SK27498A3 - Piperazino derivatives as neurokinin antagonists - Google Patents
Piperazino derivatives as neurokinin antagonists Download PDFInfo
- Publication number
- SK27498A3 SK27498A3 SK274-98A SK27498A SK27498A3 SK 27498 A3 SK27498 A3 SK 27498A3 SK 27498 A SK27498 A SK 27498A SK 27498 A3 SK27498 A3 SK 27498A3
- Authority
- SK
- Slovakia
- Prior art keywords
- substituted
- alkyl
- mmol
- formula
- heteroaryl
- Prior art date
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- 239000005557 antagonist Substances 0.000 title abstract description 12
- -1 Piperazino Chemical class 0.000 title description 46
- 150000001875 compounds Chemical class 0.000 claims abstract description 89
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- 238000000034 method Methods 0.000 claims description 72
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 32
- 125000003118 aryl group Chemical group 0.000 claims description 28
- 125000001072 heteroaryl group Chemical group 0.000 claims description 26
- 150000003839 salts Chemical group 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 17
- 125000000592 heterocycloalkyl group Chemical class 0.000 claims description 14
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 13
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- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 10
- 229910052794 bromium Inorganic materials 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 5
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Classifications
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- 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
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- 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
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- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US308495P | 1995-08-31 | 1995-08-31 | |
| PCT/US1996/005660 WO1996034864A1 (en) | 1995-05-02 | 1996-05-01 | Piperazino derivatives as neurokinin antagonists |
| US08/663,880 US5795894A (en) | 1995-05-02 | 1996-06-14 | Piperazino derivatives as neurokinn antagonists |
| PCT/IB1996/001018 WO1997008166A1 (en) | 1995-08-31 | 1996-08-29 | Piperazino derivatives as neurokinin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK27498A3 true SK27498A3 (en) | 1998-12-02 |
Family
ID=46202966
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK274-98A SK27498A3 (en) | 1995-08-31 | 1996-08-29 | Piperazino derivatives as neurokinin antagonists |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP0850236B1 (hu) |
| JP (2) | JP3447745B2 (hu) |
| CN (1) | CN1111529C (hu) |
| AT (1) | ATE202776T1 (hu) |
| AU (1) | AU708834B2 (hu) |
| BR (1) | BR9610277A (hu) |
| CA (1) | CA2228370C (hu) |
| CZ (1) | CZ22898A3 (hu) |
| DE (1) | DE69613705T2 (hu) |
| ES (1) | ES2158345T3 (hu) |
| GR (1) | GR3036675T3 (hu) |
| HU (1) | HUP9802552A3 (hu) |
| IL (1) | IL123112A (hu) |
| NO (1) | NO980848L (hu) |
| PL (1) | PL325339A1 (hu) |
| SK (1) | SK27498A3 (hu) |
| WO (1) | WO1997008166A1 (hu) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5892039A (en) * | 1995-08-31 | 1999-04-06 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5968929A (en) * | 1996-10-30 | 1999-10-19 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| CA2269128C (en) * | 1996-10-30 | 2005-01-11 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| AUPO735997A0 (en) * | 1997-06-17 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
| UA64751C2 (uk) | 1997-06-25 | 2004-03-15 | Пфайзер Продактс Інк. | Спосіб лікування інсулінової толерантності речовинами, які посилюють секрецію гормону росту (варіанти) та фармацевтична композиція (варіанти) |
| EP1047698A1 (en) * | 1998-01-14 | 2000-11-02 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| IL143577A0 (en) * | 1998-12-14 | 2002-04-21 | Fujisawa Pharmaceutical Co | Piperazine derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same |
| KR20080059687A (ko) | 2000-03-06 | 2008-06-30 | 아카디아 파마슈티칼스 인코포레이티드 | 세로토닌 관련 질병의 치료에 사용되는 아자시클릭 화합물 |
| TW591025B (en) * | 2000-06-13 | 2004-06-11 | Fujisawa Pharmaceutical Co | Production of the piperazine derivative |
| CN101050215A (zh) | 2001-12-28 | 2007-10-10 | 阿卡蒂亚药品公司 | 作为单胺受体调节剂的螺氮杂环化合物 |
| US6855724B2 (en) | 2002-04-08 | 2005-02-15 | Agouron Pharmaceuticals, Inc. | Tropane derivatives useful in therapy |
| US7253186B2 (en) | 2002-06-24 | 2007-08-07 | Carl-Magnus Andersson | N-substituted piperidine derivatives as serotonin receptor agents |
| US7538222B2 (en) | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| RU2320646C2 (ru) | 2002-06-24 | 2008-03-27 | Акадиа Фармасьютикалз Инк. | N-замещенные производные пиперидина в качестве агентов серотонинового рецептора |
| US7601740B2 (en) | 2003-01-16 | 2009-10-13 | Acadia Pharmaceuticals, Inc. | Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases |
