Drug(s) |
D0SZ1L |
Drug Info
|
Ki = 0.02 nM |
Click to Show More |
[1] |
2
|
D0F7UB
|
Drug Info
|
Ki = 0.05 nM
|
[1] |