DE60224404D1 - Substiuierte piperidine als melanocortinrezeptor-modulatoren - Google Patents
Substiuierte piperidine als melanocortinrezeptor-modulatorenInfo
- Publication number
- DE60224404D1 DE60224404D1 DE60224404T DE60224404T DE60224404D1 DE 60224404 D1 DE60224404 D1 DE 60224404D1 DE 60224404 T DE60224404 T DE 60224404T DE 60224404 T DE60224404 T DE 60224404T DE 60224404 D1 DE60224404 D1 DE 60224404D1
- Authority
- DE
- Germany
- Prior art keywords
- melanocortin receptor
- receptor modulators
- substituted piperidines
- compounds
- prophylaxis
- 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
- 102000004378 Melanocortin Receptors Human genes 0.000 title abstract 2
- 108090000950 Melanocortin Receptors Proteins 0.000 title abstract 2
- 150000003053 piperidines Chemical class 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 238000011321 prophylaxis Methods 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 208000008589 Obesity Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
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- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P9/12—Antihypertensives
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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
- C07D211/18—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
- C07D211/26—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 nitrogen atoms
- C07D211/28—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 nitrogen atoms to which a second hetero atom is attached
-
- 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
-
- 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
- C07D401/12—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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Biophysics (AREA)
- Psychiatry (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Child & Adolescent Psychology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30773301P | 2001-07-25 | 2001-07-25 | |
| US307733P | 2001-07-25 | ||
| US10/205,649 US6977264B2 (en) | 2001-07-25 | 2002-07-24 | Substituted piperidines and methods of use |
| US205649 | 2002-07-24 | ||
| PCT/US2002/023616 WO2003009847A1 (en) | 2001-07-25 | 2002-07-25 | Substituted piperidines as modulators of the melanocortin receptor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60224404D1 true DE60224404D1 (de) | 2008-02-14 |
| DE60224404T2 DE60224404T2 (de) | 2008-12-18 |
Family
ID=26900632
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60224404T Expired - Lifetime DE60224404T2 (de) | 2001-07-25 | 2002-07-25 | Substiuierte piperidine als melanocortinrezeptormodulatoren |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US6977264B2 (de) |
| EP (1) | EP1416933B8 (de) |
| JP (1) | JP2005504028A (de) |
| AT (1) | ATE382353T1 (de) |
| AU (1) | AU2002319695B8 (de) |
| CA (1) | CA2452328A1 (de) |
| DE (1) | DE60224404T2 (de) |
| ES (1) | ES2296968T3 (de) |
| MX (1) | MXPA04000625A (de) |
| PL (1) | PL370373A1 (de) |
| WO (1) | WO2003009847A1 (de) |
Families Citing this family (131)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2439152C (en) | 2001-02-28 | 2008-06-17 | Merck & Co., Inc. | Acylated piperidine derivatives as melanocortin-4 receptor agonists |
| CA2453609C (en) | 2001-07-18 | 2010-05-04 | Merck & Co., Inc. | Bridged piperidine derivatives as melanocortin receptor agonists |
| US7115607B2 (en) * | 2001-07-25 | 2006-10-03 | Amgen Inc. | Substituted piperazinyl amides and methods of use |
| US7655658B2 (en) * | 2001-08-10 | 2010-02-02 | Palatin Technologies, Inc. | Thieno [2,3-D]pyrimidine-2,4-dione melanocortin-specific compounds |
| US7456184B2 (en) * | 2003-05-01 | 2008-11-25 | Palatin Technologies Inc. | Melanocortin receptor-specific compounds |
| US7732451B2 (en) * | 2001-08-10 | 2010-06-08 | Palatin Technologies, Inc. | Naphthalene-containing melanocortin receptor-specific small molecule |
| US7718802B2 (en) | 2001-08-10 | 2010-05-18 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific piperazine compounds |
| JP2005504043A (ja) | 2001-08-10 | 2005-02-10 | パラチン テクノロジーズ インク. | 生物学的に活性な金属ペプチド類のペプチド模倣体類 |
| US7354923B2 (en) | 2001-08-10 | 2008-04-08 | Palatin Technologies, Inc. | Piperazine melanocortin-specific compounds |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| AU2003268493A1 (en) | 2002-09-11 | 2004-04-30 | Merck & Co., Inc. | Piperazine urea derivatives as melanocortin-4 receptor agonists |
| WO2004081643A1 (en) * | 2002-12-20 | 2004-09-23 | Kaiser Aerospace & Electronics Corp. | Lenslet array with polarization conversion |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| AR043434A1 (es) | 2003-03-03 | 2005-07-27 | Merck & Co Inc | Derivados de piperizacina acilados como agonistas del receptor de melanocortina-4. composiciones farmaceuticas y usos |
