UA77515C2 - Diazabicyclo alkane derivatives possessing neuroldnin-nk1 receptor antagonistic activity - Google Patents
Diazabicyclo alkane derivatives possessing neuroldnin-nk1 receptor antagonistic activity Download PDFInfo
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- UA77515C2 UA77515C2 UA20041108912A UA20041108912A UA77515C2 UA 77515 C2 UA77515 C2 UA 77515C2 UA 20041108912 A UA20041108912 A UA 20041108912A UA 20041108912 A UA20041108912 A UA 20041108912A UA 77515 C2 UA77515 C2 UA 77515C2
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- compounds
- morpholin
- ylmethyl
- disease
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- 230000003042 antagnostic effect Effects 0.000 title abstract description 7
- 150000001335 aliphatic alkanes Chemical class 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 73
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- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims abstract description 7
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- 238000002360 preparation method Methods 0.000 claims abstract description 4
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 3
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- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims abstract description 3
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- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims abstract 2
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- 235000006408 oxalic acid Nutrition 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- XAMUDJHXFNRLCY-UHFFFAOYSA-N phenthoate Chemical compound CCOC(=O)C(SP(=S)(OC)OC)C1=CC=CC=C1 XAMUDJHXFNRLCY-UHFFFAOYSA-N 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 229920000166 polytrimethylene carbonate Polymers 0.000 description 1
- 238000006268 reductive amination reaction Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 239000011435 rock Substances 0.000 description 1
- 210000004761 scalp Anatomy 0.000 description 1
- 230000007958 sleep Effects 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 238000000638 solvent extraction Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- ADNPLDHMAVUMIW-CUZNLEPHSA-N substance P Chemical compound C([C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CCCN=C(N)N)C1=CC=CC=C1 ADNPLDHMAVUMIW-CUZNLEPHSA-N 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000002466 tachykinin receptor agonist Substances 0.000 description 1
- MHYGQXWCZAYSLJ-UHFFFAOYSA-N tert-butyl-chloro-diphenylsilane Chemical compound C=1C=CC=CC=1[Si](Cl)(C(C)(C)C)C1=CC=CC=C1 MHYGQXWCZAYSLJ-UHFFFAOYSA-N 0.000 description 1
- YNJBWRMUSHSURL-UHFFFAOYSA-N trichloroacetic acid Chemical compound OC(=O)C(Cl)(Cl)Cl YNJBWRMUSHSURL-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Otolaryngology (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02076405 | 2002-04-04 | ||
PCT/EP2003/050086 WO2003084955A1 (en) | 2002-04-04 | 2003-04-02 | Diazabicyclo alkane derivatives with nk1 antagonistic activity |
Publications (1)
Publication Number | Publication Date |
---|---|
UA77515C2 true UA77515C2 (en) | 2006-12-15 |
Family
ID=28685940
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UA20041108912A UA77515C2 (en) | 2002-04-04 | 2003-02-04 | Diazabicyclo alkane derivatives possessing neuroldnin-nk1 receptor antagonistic activity |
Country Status (21)
Country | Link |
---|---|
US (1) | US7202238B2 (pt) |
EP (1) | EP1495022B1 (pt) |
JP (1) | JP2005525395A (pt) |
KR (1) | KR20040095361A (pt) |
CN (1) | CN1279041C (pt) |
AR (1) | AR039192A1 (pt) |
AT (1) | ATE435863T1 (pt) |
AU (1) | AU2003224162B2 (pt) |
BR (1) | BR0306148A (pt) |
CA (1) | CA2462708A1 (pt) |
DE (1) | DE60328272D1 (pt) |
HK (1) | HK1070356A1 (pt) |
HR (1) | HRP20040273A2 (pt) |
IL (2) | IL160943A0 (pt) |
MX (1) | MXPA04004812A (pt) |
NO (1) | NO20044775L (pt) |
PL (1) | PL371378A1 (pt) |
RU (1) | RU2310656C2 (pt) |
UA (1) | UA77515C2 (pt) |
WO (1) | WO2003084955A1 (pt) |
ZA (1) | ZA200404744B (pt) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20060205724A1 (en) * | 2002-05-29 | 2006-09-14 | The Regents Of The University Of California | Antagonizing nk-1 receptors inhibits consumption of substances of abuse |
AR045796A1 (es) * | 2003-09-26 | 2005-11-16 | Solvay Pharm Bv | Derivados de hexa y octahidro - pirido (1,2-a) pirazina con actividad antagonista de nk1. composiciones farmaceuticas. |
WO2006013205A1 (en) * | 2004-08-04 | 2006-02-09 | Solvay Pharmaceuticals B.V. | Neurokinin-1 receptor antagonists for the treatment of conditions responsive to testosterone elevation |
DE102006049452A1 (de) * | 2006-10-17 | 2008-05-08 | Grünenthal GmbH | Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln |
WO2010011912A1 (en) * | 2008-07-25 | 2010-01-28 | Smithkline Beecham Corporation | Trpv4 antagonists |
JP5607046B2 (ja) * | 2008-07-25 | 2014-10-15 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Trpv4拮抗薬 |
