SK147297A3 - Piperazino derivatives as neurokinin antagonists - Google Patents
Piperazino derivatives as neurokinin antagonists Download PDFInfo
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- SK147297A3 SK147297A3 SK1472-97A SK147297A SK147297A3 SK 147297 A3 SK147297 A3 SK 147297A3 SK 147297 A SK147297 A SK 147297A SK 147297 A3 SK147297 A3 SK 147297A3
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- 239000005557 antagonist Substances 0.000 title abstract description 4
- -1 Piperazino Chemical class 0.000 title description 39
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 229910052757 nitrogen Inorganic materials 0.000 claims description 23
- 229910052799 carbon Inorganic materials 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 150000003839 salts Chemical group 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 16
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 13
- 125000004432 carbon atom Chemical group C* 0.000 claims description 11
- 229910052794 bromium Inorganic materials 0.000 claims description 10
- 229910052740 iodine Inorganic materials 0.000 claims description 9
- 229910052801 chlorine Inorganic materials 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 5
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 3
- 229910004013 NO 2 Inorganic materials 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 150000001875 compounds Chemical class 0.000 abstract description 194
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- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 36
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 36
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- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 25
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- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 21
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- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 description 17
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 16
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- YUBDLZGUSSWQSS-UHFFFAOYSA-N 1-benzylpiperidin-4-amine Chemical compound C1CC(N)CCN1CC1=CC=CC=C1 YUBDLZGUSSWQSS-UHFFFAOYSA-N 0.000 description 14
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- 238000012360 testing method Methods 0.000 description 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 10
- PUJZPGUYDJGSAC-UHFFFAOYSA-N 2-(3,4-dichlorophenyl)piperazine Chemical compound C1=C(Cl)C(Cl)=CC=C1C1NCCNC1 PUJZPGUYDJGSAC-UHFFFAOYSA-N 0.000 description 9
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- DYHSDKLCOJIUFX-UHFFFAOYSA-N tert-butoxycarbonyl anhydride Chemical compound CC(C)(C)OC(=O)OC(=O)OC(C)(C)C DYHSDKLCOJIUFX-UHFFFAOYSA-N 0.000 description 9
- QDZOEBFLNHCSSF-PFFBOGFISA-N (2S)-2-[[(2R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2R)-2-amino-5-carbamimidamidopentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CCCNC(N)=N)C1=CC=CC=C1 QDZOEBFLNHCSSF-PFFBOGFISA-N 0.000 description 8
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 8
- 229910001868 water Inorganic materials 0.000 description 8
- RIMRLBGNCLMSNH-UHFFFAOYSA-N 2-phenylpiperazine Chemical compound C1NCCNC1C1=CC=CC=C1 RIMRLBGNCLMSNH-UHFFFAOYSA-N 0.000 description 7
- HVFQJWGYVXKLTE-UHFFFAOYSA-N 3,5-bis(trifluoromethyl)benzoic acid Chemical compound OC(=O)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1 HVFQJWGYVXKLTE-UHFFFAOYSA-N 0.000 description 7
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- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 description 5
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Classifications
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- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P27/14—Decongestants or antiallergics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P9/00—Drugs for disorders of the cardiovascular system
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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
- 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
-
- 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
- C07D487/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/432,739 US5719156A (en) | 1995-05-02 | 1995-05-02 | Piperazino derivatives as neurokinin antagonists |
| US308495P | 1995-08-31 | 1995-08-31 | |
| PCT/US1996/005660 WO1996034864A1 (en) | 1995-05-02 | 1996-05-01 | Piperazino derivatives as neurokinin antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SK147297A3 true SK147297A3 (en) | 1998-07-08 |
Family
ID=26671291
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK1472-97A SK147297A3 (en) | 1995-05-02 | 1996-05-01 | Piperazino derivatives as neurokinin antagonists |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP0823906B1 (de) |
