EA200501041A1 - Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининов - Google Patents
Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининовInfo
- Publication number
- EA200501041A1 EA200501041A1 EA200501041A EA200501041A EA200501041A1 EA 200501041 A1 EA200501041 A1 EA 200501041A1 EA 200501041 A EA200501041 A EA 200501041A EA 200501041 A EA200501041 A EA 200501041A EA 200501041 A1 EA200501041 A1 EA 200501041A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- antagonistic activity
- neurokinins
- pyrrolidin
- piperidin
- substituted derivatives
- Prior art date
Links
Classifications
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- 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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Данное изобретение относится к замещенным производным 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина, обладающим антагонистической активностью по отношению к нейрокининам, в частности антагонистической активностью в отношении NK, комбинированной антагонистической активностью в отношении NK/NKи комбинированной антагонистической активностью в отношении NK/NK/NK, их получению, композициям, содержащим их, и к их применению в качестве лекарственного средства, в частности, для лечения шизофрении, тревоги, депрессии, рвоты и IBS. Соединения по изобретению могут быть представлены общей формулой (I), где все заместители имеют значения, указанные в п.1, и к ним также относятся фармацевтически приемлемые соли присоединения кислот или оснований, стереохимически изомерные формы, N-оксиды и пролекарства таких соединений.Отчет о международном поиске был опубликован 2004.08.12.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP0214831 | 2002-12-23 | ||
PCT/EP2003/051041 WO2004056799A2 (en) | 2002-12-23 | 2003-12-17 | Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
EA200501041A1 true EA200501041A1 (ru) | 2005-12-29 |
EA009078B1 EA009078B1 (ru) | 2007-10-26 |
Family
ID=32668698
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200501041A EA009078B1 (ru) | 2002-12-23 | 2003-12-17 | Замещенные производные 1-пиперидин-4-ил-4-пирролидин-3-илпиперазина и их применение в качестве антагонистов нейрокининов |
Country Status (31)
Country | Link |
---|---|
US (1) | US7795261B2 (ru) |
EP (1) | EP1581518B1 (ru) |
JP (1) | JP4746878B2 (ru) |
KR (1) | KR101049073B1 (ru) |
CN (1) | CN100586945C (ru) |
AR (1) | AR042651A1 (ru) |
AT (1) | ATE500242T1 (ru) |
AU (1) | AU2003302488B2 (ru) |
BR (1) | BR0317658A (ru) |
CA (1) | CA2508657C (ru) |
CL (1) | CL2003002725A1 (ru) |
CY (1) | CY1112601T1 (ru) |
DE (1) | DE60336266D1 (ru) |
DK (1) | DK1581518T3 (ru) |
EA (1) | EA009078B1 (ru) |
ES (1) | ES2361161T3 (ru) |
HK (1) | HK1087703A1 (ru) |
HR (1) | HRP20050556B1 (ru) |
IL (1) | IL169336A (ru) |
JO (1) | JO2696B1 (ru) |
MX (1) | MXPA05006887A (ru) |
MY (1) | MY145135A (ru) |
NO (1) | NO331174B1 (ru) |
NZ (1) | NZ541035A (ru) |
PA (1) | PA8593301A1 (ru) |
PL (1) | PL376048A1 (ru) |
PT (1) | PT1581518E (ru) |
SI (1) | SI1581518T1 (ru) |
TW (1) | TWI329109B (ru) |
UA (1) | UA80584C2 (ru) |
WO (1) | WO2004056799A2 (ru) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2847160A1 (fr) * | 2002-11-20 | 2004-05-21 | Oreal | Composition capillaire contenant un compose pyrasol-carboxamide, son utilisation pour stimuler la pousse des cheveux et/ou freiner leur chute |
ES2431524T3 (es) | 2004-04-13 | 2013-11-26 | Incyte Corporation | Derivados de piperazinilpiperidina como antagonistas de los receptores de quimiocinas |
WO2005123081A2 (en) * | 2004-06-22 | 2005-12-29 | Janssen Pharmaceutica N.V. | (2-benzyl-4-{4-[1-(tetrahydrofuran-3-carbonyl)-pyrrolidin-3-yl]-piperazin-1-yl}-piperidin-1-yl)-(3,5-trifluoromethyl-phenyl))-methanone for the treatment of schizophrenia |
WO2006071875A1 (en) | 2004-12-29 | 2006-07-06 | Millennium Pharmaceuticals, Inc. | Compounds useful as chemokine receptor antagonists |
US7635698B2 (en) * | 2004-12-29 | 2009-12-22 | Millennium Pharmaceuticals, Inc. | Compounds useful as chemokine receptor antagonists |
EP1858896B1 (en) * | 2005-03-08 | 2010-08-18 | Janssen Pharmaceutica NV | Diaza-spiro-[4.4]-nonane derivatives as neurokinin (nk1) antagonists |
DE102005038947A1 (de) * | 2005-05-18 | 2006-11-30 | Grünenthal GmbH | Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln |
EP2099454A4 (en) * | 2006-11-17 | 2010-11-10 | Abbott Lab | AMINOPYRROLIDINES AS CHEMOKINE RECEPTOR ANTAGONISTS |
KR101240147B1 (ko) | 2007-03-31 | 2013-03-08 | 인터벳 인터내셔널 비.브이. | 질파테롤 및 이의 염의 제조 방법 |
RU2442786C2 (ru) * | 2007-03-31 | 2012-02-20 | Интервет Интернэшнл Б.В. | Способы получения зилпатерола и его солей |
