[go: up one dir, main page]

NO20092587L - LXR og FXR modulatorer - Google Patents

LXR og FXR modulatorer

Info

Publication number
NO20092587L
NO20092587L NO20092587A NO20092587A NO20092587L NO 20092587 L NO20092587 L NO 20092587L NO 20092587 A NO20092587 A NO 20092587A NO 20092587 A NO20092587 A NO 20092587A NO 20092587 L NO20092587 L NO 20092587L
Authority
NO
Norway
Prior art keywords
lxr
compounds
fxr modulators
receptors
fxr
Prior art date
Application number
NO20092587A
Other languages
English (en)
Inventor
Raju Mohan
Wei Xu
Richard Martin
Tie-Lin Wang
Brett B Busch
Shao-Po Lu
Edwin Schweiger
Jr William C Stevens
Yinong Xie
Brant Clayton Boren
Xiao-Hui Gu
Vasu Jammalamadaka
Original Assignee
Exelixis 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 Exelixis Inc filed Critical Exelixis Inc
Publication of NO20092587L publication Critical patent/NO20092587L/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members

Landscapes

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

Abstract

Forbindelser ifølge oppfinnelsen er beskrevet, slik som forbindelser med formlene LX-LXIV, og farmasøytisk akseptable salter, isomerer eller prodrug derav, som er anvendelige som modulatorer av aktiviteten til lever X-reseptorer (LXR) og farnesoid X-reseptorer (FXR), hvor R00, R200, R400, R500, J11, J21, G1, G21 og Q er som definert heri. Farmasøytiske sammensetninger som inneholder forbindelsene og fremgangsmåter for anvendelse av forbindelsene er også beskrevet.
NO20092587A 2006-12-08 2009-07-07 LXR og FXR modulatorer NO20092587L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US86919806P 2006-12-08 2006-12-08
PCT/US2007/086787 WO2008073825A1 (en) 2006-12-08 2007-12-07 Lxr and fxr modulators

Publications (1)

Publication Number Publication Date
NO20092587L true NO20092587L (no) 2009-08-31

Family

ID=39315799

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20092587A NO20092587L (no) 2006-12-08 2009-07-07 LXR og FXR modulatorer

Country Status (8)

Country Link
US (1) US7998995B2 (no)
EP (1) EP2121621B1 (no)
JP (1) JP5399262B2 (no)
KR (1) KR20090094125A (no)
CN (1) CN101679297B (no)
AU (1) AU2007333194A1 (no)
NO (1) NO20092587L (no)
WO (1) WO2008073825A1 (no)

Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101871931A (zh) 2003-07-22 2010-10-27 艾尼纳制药公司 用于预防和治疗相关病症而作为5-ht2a血清素受体调节剂的二芳基和芳基杂芳基脲衍生物
DK2559690T3 (en) 2005-05-10 2016-04-25 Incyte Holdings Corp Modulators of indoleamine 2,3-dioxygenase and methods of use thereof
JP5237799B2 (ja) 2005-06-27 2013-07-17 エグゼリクシス パテント カンパニー エルエルシー ピラゾールベースのｌｘｒモジュレーター
ES2540561T3 (es) 2005-12-20 2015-07-10 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa
JP5319532B2 (ja) 2006-09-19 2013-10-16 インサイト・コーポレイション インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル
CL2007002650A1 (es) 2006-09-19 2008-02-08 Incyte Corp Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras.
TWI415845B (zh) * 2006-10-03 2013-11-21 Arena Pharm Inc 用於治療與５-ｈｔ2ａ血清素受體相關聯病症之作為５-ｈｔ2ａ血清素受體之調節劑的吡唑衍生物
EP2167464B1 (en) * 2007-05-25 2014-12-03 AbbVie Deutschland GmbH & Co KG Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mglu2 receptor)
CN104844578B (zh) * 2007-07-19 2018-06-19 H.隆德贝克有限公司 5元杂环酰胺及相关的化合物
JP5393677B2 (ja) 2007-08-15 2014-01-22 アリーナ ファーマシューティカルズ， インコーポレイテッド ５−ＨＴ２Ａセロトニン受容体に関連した障害の治療のための５−ＨＴ２Ａセロトニン受容体のモジュレーターとしてのイミダゾ［１，２−ａ］ピリジン誘導体
US20110021538A1 (en) 2008-04-02 2011-01-27 Arena Pharmaceuticals, Inc. Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor
SI2315756T1 (sl) 2008-07-08 2014-12-31 Incyte Corporation Experimental Station 1,2,5-oksadiazoli kot inhibitorji indolamin 2,3-dioksigenaze
RU2472791C2 (ru) * 2008-08-27 2013-01-20 КалсиМедика Инк. Соединения, модулирующие внутриклеточный кальций
UA107917C2 (ru) * 2008-10-21 2015-03-10 Сімабей Терапьютікс, Інк. Арильный агонист рецептора gpr120 и его применение
US9126946B2 (en) 2008-10-28 2015-09-08 Arena Pharmaceuticals, Inc. Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto
SMT201800199T1 (it) 2008-10-28 2018-05-02 Arena Pharm Inc Composizioni di un modulatore dei recettori della serotonina 5-ht2a utili per il trattamento di disturbi correlati a esso
KR101701367B1 (ko) * 2008-11-04 2017-02-02 케모센트릭스, 인크. Ｃｘｃｒ７의 모듈레이터
US8853202B2 (en) 2008-11-04 2014-10-07 Chemocentryx, Inc. Modulators of CXCR7
AR074760A1 (es) 2008-12-18 2011-02-09 Metabolex Inc Agonistas del receptor gpr120 y usos de los mismos en medicamentos para el tratamiento de diabetes y el sindrome metabolico.
WO2010117090A1 (en) * 2009-04-10 2010-10-14 Banyu Pharmaceutical Co.,Ltd. Novel isoquinolinyloxymethyl heteroaryl derivatives
CA2761934C (en) * 2009-05-28 2018-01-09 Exelixis Patent Company Llc Substituted 1-(biphenyl-4-yl)-2-benzyl-4-hydroxyalkyl-1h-imidazole compounds and their use as lxr modulators
GB0910003D0 (en) * 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
DE102009043260A1 (de) * 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
JP5758395B2 (ja) 2009-10-15 2015-08-05 ザ チルドレンズ メディカル センター コーポレイション 疼痛を治療するためのセピアプテリンレダクターゼ阻害薬
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8252826B2 (en) * 2010-03-24 2012-08-28 Hoffmann-La Roche Inc. Cyclopentyl- and cycloheptylpyrazoles
US8299117B2 (en) 2010-06-16 2012-10-30 Metabolex Inc. GPR120 receptor agonists and uses thereof
WO2011157827A1 (de) 2010-06-18 2011-12-22 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
JP2013542183A (ja) 2010-09-07 2013-11-21 エスエヌユー アールアンドディービー ファウンデーション セスタテルペン化合物およびこれらの物質の用途
KR20130121857A (ko) 2010-12-01 2013-11-06 닛산 가가쿠 고교 가부시키 가이샤 다발성 골수종의 치료 효과를 갖는 피라졸 화합물
TW201242953A (en) * 2011-03-25 2012-11-01 Bristol Myers Squibb Co Imidazole prodrug LXR modulators
WO2012177893A2 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
CA2839703A1 (en) 2011-06-24 2012-12-27 Amgen Inc. Trpm8 antagonists and their use in treatments
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
US9289365B2 (en) * 2011-10-24 2016-03-22 Avon Products, Inc. Compositions and methods for stimulating collagen synthesis in the skin
CN103087041B (zh) * 2011-11-02 2014-06-18 中国中化股份有限公司 含二芳醚的吡唑酰胺类化合物作为农用杀菌剂的用途
