PE20050245A1 - Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos - Google Patents
Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidosInfo
- Publication number
- PE20050245A1 PE20050245A1 PE2004000552A PE2004000552A PE20050245A1 PE 20050245 A1 PE20050245 A1 PE 20050245A1 PE 2004000552 A PE2004000552 A PE 2004000552A PE 2004000552 A PE2004000552 A PE 2004000552A PE 20050245 A1 PE20050245 A1 PE 20050245A1
- Authority
- PE
- Peru
- Prior art keywords
- aril
- pyrimidin
- fluoro
- methyl
- nonaryl
- Prior art date
Links
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 title 1
- 102000034527 Retinoid X Receptors Human genes 0.000 title 1
- 108010038912 Retinoid X Receptors Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- DNUTZBZXLPWRJG-UHFFFAOYSA-M piperidine-1-carboxylate Chemical compound [O-]C(=O)N1CCCCC1 DNUTZBZXLPWRJG-UHFFFAOYSA-M 0.000 abstract 2
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 1
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 abstract 1
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 206010065390 Inflammatory pain Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical compound [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 230000001684 chronic effect Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 abstract 1
- 239000011630 iodine Substances 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 abstract 1
- 230000009278 visceral effect Effects 0.000 abstract 1
- 208000009935 visceral pain Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Addiction (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Psychology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
Abstract
REFERIDA A UN COMPUESTO DE FORMULA I DONDE HetAr ES UN ANILLO HETEROAROMATICO CON 1-2 ATOMOS DE N EN EL ANILLO, TIAZOLILO, TIADIAZOLILO; HetAr ESTA OPCIONALMENTE TIENE 1-2 SUSTITUYENTES TALES COMO ALQUILC1-C4, FLUORO, CLORO; BROMO, YODO; A ES UN ENLACE O ALQUIL-C1-C2; B ES ARIL(CH2)0-3-O-C(O)-, ARIL(CH2)1-3-C(O)-, ARIL-CICLOPROPIL-C(O)-, ENTRE OTROS. TAMBIEN REFERIDA A UNA COMPOSICION FARMACEUTICA QUE CONTIENE DICHO COMPUESTO CUYOS PREFERIDOS SON: (3R,4S)3-FLUORO-4-[(PIRIMIDIN-2-ILAMINO)METIL]PIPERIDINA-1-CARBOXILATO DE 4-METILBENCILO; 3-FLUORO-4-[(PIRIMIDIN-2-ILAMINO)METIL]PIPERIDINA-1-CARBOXILATO DE (-)-TRANS-4-METILBENCILO Y (3R,4S)-N-[(3-CIS-FLUORO-1-{[(1R,2R)-2-FENILCICLOPROPIL]CARBONIL}PIPERIDIN-4-IL)METIL]PIRIMIDIN-2-AMINA; ENTRE OTROS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE PARKINSON, DE DOLORES CRONICOS, VISCERALES, INFLAMATORIOS Y NEUROPATICOS, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47593803P | 2003-06-04 | 2003-06-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20050245A1 true PE20050245A1 (es) | 2005-04-13 |
Family
ID=33511734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2004000552A PE20050245A1 (es) | 2003-06-04 | 2004-06-01 | Antagonistas de nmda/nr2b nonaril - heterociclicos n-sustituidos |
Country Status (30)
| Country | Link |
|---|---|
| EP (1) | EP1648882B1 (es) |
| JP (1) | JP3927228B2 (es) |
| KR (1) | KR20060017839A (es) |
| CN (1) | CN1798744A (es) |
| AR (1) | AR044579A1 (es) |
| AT (1) | ATE403651T1 (es) |
| AU (1) | AU2004245522B2 (es) |
| BR (1) | BRPI0410837A (es) |
| CA (1) | CA2527093C (es) |
| CL (1) | CL2004001365A1 (es) |
| CO (1) | CO5700762A2 (es) |
| DE (1) | DE602004015610D1 (es) |
| DK (1) | DK1648882T3 (es) |
| EC (1) | ECSP056192A (es) |
| ES (1) | ES2309540T3 (es) |
| HR (1) | HRP20080490T3 (es) |
| IS (1) | IS8117A (es) |
| MA (1) | MA27781A1 (es) |
| MX (1) | MXPA05013151A (es) |
| MY (1) | MY138547A (es) |
| NO (1) | NO20060020L (es) |
| PE (1) | PE20050245A1 (es) |
| PL (1) | PL1648882T3 (es) |
| PT (1) | PT1648882E (es) |
| RU (1) | RU2339630C2 (es) |
| SI (1) | SI1648882T1 (es) |
| TW (1) | TW200510378A (es) |
| UA (1) | UA81319C2 (es) |
| WO (1) | WO2004108705A1 (es) |
| ZA (1) | ZA200509000B (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2021005A4 (en) * | 2006-05-03 | 2009-11-25 | Cnsbio Pty Ltd | METHOD AND COMPOSITION FOR THE TREATMENT OF INFLAMMATORY PAIN |
