HUP0203131A2 - Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

Info

Publication number
HUP0203131A2
HUP0203131A2 HU0203131A HUP0203131A HUP0203131A2 HU P0203131 A2 HUP0203131 A2 HU P0203131A2 HU 0203131 A HU0203131 A HU 0203131A HU P0203131 A HUP0203131 A HU P0203131A HU P0203131 A2 HUP0203131 A2 HU P0203131A2
Authority
HU
Hungary
Prior art keywords
alkyl
cycloalkyl
group
carbon atoms
nr8r9
Prior art date
Application number
HU0203131A
Other languages
English (en)
Inventor
Charles Blum
Philip Albert Carpino
James W. Darrow
Stephane De Lombaert
Mark Giangiordano
David Andrew Griffith
Jennifer Tran
Original Assignee
Neurogen Corporation
Pfizer 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 Neurogen Corporation, Pfizer Inc. filed Critical Neurogen Corporation
Publication of HUP0203131A2 publication Critical patent/HUP0203131A2/hu
Publication of HUP0203131A3 publication Critical patent/HUP0203131A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/575—Hormones
    • G01N2333/5755—Neuropeptide Y
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70571—Assays involving receptors, cell surface antigens or cell surface determinants for neuromediators, e.g. serotonin receptor, dopamine receptor

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Pulmonology (AREA)
  • Reproductive Health (AREA)
  • Child & Adolescent Psychology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

A találmány (I) általános képletű vegyületekre vonatkozik, amelyekképletében R1, R2, R3, R4, R5, R6 és X jelentése az alábbiakbanmegadott. E vegyületek szelektív NPY1 receptormodulátorok. Ezek avegyületek számos CNS rendellenesség, anyagcserezavarok, perifériásrendellenességek, különösen táplálkozási zavarok és magas vérnyomáskezelésére alkalmasak. A találmány tárgyát képezik továbbá az ilyenrendellenességek kezelésére szolgáló kezelési eljárások, valamintezeket tartalmazó gyógyszerkészítmények. X jelentése N vagy CHR14; R1jelentése hidrogénatom, 1-6 szénatomszámú alkil-, 3-10 szénatomszámúcikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6 szén<- >atomszámúalkil)-, 2-6 szénatomszámú alkenil, 2-6 szén<- >atomszámú alkinil-,ciano-, halo-, 1-6 szénatomszámú halo-alkil-, -OR7, -(1-6szénatomszámú alkil)-OR7, 1-6 szénatomszámú ciano-alkil-, -NR8R9, és -(1-6 szénatomszámú alkil)-NR8R9 közül választott csoport; R2 jelentésehidrogénatom, 1-6 szénatomszámú alkilcsoport, amely adott esetben az Avagy a B csoporttal 3-6 szénatomszámú amino-karbociklust vagy 2-5szénatomszámú amino-heterociklust képez, amelyek mindegyike adottesetben R7 csoporttal helyettesített, 3-10 szénatomszámú cikloalkil-vagy (3-10 szénatomszámú cikloalkil)-(1-6 szénatomszámú alkil)-csoport; vagy R2 és R6 együttesen azzal a két nitrogénatommal,amelyhez kapcsolódnak 2-5 szénatomszámú amino- heterociklust képez,amely adott esetben R7 csoporttal helyettesített; A jelentése (CH2)mcsoport, amelyben m értéke 1, 2 vagy 3 és mindegyik szénatom adottesetben 1-6 szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10 szénatomszámú ciklo-alkil)-(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatom-számú halo-alkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, B jelentése (CH2)m csoport, amelybenm értéke 1, 2 vagy 3 és mindegyik szénatom adott esetben 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú ciklo-alkil)-<- >(1-6 szénatomszámú alkil)-, 2-6szénatomszámú alkenil, 2-6 szénatomszámú alkinil-, ciano-, halo-, 1-6szénatomszámú haloalkil-, -OR7, -(1-6 szénatomszámú alkil)-OR7, 1-6szénatomszámú ciano-alkil-, -NR8R9, vagy -(1-6 szénatomszámú alkil)-NR8R9 csoporttal helyettesített, R3 jelentése hidrogénatom, 1-6szénatomszámú alkil-, 3-10 szénatomszámú cikloalkil-, (3-10szénatomszámú cikloalkil)-(1-6 szén<- >atomszámú alkil)-, 2-6szénatomszámú alkenilcsoport; R4 jelentése aril- vagyheteroarilcsoport, amely adott esetben 1-6 szénatomszámú alkil-, 3-10szénatomszámú cikloalkil-, (3-10 szénatomszámú cikloalkil)-(1-6szénatomszámú alkil)-, 2-6 szénatomszámú alkenil, 2-6 szénatomszámúalkinil-, halo-, 1-6 szénatomszámú halo-alkil-, tri
HU0203131A 1999-09-30 2000-09-29 Amino substituted pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use HUP0203131A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15686899P 1999-09-30 1999-09-30
PCT/US2000/026885 WO2001023388A2 (en) 1999-09-30 2000-09-29 AMINO SUBSTITUTED PYRAZOLO[1,5,-a]-1,5-PYRIMIDINES AND PYRAZOLO[1,5-a]-1,3,5-TRIAZINES

