WO2001023389A3 - Certain alkylene diamine-substituted heterocycles - Google Patents

Certain alkylene diamine-substituted heterocycles Download PDF

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Publication number
WO2001023389A3
WO2001023389A3 PCT/US2000/026886 US0026886W WO0123389A3 WO 2001023389 A3 WO2001023389 A3 WO 2001023389A3 US 0026886 W US0026886 W US 0026886W WO 0123389 A3 WO0123389 A3 WO 0123389A3
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WO
WIPO (PCT)
Prior art keywords
present
alkylene diamine
substituted heterocycles
tri
mono
Prior art date
Application number
PCT/US2000/026886
Other languages
French (fr)
Other versions
WO2001023389A2 (en
Inventor
Raymond F Horvath
Jennifer Tran
Lombaert Stephane De
Kevin Julian Hodgetts
Philip A Carpino
David A Griffith
Original Assignee
Neurogen Corp
Pfizer
Raymond F Horvath
Jennifer Tran
Lombaert Stephane De
Kevin Julian Hodgetts
Philip A Carpino
David A Griffith
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
Priority to AU77380/00A priority Critical patent/AU7738000A/en
Priority to CA002379640A priority patent/CA2379640C/en
Priority to PL00354784A priority patent/PL354784A1/en
Priority to HU0202636A priority patent/HUP0202636A3/en
Application filed by Neurogen Corp, Pfizer, Raymond F Horvath, Jennifer Tran, Lombaert Stephane De, Kevin Julian Hodgetts, Philip A Carpino, David A Griffith filed Critical Neurogen Corp
Priority to JP2001526541A priority patent/JP2003510327A/en
Priority to DE60026155T priority patent/DE60026155T2/en
Priority to NZ517575A priority patent/NZ517575A/en
Priority to EP00967133A priority patent/EP1224187B1/en
Priority to IL14890300A priority patent/IL148903A0/en
Priority to EA200200424A priority patent/EA200200424A1/en
Priority to KR1020027004150A priority patent/KR20020043223A/en
Publication of WO2001023389A2 publication Critical patent/WO2001023389A2/en
Priority to BG106508A priority patent/BG106508A/en
Priority to NO20021358A priority patent/NO20021358L/en
Publication of WO2001023389A3 publication Critical patent/WO2001023389A3/en

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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Abstract

The present invention also provides a general method to whereby mono-, bi-, or tri-cyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula (I-XV).
PCT/US2000/026886 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles WO2001023389A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
DE60026155T DE60026155T2 (en) 1999-09-30 2000-09-29 SOME ALKYLENDIAMINE-SUBSTITUTED HETEROCYCLES
PL00354784A PL354784A1 (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
HU0202636A HUP0202636A3 (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
EP00967133A EP1224187B1 (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
JP2001526541A JP2003510327A (en) 1999-09-30 2000-09-29 Heterocycle substituted with specific alkylenediamine
CA002379640A CA2379640C (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
NZ517575A NZ517575A (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
AU77380/00A AU7738000A (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
IL14890300A IL148903A0 (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
