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PE20090219A1 - Compuestos mimeticos de glucocorticoides, metodos de preparacion y composiciones farmaceuticas - Google Patents

Compuestos mimeticos de glucocorticoides, metodos de preparacion y composiciones farmaceuticas

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Publication number
PE20090219A1
PE20090219A1 PE2008001807A PE2008001807A PE20090219A1 PE 20090219 A1 PE20090219 A1 PE 20090219A1 PE 2008001807 A PE2008001807 A PE 2008001807A PE 2008001807 A PE2008001807 A PE 2008001807A PE 20090219 A1 PE20090219 A1 PE 20090219A1
Authority
PE
Peru
Prior art keywords
alkyl
diabetes
methyl
optionally substituted
hydroxy
Prior art date
Application number
PE2008001807A
Other languages
English (en)
Inventor
Pingrong Liu
Younes Bekkali
Michel J Emmanuel
Christian H J J Harcken
Daniel Kuzmich
Usha R Patel
Doris Riether
Ji Wang
John Robert Proudfoot
Hidenori Takahashi
Rajashekhar Betageri
Abdelhakim Hammach
Thomas M Kirrane
Thomas Wai-Ho Lee
Hossein Razavi
David S Thomson
Renee Zindell
Original Assignee
Boehringer Ingelheim Pharma
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 Pharma filed Critical Boehringer Ingelheim Pharma
Publication of PE20090219A1 publication Critical patent/PE20090219A1/es

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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
    • C07D213/60—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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
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Abstract

SE REFIERE A COMPUESTOS DE FORMULA (IB) DONDE R1 ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R2 Y R3 SON CADA UNO ALQUILO C1-C5; R4 ES ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5 OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C3, HIDROXI, HALOGENO, AMINO, OXO; R5 ES HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALCOXICARBONILO C1-C5, ALCANOILOXI C1-C5, AMINOCARBONILO, ENTRE OTROS; R6 ES H, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS, NO PUDIENDO SER TRIFLUOROMETILO, OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-CICLOPROPIL-4-(5-FLUORO-2-METOXIFENIL)-4-METIL-1-(1H-PIRROLO[3,2-c]PIRIDIN-2-IL)PENTAN-2-OL, METIL ESTER DEL ACIDO 4-(5-FLUORO-2-METOXIFENIL)-2-HIDROXI-4-METIL-2-(1H-PIRROLO[2,3-c]PIRIDIN-2-ILMETIL)PENTANOICO, 2-[2-DIFLUOROMETIL-2-HIDROXI-4-(5-METANSULFONIL-2,3-DIHIDROBENZOFURAN-7-IL)-4-METILPENTIL]-4-METIL-1H-INDOL-6-CARBONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE GLUCOCORTICOIDES SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES PULMONARES, REUMATICAS, ALERGICAS, RENALES, HEPATICAS, CARDIOVASCULARES, NEUROLOGICAS, DIABETES TIPO I y II, OBESIDAD, ENFERMEDAD DE ALZHEIMER, ARTERIOESCLEROSIS, OSTEOARTRITIS, DOLOR GRAVE Y CRONICO
PE2008001807A 2003-09-24 2004-09-21 Compuestos mimeticos de glucocorticoides, metodos de preparacion y composiciones farmaceuticas PE20090219A1 (es)

