AR072063A1 - Mimeticos de glucocorticoides metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos - Google Patents

Mimeticos de glucocorticoides metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos

Info

Publication number
AR072063A1
AR072063A1 ARP090102043A ARP090102043A AR072063A1 AR 072063 A1 AR072063 A1 AR 072063A1 AR P090102043 A ARP090102043 A AR P090102043A AR P090102043 A ARP090102043 A AR P090102043A AR 072063 A1 AR072063 A1 AR 072063A1
Authority
AR
Argentina
Prior art keywords
methods
optionally
pharmaceutical compositions
manufacturing
alkylthio
Prior art date
Application number
ARP090102043A
Other languages
English (en)
Inventor
Christian Harcken
Pingrong Liu
Rajashekhar Betageri
Hossein Razavi
Thomas Wai-Ho Lee
Todd Bosanac
Soojin Kim
Michael Jason Burke
David Thompson
David Thomson
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR072063A1 publication Critical patent/AR072063A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P3/08Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones farmaceuticas que contienen dichos compuestos, y metodos para modular la funcion del receptor de glucocorticoides y metodos para tratar estados de enfermedad o afecciones mediadas por la funcion del receptor de glucocorticoides o caracterizadas por procesos inflamatorios, alergicos o proliferativos en un paciente usando estos compuestos. Reivindicacion 1: Un compuesto caracterizado porque tiene de Formula (1) en la que: R1 es un grupo arilo o heteroarilo, cada uno opcional e independientemente sustituido con uno, dos o tres grupos sustituyentes seleccionados entre alquilo C1-5, aminocarbonilo, alquilaminocarbonilo C1-5, dialquilaminocarbonilo C1-5, aminosulfonilo, alquilaminosulfonilo C1-5, dialquilaminosulfonilo C1-5, halogeno, hidroxilo, ciano y alquiltio C1-5, donde el  tomo de azufre est  opcionalmente oxidado a un sulfoxido o una sulfona; R2 es alquiltio C1-5, donde el  tomo de azufre est  opcionalmente oxidado a un sulfoxido o una sulfona, opcional e independientemente sustituido con uno, dos o tres grupos sustituyentes seleccionados entre halogeno, hidroxi, oxo, ciano, alcoxialquilo y amino carbonilo; X es CH o N; y Y es CH o N, donde X y Y no son ambos CH, o un tautomero, isomero optico, prof rmaco, co-cristal o sal de los mismos.
ARP090102043A 2008-06-06 2009-06-05 Mimeticos de glucocorticoides metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos AR072063A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5938808P 2008-06-06 2008-06-06

Publications (1)

Publication Number Publication Date
AR072063A1 true AR072063A1 (es) 2010-08-04

Family

ID=41068652

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102043A AR072063A1 (es) 2008-06-06 2009-06-05 Mimeticos de glucocorticoides metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos

Country Status (23)