EA200200424A EA200200424A1 (en) 1999-09-30 2000-09-29 Some heterocycles substituted by alkylene diamin
KR1020027004150A KR20020043223A (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles
BG106508A BG106508A (en) 1999-09-30 2002-03-11 Alkylene diamine-substituted heterocycles
NO20021358A NO20021358L (en) 1999-09-30 2002-03-19 Alkylenediamine-substituted heterocycles

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15687099P 1999-09-30 1999-09-30
US60/156,870 1999-09-30

Publications (2)

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WO2001023389A2 WO2001023389A2 (en) 2001-04-05
WO2001023389A3 true WO2001023389A3 (en) 2002-05-10

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PCT/US2000/026886 WO2001023389A2 (en) 1999-09-30 2000-09-29 Certain alkylene diamine-substituted heterocycles

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US (3) US6506762B1 (en)
EP (1) EP1224187B1 (en)
JP (2) JP2003510327A (en)
KR (1) KR20020043223A (en)
CN (1) CN1377356A (en)
AT (1) ATE318267T1 (en)
AU (1) AU7738000A (en)
BG (1) BG106508A (en)
CA (1) CA2379640C (en)
CZ (1) CZ20021086A3 (en)
DE (1) DE60026155T2 (en)
EA (1) EA200200424A1 (en)
ES (1) ES2258476T3 (en)
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8835430B2 (en) 2002-02-01 2014-09-16 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9266912B2 (en) 2005-01-19 2016-02-23 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses

Families Citing this family (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6989379B1 (en) 1999-04-22 2006-01-24 H. Lundbick A/S Selective NPY (Y5) antagonists
US6340683B1 (en) 1999-04-22 2002-01-22 Synaptic Pharmaceutical Corporation Selective NPY (Y5) antagonists (triazines)
PT1183245E (en) 1999-04-22 2007-07-12 Lundbeck & Co As H Selective npy (y5) antagonists
US7273880B2 (en) 1999-06-30 2007-09-25 H. Lunbeck A/S Selective NPY (Y5) antagonists
EA200200424A1 (en) * 1999-09-30 2002-12-26 Ньюроджен Корпорейшн Some heterocycles substituted by alkylene diamin
YU23802A (en) * 1999-09-30 2004-09-03 Neurogen Corporation Certain alkylene diamine-substituted pyrazolo/1,5-a/1,5- pyrimidines and pyrazolo/1,5-a/-1,3,5-triazines
EP1263768A4 (en) * 2000-01-28 2004-05-12 Neurogen Corp Chimeric neuropeptide y receptors
ATE423120T1 (en) * 2000-06-26 2009-03-15 Pfizer Prod Inc PYRROLOÄ2,3-DÜPYRIMIDINE COMPOUNDS AS IMMUNOSUPPRESSIVE ACTIVES
DE60115092T2 (en) * 2000-12-12 2006-03-30 Neurogen Corp., Brandford SPIRO [ISOBENZOFURAN-1,4'-PIPERIDIN] -3-ONE AND 3H-SPIROISOBENZOFURAN-1,4'-PIPERIDINE
JP2005503345A (en) * 2001-04-30 2005-02-03 バイエル・コーポレーシヨン Novel 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidine
BR0209267A (en) 2001-04-30 2004-06-15 Glaxo Group Ltd Fused pyrimidines as corticotropin releasing factor (crf) antagonists
US6805853B2 (en) * 2001-11-09 2004-10-19 Alexza Molecular Delivery Corporation Delivery of diazepam through an inhalation route
US7498019B2 (en) 2001-05-24 2009-03-03 Alexza Pharmaceuticals, Inc. Delivery of compounds for the treatment of headache through an inhalation route
ES2316571T3 (en) * 2001-05-24 2009-04-16 Alexza Pharmaceuticals, Inc. ADMINISTRATION OF ALPRAZOLAM, ESTAZOLAM, MIDAZOLAM OR TRIAZOLAM THROUGH AN INHALATORY ROAD.
