[go: up one dir, main page]

DE60224404D1 - Substiuierte piperidine als melanocortinrezeptor-modulatoren - Google Patents

Substiuierte piperidine als melanocortinrezeptor-modulatoren

Info

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
Application number
DE60224404T
Other languages
English (en)
Other versions
DE60224404T2 (de
Inventor
Christopher H Fotsch
Michael Croghan
Elizabeth M Doherty
Michael G Kelly
Mark H Norman
Duncan Smith
Nuria Tamayo
Ning Xi
Shimin Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Amgen Inc
Original Assignee
Amgen Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of DE60224404D1 publication Critical patent/DE60224404D1/de
Application granted granted Critical
Publication of DE60224404T2 publication Critical patent/DE60224404T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/26Heterocyclic 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
    • C07D211/28Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic 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
    • C07D211/08Heterocyclic 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
    • C07D211/18Heterocyclic 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
    • C07D211/34Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
DE60224404T 2001-07-25 2002-07-25 Substiuierte piperidine als melanocortinrezeptormodulatoren Expired - Lifetime DE60224404T2 (de)

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)

* Cited by examiner, † Cited by third party
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
WO2007048027A2 (en) 2005-10-21 2007-04-26 Novartis Ag Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent
CA2627139A1 (en) 2005-10-27 2007-05-03 Banyu Pharmaceutical Co., Ltd. Novel benzoxathiin derivative
WO2007055418A1 (ja) 2005-11-10 2007-05-18 Banyu Pharmaceutical Co., Ltd. アザ置換スピロ誘導体
PE20071079A1 (es) * 2005-11-15 2007-12-16 Cytokinetics Inc Compuestos de piperidina como inhibidores de la proliferacion celular
EP1801098A1 (de) 2005-12-16 2007-06-27 Merck Sante 2-Adamantylharnstoff Derivative als selektive 11B-HSD1 Inhibitoren
US7601844B2 (en) * 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US7615556B2 (en) 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
EP1842846A1 (de) * 2006-04-07 2007-10-10 Santhera Pharmaceuticals (Schweiz) AG Phenylpiperidinderivate als Melanocortin-4 Rezeptor-Modulatoren
DK2041093T3 (da) * 2006-06-28 2010-08-02 Glaxo Group Ltd Til behandling af GPR38-receptor medierede sygdomme anvendelige piperazinylderivativer
CN101522614B (zh) * 2006-08-09 2014-06-25 史密丝克莱恩比彻姆公司 作为阿片样物质受体的拮抗剂或反向激动剂的化合物
US7834017B2 (en) 2006-08-11 2010-11-16 Palatin Technologies, Inc. Diamine-containing, tetra-substituted piperazine compounds having identical 1- and 4-substituents
EP2698157B1 (de) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Verfahren zur Behandlung von Fettsäure-Synthese-Hemmern
AU2007301126A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
GB0624987D0 (en) 2006-12-14 2007-01-24 Acure Pharma Ab Novel aminoguanidines as melanocortin receptor ligands
EP1935420A1 (de) 2006-12-21 2008-06-25 Merck Sante 2-Adamantyl-Butyramid Derivate als selektive 11Beta-HSD1 Inhibitoren
JP5319518B2 (ja) 2007-04-02 2013-10-16 Msd株式会社 インドールジオン誘導体
WO2008140810A1 (en) * 2007-05-11 2008-11-20 Cytokinetics, Incorporated Certain chemical entities, compositions, and methods
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
WO2008151257A2 (en) 2007-06-04 2008-12-11 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2019100A1 (de) * 2007-07-19 2009-01-28 Santhera Pharmaceuticals (Schweiz) AG Substituierte Heteroarylpiperidinderivate als Melanocortin-4-Rezeptormodulatoren
EP2020405A1 (de) * 2007-07-30 2009-02-04 Santhera Pharmaceuticals (Schweiz) AG Substituierte Aryl- oder Heteroarylpiperidinderivate als Melanocortin-4-Rezeptormodulatoren
EP2072050A1 (de) * 2007-12-21 2009-06-24 Santhera Pharmaceuticals (Schweiz) AG Komponenten mit anti-emetischer Wirkung
US8602959B1 (en) 2010-05-21 2013-12-10 Robert Park Methods and devices for delivery of radiation to the posterior portion of the eye
ES2579355T3 (es) * 2008-01-07 2016-08-10 Salutaris Medical Devices, Inc Dispositivos para la administración extraocular mínimamente invasiva de radiación a la porción posterior del ojo
US20110207987A1 (en) * 2009-11-02 2011-08-25 Salutaris Medical Devices, Inc. Methods And Devices For Delivering Appropriate Minimally-Invasive Extraocular Radiation
US9873001B2 (en) 2008-01-07 2018-01-23 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
US9056201B1 (en) 2008-01-07 2015-06-16 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
US10022558B1 (en) 2008-01-07 2018-07-17 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive delivery of radiation to the eye
US8608632B1 (en) 2009-07-03 2013-12-17 Salutaris Medical Devices, Inc. Methods and devices for minimally-invasive extraocular delivery of radiation and/or pharmaceutics to the posterior portion of the eye
JPWO2009110510A1 (ja) 2008-03-06 2011-07-14 Msd株式会社 アルキルアミノピリジン誘導体
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
EP2110374A1 (de) 2008-04-18 2009-10-21 Merck Sante Benzofuran, Benzothiophen, Benzothiazolderivate als FXR-Modulatoren
WO2009149279A2 (en) 2008-06-04 2009-12-10 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
CA2727914A1 (en) 2008-06-19 2009-12-23 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diaryl ketoxime derivative technical field
TWI433838B (zh) 2008-06-25 2014-04-11 必治妥美雅史谷比公司 作為趨化因子受體活性調節劑之六氫吡啶衍生物
CA2730603C (en) 2008-07-16 2019-09-24 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2319841A1 (de) 2008-07-30 2011-05-11 Msd K.K. (5-gliedriges)-(5-gliedriges) oder (5-gliedriges)-(6-gliedriges) kondensiertes ringcycloalkylaminderivat
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