| ES2400710T3 (es) * | 2007-04-23 | 2013-04-11 | Janssen Pharmaceutica, N.V. | Tia(dia)zoles como antagonistas del receptor de dopamina 2 de disociación rápida |
| US20100316678A1 (en) * | 2007-06-28 | 2010-12-16 | Cnsbio Pty Ltd. | Combination methods and compositions for treatment of neuropathic pain |
| CN102762554A (zh) | 2010-02-16 | 2012-10-31 | 辉瑞大药厂 | 5-ht4受体的部分激动剂(r)-4-((4-((4-(四氢呋喃-3-基氧基)苯并[d]异*唑-3-基氧基)甲基)哌啶-1-基)甲基)四氢-2h-吡喃-4-醇 |
| AU2013251079B2 (en) | 2012-04-20 | 2017-03-23 | Ucb Pharma S.A. | Methods for treating Parkinson's disease |
| CN103936663B (zh) * | 2013-01-23 | 2016-12-28 | 艾琪康医药科技（上海）有限公司 | 一种1-r1-3,3-二氟(或3-氟)-4-r2-4-氨甲基哌啶及其衍生物的制备方法 |
| US9187506B2 (en) | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
| US9221796B2 (en) | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| JP2017516836A (ja) | 2014-06-04 | 2017-06-22 | リューゲン ホールディングス （ケイマン） リミテッド | Ｎｒ２ｂｎｍｄａ受容体アンタゴニストとしてのジフルオロエチルピリジン誘導体 |
| EP3194403B1 (en) | 2014-09-15 | 2019-02-06 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| US20180271869A1 (en) * | 2014-09-22 | 2018-09-27 | Jie Liu | Treatment of anxiety disorders and autism spectrum disorders |
| EP3237399B1 (en) * | 2014-12-23 | 2022-11-30 | Avalo Therapeutics, Inc. | Compounds, compositions and methods |
| US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
| CN107849010B (zh) * | 2015-06-01 | 2021-11-09 | 卢郡控股(开曼)有限公司 | 作为nr2b nmda受体拮抗剂的3,3‐二氟哌啶氨基甲酸酯杂环化合物 |
| KR20180063306A (ko) | 2015-10-14 | 2018-06-11 | 브리스톨-마이어스 스큅 컴퍼니 | 선택적 nr2b 길항제 |
| WO2017066368A1 (en) | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
| US10227349B2 (en) | 2016-08-31 | 2019-03-12 | Eisai R&D Management Co., Ltd. | Pyrazolo[1,5-a]pyrimidine compound |
| WO2018098128A1 (en) | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| YU64303A (sh) * | 2001-02-23 | 2006-05-25 | Merck & Co.Inc. | N-supstituisani nearil-heterociklični antagonisti nmda/nr2b |
-
2004
- 2004-05-28 AT AT04753896T patent/ATE403651T1/de not_active IP Right Cessation
- 2004-05-28 SI SI200430845T patent/SI1648882T1/sl unknown
- 2004-05-28 JP JP2006515051A patent/JP3927228B2/ja not_active Expired - Lifetime
- 2004-05-28 WO PCT/US2004/017175 patent/WO2004108705A1/en not_active Ceased
- 2004-05-28 UA UAA200511411A patent/UA81319C2/uk unknown
- 2004-05-28 PT PT04753896T patent/PT1648882E/pt unknown
- 2004-05-28 ES ES04753896T patent/ES2309540T3/es not_active Expired - Lifetime
- 2004-05-28 DE DE602004015610T patent/DE602004015610D1/de not_active Expired - Lifetime
- 2004-05-28 CA CA002527093A patent/CA2527093C/en not_active Expired - Lifetime
- 2004-05-28 RU RU2005137704/04A patent/RU2339630C2/ru not_active IP Right Cessation
- 2004-05-28 HR HR20080490T patent/HRP20080490T3/xx unknown
- 2004-05-28 PL PL04753896T patent/PL1648882T3/pl unknown
- 2004-05-28 DK DK04753896T patent/DK1648882T3/da active
- 2004-05-28 EP EP04753896A patent/EP1648882B1/en not_active Expired - Lifetime
- 2004-05-28 BR BRPI0410837-0A patent/BRPI0410837A/pt not_active IP Right Cessation
- 2004-05-28 AU AU2004245522A patent/AU2004245522B2/en not_active Expired
- 2004-05-28 KR KR1020057023218A patent/KR20060017839A/ko not_active Ceased
- 2004-05-28 CN CNA2004800153228A patent/CN1798744A/zh active Pending
- 2004-05-28 MX MXPA05013151A patent/MXPA05013151A/es active IP Right Grant
- 2004-05-31 AR ARP040101878A patent/AR044579A1/es unknown
- 2004-05-31 MY MYPI20042091A patent/MY138547A/en unknown
- 2004-06-01 PE PE2004000552A patent/PE20050245A1/es not_active Application Discontinuation
- 2004-06-03 TW TW093115972A patent/TW200510378A/zh unknown
- 2004-06-03 CL CL200401365A patent/CL2004001365A1/es unknown
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2005
- 2005-11-07 IS IS8117A patent/IS8117A/is unknown
- 2005-11-07 ZA ZA200509000A patent/ZA200509000B/en unknown
- 2005-11-28 MA MA28626A patent/MA27781A1/fr unknown
- 2005-11-29 EC EC2005006192A patent/ECSP056192A/es unknown
- 2005-11-30 CO CO05121658A patent/CO5700762A2/es not_active Application Discontinuation
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2006
- 2006-01-03 NO NO20060020A patent/NO20060020L/no not_active Application Discontinuation
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