US20030051728A1 (en) 2001-06-05 2003-03-20 Lloyd Peter M. Method and device for delivering a physiologically active compound
US20070122353A1 (en) 2001-05-24 2007-05-31 Hale Ron L Drug condensation aerosols and kits
US6759029B2 (en) * 2001-05-24 2004-07-06 Alexza Molecular Delivery Corporation Delivery of rizatriptan and zolmitriptan through an inhalation route
US7645442B2 (en) 2001-05-24 2010-01-12 Alexza Pharmaceuticals, Inc. Rapid-heating drug delivery article and method of use
US7090830B2 (en) * 2001-05-24 2006-08-15 Alexza Pharmaceuticals, Inc. Drug condensation aerosols and kits
CA2446904A1 (en) * 2001-05-24 2003-04-03 Alexza Molecular Delivery Corporation Delivery of drug esters through an inhalation route
US7458374B2 (en) * 2002-05-13 2008-12-02 Alexza Pharmaceuticals, Inc. Method and apparatus for vaporizing a compound
US7078016B2 (en) 2001-11-21 2006-07-18 Alexza Pharmaceuticals, Inc. Delivery of caffeine through an inhalation route
GB0117396D0 (en) 2001-07-17 2001-09-05 Glaxo Group Ltd Chemical compounds
US7323469B2 (en) 2001-08-07 2008-01-29 Novartis Ag 7H-pyrrolo[2,3-d]pyrimidine derivatives
GB0119249D0 (en) 2001-08-07 2001-10-03 Novartis Ag Organic compounds
US6787558B2 (en) 2001-09-28 2004-09-07 Hoffmann-La Roche Inc. Quinoline derivatives
CA2403307A1 (en) 2001-10-23 2003-04-23 Neurogen Corporation Substituted 2-cyclohexyl-4-phenyl-1h-imidazole derivatives
AU2003239433A1 (en) 2002-05-13 2003-11-11 Alexza Molecular Delivery Corporation Delivery of drug amines through an inhalation route
US20060193788A1 (en) * 2002-11-26 2006-08-31 Hale Ron L Acute treatment of headache with phenothiazine antipsychotics
ES2464157T3 (en) 2002-06-26 2014-05-30 Ono Pharmaceutical Co., Ltd. Remedies for diseases caused by vascular contraction or dilation
US7105526B2 (en) 2002-06-28 2006-09-12 Banyu Pharmaceuticals Co., Ltd. Benzimidazole derivatives
CA2489251A1 (en) 2002-07-05 2004-01-15 F. Hoffmann-La Roche Ag Quinazoline derivatives
ES2445208T3 (en) 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. 2,4-Pyrimidinediamine compounds for use in methods to treat or prevent autoimmune diseases
BR0313278A (en) 2002-08-07 2005-07-05 Hoffmann La Roche Compounds, process for the preparation of a compound, pharmaceutical composition comprising the same and its use, method for treating and prophylaxis of diseases and obesity and use of the compounds
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
US7550133B2 (en) * 2002-11-26 2009-06-23 Alexza Pharmaceuticals, Inc. Respiratory drug condensation aerosols and methods of making and using them
CN1726037B (en) * 2002-11-26 2010-05-05 艾利斯达医药品公司 Treatment of headache with antipsychotics delivered by inhalation
US20040105818A1 (en) * 2002-11-26 2004-06-03 Alexza Molecular Delivery Corporation Diuretic aerosols and methods of making and using them
PT1567164E (en) * 2002-11-26 2009-03-31 Alexza Pharmaceuticals Inc Use of loxapine for the manufacture of a medicament for the treatment of pain
US7913688B2 (en) * 2002-11-27 2011-03-29 Alexza Pharmaceuticals, Inc. Inhalation device for producing a drug aerosol
US20040192583A1 (en) * 2002-12-19 2004-09-30 Satyanarayana Medicherla Treatment of obesity and associated conditions with TGF-beta inhibitors
DK1599468T3 (en) 2003-01-14 2008-02-04 Arena Pharm Inc 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prevention and treatment of disorders associated therewith such as diabetes and hyperglycemia
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
GB0308208D0 (en) 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
WO2004096810A1 (en) 2003-04-29 2004-11-11 Pfizer Limited 5,7-diaminopyrazolo`4,3-d!pyrimidines useful in the treatment of hypertension
