PE20061093A1 - Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3 - Google Patents

Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3

Info

Publication number
PE20061093A1
PE20061093A1 PE2006000177A PE2006000177A PE20061093A1 PE 20061093 A1 PE20061093 A1 PE 20061093A1 PE 2006000177 A PE2006000177 A PE 2006000177A PE 2006000177 A PE2006000177 A PE 2006000177A PE 20061093 A1 PE20061093 A1 PE 20061093A1
Authority
PE
Peru
Prior art keywords
alkyl
cxcr3
substituted
hydroxyalkyl
heterocycles
Prior art date
Application number
PE2006000177A
Other languages
English (en)
Inventor
Seong Heon Kim
Michael K C Wong
Stuart B Rosenblum
Yuefei Shao
Douglas W Hobbs
Brian F Mcguinness
Joseph A Kozlowski
Qingbei Zeng
Gopinadhan N Anilkumar
Original Assignee
Schering Corp
Pharmacopeia 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 Schering Corp, Pharmacopeia Inc filed Critical Schering Corp
Publication of PE20061093A1 publication Critical patent/PE20061093A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A COMPUESTOS DE PIPERAZINAS SUSTITUIDAS CON HETEROCICLOS, DE FORMULA (I), EN DONDE G ES HETEROARILO O HETEROCICLENILO DE 5 MIEMBROS QUE AL MENOS CONTIENE UN RESTO -C=N-, Y EN FORMA OPCIONAL Y ADICIONAL UN GRUPO N, N(O), O, S, S(O)(1-2) SOBRE EL ANILLO Y OPCIONALMENTE SUSTITUIDOS; R3 Y R6 SON INDEPENDIENTEMENTE H, ALQUILO, HALOALQUILO, HIDROXIALQUILO, HALOGENO, -N(R30), -OR30, CN, -N=CH-ALQUILO, NR30C(=O)ALQUILO, ENTRE OTROS; R10 Y R11 SON INDEPENDIENTEMENTE H, ALQUILO, ARALQUILO, HIDROXIALQUILO, CARBONILO, ENTRE OTROS; R12 ES H, CN, -C(=O)N(R30)2 Y ALQUILO; D ES ARILO, HATEROARILO, HETEROCICLENILO O HETEROCICLILO DE 5 MIEMBROS Y SUSTITUIDO DE 0 A 4 RESTOS DE R20; Y ES -(CHR13)r-, -(CR13R13)r-, -C(=O)-, -CHR13C(=O)-, ENTRE OTROS. SON PREFERIDOS: 5-CLORO-3-(5-METIL-1,3,4-OXADIAZOL-2-IL)-6-[(1-(4-CLOROBENZIL)-4-METILPIPERIDINA-4-IL)-3-ETILPIPERAZIN-1-IL]-PIRAZIN-2-AMINA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON ANTAGONISTAS DE QUIMIOCINAS: CXCR3, POR LO QUE SON UTILES EN EL TRATAMIENTO DE AFECCIONES INFLAMATORIAS (PSORIASIS Y ENFERMEDADES INTESTINALES INFLAMATORIAS), AUNTOINMUNES(ESCLEROSIS MULTIPLES, ARTRITIS), RECHAZO A INJERTOS
PE2006000177A 2005-02-16 2006-02-14 Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3 PE20061093A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US65330905P 2005-02-16 2005-02-16

Publications (1)

Publication Number Publication Date
PE20061093A1 true PE20061093A1 (es) 2006-11-10

Family

ID=36637011

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000177A PE20061093A1 (es) 2005-02-16 2006-02-14 Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3

Country Status (17)

Country Link
US (2) US7868006B2 (es)
EP (1) EP1848710B1 (es)
JP (2) JP4873352B2 (es)
KR (1) KR20070107046A (es)
CN (1) CN101163692B (es)
AR (1) AR052911A1 (es)
AU (1) AU2006214477A1 (es)
BR (1) BRPI0607385A2 (es)
CA (1) CA2598456A1 (es)
IL (1) IL185072A0 (es)
MX (1) MX2007009945A (es)
NO (1) NO20074690L (es)
PE (1) PE20061093A1 (es)
RU (1) RU2007134259A (es)
TW (1) TW200640907A (es)
WO (1) WO2006088837A2 (es)
ZA (1) ZA200706790B (es)

