BRPI0607385A2 - piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3 - Google Patents

piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3

Info

Publication number
BRPI0607385A2
BRPI0607385A2 BRPI0607385-9A BRPI0607385A BRPI0607385A2 BR PI0607385 A2 BRPI0607385 A2 BR PI0607385A2 BR PI0607385 A BRPI0607385 A BR PI0607385A BR PI0607385 A2 BRPI0607385 A2 BR PI0607385A2
Authority
BR
Brazil
Prior art keywords
compound
diseases
limiting example
therapy
antagonist activity
Prior art date
Application number
BRPI0607385-9A
Other languages
English (en)
Inventor
Seong Heon Kim
Gopinadhan N Anilkumar
Michael K C Wong
Qingbei Zeng
Yuefei Shao
Brian F Mc Guinness
Stuart B Rosenblum
Joseph A Kozlowski
Douglas W Hobbs
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 BRPI0607385A2 publication Critical patent/BRPI0607385A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/06Antibacterial agents for tuberculosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • A61P31/08Antibacterial agents for leprosy
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • 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
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (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

PIPERAZINAS SUBSTITUìDAS HETEROCìCLICAS COM ATIVIDADE DE ANTAGONISTA DE CXCR3. A presente invenção refere-se a um composto, ou enantiómeros, estereoisómeros, rotâmeros, tautómeros, racematos ou pró-fármacos do dito composto, ou sais, solvatos ou ésteres do dito composto farmaceuticamente aceitáveis, ou do dito pró-fármaco, o dito composto tendo uma estrutura geral apresentada na Fórmula 1: ou um sal, solvato ou éster do mesmo farmaceuticamente aceitável, em que as diversas porções estão definidas aqui. Está também descrito um método de tratar doenças mediadas por quimiocina, tais como, terapia paliativa, terapia curativa, terapia profilática de certas doenças e condições tais como doenças inflamatórias (exemplo(s) não limitante(s) inclui(incluem) psoríase), doenças auto-imunes (exemplo(s) não limitante(s) inclui(incluem) artrite reumatóide, esclerose múltipla), rejeição de enxerto (exemplo(s) não limitante(s) inclui(incluem) rejeição de aloenxerto, rejeição de xenoenxerto), doenças infecciosas (por exemplo, lepra tuberculóide), erupções fixas por fármaco, respostas de hipersensibilidade do tipo demorado cutâneo, inflamação oftálmica, diabetes tipo 1, meningite viral e tumores usando um composto da Fórmula 1.
BRPI0607385-9A 2005-02-16 2006-02-14 piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3 BRPI0607385A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65330905P 2005-02-16 2005-02-16
PCT/US2006/005123 WO2006088837A2 (en) 2005-02-16 2006-02-14 Heterocyclic substituted piperazines with cxcr3 antagonist activity

Publications (1)

Publication Number Publication Date
BRPI0607385A2 true BRPI0607385A2 (pt) 2009-09-01

Family

ID=36637011

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0607385-9A BRPI0607385A2 (pt) 2005-02-16 2006-02-14 piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3

Country Status (17)