US20040234916A1 (en) 2003-05-21 2004-11-25 Alexza Molecular Delivery Corporation Optically ignited or electrically ignited self-contained heating unit and drug-supply unit employing same
WO2004110454A1 (en) * 2003-06-13 2004-12-23 Ishihara Sangyo Kaisha, Ltd. COMPOSITION FOR TREATMENT FOR OR PREVENTION OF DISEASE NECESSITATING ADMINISTRATION OF ADENOSINE A2a RECEPTOR AGONIST
EP2287166A3 (en) * 2003-07-14 2011-06-22 Arena Pharmaceuticals, Inc. Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
KR101201603B1 (en) 2003-07-30 2012-11-14 리겔 파마슈티칼스, 인크. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
WO2005019222A1 (en) * 2003-08-15 2005-03-03 Merck & Co., Inc. 4-cycloalkylaminopyrazolo pyrimidine nmda/nr2b antagonists
CA2535347A1 (en) 2003-08-15 2005-03-03 Merck & Co., Inc. 4-cycloalkylaminopyrazolo pyrimidine nmda/nr2b antagonists
BRPI0413563A (en) * 2003-08-15 2006-10-17 Irm Llc compounds and compositions as inhibitors of tyrosine kinase receptor activity
WO2005028438A1 (en) 2003-09-22 2005-03-31 Banyu Pharmaceutical Co., Ltd. Novel piperidine derivative
US7572799B2 (en) 2003-11-24 2009-08-11 Pfizer Inc Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
PT1711184E (en) * 2004-01-06 2007-09-24 Janssen Pharmaceutica Nv (3-oxo-3,4-dihydro-quinoxalin-2-yl-amino)-benzamide derivatives and related compounds as glycogen phosphorylase inhibitors for the treatment of diabetes and obesity
US7501426B2 (en) * 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
EP1735314A1 (en) 2004-03-16 2006-12-27 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
WO2005097799A1 (en) 2004-04-07 2005-10-20 Pfizer Limited Pyrazolo`4,3-d! pyrimidines
US7540286B2 (en) * 2004-06-03 2009-06-02 Alexza Pharmaceuticals, Inc. Multiple dose condensation aerosol devices and methods of forming condensation aerosols
US20100006092A1 (en) * 2004-08-12 2010-01-14 Alexza Pharmaceuticals, Inc. Aerosol Drug Delivery Device Incorporating Percussively Activated Heat Packages
EP1781360A1 (en) * 2004-08-12 2007-05-09 Alexza Pharmaceuticals, Inc. Aerosol drug delivery device incorporating percussively activated heat packages
WO2006044821A1 (en) * 2004-10-19 2006-04-27 Sb Pharmco Puerto Rico Inc. Crf receptor antagonists and methods relating thereto
EP1814590B2 (en) 2004-11-01 2013-12-11 Amylin Pharmaceuticals, Inc. Treatment of obesity and related disorders
EP1814878B1 (en) 2004-11-24 2012-01-04 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
US20090286723A1 (en) 2005-02-11 2009-11-19 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
ES2574014T3 (en) 2005-05-30 2016-06-14 Msd K.K. Novel Piperidine Derivative
US7932257B2 (en) 2005-07-22 2011-04-26 Sunesis Pharmaceuticals, Inc. Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors
EP1916239A4 (en) 2005-08-10 2009-10-21 Banyu Pharma Co Ltd Pyridone compound
BRPI0614649A2 (en) 2005-08-11 2011-04-12 Amylin Pharmaceuticals Inc hybrid polypeptides with selectable properties
EP1921065B1 (en) 2005-08-24 2010-10-20 Banyu Pharmaceutical Co., Ltd. Phenylpyridone derivative
WO2007029847A1 (en) 2005-09-07 2007-03-15 Banyu Pharmaceutical Co., Ltd. Bicyclic aromatic substituted pyridone derivative
US7915286B2 (en) 2005-09-16 2011-03-29 Ranbaxy Laboratories Limited Substituted pyrazolo [3,4-b] pyridines as phosphodiesterase inhibitors
EP1940842B1 (en) 2005-09-29 2012-05-30 Merck Sharp & Dohme Corp. Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators
BRPI0617621A2 (en) 2005-10-21 2011-08-02 Novartis Ag combination of organic compounds
AU2006307046A1 (en) 2005-10-27 2007-05-03 Msd K.K. Novel benzoxathiin derivative