Publications (2)

Publication Number Publication Date
HUP0203131A2 true HUP0203131A2 (hu) 2003-01-28
HUP0203131A3 HUP0203131A3 (en) 2004-06-28

Family

ID=22561433

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0203131A HUP0203131A3 (en) 1999-09-30 2000-09-29 Amino substituted pyrazolo[1,5-a]-1,5-pyrimidines and pyrazolo[1,5-a]-1,3,5-triazines, pharmaceutical compositions containing them and their use

Country Status (21)

Country Link
US (1) US6476038B1 (hu)
EP (1) EP1218381B1 (hu)
JP (2) JP2003510326A (hu)
KR (1) KR20020047201A (hu)
CN (1) CN1377355A (hu)
AT (1) ATE347553T1 (hu)
AU (1) AU7737900A (hu)
BG (1) BG106507A (hu)
CA (1) CA2379633C (hu)
CZ (1) CZ20021089A3 (hu)
DE (1) DE60032249T2 (hu)
EA (1) EA200200421A1 (hu)
ES (1) ES2277855T3 (hu)
HU (1) HUP0203131A3 (hu)
IL (1) IL148904A0 (hu)
NO (1) NO20021357L (hu)
OA (1) OA12049A (hu)
PL (1) PL354982A1 (hu)
WO (1) WO2001023388A2 (hu)
YU (1) YU23602A (hu)
ZA (1) ZA200202517B (hu)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6472528B1 (en) * 1999-08-10 2002-10-29 Neurocrine Biosciences, Inc. Synthesis of substituted pyrazolopyrimidines
CZ20021067A3 (cs) 1999-09-30 2002-11-13 Neurogen Corporation Určité alkylendiaminové substituované pyrazolo[1,5-a]- 1,5-pyrimidiny a pyrazolo[1,5-a]-1,3,5-triaziny
WO2003076441A1 (en) 2002-03-07 2003-09-18 Smithkline Beecham Corporation Pyrazolopyrimidine and pyrazolotriazine derivatives and pharmaceutical compositions containing them
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
FR2842809A1 (fr) * 2002-07-26 2004-01-30 Greenpharma Sas NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
KR20110010824A (ko) 2003-01-14 2011-02-07 아레나 파마슈티칼스, 인크. 대사 조절제로서의 １,２,３-삼치환된 아릴 및 헤테로아릴 유도체, 및 당뇨병 및 고혈당증을 비롯한 이에 관련된 장애의 예방 및 치료
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
US7329658B2 (en) * 2003-02-06 2008-02-12 Pfizer Inc Cannabinoid receptor ligands and uses thereof
US7176210B2 (en) * 2003-02-10 2007-02-13 Pfizer Inc. Cannabinoid receptor ligands and uses thereof
OA13050A (en) 2003-04-29 2006-11-10 Pfizer Ltd 5,7-diaminopyrazolo [4,3-D] pyrimidines useful in the treatment of hypertension.
JP4920410B2 (ja) * 2003-07-14 2012-04-18 アリーナ ファーマシューティカルズ， インコーポレイテッド 代謝モジュレーターとしての縮合アリールおよびヘテロアリール誘導体ならびに代謝に関連する障害の予防および治療
ATE547404T1 (de) 2003-09-22 2012-03-15 Msd Kk Piperidinderivate
US7153961B2 (en) 2003-11-25 2006-12-26 Bristol-Myers Squibb Pharma Co. Salt and crystalline form thereof of a corticotropin releasing factor receptor antagonist
US7208596B2 (en) 2003-11-25 2007-04-24 Bristol-Myers Squibb Pharma Company Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof
EP1697369A1 (en) * 2003-12-22 2006-09-06 SB Pharmco Puerto Rico Inc Crf receptor antagonists and methods relating thereto
CA2550948A1 (en) 2003-12-22 2005-07-14 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
GB0519957D0 (en) * 2005-09-30 2005-11-09 Sb Pharmco Inc Chemical compound
EP2286837A3 (en) 2004-11-01 2013-09-04 Amylin Pharmaceuticals, LLC Treatment of obesity and obesity related diseases
EP1836205B1 (en) * 2004-12-21 2009-06-10 Schering Corporation PYRAZOLO[1,5-A]PYRIMIDINE ADENOSINE A2a RECEPTOR ANTAGONISTS