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

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE602004010531T2 (de) 2003-09-09 2008-07-03 Fumapharm Ag Verwendung von fumarsäure-derivaten zur behandlung von herzinsuffizienz und asthma
CN103012374B (zh) 2004-04-13 2015-05-20 因塞特公司 作为趋化因子受体拮抗剂的哌嗪基哌啶衍生物
JP2008530213A (ja) * 2005-02-16 2008-08-07 シェーリング コーポレイション Cxcr3アンタゴニスト活性を有する、ヘテロアリールで置換されたピラジニル−ピペラジン−ピペリジン
PE20061093A1 (es) * 2005-02-16 2006-11-10 Schering Corp Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3
US7868005B2 (en) * 2005-02-16 2011-01-11 Schering Corporation Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity
WO2006088920A1 (en) * 2005-02-16 2006-08-24 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
CA2598457A1 (en) * 2005-02-16 2006-08-24 Schering Corporation Pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
ATE518855T1 (de) * 2005-02-16 2011-08-15 Schering Corp Neue heterozyklische substituierte pyridin- oder phenylverbindungen mit cxcr3-antagonistischer aktivität
TW200714610A (en) 2005-02-16 2007-04-16 Univ Maryland CXCR3 is a gliadin receptor
JP2009511582A (ja) * 2005-10-11 2009-03-19 シェーリング コーポレイション Cxcr3拮抗薬活性を有する置換複素環式化合物
PE20071144A1 (es) * 2006-03-21 2008-01-10 Schering Corp COMPUESTOS HETEROCICLICOS DE PIRIDINA SUSTITUIDA COMO ANTAGONISTAS DEL RECEPTOR 3 DE a-QUIMIOCINA (CXCR3)
EP2041117B1 (en) * 2006-07-14 2012-08-22 Merck Sharp & Dohme Corp. Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity
WO2008070707A1 (en) * 2006-12-05 2008-06-12 Smithkline Beecham Corporation Il-8 receptor antagonists
HRP20220902T3 (hr) 2007-02-08 2022-10-14 Biogen Ma Inc. Pripravci i njihova upotreba u liječenju multiple skleroze
AU2008219007A1 (en) 2007-02-20 2008-08-28 Merrimack Pharmaceuticals, Inc. Methods of treating multiple sclerosis by administration of alpha-fetoprotein in combination with an integrin antagonist
CA2678577A1 (en) * 2007-02-26 2008-09-04 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
WO2008116347A1 (en) 2007-03-26 2008-10-02 General Regeneratives Limited Methods for promoting protection and regeneration of bone marrow using cxcl9 and anti-cxcl9 antibodies
CL2008002199A1 (es) * 2007-07-26 2009-10-23 Vitae Pharmaceuticals Inc Compuestos derivados de 1,3-oxazin-2-ona; composicion farmaceutica que comprende a dichos compuestos; y uso para tratar una enfermedad asociada con la actividad de la 11beta-hidroxiesteroide deshidrogenasa tipo 1 (11beta-hsd1) tales como dislipidemia, hiperlipidemia, hipertension, obesidad y enfermedad cardiovascular, entre otras.
MX2010001400A (es) * 2007-08-03 2010-04-22 Schering Corp Metodo para tratar enfermedades mediadas cxcr3 usando piperazinas heterociclicas sustituidas.
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
US8440658B2 (en) 2007-12-11 2013-05-14 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
US20110124867A1 (en) * 2007-12-18 2011-05-26 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
JP5490020B2 (ja) 2008-01-24 2014-05-14 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の環状カルバゼート及びセミカルバジドインヒビター
CA2714532A1 (en) * 2008-02-11 2009-08-20 Vitae Pharmaceuticals, Inc. 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
JP5730021B2 (ja) * 2008-02-15 2015-06-03 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の阻害剤としてのシクロアルキルラクタム誘導体
WO2009134384A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
AR071236A1 (es) 2008-05-01 2010-06-02 Vitae Pharmaceuticals Inc Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
BRPI0911764A2 (pt) 2008-05-01 2015-10-06 Boehringer Ingelheim Int inibidores cíclicos de 11beta-hidroxiesteroide desigrogenase 1
WO2009134387A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
KR20110050459A (ko) 2008-07-25 2011-05-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
JP5777030B2 (ja) 2008-07-25 2015-09-09 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 11β−ヒドロキシステロイドデヒドロゲナーゼ1の阻害剤
WO2010127237A2 (en) * 2009-04-30 2010-11-04 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
AU2009313198B2 (en) 2008-11-10 2016-03-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
MX2011006503A (es) 2008-12-19 2011-09-06 Vertex Pharma Derivados de pirazina utiles como inhibidores de la cinasa de atr.
US8637505B2 (en) 2009-02-04 2014-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
EP2440537A1 (en) 2009-06-11 2012-04-18 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
