RU2003115490A - AMIDIC DERIVATIVES AS AN NMDA RECEPTOR ANTAGONISTS - Google Patents
AMIDIC DERIVATIVES AS AN NMDA RECEPTOR ANTAGONISTSInfo
- Publication number
- RU2003115490A RU2003115490A RU2003115490/04A RU2003115490A RU2003115490A RU 2003115490 A RU2003115490 A RU 2003115490A RU 2003115490/04 A RU2003115490/04 A RU 2003115490/04A RU 2003115490 A RU2003115490 A RU 2003115490A RU 2003115490 A RU2003115490 A RU 2003115490A
- Authority
- RU
- Russia
- Prior art keywords
- formula
- values
- same
- acids
- acid
- Prior art date
Links
- 108090001041 N-methyl-D-aspartate receptors Proteins 0.000 title claims 2
- 239000002464 receptor antagonist Substances 0.000 title claims 2
- 102000004868 N-methyl-D-aspartate receptors Human genes 0.000 title 1
- 239000002253 acid Substances 0.000 claims 13
- 150000001408 amides Chemical class 0.000 claims 9
- -1 hydroxydiphenylmethyl Chemical group 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 7
- 150000007513 acids Chemical class 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 238000007112 amidation reaction Methods 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N Imidazole Chemical compound C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 2
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 230000003042 antagnostic Effects 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 150000001735 carboxylic acids Chemical class 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- QNLOWBMKUIXCOW-UHFFFAOYSA-N indol-2-one Chemical compound C1=CC=CC2=NC(=O)C=C21 QNLOWBMKUIXCOW-UHFFFAOYSA-N 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 2
- 108010038912 retinoid X receptors Proteins 0.000 claims 2
- MECHQXUWFDXHDS-UHFFFAOYSA-N (4-benzylpiperidin-1-yl)-(3,6-dihydropyrrolo[3,2-e]benzimidazol-7-yl)methanone Chemical compound C=1C(C=2NC=NC=2C=C2)=C2NC=1C(=O)N(CC1)CCC1CC1=CC=CC=C1 MECHQXUWFDXHDS-UHFFFAOYSA-N 0.000 claims 1
- XISPDFMAOWZEQG-UHFFFAOYSA-N 4H-1,4-oxazin-3-one Chemical compound O=C1COC=CN1 XISPDFMAOWZEQG-UHFFFAOYSA-N 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 108009000433 Amyotrophic lateral sclerosis (ALS) Proteins 0.000 claims 1
- 206010002855 Anxiety Diseases 0.000 claims 1
- 206010057666 Anxiety disease Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 206010060945 Bacterial infection Diseases 0.000 claims 1
- 206010058019 Cancer pain Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012335 Dependence Diseases 0.000 claims 1
- 206010013754 Drug withdrawal syndrome Diseases 0.000 claims 1
- 206010015037 Epilepsy Diseases 0.000 claims 1
- 102100012245 GRIN2B Human genes 0.000 claims 1
- 208000004559 Hearing Loss Diseases 0.000 claims 1
- 206010011879 Hearing loss Diseases 0.000 claims 1
- 201000001971 Huntington's disease Diseases 0.000 claims 1
- 206010020993 Hypoglycaemia Diseases 0.000 claims 1
- 208000002780 Macular Degeneration Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010027599 Migraine Diseases 0.000 claims 1
- 208000008085 Migraine Disorders Diseases 0.000 claims 1
- 208000007101 Muscle Cramp Diseases 0.000 claims 1
- 206010028334 Muscle spasms Diseases 0.000 claims 1
- 102000014649 NMDA glutamate receptor activity proteins Human genes 0.000 claims 1
- 208000004296 Neuralgia Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 206010061920 Psychotic disease Diseases 0.000 claims 1
- 206010038910 Retinitis Diseases 0.000 claims 1
- 208000008513 Spinal Cord Injury Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 208000005765 Traumatic Brain Injury Diseases 0.000 claims 1
- 210000003932 Urinary Bladder Anatomy 0.000 claims 1
- 206010047461 Viral infection Diseases 0.000 claims 1
- 208000001756 Virus Disease Diseases 0.000 claims 1