WO2007022123A2 (en) 2005-08-11 2007-02-22 Amylin Pharmaceuticals, Inc. Hybrid polypeptides with selectable properties
US7737155B2 (en) 2005-05-17 2010-06-15 Schering Corporation Nitrogen-containing heterocyclic compounds and methods of use thereof
NZ562766A (en) 2005-05-30 2011-03-31 Banyu Pharma Co Ltd Piperidine derivatives as histamine-H3 receptor antagonists
BRPI0612833A2 (pt) 2005-06-23 2010-11-30 Statens Seruminstitut composição imunogênica, vacina, composição farmacêutica, polipeptìdeo de fusão e uso das três primeiras
JPWO2007018248A1 (ja) 2005-08-10 2009-02-19 萬有製薬株式会社 ピリドン化合物
EP2330125A3 (en) 2005-08-11 2012-12-12 Amylin Pharmaceuticals, Inc. Hybrid polypeptides with selectable properties
US7875633B2 (en) 2005-08-24 2011-01-25 Banyu Pharmaceutical Co., Ltd. Phenylpyridone derivative
JPWO2007029847A1 (ja) 2005-09-07 2009-03-19 萬有製薬株式会社 二環性芳香族置換ピリドン誘導体
AU2006297443B2 (en) 2005-09-29 2010-08-12 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
BRPI0617621A2 (pt) 2005-10-21 2011-08-02 Novartis Ag combinação de compostos orgánicos
JPWO2007049798A1 (ja) 2005-10-27 2009-04-30 萬有製薬株式会社 新規ベンゾオキサチイン誘導体
NZ568292A (en) 2005-11-10 2011-08-26 Msd Kk Spiro[cyclohexane-1,1'-(3'H)-4'-azaisobenzofuran]-4-carboxamide derivatives
MX2009003098A (es) 2006-09-20 2009-04-01 Lilly Co Eli Compuestos de tiofen pirazolopirimidina.
US8030304B2 (en) 2006-09-20 2011-10-04 Eli Lilly And Company Thiazole pyrazolopyrimidines CRF1 receptor antagonists
CA2664113C (en) 2006-09-22 2013-05-28 Merck & Co., Inc. Use of platencin and platensimycin as fatty acid synthesis inhibitors to treat obesity, diabetes and cancer
EP2072519A4 (en) 2006-09-28 2009-10-21 Banyu Pharma Co Ltd DIARYLKETIMINDERIVAT
CA2682727C (en) 2007-04-02 2016-03-22 Banyu Pharmaceutical Co., Ltd. Indoledione derivative
EP2170930B3 (en) 2007-06-04 2013-10-02 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
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
WO2008153870A1 (en) * 2007-06-07 2008-12-18 Schering Corporation Synthesis of substituted-3-aminopyrazoles
CA2714617A1 (en) 2008-03-06 2009-09-11 Banyu Pharmaceutical Co., Ltd. Alkylaminopyridine derivative
AU2009229860A1 (en) 2008-03-28 2009-10-01 Msd K.K. Diarylmethylamide derivative having antagonistic activity on melanin-concentrating hormone receptor
JP2011522828A (ja) 2008-06-04 2011-08-04 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 胃腸障害、炎症、癌、およびその他の障害の治療のために有用なグアニル酸シクラーゼのアゴニスト
AU2009261248A1 (en) 2008-06-19 2009-12-23 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
US20100015171A1 (en) 2008-07-15 2010-01-21 Statens Serum Institute Vaccines comprising tb 10.4
AU2009270833B2 (en) 2008-07-16 2015-02-19 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
WO2010013595A1 (ja) 2008-07-30 2010-02-04 萬有製薬株式会社 ５員－５員又は５員－６員縮環シクロアルキルアミン誘導体
CN102264228A (zh) 2008-10-22 2011-11-30 默沙东公司 用于抗糖尿病药的新的环状苯并咪唑衍生物
CA2741644C (en) 2008-10-30 2013-05-07 Merck Sharp & Dohme Corp. Isonicotinamide orexin receptor antagonists
AU2009309037A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
EP2379547A1 (en) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
EP2379562A1 (en) 2008-12-16 2011-10-26 Schering Corporation Bicyclic pyranone derivatives as nicotinic acid receptor agonists