JP5749263B2 (ja) 2009-07-01 2015-07-15 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
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
NZ603478A (en) 2010-05-12 2014-09-26 Vertex Pharma 2 -aminopyridine derivatives useful as inhibitors of atr kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569313A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2013526540A (ja) 2010-05-12 2013-06-24 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
EP2569289A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
WO2011159760A1 (en) 2010-06-16 2011-12-22 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
CA2803802A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
WO2011161128A1 (en) 2010-06-25 2011-12-29 Boehringer Ingelheim International Gmbh Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders
US9095591B2 (en) 2010-06-28 2015-08-04 Institut National De La Sante Et De La Recherche Medicale (Inserm) Pharmaceutical composition for use in the treatment of glaucoma
EA201300522A1 (ru) 2010-11-02 2013-11-29 Бёрингер Ингельхайм Интернациональ Гмбх Фармацевтические комбинации для лечения метаболических нарушений
CN103562204A (zh) 2011-04-05 2014-02-05 沃泰克斯药物股份有限公司 可用作tra激酶的抑制剂的氨基吡嗪化合物
EP2723745A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
JP2014522818A (ja) 2011-06-22 2014-09-08 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
WO2013049719A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2940121T3 (es) 2011-09-30 2023-05-03 Vertex Pharma Tratamiento de cáncer de pulmón de células no pequeñas con inhibidores de ATR
JP2014528419A (ja) 2011-09-30 2014-10-27 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キナーゼ阻害剤として有用な化合物
KR102184246B1 (ko) 2011-09-30 2020-12-01 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물의 제조 방법
WO2013049720A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
ES2604958T3 (es) 2011-10-28 2017-03-10 Vanderbilt University Análogos de 2-(4-heterociclilbencil)isoindolin-1-ona sustituidos como moduladores alostéricos positivos del receptor muscarínico de acetilcolina M1
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 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
JP2015502925A (ja) 2011-11-09 2015-01-29 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ピラジン化合物
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SG11201402226PA (en) 2011-11-11 2014-10-30 Sansho Co Therapeutic agent for arthrosis
EA027595B1 (ru) 2012-02-02 2017-08-31 Актелион Фармасьютиклз Лтд. 4-(бензоимидазол-2-ил)тиазольные соединения и родственные азапроизводные
DK2833973T3 (en) 2012-04-05 2018-01-02 Vertex Pharma Compounds useful as ATR kinase inhibitors and combination therapies thereof
WO2014055756A1 (en) 2012-10-04 2014-04-10 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
EP2909202A1 (en) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
HRP20180859T1 (hr) 2012-12-07 2018-07-13 Vertex Pharmaceuticals Incorporated 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid kao inhibitor atr kinaze
AU2014209141B2 (en) 2013-01-24 2018-05-10 Palvella Therapeutics, Inc. Compositions for transdermal delivery of mTOR inhibitors
JP2016512815A (ja) 2013-03-15 2016-05-09 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縮合ピラゾロピリミジン誘導体
EP3024832B1 (en) 2013-07-22 2018-03-28 Idorsia Pharmaceuticals Ltd 1-(piperazin-1-yl)-2-([1,2,4]triazol-1-yl)-ethanone derivatives
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
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
KR102575125B1 (ko) 2014-06-05 2023-09-07 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 저해제로서 유용한 2-아미노-6-플루오로-n-[5-플루오로-피리딘-3-일]-피라졸로[1,5-a]피리미딘-3-카복스아미드 화합물의 방사성표지된 유도체, 상기 화합물의 제조 및 이의 다양한 고체 형태
CA2950780C (en) 2014-06-17 2023-05-16 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of chk1 and atr inhibitors
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
AU2016207988B2 (en) 2015-01-15 2019-08-15 Idorsia Pharmaceuticals Ltd Hydroxyalkyl-piperazine derivatives as CXCR3 receptor modulators
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
CN110520097B (zh) 2017-01-06 2023-10-27 帕尔维拉治疗股份有限公司 Mtor抑制剂的无水组合物及其使用方法
BR112020007058A2 (pt) * 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
EP3817743A4 (en) 2018-07-02 2022-07-06 Palvella Therapeutics, Inc. ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE
US20250263412A1 (en) * 2021-03-15 2025-08-21 The Regents Of The University Of Michigan Non-hydroxamate hdac6 inhibitors and related methods of use