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Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101022977B1 (ko) * 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
CN1678306A (zh) * 2002-08-29 2005-10-05 贝林格尔·英格海姆药物公司 在炎性、变应性和增生性疾病中用作糖皮质激素模拟物的3－(磺酰氨基乙基)－吲哚衍生物
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
CA2558019A1 (en) * 2004-03-22 2005-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
WO2006042102A2 (en) * 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
ES2326907T3 (es) * 2004-12-27 2009-10-21 Boehringer Ingelheim Pharmaceuticals Inc. Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y su uso.
US8093281B2 (en) 2005-04-14 2012-01-10 Glaxo Group Limited Indazoles as glucocorticoid receptor ligands
JP2008543780A (ja) 2005-06-10 2008-12-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グルココルチコイド模倣薬、それらの製造方法、医薬組成物及びそれらの使用
GB0513297D0 (en) * 2005-06-29 2005-08-03 Glaxo Group Ltd Novel compounds
ES2333820T3 (es) * 2005-09-30 2010-03-01 Boehringer Ingelheim International Gmbh Sintesis estereoselectiva de determinados alcoholes trifluorometilo-sustituidos.
BRPI0710240A2 (pt) 2006-04-20 2011-08-09 Glaxo Group Ltd composto, uso de um composto, método para o tratamento de um paciente humano ou animal com uma condição ou doença, composição farmacêutica, combinação, e, processo para a preparação de um composto
GB0611587D0 (en) * 2006-06-12 2006-07-19 Glaxo Group Ltd Novel compounds
WO2008000777A2 (en) * 2006-06-29 2008-01-03 Glaxo Group Limited Phenyl- pyrazole derivatives, process for their preparation and their pharmaceutical use
RU2431502C2 (ru) * 2006-07-07 2011-10-20 Бош Энд Ломб Инкорпорейтед Фармацевтические композиции для лечения сухости глаз
CA2660151C (en) 2006-08-07 2012-04-17 Bausch & Lomb Incorporated Compositions and methods for treating, controlling, reducing, or ameliorating infections and sequelae thereof
WO2008027796A2 (en) * 2006-08-31 2008-03-06 Bausch & Lomb Incorporated Compositions and methods for treating or preventing glaucoma or progression thereof
US20110104159A1 (en) * 2006-09-11 2011-05-05 Rohrs Brian R Compositions and methods for treating, controlling, reducing, ameliorating, or preventing allergy
US20110105559A1 (en) * 2006-09-11 2011-05-05 Rohrs Brian R Compositions and Methods for Treating, Controlling, Reducing, Ameliorating, or Preventing Allergy
DK2061444T3 (da) * 2006-09-11 2011-06-27 Bausch & Lomb Sammensætninger og fremgangsmåder til behandling, kontrol, reducering, forbedring eller forebyggelse af allergi
GB0620385D0 (en) 2006-10-13 2006-11-22 Glaxo Group Ltd Novel compounds
RU2009125614A (ru) 2006-12-06 2011-01-20 Бёрингер Ингельхайм Интернациональ Гмбх (De) Глюкокортикоидные миметики, способы их получения, фармацевтические композиции и их применения
US20100035926A1 (en) * 2006-12-20 2010-02-11 Ian Baxter Campbell Pyrazole derivatives as non-steroidal glucocorticoid receptor ligands
US20090042936A1 (en) * 2007-08-10 2009-02-12 Ward Keith W Compositions and Methods for Treating or Controlling Anterior-Segment Inflammation
US20090087443A1 (en) * 2007-09-27 2009-04-02 Bartels Stephen P Pharmacological Adjunctive Treatment Associated with Glaucoma Filtration Surgery
US8143280B2 (en) 2007-09-27 2012-03-27 Hoffmann-La Roche Inc. Glucocorticoid receptor antagonists
GB0720544D0 (en) * 2007-10-19 2007-11-28 Glaxo Group Ltd Novel compounds
GB0720557D0 (en) * 2007-10-19 2007-11-28 Glaxo Group Ltd Novel compounds
GB0720546D0 (en) * 2007-10-19 2007-11-28 Glaxo Group Ltd Novel compounds
US20090239836A1 (en) * 2008-03-24 2009-09-24 Mary Lee Ciolkowski Multifunctional Ophthalmic Compositions
US20090291073A1 (en) * 2008-05-20 2009-11-26 Ward Keith W Compositions Comprising PKC-theta and Methods for Treating or Controlling Ophthalmic Disorders Using Same
BRPI0915680A2 (pt) * 2008-06-06 2019-09-24 Boehringer Ingelheim Int miméticos de glicocorticoide, métodos de prepará-los, composições farmacêuticas, e usos dos mesmos
US8268820B2 (en) 2009-03-26 2012-09-18 Hoffmann-La Roche Inc. 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
US8138189B2 (en) 2009-03-26 2012-03-20 Hoffman-La Roche Inc. Substituted benzene compounds as modulators of the glucocorticoid receptor
US20110077270A1 (en) * 2009-04-21 2011-03-31 Pfeffer Bruce A Compositions and Methods for Treating Ocular Inflammation with Lower Risk of Increased Intraocular Pressure
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
US20110130567A1 (en) * 2009-06-03 2011-06-02 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
US8324239B2 (en) 2010-04-21 2012-12-04 Novartis Ag Furopyridine compounds and uses thereof
EP2714688B1 (en) * 2011-05-26 2016-02-24 Daiichi Sankyo Company, Limited Heterocyclic compounds as protein kinase inhibitors
US20120316199A1 (en) 2011-06-07 2012-12-13 Ward Keith W Compositions and methods for treating, controlling, reducing, or ameliorating inflammatory pain
EP2738172A1 (en) * 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
CN103468812B (zh) * 2013-09-17 2015-02-25 安徽医科大学 一种检测糖皮质激素治疗sle疗效的试剂盒
CN105085384A (zh) * 2014-05-16 2015-11-25 泰州市高港区进燕生物技术有限公司 2-溴-4-甲氧基吡啶的制备方法
CA2961489A1 (en) 2014-09-17 2016-03-24 Glen Robert RENNIE Sgc stimulators
CN104774950B (zh) * 2015-04-21 2017-10-03 安徽医科大学 一种基于hsp90aa1基因型预测糖皮质激素治疗sle疗效的试剂盒
WO2016187028A1 (en) * 2015-05-15 2016-11-24 Celgene Avilomics Research, Inc. Heteroaryl compounds, synthesis thereof, and intermediates thereto
HRP20200064T1 (hr) 2015-06-09 2020-04-03 Abbvie Inc. Modulatori nuklearnih receptora (ror) namijenjeni liječenju upalnih i autoimunih bolesti
WO2016198908A1 (en) 2015-06-09 2016-12-15 Abbvie Inc. Ror nuclear receptor modulators
WO2021122645A1 (en) 2019-12-20 2021-06-24 Syngenta Crop Protection Ag Pesticidally active azole-amide compounds
EP4232027A4 (en) * 2020-10-26 2024-12-25 Yale University INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR, AND METHODS OF MAKING AND USING THE SAME
CN120842201B (zh) * 2025-09-22 2026-01-06 浙江伟锋药业有限公司 N-（5-嘧啶甲基）-2-吡啶胺的制备方法

