BRPI0607946A2 - piperazina-piperidinas substituìdas por pirazinila com atividade de antagonista cxcr3 - Google Patents

piperazina-piperidinas substituìdas por pirazinila com atividade de antagonista cxcr3

Info

Publication number
BRPI0607946A2
BRPI0607946A2 BRPI0607946-6A BRPI0607946A BRPI0607946A2 BR PI0607946 A2 BRPI0607946 A2 BR PI0607946A2 BR PI0607946 A BRPI0607946 A BR PI0607946A BR PI0607946 A2 BRPI0607946 A2 BR PI0607946A2
Authority
BR
Brazil
Prior art keywords
compound
diseases
limiting examples
examples include
therapy
Prior art date
Application number
BRPI0607946-6A
Other languages
English (en)
Inventor
Stuart B Rosenblum
Wensheng Yu
Joseph A Kozlowski
Neng-Yang Shih
Bandarpalle B Shankar
Brian F Mcguinness
Guizhen Dong
Lisa Guise Zawacki
Douglas W Hobbs
John J Baldwin
Yuefei Shao
Seong Heon Kim
Qingbei Zeng
Michael K C Wong
Gopinadhan N Anilkumar
Yueheng Jiang
Original Assignee
Schering Corp
Pharmacopeia Inc
Seong Heon Kim
Qingbei Zeng
Michael K C Wong
Gopinadhan N Anilkumar
Yueheng Jiang
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, Seong Heon Kim, Qingbei Zeng, Michael K C Wong, Gopinadhan N Anilkumar, Yueheng Jiang filed Critical Schering Corp
Publication of BRPI0607946A2 publication Critical patent/BRPI0607946A2/pt

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
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    • A61P17/00—Drugs for dermatological disorders
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    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • 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
    • 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
    • C07D401/02—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
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

PIPERAZINA-PIPERIDINAS SUBSTITUìDAS POR PIRAZINILA COM ATIVIDADE DE ANTAGONISTA CXCR3. O presente pedido descreve um composto, ou enantiómeros, estereoisómeros, rotâmeros, tautómeros, racematos ou profármaco do referido composto, ou sais farmaceuticamente aceitáveis, solvatos ou ésteres do referido composto, ou do referido profármaco, o referido composto tendo a estrutura geral mostrada na Fórmula 1: e os sais farmaceuticamente aceitáveis, solvatos e ésteres deste. Também descrito é 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 (exemplos não limitantes incluem psoríase), doenças autoimunes (exemplos não limitantes incluem, artrite reumatóide, esclerose múltipla), rejeição a enxerto (exemplos não limitantes incluem, rejeição a aloenxerto, rejeição a xenoenxerto), doenças infecciosas (por exemplo, lepra tuberculóide), erupções de fármaco fixo, respostas de hipersensibilidade tipo retardo cutâneo, inflamação oftálmica, diabetes tipo I, meningite viral e tumores empregando-se um composto da Fórmula 1.
BRPI0607946-6A 2005-02-16 2006-02-14 piperazina-piperidinas substituìdas por pirazinila com atividade de antagonista cxcr3 BRPI0607946A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65333805P 2005-02-16 2005-02-16
PCT/US2006/005267 WO2006088921A2 (en) 2005-02-16 2006-02-14 Pyrazinyl substituted piperazine-piperidines with cxcr3 antagonist activity

Publications (1)

Publication Number Publication Date
BRPI0607946A2 true BRPI0607946A2 (pt) 2009-10-20

Family

ID=36636289

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0607946-6A BRPI0607946A2 (pt) 2005-02-16 2006-02-14 piperazina-piperidinas substituìdas por pirazinila com atividade de antagonista cxcr3

Country Status (17)