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW221996B (pt) * 1991-11-14 1994-04-01 Glaxo Group Ltd
JPH07503459A (ja) * 1992-01-21 1995-04-13 グラクソ、グループ、リミテッド 酢酸誘導体
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
SI0876366T1 (en) * 1996-01-15 2001-12-31 Janssen Pharmaceutica Nv Angiogenesis inhibiting pyridazinamines
US6124319A (en) * 1997-01-21 2000-09-26 Merck & Co., Inc. 3,3-disubstituted piperidines as modulators of chemokine receptor activity
JP2002505680A (ja) * 1997-06-24 2002-02-19 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 血管形成抑制5−置換−1,2,4−チアジアゾリル誘導体
AR013693A1 (es) 1997-10-23 2001-01-10 Uriach & Cia Sa J Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria
JP3894729B2 (ja) * 1999-05-04 2007-03-22 シェーリング コーポレイション Ccr5アンタゴニストとして有用なピペラジン誘導体
AU2001253496A1 (en) * 2000-04-14 2001-10-30 Millennium Pharmaceuticals, Inc. Treating graft rejection with cxcr3 inhibitors
WO2002083143A1 (en) * 2000-12-11 2002-10-24 Tularik Inc. Cxcr3 antagonists
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
ES2347544T3 (es) * 2002-03-13 2010-11-02 Janssen Pharmaceutica Nv Inhibidores de histona-desacetilasas.
JPWO2003082855A1 (ja) * 2002-03-28 2005-08-04 協和醗酵工業株式会社 抗炎症剤
JPWO2003082335A1 (ja) 2002-04-03 2005-07-28 住友製薬株式会社 新規血糖調節薬及びそのスクリーニング方法
US7244555B2 (en) 2002-05-14 2007-07-17 Renovak Inc Systems and methods for identifying organ transplant risk
JP2005530813A (ja) 2002-06-03 2005-10-13 スミスクライン・ビーチャム・コーポレイション イミダゾリウムcxcr3阻害剤
SE0300456D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
SE0300457D0 (sv) 2003-02-19 2003-02-19 Astrazeneca Ab Novel compounds
EP1595869A1 (en) * 2003-02-21 2005-11-16 Kyowa Hakko Kogyo Co., Ltd. Pyrimidine derivatives
BRPI0411414A (pt) * 2003-06-13 2006-07-25 Schering Ag derivados de quinolil amida como antagonistas de cdr-5
CA2598457A1 (en) * 2005-02-16 2006-08-24 Schering Corporation Pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
JP2008530213A (ja) * 2005-02-16 2008-08-07 シェーリング コーポレイション Cxcr3アンタゴニスト活性を有する、ヘテロアリールで置換されたピラジニル−ピペラジン−ピペリジン
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
WO2006088920A1 (en) * 2005-02-16 2006-08-24 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
PE20061093A1 (es) * 2005-02-16 2006-11-10 Schering Corp Piperazinas sustituidas con heterociclos con actividad antagonista de cxcr3
US7868005B2 (en) * 2005-02-16 2011-01-11 Schering Corporation Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity
ATE518855T1 (de) * 2005-02-16 2011-08-15 Schering Corp Neue heterozyklische substituierte pyridin- oder phenylverbindungen mit cxcr3-antagonistischer aktivität
JP2009511582A (ja) * 2005-10-11 2009-03-19 シェーリング コーポレイション Cxcr3拮抗薬活性を有する置換複素環式化合物
PE20071144A1 (es) * 2006-03-21 2008-01-10 Schering Corp COMPUESTOS HETEROCICLICOS DE PIRIDINA SUSTITUIDA COMO ANTAGONISTAS DEL RECEPTOR 3 DE a-QUIMIOCINA (CXCR3)
EP2041117B1 (en) * 2006-07-14 2012-08-22 Merck Sharp & Dohme Corp. Heterocyclic substituted piperazine compounds with cxcr3 antagonist activity
WO2008079279A1 (en) 2006-12-22 2008-07-03 Schering Corporation Heterocyclic compounds with cxcr3 antagonist activity