Families Citing this family (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0410805A (pt) 2003-09-09 2006-06-27 Fumapharm Ag uso de derivados do ácido fumárico para tratamento da insuficiência cardìaca e asma
WO2005101838A2 (en) 2004-04-13 2005-10-27 Incyte Corporation Piperazinylpiperidine derivatives as chemokine receptor antagonists
AU2006216941B2 (en) * 2005-02-16 2009-12-03 Pharmacopeia, Llc Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity
AU2006214378A1 (en) * 2005-02-16 2006-08-24 Pharmacopeia, Inc. Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
EP1853583B1 (en) * 2005-02-16 2011-09-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
AU2006214480A1 (en) * 2005-02-16 2006-08-24 Pharmacopeia, Inc. Novel heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity
TW200714610A (en) * 2005-02-16 2007-04-16 Univ Maryland CXCR3 is a gliadin receptor
CN101142209A (zh) * 2005-02-16 2008-03-12 先灵公司 具有cxcr3拮抗剂活性的吡嗪基取代的哌嗪-哌啶
US7868006B2 (en) * 2005-02-16 2011-01-11 Schering Corporation Heterocyclic substituted piperazines with CXCR3 antagonist activity
CA2625762A1 (en) * 2005-10-11 2007-04-26 Schering Corporation Substituted heterocyclic compounds with cxcr3 antagonist activity
CN101460482B (zh) 2006-03-21 2013-03-27 默沙东公司 具有cxcr3拮抗剂活性的杂环取代的吡啶化合物
EP2041117B1 (en) * 2006-07-14 2012-08-22 Merck Sharp & Dohme Corp. Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity
JP2010511728A (ja) * 2006-12-05 2010-04-15 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｉｌ−８受容体アンタゴニスト
HRP20220902T3 (hr) 2007-02-08 2022-10-14 Biogen Ma Inc. Pripravci i njihova upotreba u liječenju multiple skleroze
EP2124996A4 (en) 2007-02-20 2010-03-24 Merrimack Pharmaceuticals Inc METHODS OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING ALPHA-FETOPROTEIN COMBINED WITH INTEGRIN ANTAGONIST
EP2125750B1 (en) * 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN101678082B (zh) 2007-03-26 2013-06-19 再生医药有限公司 使用cxcl9和抗cxcl9抗体促进骨髓保护和再生的方法
EP2183228B1 (en) * 2007-07-26 2014-08-20 Vitae Pharmaceuticals, Inc. CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1
CA2695365A1 (en) * 2007-08-03 2009-02-12 Schering Corporation Method of treating cxcr3 mediated diseases using heterocyclic substituted piperazines
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2009079490A1 (en) * 2007-12-18 2009-06-25 Schering Corporation Process and intermediates for the synthesis of heterocyclic substituted piperazines with cxcr3 antagonist activity
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
CA2712500A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2009102428A2 (en) * 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-OXAZEPAN-2-ONE AND 1,3-DIAZEPAN-2-ONE INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE 1
EP2254872A2 (en) * 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
CA2723039A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5451752B2 (ja) * 2008-05-01 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
CA2722427A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010010157A2 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
AU2009274567B2 (en) 2008-07-25 2013-04-04 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
JP5702293B2 (ja) 2008-11-10 2015-04-15 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒキナーゼの阻害剤として有用な化合物
LT3354650T (lt) 2008-12-19 2022-06-27 Vertex Pharmaceuticals Incorporated Junginiai, naudingi kaip atr kinazės inhibitoriai
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US20100331320A1 (en) * 2009-04-30 2010-12-30 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
RU2012153675A (ru) 2010-05-12 2014-06-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, пригодные в качестве ингибиторов atr киназы