US8669255B2 (en) | 2011-09-29 | 2014-03-11 | Abbvie Inc. | Substituted octahydropyrrolo[1,2-a]pyrazines as calcium channel blockers |
AR088064A1 (es) | 2011-09-29 | 2014-05-07 | Abbvie Inc | Octahidropirrolo[1,2-a]pirazina sulfonamidas sustituidas como bloqueadores de canales de calcio |
PL2817312T3 (pl) * | 2012-02-22 | 2016-08-31 | Leo Pharma As | Nowe związki będące antagonistami receptora neurokininy 1 |
KR20150093237A (ko) | 2012-12-12 | 2015-08-17 | 애브비 인코포레이티드 | 통증 치료시 칼슘 채널 차단제로서 유용한 디아제핀 유도체 |
JP6574769B2 (ja) * | 2013-07-25 | 2019-09-11 | ニューレン ファーマシューティカルズ リミテッド | 二環式化合物ならびに自閉症スペクトラム障害および神経発達障害の治療におけるそれらの使用方法 |
WO2015024203A1 (en) * | 2013-08-20 | 2015-02-26 | Leo Pharma A/S | Novel neurokinin 1 receptor antagonist compounds ii |
JP7306997B2 (ja) | 2017-03-20 | 2023-07-11 | ザ・ブロード・インスティテュート・インコーポレイテッド | 寄生虫性疾患の処置のための化合物および方法 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1125112A (en) * | 1966-01-07 | 1968-08-28 | Science Union & Cie | New derivatives of diazabicyclo-decane and process for preparing them |
IL111730A (en) * | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them |
EP0827500B1 (en) * | 1995-05-23 | 2001-11-14 | Janssen Pharmaceutica N.V. | (2-morpholinylmethyl)benzamide derivatives |
GB9510600D0 (en) | 1995-05-25 | 1995-07-19 | Fujisawa Pharmaceutical Co | Piperazine derivatives |
HUP9900822A3 (en) | 1995-05-25 | 1999-11-29 | Fujisawa Pharmaceutical Co | Piperazine derivatives, process for producing them, pharmaceutical compositions containing them and method for treating tachykinin-mediated diseases |
EP0873320B1 (en) | 1995-12-18 | 2002-06-12 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives as tachykinin antagonists |
AUPO735997A0 (en) | 1997-06-17 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
DE59814233D1 (de) | 1997-08-27 | 2008-07-03 | Solvay Pharm Gmbh | Indolmethyl-N,N'-bisacylpiperazine als Neurokininrezeptorantagonisten |
EP0982030A3 (en) * | 1998-08-17 | 2000-05-10 | Pfizer Products Inc. | 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands |
JP3454427B2 (ja) * | 1998-12-14 | 2003-10-06 | 藤沢薬品工業株式会社 | ピペラジン誘導体 |
DE10036818A1 (de) | 2000-07-28 | 2002-02-07 | Solvay Pharm Gmbh | Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten |
-
2003
- 2003-02-04 UA UA20041108912A patent/UA77515C2/uk unknown
- 2003-03-28 AR ARP030101105A patent/AR039192A1/es unknown
- 2003-04-02 PL PL03371378A patent/PL371378A1/xx not_active Application Discontinuation
- 2003-04-02 CA CA002462708A patent/CA2462708A1/en not_active Abandoned
- 2003-04-02 WO PCT/EP2003/050086 patent/WO2003084955A1/en active Application Filing
- 2003-04-02 US US10/490,364 patent/US7202238B2/en not_active Expired - Lifetime
- 2003-04-02 MX MXPA04004812A patent/MXPA04004812A/es active IP Right Grant
- 2003-04-02 IL IL16094303A patent/IL160943A0/xx unknown
- 2003-04-02 RU RU2004112415/04A patent/RU2310656C2/ru active
- 2003-04-02 EP EP03720571A patent/EP1495022B1/en not_active Expired - Lifetime
- 2003-04-02 KR KR10-2004-7015635A patent/KR20040095361A/ko not_active Application Discontinuation
- 2003-04-02 DE DE60328272T patent/DE60328272D1/de not_active Expired - Fee Related
- 2003-04-02 BR BR0306148-5A patent/BR0306148A/pt not_active IP Right Cessation
- 2003-04-02 CN CNB038015595A patent/CN1279041C/zh not_active Expired - Fee Related
- 2003-04-02 JP JP2003582152A patent/JP2005525395A/ja active Pending
- 2003-04-02 AU AU2003224162A patent/AU2003224162B2/en not_active Ceased
- 2003-04-02 AT AT03720571T patent/ATE435863T1/de not_active IP Right Cessation
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2004
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- 2004-03-19 HR HR20040273A patent/HRP20040273A2/xx not_active Application Discontinuation
- 2004-06-15 ZA ZA200404744A patent/ZA200404744B/en unknown
- 2004-11-03 NO NO20044775A patent/NO20044775L/no not_active Application Discontinuation
-
2005
- 2005-04-08 HK HK05102968A patent/HK1070356A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
EP1495022B1 (en) | 2009-07-08 |
HK1070356A1 (en) | 2005-06-17 |
AR039192A1 (es) | 2005-02-09 |
DE60328272D1 (de) | 2009-08-20 |
WO2003084955A1 (en) | 2003-10-16 |
RU2310656C2 (ru) | 2007-11-20 |
JP2005525395A (ja) | 2005-08-25 |
MXPA04004812A (es) | 2004-08-11 |
AU2003224162B2 (en) | 2008-06-12 |
ATE435863T1 (de) | 2009-07-15 |
PL371378A1 (en) | 2005-06-13 |
KR20040095361A (ko) | 2004-11-12 |
IL160943A0 (en) | 2004-08-31 |
CN1279041C (zh) | 2006-10-11 |
CA2462708A1 (en) | 2003-10-16 |
ZA200404744B (en) | 2005-09-21 |
RU2004112415A (ru) | 2005-03-27 |
EP1495022A1 (en) | 2005-01-12 |
US20050119267A1 (en) | 2005-06-02 |
AU2003224162A1 (en) | 2003-10-20 |
HRP20040273A2 (en) | 2005-02-28 |
CN1592747A (zh) | 2005-03-09 |
NO20044775L (no) | 2004-12-16 |
BR0306148A (pt) | 2004-10-19 |
US7202238B2 (en) | 2007-04-10 |
IL160943A (en) | 2008-11-03 |
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