Country Link
US (1) US7868005B2 (pt)
EP (1) EP1856098B1 (pt)
JP (1) JP2008530220A (pt)
KR (1) KR20070107060A (pt)
CN (1) CN101142209A (pt)
AR (1) AR054224A1 (pt)
AU (1) AU2006214380A1 (pt)
BR (1) BRPI0607946A2 (pt)
CA (1) CA2598458A1 (pt)
IL (1) IL185073A0 (pt)
MX (1) MX2007009947A (pt)
NO (1) NO20074698L (pt)
PE (1) PE20061164A1 (pt)
RU (1) RU2007134260A (pt)
TW (1) TW200640903A (pt)
WO (1) WO2006088921A2 (pt)
ZA (1) ZA200706789B (pt)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2526586C (en) 2003-09-09 2010-03-16 Biogen International Gmbh The use of fumaric acid derivatives for treating cardiac insufficiency, and asthma
EA015517B1 (ru) 2004-04-13 2011-08-30 Инсайт Корпорейшн Производные пиперазинилпиперидина в качестве антагонистов хемокинового рецептора
WO2006071875A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
WO2006071958A1 (en) 2004-12-29 2006-07-06 Millennium Pharmaceuticals, Inc. Compounds useful as chemokine receptor antagonists
TW200714610A (en) * 2005-02-16 2007-04-16 Univ Maryland CXCR3 is a gliadin receptor
MX2007010068A (es) * 2005-02-16 2007-10-10 Schering Corp Piperazino-piperidinas con actividad antagonista de cxcr3.
MX2007009949A (es) * 2005-02-16 2007-09-26 Schering Corp Pirazinil-piperazin-piperidinas sustituidas con heteroarilo con actividad antagonista de cxcr3.
PE20061164A1 (es) 2005-02-16 2006-10-27 Schering Corp Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3
JP2008530218A (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、ピリジルおよびフェニルで置換されたピペラジン−ピペリジン
MX2007010067A (es) * 2005-02-16 2007-12-07 Schering Corp Compuestos heterociclicos novedosos sustituidos con piridina o fenilo con actividad antagonista de cxcr3.
JP4873352B2 (ja) * 2005-02-16 2012-02-08 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、複素環で置換されたピペラジン
CA2625762A1 (en) * 2005-10-11 2007-04-26 Schering Corporation Substituted heterocyclic compounds with cxcr3 antagonist activity
WO2007100610A2 (en) * 2006-02-23 2007-09-07 Merck & Co., Inc. Pyridine, pyrimidine and pyrazine derivatives as cxcr3 receptor modulators
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
MX2009000577A (es) * 2006-07-14 2009-03-09 Schering Corp Compuestos de piperazina sustituida heterociclica con actividad antagonista de cxcr3.
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.
EP2680010A1 (en) 2007-02-08 2014-01-01 Biogen Idec MA Inc. Nrf2 screening assays and related methods and compositions
CA2678577A1 (en) * 2007-02-26 2008-09-04 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11.beta.-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
JP5470557B2 (ja) * 2007-07-26 2014-04-16 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型の阻害剤の合成
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
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) * 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
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
US8598160B2 (en) * 2008-02-15 2013-12-03 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
PE20091576A1 (es) 2008-02-19 2009-11-05 Sanofi Aventis DERIVADOS DE 3-(AMIDO O SULFAMIDO)-4-(4-AZINIL SUSTITUIDO)BENZAMIDA COMO INHIBIDORES DEL RECEPTOR DE QUIMIOQUINAS CxCR3
WO2009117109A1 (en) * 2008-03-18 2009-09-24 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
RU2531272C2 (ru) 2008-05-01 2014-10-20 Вайтаи Фармасьютиклз, Инк. Циклические ингибиторы 11бета-гидроксистероид-дегидрогеназы 1
JP5696037B2 (ja) 2008-05-01 2015-04-08 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
US8242111B2 (en) * 2008-05-01 2012-08-14 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
NZ590495A (en) 2008-07-25 2012-10-26 Vitae Pharmaceuticals Inc Dihydropyridin-phenyl-3-oxazinan-2-ones as inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010010157A2 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
JP5679997B2 (ja) 2009-02-04 2015-03-04 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 １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状阻害剤
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
GEP20156309B (en) * 2009-04-30 2015-07-10 Vitae Pharmaceuticals Inc Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
US8927539B2 (en) 2009-06-11 2015-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
EP2448928B1 (en) 2009-07-01 2014-08-13 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
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
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
GB201017345D0 (en) 2010-10-14 2010-11-24 Proximagen Ltd Receptor antagonists
WO2012059416A1 (en) 2010-11-02 2012-05-10 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
US20140329809A1 (en) 2011-10-28 2014-11-06 Galderma Research & Development New leukocyte infiltrate markers for rosacea and uses thereof
US9073856B2 (en) * 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
AU2013216354B2 (en) 2012-02-02 2017-08-31 Idorsia Pharmaceuticals Ltd 4-(benzoimidazol-2-yl)-thiazole compounds and related aza derivatives
AU2014209141B2 (en) 2013-01-24 2018-05-10 Palvella Therapeutics, Inc. Compositions for transdermal delivery of mTOR inhibitors
JP6330040B2 (ja) 2013-07-22 2018-05-23 イドーシア ファーマシューティカルズ リミテッドＩｄｏｒｓｉａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ １−（ピペラジン−１−イル）−２−（［１，２，４］トリアゾール−１−イル）−エタノン誘導体
US9763992B2 (en) 2014-02-13 2017-09-19 Father Flanagan's Boys' Home Treatment of noise induced hearing loss
CN103772262B (zh) * 2014-02-24 2015-10-14 陕西理工学院 一种具有抗肿瘤活性的异邻苯二甲酰亚胺类化合物及其应用
AR099789A1 (es) 2014-03-24 2016-08-17 Actelion Pharmaceuticals Ltd Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina
AR103399A1 (es) 2015-01-15 2017-05-10 Actelion Pharmaceuticals Ltd Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3
PL3245203T3 (pl) 2015-01-15 2019-05-31 Idorsia Pharmaceuticals Ltd Pochodne hydroksyalkilopiperazyny jako modulatory receptora cxcr3
AU2016242118B2 (en) 2015-04-02 2021-07-08 Proximagen, Llc Novel therapies for cancer
EP3565520B1 (en) 2017-01-06 2026-02-25 Palvella Therapeutics, Inc. Anhydrous compositions of mtor inhibitors and methods of use
US11000513B2 (en) 2018-07-02 2021-05-11 Palvella Therapeutics, Inc. Anhydrous compositions of mTOR inhibitors and methods of use
CN117794527A (zh) * 2021-06-04 2024-03-29 学校法人京都药科大学 新型活化amp的蛋白激酶活化剂
CN117800969B (zh) * 2023-09-19 2024-11-29 武汉厚先生物医药有限公司 肿瘤坏死因子受体复合物抑制剂及其用途