Family Cites Families (86)

* 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.
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
GB8617653D0 (en) 1986-07-18 1986-08-28 Ici Plc Amide derivatives
GB8617652D0 (en) 1986-07-18 1986-08-28 Ici Plc Acylanilide derivatives
US5114946A (en) 1987-06-12 1992-05-19 American Cyanamid Company Transdermal delivery of pharmaceuticals
US4818541A (en) 1987-08-19 1989-04-04 Schering Corporation Transdermal delivery of enantiomers of phenylpropanolamine
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
IL107120A (en) 1992-09-29 1997-09-30 Boehringer Ingelheim Int Atomising nozzle and filter and spray generating device
US5948820A (en) * 1994-08-22 1999-09-07 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and pharmaceutical use thereof
HUT78117A (hu) 1994-12-22 1999-11-29 Ligand Pharmaceuticals Incorporated Szteroid receptor modulátor kinolin- és kondenzált kinolinszármazékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények
US5696133A (en) * 1994-12-22 1997-12-09 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
DE19536902A1 (de) 1995-10-04 1997-04-10 Boehringer Ingelheim Int Vorrichtung zur Hochdruckerzeugung in einem Fluid in Miniaturausführung
DE19536903C2 (de) 1995-10-04 1998-09-10 Boehringer Ingelheim Int Vorrichtung zum Haltern eines fluidischen Bauteils
DE19545226C1 (de) 1995-12-05 1997-06-19 Boehringer Ingelheim Int Sperrspannwerk für einen federbetätigten Abtrieb
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
US6372779B1 (en) 1997-12-29 2002-04-16 Ortho Pharmaceutical Corporation Anti-inflammatory compounds
BR9907788A (pt) 1998-02-13 2001-10-30 Abbott Lab Agentes antiinflamatórios seletivos paraglicocorticóides
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
ES2196721T3 (es) * 1998-02-16 2003-12-16 Ajinomoto Kk Metodo para producir un derivado de acido fenilpropionico opticamente activo.
US6169106B1 (en) * 1998-04-15 2001-01-02 Boehringer Ingelheim Pharma Kg Indolinones having kinase inhibitory activity
DE19816624A1 (de) 1998-04-15 1999-10-21 Boehringer Ingelheim Pharma Neue substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel
JP2002527355A (ja) 1998-06-08 2002-08-27 カロ バイオ アクチェブラーグ 糖尿病の治療
US6187918B1 (en) * 1999-03-15 2001-02-13 Dupont Pharmaceuticals Company Catalysts for asymmetric addition of organozinc reagents to aldehydes and method for preparation
PT1115704E (pt) 1998-09-25 2003-11-28 Boehringer Ingelheim Pharma Novas indolinonas substituidas com accao inibidora sobre varias quinases e complexos ciclina/cdk
DE19856475A1 (de) 1998-11-27 2000-05-31 Schering Ag Nichtsteroidale Entzündungshemmer
TR200103104T2 (tr) * 1999-04-30 2002-05-21 Pfizer Products Inc. Glukortikoid alıcı modülatörleri
CA2380727A1 (en) 1999-07-16 2001-01-25 Bristol-Myers Squibb Pharma Company Nitrogen containing heterobicycles as factor xa inhibitors
US6329534B1 (en) 1999-09-01 2001-12-11 Abbott Laboratories Glucocorticoid receptor antagonists for treatment of diabetes
US6436986B1 (en) 1999-09-01 2002-08-20 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
JPWO2001083471A1 (ja) 2000-05-02 2004-04-15 明治製菓株式会社 キマーゼ阻害作用を有する新規インドール誘導体、及びインドール誘導体の製造法
DE10038639A1 (de) * 2000-07-28 2002-02-21 Schering Ag Nichtsteroidale Entzündungshemmer
AR035651A1 (es) 2000-07-28 2004-06-23 Univ Madrid Complutense Uso de derivados de indol para la manufactura de un medicamento para reducir la presion intraocular y una composicion
CA2433520A1 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
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
US20030017503A1 (en) 2001-05-18 2003-01-23 Boehringer Ingelheim Pharmaceuticals, Inc. Methods and labeled molecules for determining ligand binding to steroid receptors
