CA2439149C - Acylated piperidine derivatives as melanocortin-4 receptor agonists - Google Patents
Acylated piperidine derivatives as melanocortin-4 receptor agonists Download PDFInfo
- Publication number
- CA2439149C CA2439149C CA2439149A CA2439149A CA2439149C CA 2439149 C CA2439149 C CA 2439149C CA 2439149 A CA2439149 A CA 2439149A CA 2439149 A CA2439149 A CA 2439149A CA 2439149 C CA2439149 C CA 2439149C
- Authority
- CA
- Canada
- Prior art keywords
- compound
- trans
- alkyl
- phenyl
- independently selected
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 CC*(C(*)C(C(*(C)N1*)I(C)C)C(N2CCC(*)(*)CC2)=O)C1I(C)S Chemical compound CC*(C(*)C(C(*(C)N1*)I(C)C)C(N2CCC(*)(*)CC2)=O)C1I(C)S 0.000 description 2
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
-
- A—HUMAN NECESSITIES
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
-
- 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
- C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
- C07D211/64—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Gynecology & Obstetrics (AREA)
- Child & Adolescent Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27225801P | 2001-02-28 | 2001-02-28 | |
| US60/272,258 | 2001-02-28 | ||
| US30057201P | 2001-06-22 | 2001-06-22 | |
| US60/300,572 | 2001-06-22 | ||
| PCT/US2002/005623 WO2002068387A2 (en) | 2001-02-28 | 2002-02-25 | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2439149A1 CA2439149A1 (en) | 2002-09-06 |
| CA2439149C true CA2439149C (en) | 2012-04-24 |
Family
ID=26955403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2439149A Expired - Fee Related CA2439149C (en) | 2001-02-28 | 2002-02-25 | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US7015235B2 (enExample) |
| EP (1) | EP1372653B1 (enExample) |
| JP (1) | JP4323169B2 (enExample) |
| AT (1) | ATE341327T1 (enExample) |
| AU (1) | AU2002255597B8 (enExample) |
| CA (1) | CA2439149C (enExample) |
| DE (1) | DE60215132T2 (enExample) |
| ES (1) | ES2272703T3 (enExample) |
| WO (1) | WO2002068387A2 (enExample) |
Families Citing this family (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4104983B2 (ja) * | 2001-02-28 | 2008-06-18 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン−４受容体作動薬としてのアシル化ピペリジン誘導体 |
| ATE430565T1 (de) | 2001-02-28 | 2009-05-15 | Merck & Co Inc | Acylierte piperidinderivate als melanocortin-4- rezeptoragonisten |
| US6911447B2 (en) | 2001-04-25 | 2005-06-28 | The Procter & Gamble Company | Melanocortin receptor ligands |
| ATE411021T1 (de) | 2001-07-18 | 2008-10-15 | Merck & Co Inc | Überbrückte piperidinderivate als melanocortin- rezeptor-agonisten |
| US7115607B2 (en) | 2001-07-25 | 2006-10-03 | Amgen Inc. | Substituted piperazinyl amides and methods of use |
| US6977264B2 (en) | 2001-07-25 | 2005-12-20 | Amgen Inc. | Substituted piperidines and methods of use |
| CA2462200A1 (en) | 2001-08-10 | 2003-02-20 | Palatin Technologies, Inc. | Peptidomimetics of biologically active metallopeptides |
| US7354923B2 (en) | 2001-08-10 | 2008-04-08 | Palatin Technologies, Inc. | Piperazine melanocortin-specific compounds |
| US7456184B2 (en) | 2003-05-01 | 2008-11-25 | Palatin Technologies Inc. | Melanocortin receptor-specific compounds |
| US7026335B2 (en) | 2002-04-30 | 2006-04-11 | The Procter & Gamble Co. | Melanocortin receptor ligands |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| WO2004024720A1 (en) | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Piperazine urea derivatives as melanocortin-4 receptor agonists |
| US7132539B2 (en) | 2002-10-23 | 2006-11-07 | The Procter & Gamble Company | Melanocortin receptor ligands |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| WO2004078717A1 (en) * | 2003-03-03 | 2004-09-16 | Merck & Co., Inc. | Acylated piperazine derivatives as melanocortin-4 receptor agonists |
| US6998488B2 (en) | 2003-03-10 | 2006-02-14 | Merck & Co., Inc. | Process and intermediates for the preparation of 4-aryl piperidines |
| US7276520B2 (en) | 2003-03-26 | 2007-10-02 | Merck & Co., Inc. | Bicyclic piperidine derivatives as melanocortin-4 receptor agonists |
| JP3856815B2 (ja) | 2003-04-04 | 2006-12-13 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン−４受容体アゴニストとしてのアシル化スピロピペリジン誘導体 |
