CA2137221C - Preparation of 3,4,4-trisubstituted piperidinyl-n-alkylcarboxylates and intermediates - Google Patents
Preparation of 3,4,4-trisubstituted piperidinyl-n-alkylcarboxylates and intermediates Download PDFInfo
- Publication number
- CA2137221C CA2137221C CA2137221A CA2137221A CA2137221C CA 2137221 C CA2137221 C CA 2137221C CA 2137221 A CA2137221 A CA 2137221A CA 2137221 A CA2137221 A CA 2137221A CA 2137221 C CA2137221 C CA 2137221C
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- Prior art keywords
- compound
- alkyl
- crystalline
- salt
- compounds
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- MQZOZIODQPLFRF-SSLSWHBASA-N 2-methylpropyl 2-[[(2s)-2-benzyl-3-[(3r,4r)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]propanoyl]amino]acetate Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@@H](C(=O)NCC(=O)OCC(C)C)CC=2C=CC=CC=2)=CC=CC(O)=C1 MQZOZIODQPLFRF-SSLSWHBASA-N 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 2
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/10—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
- C07D211/14—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/164,074 | 1993-12-08 | ||
| US08/164,074 US5434171A (en) | 1993-12-08 | 1993-12-08 | Preparation of 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates and intermediates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2137221A1 CA2137221A1 (en) | 1995-06-09 |
| CA2137221C true CA2137221C (en) | 2011-02-22 |
Family
ID=22592858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2137221A Expired - Fee Related CA2137221C (en) | 1993-12-08 | 1994-12-02 | Preparation of 3,4,4-trisubstituted piperidinyl-n-alkylcarboxylates and intermediates |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US5434171A (en, 2012) |
| EP (3) | EP0657428B1 (en, 2012) |
| JP (2) | JP3834075B2 (en, 2012) |
| KR (1) | KR100356239B1 (en, 2012) |
| CN (2) | CN1057294C (en, 2012) |
| AT (1) | ATE200279T1 (en, 2012) |
| AU (1) | AU681198B2 (en, 2012) |
| BR (1) | BR9404842A (en, 2012) |
| CA (1) | CA2137221C (en, 2012) |
| CO (1) | CO4290427A1 (en, 2012) |
| CZ (1) | CZ290559B6 (en, 2012) |
| DE (1) | DE69427017T2 (en, 2012) |
| DK (1) | DK0657428T3 (en, 2012) |
| ES (1) | ES2155844T3 (en, 2012) |
| FI (2) | FI106455B (en, 2012) |
| GR (1) | GR3036136T3 (en, 2012) |
| HU (1) | HUT71489A (en, 2012) |
| IL (1) | IL111843A (en, 2012) |
| MY (1) | MY121543A (en, 2012) |
| NO (1) | NO302884B1 (en, 2012) |
| NZ (1) | NZ270039A (en, 2012) |
| PE (1) | PE41495A1 (en, 2012) |
| PL (1) | PL181734B1 (en, 2012) |
| PT (1) | PT657428E (en, 2012) |
| RU (1) | RU2145958C1 (en, 2012) |
| SI (1) | SI0657428T1 (en, 2012) |
| TW (1) | TW290540B (en, 2012) |
| UA (1) | UA52577C2 (en, 2012) |
| YU (2) | YU49312B (en, 2012) |
| ZA (1) | ZA949584B (en, 2012) |
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| HN1999000149A (es) * | 1998-09-09 | 2000-01-12 | Pfizer Prod Inc | Derivados de 4,4-biarilpiperidina |
| GB9912410D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912413D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912415D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912411D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912417D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| GB9912416D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
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| CA2449175A1 (en) * | 2001-06-05 | 2002-12-12 | University Of Chicago | Use of methylnaltrexone to treat immune suppression |
| US20030068829A1 (en) * | 2001-06-25 | 2003-04-10 | Symyx Technologies, Inc. | High throughput crystallographic screening of materials |
| DK1436012T3 (en) | 2001-10-18 | 2018-01-22 | Nektar Therapeutics | Polymer Conjugates of Opioid Antagonists |
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| US6992090B2 (en) * | 2003-06-16 | 2006-01-31 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| FR2861304B1 (fr) * | 2003-10-23 | 2008-07-18 | Univ Grenoble 1 | Modulateurs des canaux cftr |
| US20050148630A1 (en) * | 2003-12-02 | 2005-07-07 | Carpenter Randall L. | Methods of preventing and treating non-opioid induced gastrointestinal dysfunction |
| US8946262B2 (en) * | 2003-12-04 | 2015-02-03 | Adolor Corporation | Methods of preventing and treating gastrointestinal dysfunction |
| EA018427B1 (ru) * | 2003-12-16 | 2013-07-30 | Нектар Терапьютикс | Химически модифицированный налоксон |
| US20060182692A1 (en) * | 2003-12-16 | 2006-08-17 | Fishburn C S | Chemically modified small molecules |