MY146564A (en) 2005-11-10 2012-08-30 Msd Kk Aza-substituted spiro derivatives
EP2698157B1 (en) 2006-09-22 2015-05-20 Merck Sharp & Dohme Corp. Method of treatment using fatty acid synthesis inhibitors
WO2008038692A1 (en) 2006-09-28 2008-04-03 Banyu Pharmaceutical Co., Ltd. Diaryl ketimine derivative
US20080216828A1 (en) 2007-03-09 2008-09-11 Alexza Pharmaceuticals, Inc. Heating unit for use in a drug delivery device
AU2008233662B2 (en) 2007-04-02 2012-08-23 Msd K.K. Indoledione derivative
CN105250285B (en) * 2007-04-11 2019-09-06 奥默罗斯公司 Prevent and treat the composition and method of habituation
US11241420B2 (en) 2007-04-11 2022-02-08 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
US20160331729A9 (en) 2007-04-11 2016-11-17 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
US7879802B2 (en) 2007-06-04 2011-02-01 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
WO2009034411A1 (en) * 2007-09-12 2009-03-19 Centre National De La Recherche Scientifique Perharidines as cdk inhibitors
CA2714617A1 (en) 2008-03-06 2009-09-11 Banyu Pharmaceutical Co., Ltd. Alkylaminopyridine derivative
US20110015198A1 (en) 2008-03-28 2011-01-20 Banyu Pharmaceutical Co., Inc. Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism
CN102015704A (en) 2008-04-29 2011-04-13 霍夫曼-拉罗奇有限公司 Pyrimidinyl pyridone inhibitors of JNK
EP3239170B1 (en) 2008-06-04 2019-03-20 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
EP2301936A1 (en) 2008-06-19 2011-03-30 Banyu Pharmaceutical Co., Ltd. Spirodiamine-diarylketoxime derivative
EP3241839B1 (en) 2008-07-16 2019-09-04 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders
EP2319841A1 (en) 2008-07-30 2011-05-11 Msd K.K. (5-membered)-(5-membered) or (5-membered)-(6-membered) fused ring cycloalkylamine derivative
RU2493157C2 (en) * 2008-08-20 2013-09-20 Пфайзер Инк. PYRROLO[2,3-d]PYRIMIDINE DERIVATIVES
CA2741125A1 (en) 2008-10-22 2010-04-29 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
CA2741644C (en) 2008-10-30 2013-05-07 Merck Sharp & Dohme Corp. Isonicotinamide orexin receptor antagonists
WO2010051206A1 (en) 2008-10-31 2010-05-06 Merck Sharp & Dohme Corp. Novel cyclic benzimidazole derivatives useful anti-diabetic agents
US20110243940A1 (en) 2008-12-16 2011-10-06 Schering Corporation Bicyclic pyranone derivatives and methods of use thereof
EP2379547A1 (en) 2008-12-16 2011-10-26 Schering Corporation Pyridopyrimidine derivatives and methods of use thereof
PL2473487T3 (en) * 2009-09-03 2017-07-31 Bristol-Myers Squibb Company Quinazolines as potassium ion channel inhibitors
EP2526102B1 (en) 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III Inhibitors of PI3 kinase
ES2937386T3 (en) 2010-01-27 2023-03-28 Arena Pharm Inc Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts of same
US8895596B2 (en) 2010-02-25 2014-11-25 Merck Sharp & Dohme Corp Cyclic benzimidazole derivatives useful as anti-diabetic agents
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
SG188548A1 (en) 2010-09-22 2013-04-30 Arena Pharm Inc Modulators of the gpr119 receptor and the treatment of disorders related thereto
EP2677869B1 (en) 2011-02-25 2017-11-08 Merck Sharp & Dohme Corp. Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents
CN102219791A (en) * 2011-04-08 2011-10-19 天津希恩思生化科技有限公司 Color biotin used for large biological molecule marking, as well as applications in preparing large biological molecule marking reagent
WO2012167053A1 (en) * 2011-06-01 2012-12-06 Janus Biotherapeutics, Inc. Novel immune system modulators
AR088352A1 (en) 2011-10-19 2014-05-28 Merck Sharp & Dohme ANTAGONISTS OF THE RECEIVER OF 2-PIRIDILOXI-4-NITRILE OREXINE
AU2012340869B2 (en) 2011-11-23 2017-03-02 Cancer Research Technology Limited Thienopyrimidine inhibitors of atypical protein kinase C
