DE60215132T2 - Acylierte piperidin-derivate als melanocortin-4-rezeptor-agonisten - Google Patents
Acylierte piperidin-derivate als melanocortin-4-rezeptor-agonisten Download PDFInfo
- Publication number
- DE60215132T2 DE60215132T2 DE60215132T DE60215132T DE60215132T2 DE 60215132 T2 DE60215132 T2 DE 60215132T2 DE 60215132 T DE60215132 T DE 60215132T DE 60215132 T DE60215132 T DE 60215132T DE 60215132 T2 DE60215132 T2 DE 60215132T2
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- phenyl
- independently selected
- heteroaryl
- substituted
- 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 - Lifetime
Links
- 0 C*(C1)N(*)C[C@@](*)[C@@]1(*)C(N1CCC(*)(*)CC1)=O Chemical compound C*(C1)N(*)C[C@@](*)[C@@]1(*)C(N1CCC(*)(*)CC1)=O 0.000 description 7
- KNBARVOBYLRMMT-DCWQJPKNSA-N CCN(CC[C@H]1C(N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)=O)CC1c(cc1)ccc1F Chemical compound CCN(CC[C@H]1C(N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)=O)CC1c(cc1)ccc1F KNBARVOBYLRMMT-DCWQJPKNSA-N 0.000 description 2
- MCTADDXBWAMMJL-DCWQJPKNSA-N CC(C)(CO1)N(CC(CC2)(CCN2C([C@H](CCN(C)C2)C2c(cc2)ccc2Cl)=O)C2CCCCC2)C1=O Chemical compound CC(C)(CO1)N(CC(CC2)(CCN2C([C@H](CCN(C)C2)C2c(cc2)ccc2Cl)=O)C2CCCCC2)C1=O MCTADDXBWAMMJL-DCWQJPKNSA-N 0.000 description 1
- GZQUOGPCEWEENG-UHFFFAOYSA-N CC(C)N(CC1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(c(F)c1)ccc1F Chemical compound CC(C)N(CC1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(c(F)c1)ccc1F GZQUOGPCEWEENG-UHFFFAOYSA-N 0.000 description 1
- VWFHLCARTPZBHX-ONJSCSTBSA-N CC(C)N(CC1[C@@H](N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)O)CC1c(c(F)c1)ccc1F Chemical compound CC(C)N(CC1[C@@H](N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)O)CC1c(c(F)c1)ccc1F VWFHLCARTPZBHX-ONJSCSTBSA-N 0.000 description 1
- VSIFOQCHGOPMQB-GEVKEYJPSA-N CC(C)N(CCC1C(N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)=O)C[C@H]1c(cc1)ccc1F Chemical compound CC(C)N(CCC1C(N(CC2)CCC2(C2CCCCC2)C(NC(C)(C)C)=O)=O)C[C@H]1c(cc1)ccc1F VSIFOQCHGOPMQB-GEVKEYJPSA-N 0.000 description 1
- GZQUOGPCEWEENG-FXDYGKIASA-N CC(C)N(C[C@H]1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(c(F)c1)ccc1F Chemical compound CC(C)N(C[C@H]1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(c(F)c1)ccc1F GZQUOGPCEWEENG-FXDYGKIASA-N 0.000 description 1
- HSKFWUNQSAWFDR-UHFFFAOYSA-N CC(CO1)N(C)C1=O Chemical compound CC(CO1)N(C)C1=O HSKFWUNQSAWFDR-UHFFFAOYSA-N 0.000 description 1
- KYRDJBPOBQOPNY-UHFFFAOYSA-N CCN(CCC1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(cc1)ccc1F Chemical compound CCN(CCC1C(N(CC2)CCC2(CN(C(C)(C)CO2)C2=O)C2CCCCC2)=O)CC1c(cc1)ccc1F KYRDJBPOBQOPNY-UHFFFAOYSA-N 0.000 description 1
- SVSWYHCUSYVBHW-UHFFFAOYSA-N CN(C1(CC1)CO1)C1=O Chemical compound CN(C1(CC1)CO1)C1=O SVSWYHCUSYVBHW-UHFFFAOYSA-N 0.000 description 1
- QWEXMZQMVVAVQB-UHFFFAOYSA-N CN(C1(CCCC1)CO1)C1=O Chemical compound CN(C1(CCCC1)CO1)C1=O QWEXMZQMVVAVQB-UHFFFAOYSA-N 0.000 description 1
- HWHNFJYQDMSYAF-UHFFFAOYSA-N Cc1nnn[n]1C Chemical compound Cc1nnn[n]1C HWHNFJYQDMSYAF-UHFFFAOYSA-N 0.000 description 1
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)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Pregnancy & Childbirth (AREA)
- Child & Adolescent Psychology (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 | |
| US272258P | 2001-02-28 | ||
| US30057201P | 2001-06-22 | 2001-06-22 | |
| US300572P | 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 |
|---|---|
| DE60215132D1 DE60215132D1 (de) | 2006-11-16 |
| DE60215132T2 true DE60215132T2 (de) | 2007-08-23 |
Family
ID=26955403