- UQYZFNUUOSSNKT-UHFFFAOYSA-N [benzotriazol-1-yloxy(dimethylamino)methylidene]-dimethylazanium;hexafluorophosphate Chemical compound F[P-](F)(F)(F)(F)F.C1=CC=C2N(OC(N(C)C)=[N+](C)C)N=NC2=C1 UQYZFNUUOSSNKT-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229930002945 all-trans-retinaldehyde Natural products 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 239000002647 aminoglycoside antibiotic agent Substances 0.000 claims 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 230000001580 bacterial Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000006474 brain ischemia Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 238000005755 formation reaction Methods 0.000 claims 1
- 150000004820 halides Chemical class 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 125000005842 heteroatoms Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 230000002218 hypoglycaemic Effects 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 125000004430 oxygen atoms Chemical group O* 0.000 claims 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000002980 postoperative Effects 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- KAESVJOAVNADME-UHFFFAOYSA-N pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 1
- 230000002207 retinal Effects 0.000 claims 1
- 235000020945 retinal Nutrition 0.000 claims 1
- 239000011604 retinal Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 230000017613 viral reproduction Effects 0.000 claims 1
Claims (11)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
HUP0004123 | 2000-10-24 | ||
HU0004123A HU227197B1 (en) | 2000-10-24 | 2000-10-24 | Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2003115490A true RU2003115490A (en) | 2004-11-27 |
RU2271361C2 RU2271361C2 (en) | 2006-03-10 |
Family
ID=89978688
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2003115490/04A RU2271361C2 (en) | 2000-10-24 | 2001-10-15 | Amide derivatives of carboxylic acid, method for their preparing and pharmaceutical compositions based on thereof |
Country Status (9)
Country | Link |
---|---|
US (5) | US6919355B2 (en) |
EP (1) | EP1328514A1 (en) |
JP (1) | JP4225779B2 (en) |
AU (1) | AU2002210782A1 (en) |
HU (1) | HU227197B1 (en) |
PL (1) | PL365377A1 (en) |
RU (1) | RU2271361C2 (en) |
UA (1) | UA74850C2 (en) |
WO (1) | WO2002034718A1 (en) |
Families Citing this family (54)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7709510B2 (en) * | 2001-02-20 | 2010-05-04 | Chugai Seiyaku Kabushiki Kaisha | Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators |
JP4155351B2 (en) * | 2001-02-20 | 2008-09-24 | 中外製薬株式会社 | Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic regulators |
WO2003027068A2 (en) * | 2001-09-24 | 2003-04-03 | Elan Pharmaceuticals, Inc. | Substituted amines for the treatment of neurological disorders |
ATE372335T1 (en) * | 2002-02-01 | 2007-09-15 | Novo Nordisk As | AMIDES OF AMINOALKYL-SUBSTITUTED AZETIDINES, PYRROLIDINES, PIPERIDINES AND AZEPANES |
US7101898B2 (en) | 2002-02-01 | 2006-09-05 | Novo Nordisk A/S | Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes |
GB0205175D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
GB0205166D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
GB0205176D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
GB0205165D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
GB0205170D0 (en) | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
GB0205162D0 (en) * | 2002-03-06 | 2002-04-17 | Astrazeneca Ab | Chemical compounds |
WO2004035571A1 (en) * | 2002-10-15 | 2004-04-29 | Rigel Pharmaceuticals, Inc. | Substituted indoles and their use as hcv inhibitors |