Country Link
US (1) US8268859B2 (es)
EP (1) EP2300472B1 (es)
JP (1) JP2011524867A (es)
KR (1) KR20110020902A (es)
CN (1) CN102112476A (es)
AR (1) AR072063A1 (es)
AT (1) ATE541846T1 (es)
AU (1) AU2009256289A1 (es)
BR (1) BRPI0915680A2 (es)
CA (1) CA2726449A1 (es)
CL (1) CL2010001363A1 (es)
CO (1) CO6321245A2 (es)
CY (1) CY1113004T1 (es)
DK (1) DK2300472T3 (es)
ES (1) ES2381257T3 (es)
HR (1) HRP20120311T1 (es)
MX (1) MX2010013095A (es)
PT (1) PT2300472E (es)
SI (1) SI2300472T1 (es)
TW (1) TW201002708A (es)
UY (1) UY31878A (es)
WO (1) WO2009149139A1 (es)
ZA (1) ZA201008379B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04009329A (es) * 2002-03-26 2005-01-25 Boehringer Ingelheim Pharma Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y usos de los mismos.
RS20050174A (en) * 2002-08-29 2007-06-04 Boehringer Ingelheim Pharmaceuticals Inc., -3(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
UY28526A1 (es) * 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
US7795272B2 (en) * 2004-03-13 2010-09-14 Boehringer Ingelheim Pharmaceutical, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
US7741361B2 (en) * 2004-12-27 2010-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2008070507A2 (en) * 2006-12-06 2008-06-12 Boehringer Ingelheim International Gmbh Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2009256289A1 (en) 2008-06-06 2009-12-10 Boehringer Ingelheim International Gmbh Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US20100312013A1 (en) * 2009-06-03 2010-12-09 Boehringer Ingelheim International Gmbh Steroselective synthesis of certain trifluoromethyl-substituted alcohols
US20110130578A1 (en) 2009-06-03 2011-06-02 Boehringer Ingelheim International Gmbh Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US8420819B2 (en) 2009-06-03 2013-04-16 Boehringer Ingelheim International Gmbh Process for optimizing the particle size of an active pharmaceutical ingredient by crystallization
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
TW201422590A (zh) 2012-09-07 2014-06-16 Abbvie Inc 雜環核激素受體調節劑
EP2935284A4 (en) * 2012-12-21 2016-04-27 Abbvie Inc HETEROCYCLIC MODULATORS OF HORMONE NUCLEAR RECEPTORS
CN105481777B (zh) * 2015-12-29 2018-12-14 江西同和药业股份有限公司 一种替格瑞洛中间体的制备方法
CA3123490A1 (en) 2019-01-22 2020-07-30 Akribes Biomedical Gmbh Selective glucocorticoid receptor modifiers for treating impaired skin wound healing