WO2010051206A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
FR2937972B1 (fr) * 2008-11-04 2013-03-29 Galderma Res & Dev Derives d'oxoazetidine, leur procede de preparation et leur utilisation en medecine humaine ainsi qu'en cosmetique
FR2937973B1 (fr) * 2008-11-04 2010-11-05 Galderma Res & Dev Modulateurs des recepteurs de la melanocortine, leur procede de preparation et leur utilisation en medecine humaine ainsi qu'en cosmetique
FR2937868B1 (fr) * 2008-11-04 2010-11-05 Galderma Res & Dev Composes antagonistes des recepteurs de la melanocortine, leur procede de preparation et leur utilisation en medecine humaine ainsi qu'en cosmetique
UA99555C2 (en) 2008-11-12 2012-08-27 Элджи Лайф Саенсез Лтд. Melanocortin receptor agonists
AU2009314200B2 (en) 2008-11-17 2011-11-17 Merck Sharp & Dohme Corp. Substituted bicyclic amines for the treatment of diabetes
USD691270S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to an eye
USD691268S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to eye
USD691267S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to eye
USD691269S1 (en) 2009-01-07 2013-10-08 Salutaris Medical Devices, Inc. Fixed-shape cannula for posterior delivery of radiation to an eye
WO2011011508A1 (en) 2009-07-23 2011-01-27 Schering Corporation Benzo-fused oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
WO2011011506A1 (en) 2009-07-23 2011-01-27 Schering Corporation Spirocyclic oxazepine compounds as stearoyl-coenzyme a delta-9 desaturase inhibitors
CA2779088A1 (en) 2009-11-16 2011-05-19 Mellitech [1,5]-diazocin derivatives
US8648073B2 (en) 2009-12-30 2014-02-11 Fochon Pharma, Inc. Certain dipeptidyl peptidase inhibitors
US8476227B2 (en) 2010-01-22 2013-07-02 Ethicon Endo-Surgery, Inc. Methods of activating a melanocortin-4 receptor pathway in obese subjects
US9044606B2 (en) 2010-01-22 2015-06-02 Ethicon Endo-Surgery, Inc. Methods and devices for activating brown adipose tissue using electrical energy
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
WO2011137024A1 (en) 2010-04-26 2011-11-03 Merck Sharp & Dohme Corp. Novel spiropiperidine prolylcarboxypeptidase inhibitors
US9365539B2 (en) 2010-05-11 2016-06-14 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
US9006268B2 (en) 2010-06-11 2015-04-14 Merck Sharp & Dohme Corp. Prolylcarboxypeptidase inhibitors
US8642622B2 (en) 2010-06-16 2014-02-04 Bristol-Myers Squibb Company Piperidinyl compound as a modulator of chemokine receptor activity
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US9018395B2 (en) 2011-01-27 2015-04-28 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
BR112013021236B1 (pt) 2011-02-25 2021-05-25 Merck Sharp & Dohme Corp composto derivado de benzimidazol, e, composição
US9527875B2 (en) 2012-08-02 2016-12-27 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
MX2015010935A (es) 2013-02-22 2015-10-29 Merck Sharp & Dohme Compuestos biciclicos antidiabeticos.
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
EP2970384A1 (de) 2013-03-15 2016-01-20 Synergy Pharmaceuticals Inc. Agonisten der guanylatcyclase und deren verwendungen
WO2014151200A2 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
AU2014274812B2 (en) 2013-06-05 2018-09-27 Bausch Health Ireland Limited Ultra-pure agonists of guanylate cyclase C, method of making and using same
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
DK3186242T3 (da) 2014-08-29 2021-12-20 Tes Pharma S R L Alfa-amino-beta-carboxymuconsyre-semialdehyd-decarboxylasehæmmere
US10092738B2 (en) 2014-12-29 2018-10-09 Ethicon Llc Methods and devices for inhibiting nerves when activating brown adipose tissue
US10080884B2 (en) 2014-12-29 2018-09-25 Ethicon Llc Methods and devices for activating brown adipose tissue using electrical energy
USD814637S1 (en) 2016-05-11 2018-04-03 Salutaris Medical Devices, Inc. Brachytherapy device
USD815285S1 (en) 2016-05-11 2018-04-10 Salutaris Medical Devices, Inc. Brachytherapy device
USD814638S1 (en) 2016-05-11 2018-04-03 Salutaris Medical Devices, Inc. Brachytherapy device
USD808528S1 (en) 2016-08-31 2018-01-23 Salutaris Medical Devices, Inc. Holder for a brachytherapy device
USD808529S1 (en) 2016-08-31 2018-01-23 Salutaris Medical Devices, Inc. Holder for a brachytherapy device
EP3512839A4 (de) * 2016-09-18 2020-03-25 H. Lee Moffitt Cancer Center And Research Institute, Inc. Gegen interaktion von yap1 mit oct4 gerichtete yap1-inhibitoren
AR109950A1 (es) 2016-10-14 2019-02-06 Tes Pharma S R L INHIBIDORES DE LA ÁCIDO a-AMINO-b-CARBOXIMUCÓNICO SEMIALDEHÍDO DESCARBOXILASA
EP3551176A4 (de) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. Antidiabetische heterocyclische verbindungen
WO2018118670A1 (en) 2016-12-20 2018-06-28 Merck Sharp & Dohme Corp. Antidiabetic spirochroman compounds
EA202092174A1 (ru) 2018-03-14 2021-01-15 Х. Ли Моффитт Кэнсер Сентер Энд Рисерч Инститьют, Инк. Ингибиторы yap1, которые нацелены на взаимодействие yap1 с oct4
AU2019249571A1 (en) * 2018-04-06 2020-10-01 Nippon Soda Co., Ltd. (Hetero)arylsulfonamide compound and pest control agent
KR102695210B1 (ko) 2018-06-05 2024-08-13 크리네틱스 파마슈티칼스, 인크. 멜라노코르틴 아형-2 수용체(mc2r) 길항제 및 이의 용도
BR112021009589A2 (pt) 2018-11-20 2021-08-17 Tes Pharma S.R.L. inibidores de semialdeído descarboxilase de ácido alfa-amino-beta-carboximucônico
JP7657792B2 (ja) 2019-11-07 2025-04-07 クリネティックス ファーマシューティカルズ,インク. メラノコルチンサブタイプ-2受容体(mc2r)アンタゴニストおよびその使用
PT4077307T (pt) 2019-12-18 2025-06-03 Crinetics Pharmaceuticals Inc Antagonistas do recetor de subtipo 2 da melanocortina (mc2r) à base de piperidina gem-dissubstituída e suas utilizações
US12466829B2 (en) 2019-12-23 2025-11-11 Crinetics Pharmaceuticals, Inc. Spirocyclic piperidine melanocortin subtype-2 receptor (MC2R) antagonists and uses thereof
JP2024510260A (ja) 2021-03-19 2024-03-06 クリネティックス ファーマシューティカルズ,インク. 疾患の治療のためのメラノコルチンサブタイプ-2受容体(mc2r)アンタゴニスト