EP1565453A4 (en) * | 2002-11-22 | 2007-10-10 | Merck & Co Inc | 2- (4-benzyl)-1-piperidinyl)methyl|benzimidazole-5-ol derivatives as nr2b receptor antagonists |
US7732162B2 (en) | 2003-05-05 | 2010-06-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase for treating neurodegenerative diseases |
ATE400272T1 (en) * | 2003-08-01 | 2008-07-15 | Chugai Pharmaceutical Co Ltd | PIPERIDINE COMPOUNDS AS MALONYL-COA DECARBOXYLASE INHIBITORS |
DE602004016530D1 (en) * | 2003-08-01 | 2008-10-23 | Chugai Pharmaceutical Co Ltd | CYANOGUANIDIN-BASED AZOL COMPOUNDS AS MALONYL-COA DECARBOXYLASE HEMMER |
ATE487475T1 (en) * | 2003-08-01 | 2010-11-15 | Chugai Pharmaceutical Co Ltd | HETEROCYCLIC COMPOUNDS AS USEFUL MALONYL-COA DECARBOXYLASE INHIBITORS |
KR20120117948A (en) | 2004-05-28 | 2012-10-24 | 유니젠, 인크. | Diarylalkanes as potent inhibitors of binuclear enzymes |
DE602005006567D1 (en) * | 2004-06-21 | 2008-06-19 | Hoffmann La Roche | INDOLE DERIVATIVES AS HISTAMINE RECEPTOR ANTAGONISTS |
HU227119B1 (en) * | 2004-07-29 | 2010-07-28 | Richter Gedeon Nyrt | Indole and benzimidazole carboxylic acid amide derivatives and pharmaceutical compositions containing them |
HUP0401523A3 (en) * | 2004-07-29 | 2007-05-02 | Richter Gedeon Vegyeszet | Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them |
EP2425846A1 (en) * | 2004-12-23 | 2012-03-07 | Voyager Pharmaceutical Corporation | Acetylcholinesterase Inhibitors and leuprolide acetate for the treatment of Alzheimer's disease |
CN101291938A (en) * | 2005-08-16 | 2008-10-22 | Irm责任有限公司 | Compounds and compositions as protein kinase inhibitors |
WO2007063839A1 (en) * | 2005-11-30 | 2007-06-07 | Shionogi & Co., Ltd. | Cyclohexane derivative |
US7935706B2 (en) | 2006-02-23 | 2011-05-03 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
JP2010501542A (en) * | 2006-08-23 | 2010-01-21 | ファイザー・プロダクツ・インク | Piperidine derivatives |
EP2089383B1 (en) | 2006-11-09 | 2015-09-16 | Probiodrug AG | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
WO2008059370A2 (en) | 2006-11-17 | 2008-05-22 | Pfizer Japan Inc. | Substituted bicyclocarboxyamide compounds |
JP5523107B2 (en) | 2006-11-30 | 2014-06-18 | プロビオドルグ エージー | Novel inhibitors of glutaminyl cyclase |
ATE527249T1 (en) | 2006-12-08 | 2011-10-15 | Hoffmann La Roche | INDOLE |
ES2627221T3 (en) | 2006-12-28 | 2017-07-27 | Rigel Pharmaceuticals, Inc. | N-substituted heterocycloalkyloxybenzamide compounds and methods of use |
WO2008104580A1 (en) | 2007-03-01 | 2008-09-04 | Probiodrug Ag | New use of glutaminyl cyclase inhibitors |
US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
CN101796017A (en) | 2007-09-21 | 2010-08-04 | 塞诺菲-安万特股份有限公司 | (carboxylalkylene-phenyl)-phenyl-oxalamides, method for the production thereof, and use of same as a medicament |
CA2730265C (en) | 2008-07-21 | 2016-06-28 | Unigen, Inc. | Series of skin-whitening (lightening) compounds |
ES2548913T3 (en) | 2009-09-11 | 2015-10-21 | Probiodrug Ag | Heterocyclic derivatives such as glutaminyl cyclase inhibitors |
JP5851998B2 (en) * | 2009-10-27 | 2016-02-03 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH | Haloalkyl-substituted amides as insecticides and acaricides |
WO2011058766A1 (en) | 2009-11-16 | 2011-05-19 | Raqualia Pharma Inc. | Aryl carboxamide derivatives as ttx-s blockers |
EP2542549B1 (en) | 2010-03-03 | 2016-05-11 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
EP2545047B9 (en) | 2010-03-10 | 2015-06-10 | Probiodrug AG | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
JP5945532B2 (en) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
WO2012123563A1 (en) | 2011-03-16 | 2012-09-20 | Probiodrug Ag | Benz imidazole derivatives as inhibitors of glutaminyl cyclase |