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1017612B (de) 1954-02-05 1957-10-17 Thomae Gmbh Dr K Verfahren zur Herstellung von tertiaeren Aminen, ihren Saeureadditionssalzen und quaternaeren Ammoniumverbindungen
US3772273A (en) * 1969-01-17 1973-11-13 Allied Chem Derivatives of quinoxaline
NL8402755A (nl) 1983-09-22 1985-04-16 Sandoz Ag Azool-derivaten, werkwijze voor het bereiden daarvan, preparaten die ze bevatten, en toepassing daarvan.
JPS60163814A (ja) 1984-02-06 1985-08-26 Wataru Mori グルココルチコイド拮抗剤
GB8406000D0 (en) 1984-03-07 1984-04-11 Ici Plc Olefine derivatives
US4551534A (en) * 1984-03-30 1985-11-05 American Home Products Corporation Aralkyl or aryloxyalkyl 1,7-naphthyridine-3-carboxylic acid esters
DE3514696A1 (de) * 1985-04-24 1986-11-06 Bayer Ag, 5090 Leverkusen N-indolylethyl-sulfonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
GB8617653D0 (en) 1986-07-18 1986-08-28 Ici Plc Amide derivatives
GB2210875B (en) 1987-10-09 1991-05-29 Farmos Oy Aromatase inhibiting 4(5)-imidazoles
US5039691A (en) * 1989-06-08 1991-08-13 Marion Merrell Dow Inc. 5-(1-(imidazol)methyl)-3,3-disubstituted-2(3H)furanone derivatives
US5206377A (en) * 1991-12-05 1993-04-27 Whitby Research, Inc. Compounds useful as antiproliferative agents
JPH05194404A (ja) 1992-01-22 1993-08-03 Zeria Pharmaceut Co Ltd カルボスチリル誘導体
GB9201755D0 (en) 1992-01-28 1992-03-11 British Bio Technology Compounds
US5948820A (en) * 1994-08-22 1999-09-07 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and pharmaceutical use thereof
CZ176197A3 (cs) 1994-12-22 1998-09-16 Ligand Pharmaceuticals Incorporated Modulátory steroidových receptorů a způsoby jejich přípravy a použití
US5688808A (en) * 1994-12-22 1997-11-18 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
WO1997027852A1 (en) 1996-01-30 1997-08-07 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
JPH1180131A (ja) 1997-09-01 1999-03-26 Mitsubishi Chem Corp エチニルピリミジン誘導体
CO4980885A1 (es) 1997-12-29 2000-11-27 Ortho Mcneil Pharm Inc Compuestos de trifenilpropanamida utiles en el tratamiento de inflamaciones y metodos para preparar dicho compuesto
US6506766B1 (en) * 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
EP0937710B1 (en) * 1998-02-16 2003-04-16 Ajinomoto Co., Inc. Method for producing an optically active phenylpropionic acid derivative
DE19816624A1 (de) 1998-04-15 1999-10-21 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
US6169106B1 (en) * 1998-04-15 2001-01-02 Boehringer Ingelheim Pharma Kg Indolinones having kinase inhibitory activity
KR20010052431A (ko) 1998-06-08 2001-06-25 오테스코그 페르 당뇨병 치료제
US6187918B1 (en) * 1999-03-15 2001-02-13 Dupont Pharmaceuticals Company Catalysts for asymmetric addition of organozinc reagents to aldehydes and method for preparation
ATE243195T1 (de) 1998-09-25 2003-07-15 Boehringer Ingelheim Pharma Neue substituierte indolinone mit einer inhibierenden wirkung auf verschiedene kinasen und cyclin/cdk-komplexe
DE19856475A1 (de) 1998-11-27 2000-05-31 Schering Ag Nichtsteroidale Entzündungshemmer
AP1542A (en) * 1999-04-30 2006-01-31 Pfizer Prod Inc Glucocorticoid receptor modulators.
BR0013200A (pt) 1999-07-16 2002-05-07 Bristol Myers Squibb Pharma Co Compostos derivados de heterobiciclos contendo nitrogênio, composições farmacêuticas, método de tratamento ou prevenção de uma disfunção tromboembólica e uso dos compostos
US6436986B1 (en) * 1999-09-01 2002-08-20 Abbott Laboratories Glucocorticoid receptor antagonists for treatment of diabetes
US6329534B1 (en) * 1999-09-01 2001-12-11 Abbott Laboratories Glucocorticoid receptor antagonists for treatment of diabetes
CO5271670A1 (es) * 1999-10-29 2003-04-30 Pfizer Prod Inc Antagonistas del factor de liberacion de corticitropina y composiciones relacionadas
US7713989B2 (en) * 2000-04-27 2010-05-11 Dow Robert L Glucocorticoid receptor modulators
CA2411165A1 (en) 2000-05-02 2002-12-11 Meiji Seika Kaisha, Ltd. Novel indole derivatives exhibiting chymase-inhibitory activities and process for preparation thereof
WO2002009702A2 (en) 2000-07-28 2002-02-07 Inspire Pharmaceuticals, Inc. Use of indole derivatives for the manufacture of a medicament for reducing intracular pressure
DE10038639A1 (de) * 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