Also Published As

Publication number Publication date
US20060276479A1 (en) 2006-12-07
ZA200706790B (en) 2008-11-26
KR20070107046A (ko) 2007-11-06
CN101163692B (zh) 2012-01-18
JP2008530214A (ja) 2008-08-07
TW200640907A (en) 2006-12-01
CN101163692A (zh) 2008-04-16
AU2006214477A1 (en) 2006-08-24
MX2007009945A (es) 2007-09-26
PE20061093A1 (es) 2006-11-10
US7868006B2 (en) 2011-01-11
WO2006088837A3 (en) 2006-11-02
JP4873352B2 (ja) 2012-02-08
JP2011126901A (ja) 2011-06-30
NO20074690L (no) 2007-11-16
WO2006088837A2 (en) 2006-08-24
RU2007134259A (ru) 2009-03-27
EP1848710B1 (en) 2013-10-16
US20110065651A1 (en) 2011-03-17
EP1848710A2 (en) 2007-10-31
IL185072A0 (en) 2007-12-03
CA2598456A1 (en) 2006-08-24
US8207170B2 (en) 2012-06-26
AR052911A1 (es) 2007-04-11

Similar Documents

Publication Publication Date Title
BRPI0607385A2 (pt) piperazinas substituìdas heterocìclicas com atividade de antagonista de cxcr3
BRPI0607946A2 (pt) piperazina-piperidinas substituìdas por pirazinila com atividade de antagonista cxcr3
MX2008012161A (es) Compuestos heterociclicos de piridina sustituida con actividad antagonista de cxcr3.
IL185188A0 (en) Novel heterocyclic substituted pyridine or phenyl compounds with cxcr3 antagonist activity
TW200640902A (en) Amine-linked pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
TW200640901A (en) Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity
TW200640906A (en) Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity
ATE546445T1 (de) Substituierte heterocyclische verbindungen mit cxcr3-antagonistischer wirkung
AU2017272286B2 (en) Methods for improving diaphragm function
MX340965B (es) Combinaciones para el tratamiento de enfermedades que involucran la proliferacion celular.
AR023823A1 (es) Compuestos derivados de piperazina utiles como antagonistas ccr5, composiciones farmaceuticas que los comprenden, y el uso de los mismos para la preparacion de medicamentos.
BR112017011798A2 (pt) 4,6-substituído-pirazolo[1,5-a] pirazinas como inibidores janus cinase
DE60024604D1 (de) Xanthinderivate und analoge als zellsignalisierung inhibitoren
EA200501516A1 (ru) Производные 2,3,6-тризамещённого-4-пиримидона
BRPI0508461B8 (pt) diaminopirimidinas, seus usos, e composição farmacêutica
MX9706381A (es) Antagonista muscararinicos.
KR20050055022A (ko) Rho 키나아제 억제제를 함유하는 약제
BRPI0409921A (pt) derivados de éster e amida de ácido 2-cianopropanóico e métodos de seu uso
RU2008135131A (ru) Лечение туберозного склероза
AR063118A1 (es) Derivados de sulfonamida-piperidina composiciones farmaceuticas que los contienen y usos en enfermedades y trastornos inflamatorios alergicos y respiratorios
WO2007135026A2 (de) Substituierte pteridine als therapeutika
ATE422496T1 (de) Als medikamente für die behandlung von autoimmunerkrankungen geeignete substituierte pyridoä2,3-düpyrimidinderivate
CO2023004420A2 (es) Compuestos heterocíclicos como inhibidores del bromodominio cbp/ep300
NO331174B1 (no) Substituerte 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazinderivater og deres anvendelse som neurokininantagonister
TW200602339A (en) Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012.