US9062008B2 (en) 2010-05-12 2015-06-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2569287B1 (en) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8933072B2 (en) 2010-06-16 2015-01-13 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
NZ605627A (en) 2010-06-23 2015-06-26 Vertex Pharma Pyrrolo-pyrazine derivatives useful as inhibitors of atr kinase
JP5813106B2 (ja) 2010-06-25 2015-11-17 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 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン
JP5874124B2 (ja) 2010-06-28 2016-03-02 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 緑内障の処置に使用するための薬学的組成物
EP2635268A1 (en) 2010-11-02 2013-09-11 Boehringer Ingelheim International GmbH Pharmaceutical combinations for the treatment of metabolic disorders
EP2694498B1 (en) 2011-04-05 2016-03-30 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
WO2012178124A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014517079A (ja) 2011-06-22 2014-07-17 バーテックス ファーマシューティカルズ インコーポレイテッド Ａｔｒキナーゼ阻害剤として有用な化合物
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2751741T3 (es) 2011-09-30 2020-04-01 Vertex Pharma Procedimiento para fabricar compuestos útiles como inhibidores de la quinasa ATR
WO2013049722A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP6162126B2 (ja) 2011-09-30 2017-08-23 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ａｔｒ阻害剤による膵臓癌及び非小細胞肺癌の治療
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
HUE031313T2 (hu) 2011-10-28 2017-07-28 Univ Vanderbilt Szubsztituált 2-(4-heterociklilbenzil)izoindolin-1-on analógok mint muszkarin acetilkolin receptor M1 pozitív allosztérikus modulátorai
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776419B1 (en) 2011-11-09 2016-05-11 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
JP5465815B2 (ja) 2011-11-11 2014-04-09 Ｓａｎｓｈｏ株式会社 関節症治療剤
UA113638C2 (xx) 2012-02-02 2017-02-27 4-(бензоімідазол-2-іл)-тіазольні сполуки та споріднені азапохідні
SI2833973T1 (en) 2012-04-05 2018-04-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase and their combination therapy
EP2904406B1 (en) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
US8912198B2 (en) 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2892608C (en) 2012-12-07 2021-10-19 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2948134B1 (en) 2013-01-24 2020-03-04 Palvella Therapeutics, Inc. Compositions for transdermal delivery of mtor inhibitors
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CA2916338C (en) 2013-07-22 2021-07-06 Actelion Pharmaceuticals Ltd 1-(piperazin-1-yl)-2-([1,2,4]triazol-1-yl)-ethanone derivatives
SG10201804791UA (en) 2013-12-06 2018-07-30 Vertex Pharma 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
US9763992B2 (en) 2014-02-13 2017-09-19 Father Flanagan's Boys' Home Treatment of noise induced hearing loss
AR099789A1 (es) 2014-03-24 2016-08-17 Actelion Pharmaceuticals Ltd Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina
PT3152212T (pt) 2014-06-05 2020-03-13 Vertex Pharma Derivados radiomarcados de um composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor de atr quinase, preparação do dito composto e diferentes formas sólidas do mesmo
KR20170016498A (ko) 2014-06-17 2017-02-13 버텍스 파마슈티칼스 인코포레이티드 Chk1 및 atr 저해제의 병용물을 사용하는 암의 치료 방법
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
TR201900680T4 (tr) 2015-01-15 2019-02-21 Idorsia Pharmaceuticals Ltd CXCR3 Reseptör modülatörleri olarak hidroksialkil- piperazin türevleri.
JP7187308B2 (ja) 2015-09-30 2022-12-12 バーテックス ファーマシューティカルズ インコーポレイテッド Ｄｎａ損傷剤とａｔｒ阻害剤との組み合わせを使用する、がんを処置するための方法
IL267869B2 (en) 2017-01-06 2023-10-01 Palvella Therapeutics Inc Non-aqueous preparations of mTOR inhibitors and methods of use
WO2020010073A1 (en) 2018-07-02 2020-01-09 Palvella Therapeutics, Inc. ANHYDROUS COMPOSITIONS OF mTOR INHIBITORS AND METHODS OF USE