US6583180B2 (en) * 2001-02-14 2003-06-24 Abbott Laboratories Glucocorticoid receptor modulators
US6872533B2 (en) * 2001-07-27 2005-03-29 The Regents Of The University Of California STK15 (STK6) gene polymorphism and methods of determining cancer risk
GB0124299D0 (en) 2001-10-10 2001-11-28 Astrazeneca Ab Crystal structure of enzyme and uses thereof
WO2003032997A1 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
DE60309829T2 (de) * 2002-01-14 2007-09-13 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Glucocorticoidmimetika, verfahren zu ihrer herstellung, diese enthaltende pharmazeutische formulierungen und ihre verwendungen
MXPA04009329A (es) * 2002-03-26 2005-01-25 Boehringer Ingelheim Pharma Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y usos de los mismos.
US7268152B2 (en) * 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
US6897224B2 (en) * 2002-04-02 2005-05-24 Schering Ag Quinoline and isoquinoline derivatives, a process for their production and their use as inflammation inhibitors
US7186864B2 (en) * 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
ITMI20021247A1 (it) * 2002-06-07 2003-12-09 Menarini Ricerche Spa Antagonisti basici non peptidici della bradichinina e loro impiego informulazioni farmaceutiche
GB0215650D0 (en) 2002-07-05 2002-08-14 Cyclacel Ltd Bisarylsufonamide compounds
AU2003259747A1 (en) 2002-08-21 2004-03-11 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
RS20050174A (en) 2002-08-29 2007-06-04 Boehringer Ingelheim Pharmaceuticals Inc., -3(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
US7112584B2 (en) * 2002-12-20 2006-09-26 Schering Ag Nonsteroidal antiinflammatory agents
JP4373926B2 (ja) * 2003-01-03 2009-11-25 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 1−プロパノール及び1−プロピルアミン誘導体ならびにグルココルチコイドリガンドとしての使用
JP2006515014A (ja) * 2003-01-30 2006-05-18 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド PKC−θのインヒビターとして有用な2,4−ジアミノピリミジン誘導体
WO2004071389A2 (en) 2003-02-15 2004-08-26 Glaxo Group Limited Non-steroidal infalmmation inhibitors
US20040224992A1 (en) 2003-02-27 2004-11-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004089415A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST
US7429594B2 (en) * 2003-08-20 2008-09-30 Amgen Inc. Substituted heterocyclic compounds and methods of use
UY28526A1 (es) * 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
DE602004017884D1 (de) * 2003-10-03 2009-01-02 Boehringer Ingelheim Pharma Fluoreszenzsonden zur verwendung bei einem bindungsassay auf proteinkinaseinhibitoren
US7507843B2 (en) * 2003-10-16 2009-03-24 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US7795272B2 (en) * 2004-03-13 2010-09-14 Boehringer Ingelheim Pharmaceutical, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof
US7179919B2 (en) 2004-03-18 2007-02-20 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
JP2007530541A (ja) * 2004-03-22 2007-11-01 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックスとしてのα−トリフルオロメチルアルコール又はアミン
US7256300B2 (en) * 2004-03-30 2007-08-14 Boehringer Ingelheim Pharmaceuticals, Inc. Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
US20060030608A1 (en) * 2004-08-04 2006-02-09 Boehringer Ingelheim Pharmaceuticals, Inc. Anti aromatase compounds pharmaceutical compositions and uses thereof
US20090093485A1 (en) 2004-10-29 2009-04-09 Astrazeneca Ab Novel Sulphonamide Derivatives as Glucocorticoid Receptor Modulators for the Treatment of Inflammatory Diseases
US20070072870A2 (en) * 2004-12-08 2007-03-29 Solvay Pharmeceuticals B.V. Phenylpiperazine derivatives with a combination of partial dopamine-d2 receptor agonism and serotonin reuptake inhibition
US7741361B2 (en) 2004-12-27 2010-06-22 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US20090176807A1 (en) * 2005-03-04 2009-07-09 John Robinson Regan Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
MX2007014811A (es) 2005-06-10 2008-02-14 Boehringer Ingelheim Int Mimeticos de glucocorticoides, metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos.
CA2623004A1 (en) * 2005-09-30 2007-04-12 Boehringer Ingelheim International Gmbh Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
AU2009256289A1 (en) 2008-06-06 2009-12-10 Boehringer Ingelheim International Gmbh Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Also Published As