LT2794600T (en) 2011-12-22 2018-02-26 Novartis Ag 2,3-dihydro-benzo[1,4]oxazine derivatives and related compounds as phosphoinositide-3 kinase (pi3k) inhibitors for the treatment of e.g. rheumatoid arthritis
AU2013296470B2 (en) 2012-08-02 2016-03-17 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
WO2014124458A1 (en) 2013-02-11 2014-08-14 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases
AU2014219020A1 (en) 2013-02-22 2015-07-23 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2014139388A1 (en) 2013-03-14 2014-09-18 Merck Sharp & Dohme Corp. Novel 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
US9708367B2 (en) 2013-03-15 2017-07-18 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase and their uses
JP6606491B2 (en) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド Ultra high purity agonist of guanylate cyclase C, method for producing and using the same
KR101666700B1 (en) * 2013-07-15 2016-10-17 주식회사 엘지화학 Polymer and organic solar cell comprising the same
WO2015051496A1 (en) 2013-10-08 2015-04-16 Merck Sharp & Dohme Corp. Antidiabetic tricyclic compounds
JP6769963B2 (en) 2014-08-29 2020-10-14 ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ Inhibitor of α-amino-β-carboxymuconic acid semialdehyde decarboxylase
GB201416628D0 (en) * 2014-09-19 2014-11-05 Johnson Matthey Plc Complexes and methods for their preparation
EP3242666A1 (en) 2015-01-06 2017-11-15 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
JP6838744B2 (en) 2015-06-22 2021-03-03 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 (R) -2- (7- (4-cyclopentyl-3- (trifluoromethyl) benzyloxy) -1,2,3,4-tetrahydrocyclopenta [b] indole-for use in S1P1 receptor-related disorders Crystalline L-arginine salt of 3-yl) acetic acid (Compound 1)
AU2017342083A1 (en) 2016-10-14 2019-04-11 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
KR20190116416A (en) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. Compounds and Methods for Treating Primary Bile Cholangitis
CA3067695A1 (en) * 2017-06-21 2018-12-27 Mitokinin, Inc. Compositions and methods using the same for treatment of neurodegenerative and mitochondrial disease
US11427578B1 (en) 2017-07-18 2022-08-30 Bayer Pharma Aktiengesellschaft Substituted pyrrolopyridine-derivatives
US10508113B2 (en) 2018-03-12 2019-12-17 Abbvie Inc. Inhibitors of tyrosine kinase 2 mediated signaling
KR20210111248A (en) 2018-11-20 2021-09-10 테스 파마 에스.알.엘. Inhibitors of α-amino-β-carboxymuconic acid semialdehyde decarboxylase
EP3894406A1 (en) 2018-12-11 2021-10-20 Bayer Aktiengesellschaft Substituted pyrrolopyridine-derivatives
WO2020167706A1 (en) 2019-02-13 2020-08-20 Merck Sharp & Dohme Corp. 5-alkyl pyrrolidine orexin receptor agonists
WO2021026047A1 (en) 2019-08-08 2021-02-11 Merck Sharp & Dohme Corp. Heteroaryl pyrrolidine and piperidine orexin receptor agonists
EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
WO2021249913A1 (en) 2020-06-09 2021-12-16 Bayer Aktiengesellschaft 2'-(quinolin-3-yl)-5',6'-dihydrospiro[azetidine-3,4'-pyrrolo[1,2-b]pyrazole]-1-carboxylate derivatives and related compounds as map4k1 (hpk1) inhibitors for the treatment of cancer
US11691971B2 (en) 2020-06-19 2023-07-04 Incyte Corporation Naphthyridinone compounds as JAK2 V617F inhibitors
US11753413B2 (en) 2020-06-19 2023-09-12 Incyte Corporation Substituted pyrrolo[2,1-f][1,2,4]triazine compounds as JAK2 V617F inhibitors
WO2022006456A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic pyridone compounds as jak2 v617f inhibitors
MX2023000056A (en) 2020-07-02 2023-04-12 Incyte Corp Tricyclic urea compounds as jak2 v617f inhibitors.