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5721251A (en) * 1993-12-10 1998-02-24 Merck & Co., Inc. Piperidine, pyrrolidine and hexahydro-1H-azepines promote release of growth hormone
SK285631B6 (sk) * 1996-09-10 2007-05-03 Dr. Karl Thomae Gmbh Modifikované aminokyseliny, farmaceutický prostriedok s ich obsahom a ich použitie
NZ512282A (en) * 1998-12-17 2002-09-27 Wyeth Corp Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives having 5HT1A 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
MXPA02001160A (es) 1999-08-04 2002-07-02 Millennium Pharm Inc Compuestos que se unen a los receptores para melanocortina-4, y metodo de uso de estos.
US20020091090A1 (en) * 2000-12-28 2002-07-11 Cole Bridget M. Somatostatin antagonists and agonists
JP2004521117A (ja) 2001-01-23 2004-07-15 イーライ・リリー・アンド・カンパニー メラノコルチン受容体アゴニストとしての置換ピペリジン/ピペラジン
WO2002059095A1 (en) 2001-01-23 2002-08-01 Eli Lilly And Company Melanocortin receptor agonists
ATE302773T1 (de) 2001-01-23 2005-09-15 Lilly Co Eli Piperazin- und piperidinderivate als agonisten des melanocortin-rezeptors
WO2002062766A2 (en) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
WO2002068387A2 (en) 2001-02-28 2002-09-06 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
CA2439152C (en) 2001-02-28 2008-06-17 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
JP4316238B2 (ja) 2001-02-28 2009-08-19 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
WO2002069905A2 (en) 2001-03-02 2002-09-12 Bristol-Myers Squibb Company Co-administration of melanocortin receptor agonist and phosphodiesterase inhibitor for treatment of cyclic-amp associated disorders
WO2002079146A2 (en) * 2001-03-02 2002-10-10 Bristol-Myers Squibb Company Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
ES2274201T3 (es) 2002-01-23 2007-05-16 Eli Lilly And Company Agonistas del receptor de melanocortina.
US20040248956A1 (en) 2002-01-29 2004-12-09 Hagmann William K Substituted imidazoles as cannabinoid receptor modulators