Publication number Publication date
EP2300472B1 (en) 2012-01-18
WO2009149139A8 (en) 2011-02-24
TW201002708A (en) 2010-01-16
EP2300472A1 (en) 2011-03-30
CN102112476A (zh) 2011-06-29
CL2010001363A1 (es) 2011-05-13
BRPI0915680A2 (pt) 2019-09-24
ES2381257T3 (es) 2012-05-24
CO6321245A2 (es) 2011-09-20
AU2009256289A1 (en) 2009-12-10
PT2300472E (pt) 2012-02-20
SI2300472T1 (sl) 2012-05-31
CA2726449A1 (en) 2009-12-10
HRP20120311T1 (en) 2012-05-31
ZA201008379B (en) 2012-01-25
KR20110020902A (ko) 2011-03-03
WO2009149139A1 (en) 2009-12-10
US20090325988A1 (en) 2009-12-31
DK2300472T3 (da) 2012-04-10
JP2011524867A (ja) 2011-09-08
CY1113004T1 (el) 2016-04-13
ATE541846T1 (de) 2012-02-15
MX2010013095A (es) 2010-12-21
UY31878A (es) 2010-01-29
US8268859B2 (en) 2012-09-18

Similar Documents

Publication Publication Date Title
AR072063A1 (es) Mimeticos de glucocorticoides metodos para su fabricacion, composiciones farmaceuticas y usos de los mismos
AR060792A1 (es) Ligandos de gucorticoides, metodos para prepararlos, composiciones farmaceuticas, y usos de los mismos
PE20180044A1 (es) Compuestos novedosos
AR119651A1 (es) Compuestos heterocíclicos y de heteroarilo para tratar la enfermedad de huntington
PE20190656A1 (es) Compuestos de tiazolo-piridina sustituida como inhibidores de malt1
PE20180462A1 (es) Moduladores cot y metodos de uso de los mismos
AR106314A1 (es) COMPUESTOS DE ESPIRO[3H-INDOL-3,2’-PIRROLIDIN]-2(1H)-ONA Y DERIVADOS COMO INHIBIDORES DE MDM2 - p53
AR122049A2 (es) Derivados de pirimidiniloxi benceno como herbicidas
AR056511A1 (es) Derivados de 2-aminopirimidinas, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por el receptor de histamina h4
AR053195A1 (es) Compuestos inhibidores de dipeptidil peptidasa-iv metodos para preparar los mismos y composiciones farmaceuticas que los contienen como un agente activo
UY28157A1 (es) Miméticos de glucocorticoides métodos para su elaboración composiciones farmacéuticas y sus usos
ECSP16082790A (es) Composición de control de enfermedades de plantas y método para controlar enfermedades de plantas mediante su aplicación
AR086829A1 (es) Compuestos heterociclicos fusionados como moduladores del canal ionico
AR083367A1 (es) Compuestos de tipo quinazolinona como antagonistas de crth
AR054799A1 (es) Derivados de oxindol
AR048427A1 (es) Derivados de sulfonilpirroles con actividad inhibitoria de la histona deacetilasa, composiciones farmaceuticas que los contienen y el uso de las mismas para el tratamiento de enfermedades relacionadas.
AR082850A1 (es) Aminopirazoloquinazolinas
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR048789A1 (es) Derivados de oxazol y sus composiciones como moduladores de receptor activado de proliferador de peroxisoma (ppar)
AR112216A1 (es) Derivados de azaquinolina
AR052938A1 (es) Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades mediadas por el receptor vr1
AR074021A1 (es) Compuestos heterociclicos fusionados como moduladores del canal ionico
AR053435A1 (es) Derivados de 5-amminoindol, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un madicamento para el tratamiento de enfermedades asociadas a la modulacion de receptores h3.
CL2008000959A1 (es) Compuestos derivados de 1,2,4-tiadiazina o 1,4-tiazina; composiciones farmaceuticas que los contienen; y su uso para la prevencion y/o tratamiento de infecciones producidas por el virus de la hepatitis c.
ECSP088926A (es) Compuestos de piridil amida sustituidos como moduladores del receptor h3 de la histamina

Legal Events

Date Code Title Description
FB Suspension of granting procedure