CR20230089A (en) 2020-08-18 2023-04-11 Merck Sharp & Dohme Llc Bicycloheptane pyrrolidine orexin receptor agonists
US11661422B2 (en) 2020-08-27 2023-05-30 Incyte Corporation Tricyclic urea compounds as JAK2 V617F inhibitors
WO2022140231A1 (en) 2020-12-21 2022-06-30 Incyte Corporation Deazaguaine compounds as jak2 v617f inhibitors
WO2022167627A1 (en) 2021-02-05 2022-08-11 Bayer Aktiengesellschaft Map4k1 inhibitors
TW202302589A (en) 2021-02-25 2023-01-16 美商英塞特公司 Spirocyclic lactams as jak2 v617f inhibitors

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003510A1 (en) * 1996-07-24 1998-01-29 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
WO1999038868A1 (en) * 1998-01-28 1999-08-05 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
WO1999040091A1 (en) * 1998-02-06 1999-08-12 Amgen Inc. Bicyclic pyridine and pyrimidine derivatives as neuropeptide y receptor antagonists

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2465568A (en) * 1949-03-29 Pyrimidine compounds
US2437683A (en) * 1948-03-16 Pyrimedine compounds and method of
GB587550A (en) * 1944-09-25 1947-04-29 Francis Henry Swinden Curd New pyrimidine compounds
EP0239191A3 (en) 1986-01-30 1988-07-20 Beecham Group Plc Pyrazolo[4,3-b]pyridine derivatives, process for their preparation and pharmaceutical compositions containing them
US5273608A (en) 1990-11-29 1993-12-28 United Solar Systems Corporation Method of encapsulating a photovoltaic device
TW444018B (en) 1992-12-17 2001-07-01 Pfizer Pyrazolopyrimidines
DK0674641T3 (en) * 1992-12-17 1999-09-27 Pfizer Pyrrolopyrimidines as CRF antagonists
US5664057A (en) 1993-07-07 1997-09-02 Picturetel Corporation Fixed bit rate speech encoder/decoder
RU2153494C2 (en) * 1993-10-12 2000-07-27 Дзе Дюпон Мерк Фармасьютикал Компани 1-n-alkyl-n-arylpyrimodineamines, method of patient treatment, pharmaceutical composition
TW530047B (en) 1994-06-08 2003-05-01 Pfizer Corticotropin releasing factor antagonists
CN1056611C (en) 1994-06-16 2000-09-20 美国辉瑞有限公司 Pyrazolo and pyrrolopyridines
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
EP0729758A3 (en) 1995-03-02 1997-10-29 Pfizer Pyrazolopyrimidines and pyrrolopyrimidines for treatment of neuronal and other disorders
AU716993B2 (en) 1995-05-12 2000-03-16 Neurogen Corporation Novel deazapurine derivatives; a new class of CRF1 specific ligands
US6403599B1 (en) * 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
US5955613A (en) 1995-10-13 1999-09-21 Neurogen Corporation Certain pyrrolopyridine derivatives; novel CRF1 specific ligands
EP0863882B1 (en) 1995-10-17 2002-02-06 Janssen Pharmaceutica N.V. Amino substituted pyrimidines and triazines
DK0778277T3 (en) 1995-12-08 2003-10-27 Pfizer Substituted heterocyclic derivatives as CRF antagonists
CA2233307A1 (en) 1996-02-07 1997-08-14 Terence J. Moran Thiophenopyrimidines
WO1997033580A1 (en) 1996-03-11 1997-09-18 Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Maintaining kidney function during surgery or trauma
US6326368B1 (en) * 1996-03-27 2001-12-04 Dupont Pharmaceuticals Company Aryloxy- and arylthiosubstituted pyrimidines and triazines and derivatives thereof