| US7820695B2 (en) | 2004-05-21 | 2010-10-26 | Acadia Pharmaceuticals, Inc. | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US20050261278A1 (en) | 2004-05-21 | 2005-11-24 | Weiner David M | Selective serotonin receptor inverse agonists as therapeutics for disease |
| ES2530258T3 (es) | 2004-09-27 | 2015-02-27 | Acadia Pharmaceuticals Inc. | Síntesis de una forma cristalina de sal tartrato de N-(4-fluorobencil)-N-(1-metilpiperidin-4-il)-N'-(4-(2-metilpropiloxi)fenilmetil)carbamida |
| US7790899B2 (en) | 2004-09-27 | 2010-09-07 | Acadia Pharmaceuticals, Inc. | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
| WO2008090117A1 (en) | 2007-01-24 | 2008-07-31 | Glaxo Group Limited | Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1 |
| PL2134330T3 (pl) | 2007-03-19 | 2013-10-31 | Acadia Pharm Inc | Kombinacje odwrotnych agonistów i antagonistów 5-HT2A z antypsychotykami |
| EP3325444B1 (en) | 2015-07-20 | 2021-07-07 | Acadia Pharmaceuticals Inc. | Methods for preparing n-(4-fluorobenzyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and polymorphic form c |
| WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome p450 modulators |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
| WO2018118626A1 (en) | 2016-12-20 | 2018-06-28 | Acadia Pharmaceuticals Inc. | Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis |
| US11135211B2 (en) | 2017-04-28 | 2021-10-05 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
| US20210077479A1 (en) | 2017-08-30 | 2021-03-18 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
| CN115368296A (zh) * | 2022-07-27 | 2022-11-22 | 苏州汉德创宏生化科技有限公司 | 一种n-叔丁氧羰基-4-氨基哌啶的制备方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8908587D0 (en) * | 1989-04-15 | 1989-06-01 | Scras Societe De Conseils De R | New 2-substituted n,n'-ditrimethoxybenzoyl piperazines |
| WO1992020661A1 (en) * | 1991-05-22 | 1992-11-26 | Merck & Co., Inc. | N, n-diacylpiperazines |
| US5344830A (en) * | 1992-12-10 | 1994-09-06 | Merck & Co., Inc. | N,N-diacylpiperazine tachykinin antagonists |
| IL111730A (en) * | 1993-11-29 | 1998-12-06 | Fujisawa Pharmaceutical Co | Piperazine derivatives, processes for their preparation and pharmaceutical preparations containing them |
| US5607936A (en) * | 1994-09-30 | 1997-03-04 | Merck & Co., Inc. | Substituted aryl piperazines as neurokinin antagonists |
-
1996
- 1996-05-01 BR BR9610277A patent/BR9610277A/pt not_active Application Discontinuation
- 1996-08-29 IL IL12311296A patent/IL123112A/en not_active IP Right Cessation
- 1996-08-29 HU HU9802552A patent/HUP9802552A3/hu unknown
- 1996-08-29 EP EP96931188A patent/EP0850236B1/en not_active Expired - Lifetime
- 1996-08-29 ES ES96931188T patent/ES2158345T3/es not_active Expired - Lifetime
- 1996-08-29 CZ CZ98228A patent/CZ22898A3/cs unknown
- 1996-08-29 JP JP51006997A patent/JP3447745B2/ja not_active Expired - Lifetime
- 1996-08-29 CN CN96197720A patent/CN1111529C/zh not_active Expired - Fee Related
- 1996-08-29 AT AT96931188T patent/ATE202776T1/de not_active IP Right Cessation
- 1996-08-29 PL PL96325339A patent/PL325339A1/xx unknown
- 1996-08-29 WO PCT/IB1996/001018 patent/WO1997008166A1/en not_active Application Discontinuation
- 1996-08-29 DE DE69613705T patent/DE69613705T2/de not_active Expired - Lifetime
- 1996-08-29 AU AU69979/96A patent/AU708834B2/en not_active Ceased
- 1996-08-29 SK SK274-98A patent/SK27498A3/sk unknown
- 1996-08-29 CA CA002228370A patent/CA2228370C/en not_active Expired - Fee Related
-
1998
- 1998-02-27 NO NO980848A patent/NO980848L/no not_active Application Discontinuation
-
2000
- 2000-05-24 JP JP2000153870A patent/JP3315970B2/ja not_active Expired - Fee Related
-
2001
- 2001-09-20 GR GR20010401532T patent/GR3036675T3/el not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| HUP9802552A2 (hu) | 1999-10-28 |
| JP3315970B2 (ja) | 2002-08-19 |
| HUP9802552A3 (en) | 1999-11-29 |
| DE69613705D1 (de) | 2001-08-09 |
| EP0850236B1 (en) | 2001-07-04 |
| JPH10511105A (ja) | 1998-10-27 |
| CN1200120A (zh) | 1998-11-25 |
| AU708834B2 (en) | 1999-08-12 |
| JP2000344766A (ja) | 2000-12-12 |
| CA2228370A1 (en) | 1997-03-06 |
| ATE202776T1 (de) | 2001-07-15 |
| WO1997008166A1 (en) | 1997-03-06 |
| IL123112A0 (en) | 1998-09-24 |
| CN1111529C (zh) | 2003-06-18 |
| BR9610277A (pt) | 1999-07-06 |
| IL123112A (en) | 2001-04-30 |
| JP3447745B2 (ja) | 2003-09-16 |
| NO980848D0 (no) | 1998-02-27 |
| CZ22898A3 (cs) | 1998-07-15 |
| AU6997996A (en) | 1997-03-19 |
| EP0850236A1 (en) | 1998-07-01 |
| GR3036675T3 (en) | 2001-12-31 |
| NO980848L (no) | 1998-04-30 |
| PL325339A1 (en) | 1998-07-20 |
| CA2228370C (en) | 2002-10-01 |
| ES2158345T3 (es) | 2001-09-01 |
| DE69613705T2 (de) | 2002-05-16 |
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