CN105037275B (zh) * | 2007-03-31 | 2019-05-10 | 英特威国际有限公司 | 制备齐帕特罗及其盐的方法 |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
US7879802B2 (en) | 2007-06-04 | 2011-02-01 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
AU2008258665B2 (en) | 2007-06-07 | 2012-07-05 | F. Hoffmann-La Roche Ag | Prolinamide derivatives as NK3 antagonists |
ES2624828T3 (es) | 2008-07-16 | 2017-07-17 | Synergy Pharmaceuticals Inc. | Agonistas de la guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros |
US8507535B2 (en) * | 2010-07-07 | 2013-08-13 | Hoffmann-La Roche Inc. | Methyl-pyrrolidine ether derivatives |
MX2015002231A (es) * | 2012-08-23 | 2015-07-17 | Alios Biopharma Inc | Compuestos antivirales. |
JP2016514670A (ja) | 2013-03-15 | 2016-05-23 | シナジー ファーマシューティカルズ インコーポレイテッド | 他の薬物と組み合わせたグアニル酸シクラーゼ受容体アゴニスト |
JP2016514671A (ja) | 2013-03-15 | 2016-05-23 | シナジー ファーマシューティカルズ インコーポレイテッド | グアニル酸シクラーゼのアゴニストおよびその使用 |
SI3297631T1 (sl) | 2015-05-18 | 2019-12-31 | Nerre Therapeutics Limited | Antagonist NK-1/NK-3 receptorja za zdravljenje oblivov vročine |
HUE065300T2 (hu) | 2018-03-14 | 2024-05-28 | Kandy Therapeutics Ltd | Kettõs NK-1/NK-3 receptor antagonistákat tartalmazó új gyógyászati kiszerelés |
AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
MY110227A (en) | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
NZ321575A (en) | 1995-10-30 | 1999-05-28 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4- substituted piperazine derivatives |
TW382017B (en) | 1995-12-27 | 2000-02-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-(fused imidazole)-piperidine derivatives |
AU7788500A (en) | 1999-10-25 | 2001-05-08 | Janssen Pharmaceutica N.V. | Use of substance p antagonists for influencing the circadian timing system |
GB0025354D0 (en) | 2000-10-17 | 2000-11-29 | Glaxo Group Ltd | Chemical compounds |
US6642226B2 (en) | 2001-02-06 | 2003-11-04 | Hoffman-La Roche Inc. | Substituted phenyl-piperidine methanone compounds |
FR2820426B1 (fr) * | 2001-02-07 | 2007-05-11 | Condat Sa | Gel d'isolation thermique a reticulation controlee pour les lignes de transport d'hydrocarbures petroliers |
MY141736A (en) | 2002-10-08 | 2010-06-15 | Elanco Animal Health Ireland | Substituted 1,4-di-piperidin-4-yi-piperazine derivatives and their use as neurokinin antagonists |
-
2003
- 2003-12-15 JO JO2003174A patent/JO2696B1/en active
- 2003-12-17 PL PL03376048A patent/PL376048A1/xx not_active Application Discontinuation
- 2003-12-17 PT PT03810849T patent/PT1581518E/pt unknown
- 2003-12-17 CN CN200380106356A patent/CN100586945C/zh not_active Expired - Fee Related
- 2003-12-17 AT AT03810849T patent/ATE500242T1/de active
- 2003-12-17 EA EA200501041A patent/EA009078B1/ru not_active IP Right Cessation
- 2003-12-17 CA CA2508657A patent/CA2508657C/en not_active Expired - Fee Related
- 2003-12-17 EP EP03810849A patent/EP1581518B1/en not_active Expired - Lifetime
- 2003-12-17 UA UAA200505412A patent/UA80584C2/ru unknown
- 2003-12-17 MX MXPA05006887A patent/MXPA05006887A/es active IP Right Grant
- 2003-12-17 KR KR1020057009197A patent/KR101049073B1/ko not_active Expired - Fee Related
- 2003-12-17 WO PCT/EP2003/051041 patent/WO2004056799A2/en active Application Filing
- 2003-12-17 SI SI200331992T patent/SI1581518T1/sl unknown
- 2003-12-17 JP JP2004561504A patent/JP4746878B2/ja not_active Expired - Fee Related
- 2003-12-17 ES ES03810849T patent/ES2361161T3/es not_active Expired - Lifetime
- 2003-12-17 AU AU2003302488A patent/AU2003302488B2/en not_active Ceased
- 2003-12-17 NZ NZ541035A patent/NZ541035A/en not_active IP Right Cessation
- 2003-12-17 DE DE60336266T patent/DE60336266D1/de not_active Expired - Lifetime
- 2003-12-17 BR BR0317658-4A patent/BR0317658A/pt not_active IP Right Cessation
- 2003-12-17 US US10/540,447 patent/US7795261B2/en not_active Expired - Fee Related
- 2003-12-17 DK DK03810849.4T patent/DK1581518T3/da active
- 2003-12-19 PA PA20038593301A patent/PA8593301A1/es unknown
- 2003-12-19 MY MYPI20034909A patent/MY145135A/en unknown
- 2003-12-22 TW TW092136343A patent/TWI329109B/zh not_active IP Right Cessation
- 2003-12-22 AR ARP030104776A patent/AR042651A1/es unknown
- 2003-12-22 CL CL200302725A patent/CL2003002725A1/es unknown
-
2005
- 2005-06-15 HR HRP20050556AA patent/HRP20050556B1/hr not_active IP Right Cessation
- 2005-06-22 IL IL169336A patent/IL169336A/en not_active IP Right Cessation
- 2005-07-21 NO NO20053569A patent/NO331174B1/no not_active IP Right Cessation
-
2006
- 2006-07-14 HK HK06107904.4A patent/HK1087703A1/xx not_active IP Right Cessation
-
2011
- 2011-06-01 CY CY20111100532T patent/CY1112601T1/el unknown
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM RU |