US8586799B2 (en) | 2011-03-24 | 2013-11-19 | Unigen, Inc. | Compounds and methods for preparation of diarylpropanes |
CN104321057B (en) | 2012-04-20 | 2016-09-14 | Ucb医药有限公司 | For treating Parkinsonian method |
EP2892880B1 (en) * | 2012-09-07 | 2017-11-22 | Novartis AG | Indole carboxamide derivatives and uses thereof |
KR101551313B1 (en) * | 2014-07-28 | 2015-09-09 | 충남대학교산학협력단 | Novel indene derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating blindness related diseases containing the same as an active ingredient |
JP6612331B2 (en) | 2014-09-15 | 2019-11-27 | リューゲン ホールディングス (ケイマン) リミテッド | Pyrrolopyrimidine derivatives as NR2B NMDA receptor antagonists |
US10662183B2 (en) | 2014-11-07 | 2020-05-26 | The Regents Of The University Of Michigan | Inhibitors of myocardin-related transcription factor and serum response factor (MRTF/SRF)-mediated gene transcription and methods for use of the same |
WO2016196513A1 (en) | 2015-06-01 | 2016-12-08 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists |
WO2017155890A1 (en) * | 2016-03-11 | 2017-09-14 | Ohio State Innovation Foundation | Novel small molecule antimicrobials |
WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
WO2018119374A1 (en) | 2016-12-22 | 2018-06-28 | Cadent Therapeutics | Nmda receptor modulators and uses thereof |
DK3461819T3 (en) | 2017-09-29 | 2020-08-10 | Probiodrug Ag | GLUTAMINYL CYCLASE INHIBITORS |
WO2020196828A1 (en) * | 2019-03-28 | 2020-10-01 | 武田薬品工業株式会社 | Nitrogen-containing heterocyclic compound |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5965073A (en) * | 1982-10-05 | 1984-04-13 | Kowa Co | Indole derivative |
US5354758A (en) * | 1992-12-16 | 1994-10-11 | Japan Tobacco Inc. | Benzomorphans useful as NMDA receptor antagonists |
TW406075B (en) * | 1994-12-13 | 2000-09-21 | Upjohn Co | Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds |
HUP0000882A3 (en) * | 1996-09-30 | 2001-04-28 | Aventis Pharmaceuticals Inc Br | Indole derivatives as nmda (n-methyl-d-aspartate) antagonists and pharmaceutical compositions containing them |
PE20000728A1 (en) | 1998-06-26 | 2000-08-21 | Cocensys Inc | HETEROCYCLES 4-BENZYL PIPERIDINE ALKYLSULFOXIDE AND THEIR USE AS SUBTYPE-SELECTIVE NMDA RECEPTOR ANTAGONISTS |
CA2342251A1 (en) | 1998-08-28 | 2000-03-09 | Scios Inc. | Use of piperidines and/or piperazines as inhibitors of p38-alpha kinase |
WO2000042213A1 (en) * | 1999-01-13 | 2000-07-20 | The Research Foundation Of State University Of New York | A novel method for designing protein kinase inhibitors |
US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
-
2000
- 2000-10-24 HU HU0004123A patent/HU227197B1/en unknown
-
2001
- 2001-10-15 UA UA2003054619A patent/UA74850C2/en unknown
- 2001-10-15 JP JP2002537711A patent/JP4225779B2/en not_active Expired - Fee Related
- 2001-10-15 WO PCT/HU2001/000099 patent/WO2002034718A1/en active Application Filing
- 2001-10-15 EP EP01978687A patent/EP1328514A1/en not_active Withdrawn
- 2001-10-15 RU RU2003115490/04A patent/RU2271361C2/en not_active IP Right Cessation
- 2001-10-15 PL PL01365377A patent/PL365377A1/en not_active Application Discontinuation
- 2001-10-15 AU AU2002210782A patent/AU2002210782A1/en not_active Abandoned
-
2003
- 2003-04-11 US US10/412,977 patent/US6919355B2/en not_active Expired - Fee Related
-
2004
- 2004-12-28 US US11/024,637 patent/US7361670B2/en not_active Expired - Fee Related
- 2004-12-28 US US11/024,638 patent/US7365083B2/en not_active Expired - Fee Related
- 2004-12-29 US US11/025,287 patent/US7375116B2/en not_active Expired - Fee Related
- 2004-12-29 US US11/025,288 patent/US7378431B2/en not_active Expired - Fee Related
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