US6107300A (en) 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
ZA973884B (en) 1996-05-23 1998-11-06 Du Pont Merck Pharma Tetrahydropteridines and pyridylpiperazines for treatment of neurological disorders
TW477787B (en) 1996-08-27 2002-03-01 Pfizer Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same
CZ68199A3 (en) 1996-08-28 1999-11-17 Pfizer Inc. 6,5-heterobicyclic derivatives, pharmaceutical composition based thereon and method of treating diseases
WO1998029397A1 (en) * 1996-12-27 1998-07-09 Yoshitomi Pharmaceutical Industries, Ltd. Fused pyrimidine compounds and medicinal use thereof
EP0970082A2 (en) * 1997-02-18 2000-01-12 Neurocrine Biosciences, Inc. Biazacyclic crf antagonists
WO1998042706A1 (en) 1997-03-21 1998-10-01 Du Pont Pharmaceuticals Company Method of making arylamino triazolopyridines
WO1998042699A1 (en) 1997-03-26 1998-10-01 Taisho Pharmaceutical Co., Ltd. 4-tetrahydropyridylpyrimidine derivatives
JP2002501493A (en) 1997-04-22 2002-01-15 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Thiophenopyridines as CRF antagonists
US6482836B1 (en) 1997-04-22 2002-11-19 Charles Huang CRF antagonistic quino- and quinazolines
NL1010018C2 (en) 1997-09-09 1999-03-10 Duphar Int Res Quinoline and quinazoline derivatives with corticotropin releasing factor (CRF) antagonistic effect.
US6613777B1 (en) * 1998-03-06 2003-09-02 Chen Chen CRF antagonistic pyrazolo[4,3-b]pyridines
YU23802A (en) 1999-09-30 2004-09-03 Neurogen Corporation Certain alkylene diamine-substituted pyrazolo/1,5-a/1,5- pyrimidines and pyrazolo/1,5-a/-1,3,5-triazines
EA200200424A1 (en) 1999-09-30 2002-12-26 Ньюроджен Корпорейшн Some heterocycles substituted by alkylene diamin
EP1263768A4 (en) 2000-01-28 2004-05-12 Neurogen Corp Chimeric neuropeptide y receptors
DE60115092T2 (en) 2000-12-12 2006-03-30 Neurogen Corp., Brandford SPIRO [ISOBENZOFURAN-1,4'-PIPERIDIN] -3-ONE AND 3H-SPIROISOBENZOFURAN-1,4'-PIPERIDINE
CA2403307A1 (en) 2001-10-23 2003-04-23 Neurogen Corporation Substituted 2-cyclohexyl-4-phenyl-1h-imidazole derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998003510A1 (en) * 1996-07-24 1998-01-29 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
WO1999038868A1 (en) * 1998-01-28 1999-08-05 Du Pont Pharmaceuticals Company Azolo triazines and pyrimidines
WO1999040091A1 (en) * 1998-02-06 1999-08-12 Amgen Inc. Bicyclic pyridine and pyrimidine derivatives as neuropeptide y receptor antagonists

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8835430B2 (en) 2002-02-01 2014-09-16 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9018204B1 (en) 2002-02-01 2015-04-28 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9346765B2 (en) 2002-02-01 2016-05-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9416112B2 (en) 2002-02-01 2016-08-16 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9913842B2 (en) 2002-02-01 2018-03-13 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and their uses
US9266912B2 (en) 2005-01-19 2016-02-23 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses

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