| ES2286345T3 (es) * | 2003-03-20 | 2007-12-01 | Santhera Pharmaceuticals (Schweiz) Ag | Derivados de piperidina y piperazina substituidos como moduladores del receptor de melanocortina-4. |
| EP1460073A1 (de) * | 2003-03-20 | 2004-09-22 | MyoContract Ltd. | Substituierte Piperidin- und Piperazin-Derivative als Melanocortin-4 Receptor Modulatoren |
| EP1460069A1 (de) * | 2003-03-20 | 2004-09-22 | MyoContract Ltd. | Substituierte Cyclohexyl- und Piperidin-Derivative als Melanocortin-4 Receptor Modulatoren |
| JP2006521359A (ja) | 2003-03-26 | 2006-09-21 | 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受容体作働薬としての二環式ピペリジン誘導体 |
| US7968548B2 (en) * | 2003-05-01 | 2011-06-28 | Palatin Technologies, Inc. | Melanocortin receptor-specific piperazine compounds with diamine groups |
| US7727991B2 (en) | 2003-05-01 | 2010-06-01 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific single acyl piperazine compounds |
| US7727990B2 (en) | 2003-05-01 | 2010-06-01 | Palatin Technologies, Inc. | Melanocortin receptor-specific piperazine and keto-piperazine compounds |
| EP1648457A2 (de) | 2003-07-22 | 2006-04-26 | Merck & Co., Inc. | Piperidinderivate als melanocortin-4 rezeptoragonisten |
| ATE547404T1 (de) | 2003-09-22 | 2012-03-15 | Msd Kk | Piperidinderivate |
| EP1538159A1 (de) * | 2003-12-05 | 2005-06-08 | Santhera Pharmaceuticals (Schweiz) GmbH | Substituierte N-Benzyl-lactam Derivate als Melanocortin-4 Rezeptor Agonisten |
| WO2005097759A1 (en) | 2004-03-29 | 2005-10-20 | Merck & Co., Inc. | Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| EP1734963A4 (de) | 2004-04-02 | 2008-06-18 | Merck & Co Inc | Verfahren zur behandlung von menschen mit metabolischen und anthropometrischen störungen |
| US7709484B1 (en) | 2004-04-19 | 2010-05-04 | Palatin Technologies, Inc. | Substituted melanocortin receptor-specific piperazine compounds |
| GB0414438D0 (en) | 2004-06-28 | 2004-07-28 | Syngenta Participations Ag | Chemical compounds |
| 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 |
| FR2873691B1 (fr) * | 2004-07-29 | 2006-10-06 | Sanofi Synthelabo | Derives d'amino-piperidine, leur preparation et leur application en therapeutique |
| FR2873690B1 (fr) * | 2004-07-29 | 2006-10-13 | Sanofi Synthelabo | Derives d'oxopiperidine, leur preparation et leur application en therapeutique |
| WO2006017542A1 (en) | 2004-08-06 | 2006-02-16 | Merck & Co., Inc. | Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1 |
| AU2005272627A1 (en) | 2004-08-13 | 2006-02-23 | Amgen Inc. | Substituted benzofused heterocycles |
| GB0611907D0 (en) * | 2006-06-15 | 2006-07-26 | Glaxo Group Ltd | Compounds |
| NZ562766A (en) | 2005-05-30 | 2011-03-31 | Banyu Pharma Co Ltd | Piperidine derivatives as histamine-H3 receptor antagonists |
| US20070021433A1 (en) | 2005-06-03 | 2007-01-25 | Jian-Qiang Fan | Pharmacological chaperones for treating obesity |
| MY150098A (en) * | 2005-07-26 | 2013-11-29 | Glaxo Group Ltd | Benzylpiperazine derivates and their medical use |
| US20100216758A1 (en) | 2005-08-10 | 2010-08-26 | Makoto Ando | Pyridone Compounds |
| AU2006282260A1 (en) | 2005-08-24 | 2007-03-01 | Msd K.K. | Phenylpyridone derivative |
| EP1939194A4 (de) | 2005-09-07 | 2010-12-08 | Banyu Pharma Co Ltd | Bicyclisches aromatisches substituiertes pyridon-derivat |
| CN101277960A (zh) | 2005-09-29 | 2008-10-01 | 默克公司 | 作为黑皮质素-4受体调节剂的酰化螺哌啶衍生物 |
| EP1940401B1 (de) | 2005-10-18 | 2012-07-11 | Merck Sharp & Dohme Corp. | Acylierte spiropiperidin-derivate als melanocortin-4-rezeptor-modulatoren |
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2002
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- 2002-07-25 PL PL02370373A patent/PL370373A1/xx not_active Application Discontinuation
- 2002-07-25 EP EP02750299A patent/EP1416933B8/de not_active Expired - Lifetime
- 2002-07-25 AT AT02750299T patent/ATE382353T1/de not_active IP Right Cessation
- 2002-07-25 AU AU2002319695A patent/AU2002319695B8/en not_active Ceased
- 2002-07-25 DE DE60224404T patent/DE60224404T2/de not_active Expired - Lifetime
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- 2002-07-25 CA CA002452328A patent/CA2452328A1/en not_active Abandoned
- 2002-07-25 JP JP2003515239A patent/JP2005504028A/ja active Pending
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| EP1416933A1 (de) | 2004-05-12 |
| EP1416933B8 (de) | 2008-08-27 |
| AU2002319695B8 (en) | 2006-03-09 |
| ATE382353T1 (de) | 2008-01-15 |
| MXPA04000625A (es) | 2004-04-20 |
| EP1416933B1 (de) | 2008-01-02 |
| AU2002319695B2 (en) | 2006-03-02 |
| WO2003009847A1 (en) | 2003-02-06 |
| ES2296968T3 (es) | 2008-05-01 |
| PL370373A1 (en) | 2005-05-16 |
| US20040006067A1 (en) | 2004-01-08 |
| JP2005504028A (ja) | 2005-02-10 |
| US6977264B2 (en) | 2005-12-20 |
| DE60224404T2 (de) | 2008-12-18 |
| CA2452328A1 (en) | 2003-02-06 |
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