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2915892A (en) 1991-11-14 1993-06-15 Glaxo Group Limited Piperidine acetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
AU3351293A (en) * 1992-01-21 1993-08-03 Glaxo Group Limited Piperidineacetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
JPH0971564A (ja) * 1995-07-06 1997-03-18 Japan Tobacco Inc ベンズアミドオキシム誘導体及びその医薬用途
NZ326354A (en) * 1996-01-15 1999-05-28 Janssen Pharmaceutica Nv 3-(substituted-1-piperazinyl)-6-(substituted-1,2,4-thiadiazol-5 -yl)-pyridazine derivatives and medicaments
US6124319A (en) * 1997-01-21 2000-09-26 Merck & Co., Inc. 3,3-disubstituted piperidines as modulators of chemokine receptor activity
TR199903082T2 (xx) * 1997-06-24 2000-07-21 Janssen Pharmaceutica N.V. Anjiogenez inhibit�r� 5-s�bstit�e-1,2,4,-tiadiazolil t�revleri.
AR013693A1 (es) 1997-10-23 2001-01-10 Uriach & Cia Sa J Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria
HUP0203528A3 (en) * 1999-05-04 2003-11-28 Schering Corp Piperidine derivatives useful as ccr5 antagonists, pharmaceutical compositions containing them and their use
AU2001253496A1 (en) * 2000-04-14 2001-10-30 Millennium Pharmaceuticals, Inc. Treating graft rejection with cxcr3 inhibitors
EA007538B1 (ru) * 2000-12-11 2006-10-27 Туларик Инк. Антагонисты cxcr3
US6469002B1 (en) 2001-04-19 2002-10-22 Millennium Pharmaceuticals, Inc. Imidazolidine compounds
US6794379B2 (en) * 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
GB0203994D0 (en) 2002-02-20 2002-04-03 Celltech R&D Ltd Chemical compounds
WO2003075929A1 (en) * 2002-03-13 2003-09-18 Janssen Pharmaceutica N.V. Inhibitors of histone deacetylase
AU2003220968A1 (en) * 2002-03-28 2003-10-13 Kyowa Hakko Kogyo Co., Ltd. Anti-inflammatory agent
AU2003236354A1 (en) 2002-04-03 2003-10-13 Sumitomo Pharmaceuticals Co., Ltd. Novel blood sugar controller and method of screening the same
US7244555B2 (en) 2002-05-14 2007-07-17 Renovak Inc Systems and methods for identifying organ transplant risk
US20050272936A1 (en) 2002-06-03 2005-12-08 Axten Jeffrey M Imidazolium cxcr3 inhibitors
SE0300457D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
SE0300456D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
WO2004074260A1 (ja) * 2003-02-21 2004-09-02 Kyowa Hakko Kogyo Co., Ltd. ピリミジン誘導体
CA2529161A1 (en) * 2003-06-13 2004-12-29 Schering Aktiengesellschaft Quinolyl amide derivatives as ccr-5 antagonists
CN101142209A (zh) * 2005-02-16 2008-03-12 先灵公司 具有cxcr3拮抗剂活性的吡嗪基取代的哌嗪-哌啶
CN101189238A (zh) * 2005-02-16 2008-05-28 先灵公司 具有cxcr3拮抗剂活性的哌嗪-哌啶
EP1853583B1 (en) * 2005-02-16 2011-09-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
US7868006B2 (en) 2005-02-16 2011-01-11 Schering Corporation Heterocyclic substituted piperazines with CXCR3 antagonist activity
AU2006216941B2 (en) * 2005-02-16 2009-12-03 Pharmacopeia, Llc Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity
AU2006214480A1 (en) * 2005-02-16 2006-08-24 Pharmacopeia, Inc. Novel heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity
AU2006214378A1 (en) * 2005-02-16 2006-08-24 Pharmacopeia, Inc. Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
CA2625762A1 (en) * 2005-10-11 2007-04-26 Schering Corporation Substituted heterocyclic compounds with cxcr3 antagonist activity
CN101460482B (zh) * 2006-03-21 2013-03-27 默沙东公司 具有cxcr3拮抗剂活性的杂环取代的吡啶化合物
EP2041117B1 (en) * 2006-07-14 2012-08-22 Merck Sharp & Dohme Corp. Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity
AR064609A1 (es) 2006-12-22 2009-04-15 Schering Corp Piperazinas sustituidas, composiciones farmaceuticas que las comprenden y su uso en el tratamiento de enfermedades mediadas por el receptor de quimiocinas cxcr3.

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