WO2003012046A2 (en) * 2001-07-27 2003-02-13 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
UY27487A1 (es) 2001-10-17 2003-05-30 Boehringer Ingelheim Pharma Derivados de pirimidina, medicamentos que contienen estos compuestos, su empleo y procedimiento para su preparación
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
JP2005521717A (ja) 2002-03-26 2005-07-21 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、その製造方法、その医薬組成物、及び使用
KR101022977B1 (ko) * 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
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
CN1678306A (zh) 2002-08-29 2005-10-05 贝林格尔·英格海姆药物公司 在炎性、变应性和增生性疾病中用作糖皮质激素模拟物的3－(磺酰氨基乙基)－吲哚衍生物
JP2004139389A (ja) * 2002-10-18 2004-05-13 Minolta Co Ltd 画像データ管理装置、画像データ管理プログラム、および画像形成装置
US7112584B2 (en) * 2002-12-20 2006-09-26 Schering Ag Nonsteroidal antiinflammatory agents
MXPA05006872A (es) * 2003-01-03 2005-08-16 Boehringer Ingelheim Pharma Derivados de 1-propanol y 1-propilamina y su uso como ligandos glucocorticoides.
EP1590334B1 (en) * 2003-01-30 2009-08-19 Boehringer Ingelheim Pharmaceuticals Inc. 2,4-diaminopyrimidine derivatives useful as inhibitors of pkc-theta
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
EP1615667A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S Combinations of an 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist
CA2535644A1 (en) * 2003-08-20 2005-03-03 Amgen Inc. Substituted pyrimdinone derivatives 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
ATE414701T1 (de) * 2003-10-03 2008-12-15 Boehringer Ingelheim Pharma Fluoreszenzsonden zur verwendung bei einem bindungsassay auf proteinkinaseinhibitoren
JP4468369B2 (ja) * 2003-10-16 2010-05-26 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 ある種のトリフルオロメチル置換アルコールの立体選択的合成
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
CA2558019A1 (en) * 2004-03-22 2005-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics
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
BRPI0517263A (pt) 2004-10-29 2008-10-07 Astrazeneca Ab novos derivados de sulfonamida como moduladores do receptor de glicocorticóide para o tratamento de doenças inflamatórias
US20060122247A1 (en) * 2004-12-08 2006-06-08 Solvay Pharmaceuticals B.V. Aryloxyethylamine and phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition
ES2326907T3 (es) * 2004-12-27 2009-10-21 Boehringer Ingelheim Pharmaceuticals Inc. Mimeticos de glucocorticoides, metodos para su preparacion, composiciones farmaceuticas y su uso.
US20090176807A1 (en) * 2005-03-04 2009-07-09 John Robinson Regan Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
JP2008543780A (ja) * 2005-06-10 2008-12-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング グルココルチコイド模倣薬、それらの製造方法、医薬組成物及びそれらの使用
US7888381B2 (en) * 2005-06-14 2011-02-15 Bristol-Myers Squibb Company Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity, and use thereof
ES2333820T3 (es) * 2005-09-30 2010-03-01 Boehringer Ingelheim International Gmbh Sintesis estereoselectiva de determinados alcoholes trifluorometilo-sustituidos.
BRPI0915680A2 (pt) * 2008-06-06 2019-09-24 Boehringer Ingelheim Int miméticos de glicocorticoide, métodos de prepará-los, composições farmacêuticas, e usos dos mesmos

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PE20090217A1 (es) 2009-03-26
TWI340138B (en) 2011-04-11
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AU2004275757A1 (en) 2005-04-07
CN101948425A (zh) 2011-01-19
IL174475A0 (en) 2006-08-01
PE20050951A1 (es) 2005-12-12
RU2006113696A (ru) 2007-11-20
PE20090218A1 (es) 2009-03-28
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AU2004275757B2 (en) 2011-03-24
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MXPA06002880A (es) 2006-06-05
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