AU2011218830B2 (en) 2010-02-25 2014-07-24 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
US10894787B2 (en) 2010-09-22 2021-01-19 Arena Pharmaceuticals, Inc. Modulators of the GPR119 receptor and the treatment of disorders related thereto
PE20140859A1 (es) 2011-02-25 2014-07-25 Merck Sharp & Dohme Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
JP2015525782A (ja) 2012-08-02 2015-09-07 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 抗糖尿病性三環式化合物
NZ707432A (en) 2012-11-16 2020-01-31 Univ Health Network Pyrazolopyrimidine compounds
EP2958562A4 (en) 2013-02-22 2016-08-10 Merck Sharp & Dohme BICYCLIC ANTIDIABETIC COMPOUNDS
US9650375B2 (en) 2013-03-14 2017-05-16 Merck Sharp & Dohme Corp. Indole derivatives useful as anti-diabetic agents
CA2905435A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Compositions useful for the treatment of gastrointestinal disorders
WO2014151206A1 (en) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase and their uses
EP3004138B1 (en) 2013-06-05 2024-03-13 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
AU2015308350B2 (en) 2014-08-29 2020-03-05 Tes Pharma S.R.L. Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
MX2021011472A (es) 2015-01-06 2022-08-17 Arena Pharm Inc Metodos de condiciones de tratamiento relacionadas con el receptor s1p1.
KR102603199B1 (ko) 2015-06-22 2023-11-16 아레나 파마슈티칼스, 인크. Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염
CA3034705C (en) 2016-08-31 2021-08-03 Agios Pharmaceuticals, Inc. Inhibitors of cellular metabolic processes
WO2018069532A1 (en) 2016-10-14 2018-04-19 Tes Pharma S.R.L. Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase
EP3551176A4 (en) 2016-12-06 2020-06-24 Merck Sharp & Dohme Corp. ANTIDIABETIC HETEROCYCLIC COMPOUNDS
EP3558298A4 (en) 2016-12-20 2020-08-05 Merck Sharp & Dohme Corp. ANTIDIABETIC SPIROCHROMAN COMPOUNDS
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
EP3774719A1 (de) * 2018-04-10 2021-02-17 Bayer Aktiengesellschaft Verfahren zur herstellung von 2,6-dialkylphenyl-essigsäuren
PE20212196A1 (es) 2018-10-30 2021-11-16 Kronos Bio Inc Compuestos, composiciones, y metodos para modular la actividad cdk9
CN113302189A (zh) 2018-11-20 2021-08-24 Tes制药有限责任公司 α-氨基-β-羧基己二烯二酸半醛去羧酶的抑制剂
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
EP4010314B1 (en) 2019-08-08 2024-02-28 Merck Sharp & Dohme LLC Heteroaryl pyrrolidine and piperidine orexin receptor agonists
BR112023002497A2 (pt) 2020-08-12 2023-05-02 Spruce Biosciences Inc Métodos e composições para tratamento da síndrome dos ovários policísticos
BR112023002957A2 (pt) 2020-08-18 2023-04-04 Merck Sharp & Dohme Llc Composto, composição farmacêutica, e, métodos para tratar narcolepsia e para tratar hipersonia em um sujeito mamífero
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof
CN115304607B (zh) * 2022-07-06 2023-06-27 华南农业大学 吡唑并嘧啶衍生物的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0915880B1 (en) 1996-07-24 2007-10-10 Bristol-Myers Squibb Pharma Company Azolo triazines and pyrimidines
JP3711238B2 (ja) * 1997-08-05 2005-11-02 ファイザー・プロダクツ・インク 神経ペプチドＹ受容体アンタゴニストとしての４−アミノピロ−ル（３，２−ｄ）ピリミジン
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases