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| JP6606491B2 (ja) | 2013-06-05 | 2019-11-13 | 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ｃの超高純度アゴニスト、その作成および使用方法 |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| BR112017003745A2 (pt) | 2014-08-29 | 2017-12-05 | Tes Pharma S R L | inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico |
| US10080884B2 (en) | 2014-12-29 | 2018-09-25 | Ethicon Llc | Methods and devices for activating brown adipose tissue using electrical energy |
| US10092738B2 (en) | 2014-12-29 | 2018-10-09 | Ethicon Llc | Methods and devices for inhibiting nerves when activating brown adipose tissue |
| JP2020500838A (ja) | 2016-10-14 | 2020-01-16 | ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ | Α−アミノ−β−カルボキシムコン酸セミアルデヒドデカルボキシラーゼの阻害剤 |
| WO2018106518A1 (en) | 2016-12-06 | 2018-06-14 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| WO2018118670A1 (en) | 2016-12-20 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
| KR20210111248A (ko) | 2018-11-20 | 2021-09-10 | 테스 파마 에스.알.엘. | α-아미노-β-카르복시뮤콘산 세미알데하이드 데카르복실라제의 저해제 |
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| DE69429768T2 (de) * | 1993-04-05 | 2002-09-19 | Competitive Technologies, Inc. | Diagnose und behandlung von erektilen funktionsstörungen |
| JP2001526178A (ja) | 1997-08-28 | 2001-12-18 | メルク エンド カムパニー インコーポレーテッド | ピロリジン系およびピペリジン系ケモカイン受容体活性調節剤 |
| US6166037A (en) * | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
| JP2003505435A (ja) * | 1999-06-04 | 2003-02-12 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン−４受容体ゴニストとしての置換ピペリジン |
| SK11452002A3 (sk) | 2000-02-11 | 2003-03-04 | Vertex Pharmaceuticals Incorporated | Deriváty piperazínu a piperidínu na použitie pri liečení alebo prevencii poškodenia neurónov |
| US6458790B2 (en) * | 2000-03-23 | 2002-10-01 | Merck & Co., Inc. | Substituted piperidines as melanocortin receptor agonists |
| EP1289526A4 (en) * | 2000-05-30 | 2005-03-16 | Merck & Co Inc | MELANOCORTIN RECEPTOR AGONISTS |
| US6511994B2 (en) * | 2000-10-11 | 2003-01-28 | Merck & Co., Inc. | Modulators of CCR5 chemokine receptor activity |
| ATE430565T1 (de) | 2001-02-28 | 2009-05-15 | Merck & Co Inc | Acylierte piperidinderivate als melanocortin-4- rezeptoragonisten |
| JP4104983B2 (ja) * | 2001-02-28 | 2008-06-18 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン−４受容体作動薬としてのアシル化ピペリジン誘導体 |
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2002
- 2002-02-25 JP JP2002567901A patent/JP4323169B2/ja not_active Expired - Fee Related
- 2002-02-25 ES ES02725001T patent/ES2272703T3/es not_active Expired - Lifetime
- 2002-02-25 AU AU2002255597A patent/AU2002255597B8/en not_active Ceased
- 2002-02-25 WO PCT/US2002/005623 patent/WO2002068387A2/en not_active Ceased
- 2002-02-25 US US10/468,515 patent/US7015235B2/en not_active Expired - Lifetime
- 2002-02-25 CA CA2439149A patent/CA2439149C/en not_active Expired - Fee Related
- 2002-02-25 AT AT02725001T patent/ATE341327T1/de not_active IP Right Cessation
- 2002-02-25 EP EP02725001A patent/EP1372653B1/en not_active Expired - Lifetime
- 2002-02-25 DE DE60215132T patent/DE60215132T2/de not_active Expired - Lifetime
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2005
- 2005-09-30 US US11/239,721 patent/US20060035935A1/en not_active Abandoned
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| Publication number | Publication date |
|---|---|
| EP1372653A4 (en) | 2005-10-05 |
| JP2004527498A (ja) | 2004-09-09 |
| US7015235B2 (en) | 2006-03-21 |
| US20060035935A1 (en) | 2006-02-16 |
| DE60215132D1 (de) | 2006-11-16 |
| ATE341327T1 (de) | 2006-10-15 |
| AU2002255597B8 (en) | 2006-10-26 |
| EP1372653A2 (en) | 2004-01-02 |
| WO2002068387A8 (en) | 2003-09-04 |
| WO2002068387A3 (en) | 2003-02-20 |
| AU2002255597B2 (en) | 2006-03-02 |
| CA2439149A1 (en) | 2002-09-06 |
| JP4323169B2 (ja) | 2009-09-02 |
| EP1372653B1 (en) | 2006-10-04 |
| DE60215132T2 (de) | 2007-08-23 |
| WO2002068387A2 (en) | 2002-09-06 |
| US20040097546A1 (en) | 2004-05-20 |
| ES2272703T3 (es) | 2007-05-01 |
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