| JP (1) | JP4173912B2 (de) |
| KR (1) | KR19990008230A (de) |
| CN (1) | CN1111528C (de) |
| AT (1) | ATE244712T1 (de) |
| AU (1) | AU705683B2 (de) |
| BR (1) | BR9608245A (de) |
| CA (1) | CA2218887C (de) |
| CZ (1) | CZ342397A3 (de) |
| DE (1) | DE69629023T2 (de) |
| ES (1) | ES2197238T3 (de) |
| HU (1) | HUP9801382A3 (de) |
| MX (1) | MX9708416A (de) |
| NO (1) | NO315852B1 (de) |
| NZ (1) | NZ307716A (de) |
| PL (1) | PL323235A1 (de) |
| SK (1) | SK147297A3 (de) |
| WO (1) | WO1996034864A1 (de) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5892039A (en) * | 1995-08-31 | 1999-04-06 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| TR199901570T2 (xx) * | 1996-10-30 | 1999-09-21 | Schering Corporation | N�rokinin antagonistleri olarak piperazin t�revleri |
| US5968929A (en) * | 1996-10-30 | 1999-10-19 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5783579A (en) * | 1996-12-20 | 1998-07-21 | Schering Corporation | Spiro-substituted azacyclic-substituted piperazino derivatives as neurokinin antagonists |
| KR100420616B1 (ko) * | 1996-12-26 | 2004-05-17 | 동화약품공업주식회사 | 신규테레프탈산아미드유도체 |
| US6207665B1 (en) * | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
| AUPO735997A0 (en) * | 1997-06-17 | 1997-07-10 | Fujisawa Pharmaceutical Co., Ltd. | Piperazine derivatives |
| DE19737334A1 (de) * | 1997-08-27 | 1999-03-04 | Solvay Pharm Gmbh | 7-Phenyl-1,4-diazepan-Derivate, sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| TW591025B (en) | 2000-06-13 | 2004-06-11 | Fujisawa Pharmaceutical Co | Production of the piperazine derivative |
| AUPR237301A0 (en) * | 2001-01-02 | 2001-01-25 | Fujisawa Pharmaceutical Co., Ltd. | Benzhydryl derivatives |
| MXPA02002749A (es) * | 2001-03-27 | 2002-10-28 | Warner Lambert Co | Derivados de ciclohexilamina como antagonistas del subtipo selectivo del n-metil-d-aspartato. |
| UA75425C2 (en) | 2001-07-09 | 2006-04-17 | Piperazine oxime derivatives with antagonistic activity to nk-1 receptor, use thereof, a pharmaceutical composition based thereon, a method for producing and a method for producing intermediary compounds | |
| AUPR970701A0 (en) * | 2001-12-21 | 2002-01-24 | Fujisawa Pharmaceutical Co., Ltd. | Benzhydryl derivatives |
| CN107602317A (zh) * | 2017-08-02 | 2018-01-19 | 凯莱英医药集团（天津）股份有限公司 | 手性2‑氨基‑2‑芳基乙酸衍生物的制备方法 |
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 JP JP53335596A patent/JP4173912B2/ja not_active Expired - Fee Related
- 1996-05-01 CN CN96195171A patent/CN1111528C/zh not_active Expired - Fee Related
- 1996-05-01 EP EP96915342A patent/EP0823906B1/de not_active Expired - Lifetime
- 1996-05-01 AT AT96915342T patent/ATE244712T1/de not_active IP Right Cessation
- 1996-05-01 CA CA002218887A patent/CA2218887C/en not_active Expired - Fee Related
- 1996-05-01 AU AU57141/96A patent/AU705683B2/en not_active Ceased
- 1996-05-01 ES ES96915342T patent/ES2197238T3/es not_active Expired - Lifetime
- 1996-05-01 CZ CZ973423A patent/CZ342397A3/cs unknown
- 1996-05-01 BR BR9608245A patent/BR9608245A/pt not_active Application Discontinuation
- 1996-05-01 NZ NZ307716A patent/NZ307716A/en unknown
- 1996-05-01 WO PCT/US1996/005660 patent/WO1996034864A1/en not_active Application Discontinuation
- 1996-05-01 KR KR1019970707756A patent/KR19990008230A/ko active IP Right Grant
- 1996-05-01 MX MX9708416A patent/MX9708416A/es not_active IP Right Cessation
- 1996-05-01 PL PL96323235A patent/PL323235A1/xx unknown
- 1996-05-01 SK SK1472-97A patent/SK147297A3/sk unknown
- 1996-05-01 DE DE69629023T patent/DE69629023T2/de not_active Expired - Lifetime
- 1996-05-01 HU HU9801382A patent/HUP9801382A3/hu unknown
-
1997
- 1997-10-31 NO NO19975028A patent/NO315852B1/no not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| JP4173912B2 (ja) | 2008-10-29 |
| CZ342397A3 (cs) | 1998-03-18 |
| MX9708416A (es) | 1998-02-28 |
| CA2218887C (en) | 2008-04-29 |
| KR19990008230A (ko) | 1999-01-25 |
| CN1189829A (zh) | 1998-08-05 |
| CA2218887A1 (en) | 1996-11-07 |
| BR9608245A (pt) | 1999-05-04 |
| EP0823906A1 (de) | 1998-02-18 |
| WO1996034864A1 (en) | 1996-11-07 |
| NZ307716A (en) | 1999-10-28 |
| JPH11504921A (ja) | 1999-05-11 |
| ES2197238T3 (es) | 2004-01-01 |
| AU705683B2 (en) | 1999-05-27 |
| ATE244712T1 (de) | 2003-07-15 |
| HUP9801382A2 (hu) | 1999-06-28 |
| NO975028L (no) | 1997-12-30 |
| DE69629023D1 (de) | 2003-08-14 |
| NO315852B1 (no) | 2003-11-03 |
| NO975028D0 (no) | 1997-10-31 |
| HUP9801382A3 (en) | 2000-09-28 |
| DE69629023T2 (de) | 2004-04-22 |
| CN1111528C (zh) | 2003-06-18 |
| PL323235A1 (en) | 1998-03-16 |
| AU5714196A (en) | 1996-11-21 |
| EP0823906B1 (de) | 2003-07-09 |
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