Also Published As

Publication number Publication date
OA12049A (en) 2006-05-02
AU7737900A (en) 2001-04-30
EA200200421A1 (ru) 2002-10-31
NO20021357L (no) 2002-05-23
NO20021357D0 (no) 2002-03-19
EP1218381A2 (en) 2002-07-03
IL148904A0 (en) 2002-09-12
CN1377355A (zh) 2002-10-30
JP2007077144A (ja) 2007-03-29
ES2277855T3 (es) 2007-08-01
WO2001023388A2 (en) 2001-04-05
PL354982A1 (en) 2004-03-22
US6476038B1 (en) 2002-11-05
WO2001023388A3 (en) 2001-10-18
YU23602A (sh) 2004-09-03
DE60032249D1 (de) 2007-01-18
BG106507A (en) 2002-12-29
DE60032249T2 (de) 2007-07-19
CA2379633C (en) 2006-06-20
EP1218381B1 (en) 2006-12-06
CA2379633A1 (en) 2001-04-05
KR20020047201A (ko) 2002-06-21
ZA200202517B (en) 2003-05-28
JP2003510326A (ja) 2003-03-18
CZ20021089A3 (cs) 2002-11-13
ATE347553T1 (de) 2006-12-15
HUP0203131A3 (en) 2004-06-28

Similar Documents

Publication Publication Date Title
HUP0203131A2 (hu) Aminocsoporttal helyettesített pirazolo[1,5-a]-1,5-pirimidinek és pirazolo[1,5-a]-1,3,5-triazinok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0202678A2 (hu) Alkilén-diamin-csoporttal helyettesített pirazolo[1,5,-a]-1,5-pirimidin és pirazolo[1,5-a]-1,3,5-triazin-származékok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
UA66825C2 (uk) Азаполіциклічні сполуки, конденсовані з арилом, фармацевтична композиція, спосіб лікування та спосіб зниження нікотинової залежності
BG104278A (en) Methods and intermediate compounds for the preparation of anti-cancer compounds
HUP0303756A2 (hu) 1-Aril- vagy 1-alkilszulfonil-heterociklobenzazolok és eljárás ezek elõállítására és ezeket tartalmazó gyógyszerkészítmények
HUT70505A (en) Pyrrolo[2,3-d]pyrimidine derivatives, pharmaceutical compositions containing them and process for preparing them
YU11501A (sh) Derivati 4,4,-biarilpiperidina sa aktivnošću na receptor opijata
NZ337121A (en) Pyrazine compounds as good anti-convulsants for the treatment of CNS diseases such as epilepsy
IL197484A0 (en) 5-AMINO-7-(1H-INDOL-2-YL)-1,3-DIHYDRO-IMIDAZOL[4,5-b]PYRIDIN-2-ONE AND ITS N- BOC PROTECTED-7-(1H-INDOL-2-YL)-2-METHYL-3H-IMIDAZO[4,5-b]PYRIDIN-5-YLAMINE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
HUP0301801A2 (hu) Imidazo[1,2-a]pirazin-származékok és az ezeket tartalmazó gyógyszerkészítmények
SG127738A1 (en) Heterocyclic compounds based on n6-substituted adenine, methods of their preparation, their use for preparation of drugs, pharmaceutical preparations containing these compounds
WO2006069805A3 (en) Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
CA2350573A1 (en) Piperidines as ccr5 modulators
BRPI0418112A (pt) inibidores de p-38 quinase bicìclico heterocìclicos
HUP0301114A2 (hu) Pirrolo[2,3-d]pirimidin vegyületek, mint immunoszuppresszív hatóanyagok, és ezeket tartalmazó gyógyszerkészítmények
HUT71130A (en) Condensed indole derivatives of protein kinase c inhibitor activity, process for preparing them and pharmaceutical compositions containing them
CA2292984A1 (en) Ccr5 modulators
HK1098742A1 (en) Substituted 1h-pyrrolo [3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase i epsilon
HK1070054A1 (en) Arylsulfonyl derivatives with5-ht6 receptor affinity
HUP0402270A2 (hu) [1,2,4]Triazolo[1,5-c]pirimidin-5-il-aminok mint adenozin A2a receptor antagonisták és az ezeket tartalmazó gyógyszerkészítmények
GEP20033081B (en) Pharmaceutical Agents for Treatment of Parkinson&#39;s Disease, ADFD and Microadenomas
HUP0303254A2 (hu) Új pirimidinvegyületek, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
IL147149A0 (en) Novel diphenyl-piperidine derivate
CA2539549A1 (en) Pyrazolopyrrole derivatives as protein kinase inhibitors
YU64400A (sh) Aril fuzirana azapoliciklična jedinjenja