Family Cites Families (23)

* 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
AU3351293A (en) * 1992-01-21 1993-08-03 Glaxo Group Limited Piperidineacetic acid derivatives as inhibitors of fibrinogen-dependent blood platelet aggregation
US6124319A (en) 1997-01-21 2000-09-26 Merck & Co., Inc. 3,3-disubstituted piperidines as modulators of chemokine receptor activity
AR013693A1 (es) 1997-10-23 2001-01-10 Uriach & Cia Sa J Nuevas piperidinas y piperazinas como inhibidores de la agregacion plaquetaria
SK287418B6 (sk) * 1999-05-04 2010-09-07 Schering Corporation Farmaceutický prípravok s obsahom CCR5 antagonistov a súprava s obsahom tohto prípravku
AR033517A1 (es) * 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
WO2001078708A1 (en) 2000-04-14 2001-10-25 Millennium Pharmaceuticals, Inc. Treating graft rejection with cxcr3 inhibitors
NZ526622A (en) 2000-12-11 2006-07-28 Amgen Sf Llc CXCR3 antagonists
US6469002B1 (en) 2001-04-19 2002-10-22 Millennium Pharmaceuticals, Inc. Imidazolidine compounds
GB0203994D0 (en) 2002-02-20 2002-04-03 Celltech R&D Ltd Chemical compounds
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
JP4873352B2 (ja) 2005-02-16 2012-02-08 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、複素環で置換されたピペラジン
EP1853583B1 (en) 2005-02-16 2011-09-07 Schering Corporation Amine-linked pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity
PE20061164A1 (es) 2005-02-16 2006-10-27 Schering Corp Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3
MX2007009949A (es) * 2005-02-16 2007-09-26 Schering Corp Pirazinil-piperazin-piperidinas sustituidas con heteroarilo con actividad antagonista de cxcr3.
MX2007010068A (es) 2005-02-16 2007-10-10 Schering Corp Piperazino-piperidinas con actividad antagonista de cxcr3.
MX2007010067A (es) 2005-02-16 2007-12-07 Schering Corp Compuestos heterociclicos novedosos sustituidos con piridina o fenilo con actividad antagonista de cxcr3.
JP2008530218A (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、ピリジルおよびフェニルで置換されたピペラジン−ピペリジン
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
MX2009000577A (es) 2006-07-14 2009-03-09 Schering Corp Compuestos de piperazina sustituida heterociclica con actividad antagonista de cxcr3.

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WO2006088921A2 (en) 2006-08-24
US7868005B2 (en) 2011-01-11
AR054224A1 (es) 2007-06-13
RU2007134260A (ru) 2009-03-27
PE20061164A1 (es) 2006-10-27
MX2007009947A (es) 2007-09-26
EP1856098A2 (en) 2007-11-21
US20070054919A1 (en) 2007-03-08
EP1856098B1 (en) 2012-08-01
IL185073A0 (en) 2007-12-03
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CA2598458A1 (en) 2006-08-24
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