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60215132T Expired - Lifetime DE60215132T2 (de) | 2001-02-28 | 2002-02-25 | Acylierte piperidin-derivate als melanocortin-4-rezeptor-agonisten |
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 |
|---|---|---|---|---|
| DE60232238D1 (de) | 2001-02-28 | 2009-06-18 | Merck & Co Inc | Acylierte piperidinderivate als melanocortin-4-rezeptoragonisten |
| IL157253A0 (en) * | 2001-02-28 | 2004-02-19 | Merck & Co Inc | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
| US6911447B2 (en) | 2001-04-25 | 2005-06-28 | The Procter & Gamble Company | Melanocortin receptor ligands |
| DE60229393D1 (de) | 2001-07-18 | 2008-11-27 | Merck & Co Inc | Überbrückte piperidinderivate als melanocortin-rezeptor-agonisten |
| US6977264B2 (en) | 2001-07-25 | 2005-12-20 | Amgen Inc. | Substituted piperidines and methods of use |
| US7115607B2 (en) | 2001-07-25 | 2006-10-03 | Amgen Inc. | Substituted piperazinyl amides and methods of use |
| WO2003013571A1 (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 |
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| US6998488B2 (en) | 2003-03-10 | 2006-02-14 | Merck & Co., Inc. | Process and intermediates for the preparation of 4-aryl piperidines |
| EP1610789B1 (en) * | 2003-03-26 | 2010-07-21 | Merck Sharp & Dohme Corp. | Bicyclic piperidine derivatives as melanocortin-4 receptor agonists |
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| AR044510A1 (es) * | 2003-04-14 | 2005-09-14 | Merck & Co Inc | Procedimiento e intermedios para preparar acidos carboxilicos de pirrolidina |
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| ATE547404T1 (de) | 2003-09-22 | 2012-03-15 | Msd Kk | Piperidinderivate |
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| JP2008506779A (ja) | 2004-07-19 | 2008-03-06 | 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受容体作用薬としてのアシル化ピペリジン誘導体 |
| EP1814590B2 (en) | 2004-11-01 | 2013-12-11 | Amylin Pharmaceuticals, Inc. | Treatment of obesity and related disorders |
| GB0428514D0 (en) * | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| BRPI0610580B8 (pt) | 2005-05-30 | 2021-05-25 | Banyu Pharma Co Ltd | composto derivado de piperidina |
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| JP2003534377A (ja) * | 2000-05-30 | 2003-11-18 | メルク エンド カムパニー インコーポレーテッド | メラノコルチン受容体作働薬 |
| US6511994B2 (en) * | 2000-10-11 | 2003-01-28 | Merck & Co., Inc. | Modulators of CCR5 chemokine receptor activity |
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| IL157253A0 (en) * | 2001-02-28 | 2004-02-19 | Merck & Co Inc | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
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- 2002-02-25 AT AT02725001T patent/ATE341327T1/de not_active IP Right Cessation
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- 2002-02-25 JP JP2002567901A patent/JP4323169B2/ja not_active Expired - Fee Related
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| EP1372653A2 (en) | 2004-01-02 |
| US20060035935A1 (en) | 2006-02-16 |
| JP4323169B2 (ja) | 2009-09-02 |
| JP2004527498A (ja) | 2004-09-09 |
| CA2439149C (en) | 2012-04-24 |
| ES2272703T3 (es) | 2007-05-01 |
| EP1372653B1 (en) | 2006-10-04 |
| AU2002255597B8 (en) | 2006-10-26 |
| AU2002255597B2 (en) | 2006-03-02 |
| WO2002068387A3 (en) | 2003-02-20 |
| ATE341327T1 (de) | 2006-10-15 |
| WO2002068387A2 (en) | 2002-09-06 |
| US20040097546A1 (en) | 2004-05-20 |
| DE60215132D1 (de) | 2006-11-16 |
| WO2002068387A8 (en) | 2003-09-04 |
| US7015235B2 (en) | 2006-03-21 |
| CA2439149A1 (en) | 2002-09-06 |
| EP1372653A4 (en) | 2005-10-05 |
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