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| TWI489984B (zh) | 2006-08-04 | 2015-07-01 | Wyeth Corp | 用於非經腸道傳輸化合物之配方及其用途 |
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| ES2540551T3 (es) | 2007-03-29 | 2015-07-10 | Wyeth Llc | Antagonistas de receptores opioides periféricos y usos de los mismos |
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| CN103360302B (zh) * | 2012-03-29 | 2015-08-26 | 北大方正集团有限公司 | 阿维莫泮的纯化方法 |
| WO2016064914A1 (en) | 2014-10-20 | 2016-04-28 | Elysium Therapeutics, Inc. | Diversion-resistant opioid formulations |
| JP2018534269A (ja) | 2015-10-01 | 2018-11-22 | エリージウム セラピューティクス， インコーポレイテッド | 過剰摂取および乱用に抵抗性のポリサブユニットオピオイドプロドラッグ |
| US10335406B2 (en) | 2015-10-01 | 2019-07-02 | Elysium Therapeutics, Inc. | Opioid compositions resistant to overdose and abuse |
| EP3595663A4 (en) | 2017-03-17 | 2021-01-13 | Elysium Therapeutics, Inc. | MULTI-UNIT OPIOID MEDICINES RESISTANT TO OVERDOSE AND ABUSE |
| WO2024090512A1 (ja) * | 2022-10-27 | 2024-05-02 | 株式会社京都創薬研究所 | ナフタレン誘導体の結晶 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4891379A (en) * | 1987-04-16 | 1990-01-02 | Kabushiki Kaisha Kobe Seikosho | Piperidine opioid antagonists |
| US5136040A (en) * | 1991-02-26 | 1992-08-04 | Eli Lilly And Company | Preparation of substituted tetrahydropyridines |
| US5250542A (en) * | 1991-03-29 | 1993-10-05 | Eli Lilly And Company | Peripherally selective piperidine carboxylate opioid antagonists |
| NZ242117A (en) * | 1991-03-29 | 1994-11-25 | Lilly Co Eli | 4-phenylpiperidine derivatives and medicaments containing them |
| US5159081A (en) * | 1991-03-29 | 1992-10-27 | Eli Lilly And Company | Intermediates of peripherally selective n-carbonyl-3,4,4-trisubstituted piperidine opioid antagonists |
-
1993
- 1993-12-08 US US08/164,074 patent/US5434171A/en not_active Expired - Lifetime
-
1994
- 1994-12-01 ZA ZA949584A patent/ZA949584B/xx unknown
- 1994-12-01 NZ NZ270039A patent/NZ270039A/en not_active IP Right Cessation
- 1994-12-01 IL IL11184394A patent/IL111843A/xx not_active IP Right Cessation
- 1994-12-01 PE PE1994256135A patent/PE41495A1/es not_active Application Discontinuation
- 1994-12-01 AU AU79170/94A patent/AU681198B2/en not_active Ceased
- 1994-12-01 CZ CZ19942992A patent/CZ290559B6/cs not_active IP Right Cessation
- 1994-12-01 JP JP29835694A patent/JP3834075B2/ja not_active Expired - Fee Related
- 1994-12-01 TW TW083111189A patent/TW290540B/zh not_active IP Right Cessation
- 1994-12-01 PL PL94306068A patent/PL181734B1/pl not_active IP Right Cessation
- 1994-12-02 CO CO94055028A patent/CO4290427A1/es unknown
- 1994-12-02 DK DK94308951T patent/DK0657428T3/da active
- 1994-12-02 HU HU9403466A patent/HUT71489A/hu unknown
- 1994-12-02 FI FI945703A patent/FI106455B/fi not_active IP Right Cessation
- 1994-12-02 DE DE69427017T patent/DE69427017T2/de not_active Expired - Lifetime
- 1994-12-02 BR BR9404842A patent/BR9404842A/pt not_active Application Discontinuation
- 1994-12-02 AT AT94308951T patent/ATE200279T1/de not_active IP Right Cessation
- 1994-12-02 ES ES94308951T patent/ES2155844T3/es not_active Expired - Lifetime
- 1994-12-02 PT PT94308951T patent/PT657428E/pt unknown
- 1994-12-02 EP EP94308951A patent/EP0657428B1/en not_active Expired - Lifetime
- 1994-12-02 SI SI9430367T patent/SI0657428T1/xx unknown
- 1994-12-02 NO NO944644A patent/NO302884B1/no not_active IP Right Cessation
- 1994-12-02 YU YU70294A patent/YU49312B/sh unknown
- 1994-12-02 EP EP05077072A patent/EP1607387A3/en not_active Withdrawn
- 1994-12-02 RU RU94042903A patent/RU2145958C1/ru not_active IP Right Cessation
- 1994-12-02 CA CA2137221A patent/CA2137221C/en not_active Expired - Fee Related
- 1994-12-02 EP EP99203390A patent/EP0984004A3/en not_active Withdrawn
- 1994-12-02 UA UA94129124A patent/UA52577C2/uk unknown
- 1994-12-02 YU YU82304A patent/YU82304A/sh unknown
- 1994-12-03 CN CN94119376A patent/CN1057294C/zh not_active Expired - Fee Related
- 1994-12-05 MY MYPI94003238A patent/MY121543A/en unknown
- 1994-12-05 KR KR1019940032794A patent/KR100356239B1/ko not_active Expired - Fee Related
-
1998
- 1998-12-03 CN CN98123069A patent/CN1121387C/zh not_active Expired - Fee Related
-
2000
- 2000-02-17 FI FI20000353A patent/FI106860B/fi not_active IP Right Cessation
-
2001
- 2001-06-27 GR GR20010400990T patent/GR3036136T3/el not_active IP Right Cessation
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2005
- 2005-10-18 JP JP2005303195A patent/JP2006070042A/ja active Pending
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