Also Published As

Publication number Publication date
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

Similar Documents

Publication Publication Date Title
ATE382353T1 (de) Substiuierte piperidine als melanocortinrezeptor- modulatoren
DE60229530D1 (de) Substituierte piperazine als modulatoren des melanocortinrezeptors
ATE404552T1 (de) Substituierte isochinolinderivate und anwendungsverfahren
ATE453636T1 (de) Substituierte 2,3-dihydro-1h-isoindol-1-one derivate und anwendungsverfahren
SE0203713D0 (sv) Novel compounds
NO20070489L (no) 3-aminocyklopentankarboksamider som modulatorer av kjemokinreseptorer.
WO2003028641A3 (en) Mch receptor antagonists
MXPA05013366A (es) Derivados de benzazepina utiles para el tratamiento de enfermedades asociadas con el receptor 5ht2c.
NO20033181D0 (no) Substituerte alkylaminderivater og fremgangsmater for anvendelse
ATE485269T1 (de) C-verknüpfte zyklische antagonisten des p2y1- rezeptors mit eignung bei der behandlung thrombotischer leiden
MY177111A (en) Substituted amide derivatives and methods of use
SE0303180D0 (sv) Novel compounds
SE0302232D0 (sv) Novel Compounds
DE60231341D1 (de) Fluor- und sulfonylaminohaltige, 3,6-disubstituierptorantagonisten
SE0201635D0 (sv) Novel compounds
GEP20074197B (en) 5ht2c receptor modulators
NO20060278L (no) Piperazinderivater og fremgangsmater for anvendelse
DK1501808T3 (da) Tachykininreceptor-antagonister
TW200720260A (en) Prokineticin 1 receptor antagonists
TW200716566A (en) Prokineticin 2 receptor antagonists
DK1673354T3 (da) Arylindenopyridiner og arylindenopyrimidiner og deres anvendelse som adenosin-A2a-receptorantagonister
EA200701687A1 (ru) Гидрохлорид аморфного лерканидипина
BR0315092A (pt) Derivados de piperidina como inibidores de ccr5
HUP0401895A2 (hu) Paroxetin N-formil származékai, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

Legal Events

Date Code Title Description
8364 No opposition during term of opposition