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 T64765 Target Info
Target Name Histamine H3 receptor (H3R)
Synonyms Histamine receptor 3; HH3R; GPCR97; G-protein coupled receptor 97; G protein-coupled receptor 97
Target Type Successful Target
Gene Name HRH3
Biochemical Class GPCR rhodopsin
UniProt ID
HRH3_HUMAN
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 Click to Show More [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 Click to Show More [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 Click to Show More [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 Click to Show More [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 Click to Show More [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 Click to Show More [1]
2 D0D8LP Drug Info pKi = 8.96 [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 Click to Show More [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. Click to Show More [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
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) 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]
References  Top
REF 1 Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017).Expert Opin Ther Pat. 2018 Mar;28(3):175-196.

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