CN103906736A (zh) * 2011-11-09 2014-07-02 格吕伦塔尔有限公司 作为类香草素受体配体的具有被含n-基团取代的苯基基团的被取代的基于吡唑基的羧酰胺和脲衍生物
AU2012334065B2 (en) * 2011-11-09 2017-06-08 Medifron Dbt Inc. Substituted pyrazolyl-based carboxamide and urea derivatives bearing a phenyl moiety substituted with an O-containing group as vanilloid receptor ligands
KR102112879B1 (ko) 2012-03-02 2020-05-19 랄렉사르 테라퓨틱스 인코퍼레이티드 피부 질환들, 장애들 및 병태들의 치료를 위한 간 x 수용체(lxr) 조정제들
WO2013168967A1 (ko) 2012-05-07 2013-11-14 주식회사경농 카바메이트로 치환된 다이아미노아릴 유도체 및 이를 함유하는 살충제 조성물
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
AU2013302861A1 (en) 2012-08-13 2015-03-05 The Rockefeller University Treatment and diagnosis of melanoma
BR112015012366A8 (pt) 2012-11-29 2019-10-01 Chemocentryx Inc antagonistas de cxcr7, uso dos mesmos, composição farmacêutica, bem como métodos para detectar níveis elevados de cxcr7 em uma amostra e para imagear um tumor, órgão, ou tecido
EP2928471B1 (en) 2012-12-06 2020-10-14 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
ES2753386T3 (es) 2013-03-13 2020-04-08 Forma Therapeutics Inc Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer
WO2014144037A1 (en) 2013-03-15 2014-09-18 Bristol-Myers Squibb Company Lxr modulators
JP6456909B2 (ja) * 2013-03-15 2019-01-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｌｘｒ調節因子
GB2513403A (en) * 2013-04-26 2014-10-29 Agency Science Tech & Res WNT pathway modulators
JP2016532713A (ja) * 2013-09-04 2016-10-20 アレクサー セラピューティクス， インク． 肝臓ｘ受容体（ｌｘｒ）調節因子
EP3626712A3 (en) 2013-09-04 2020-04-15 Ellora Therapeutics, Inc. Liver x receptor (lxr) modulators
WO2015036442A1 (en) 2013-09-11 2015-03-19 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
WO2015070007A1 (en) 2013-11-08 2015-05-14 Incyte Corporation Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor
US10669296B2 (en) 2014-01-10 2020-06-02 Rgenix, Inc. LXR agonists and uses thereof
KR20160115933A (ko) 2014-01-10 2016-10-06 오리진 디스커버리 테크놀로지스 리미티드 Irak4 억제제로서의 인다졸 화합물
LT3805233T (lt) 2014-01-13 2024-05-10 Aurigene Oncology Limited N-(5-(3-hidroksipirolidin-1-il)-2-morfolinooksazolo[4,5-b]piridin-6-il)-2-(2- metilpiridin-4-il)oksazol-karboksamido (r) ir (s) enantiomerai, kaip irak4 inhibitoriai, skirti vėžio gydymui
KR102510427B1 (ko) * 2014-03-07 2023-03-14 바이오크리스트파마슈티컬즈,인코포레이티드 인간 혈장 칼리크레인 저해제
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
CN104045635A (zh) * 2014-06-23 2014-09-17 华东理工大学 3,4,5-三取代异恶唑类化合物及其用途
CN107207474B (zh) * 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
EP3034499A1 (en) * 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
WO2016127019A2 (en) 2015-02-06 2016-08-11 Intercept Pharmaceuticals, Inc. Pharmaceutical compositions for combination therapy
TWI698430B (zh) * 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 三環化合物及其在藥物中的應用
WO2016149111A1 (en) * 2015-03-13 2016-09-22 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid x receptor agonists to activate intestinal receptors
EP3715348A1 (en) 2015-03-26 2020-09-30 Akarna Therapeutics, Ltd. Fused bicyclic compounds for the treatment of disease
JP6879931B2 (ja) 2015-04-07 2021-06-02 インターセプト ファーマシューティカルズ， インコーポレイテッド 併用療法用の医薬組成物
MX388281B (es) 2015-06-12 2025-03-11 Axovant Sciences Gmbh Derivados de diaril y arilheteroaril urea como moduladores del receptor 5ht2a de serotonina útiles para la profilaxis y el tratamiento de un trastorno conductual del sueño rem.
TW201720439A (zh) 2015-07-15 2017-06-16 Axovant Sciences Gmbh 用於預防及治療與神經退化性疾病相關的幻覺之作為５－ｈｔ２ａ血清素受體的二芳基及芳基雜芳基脲衍生物
EP3402477A4 (en) 2016-01-11 2019-08-21 The Rockefeller University METHOD FOR THE TREATMENT OF DISEASES RELATED TO MYELOID-DERIVED SUPPRESSOR CELLS
EP3463372A4 (en) * 2016-05-25 2019-11-13 Akarna Therapeutics, Ltd. FUSIONED BICYCLIC COMPOUNDS FOR THE TREATMENT OF DISEASE
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
SG11201810600WA (en) 2016-06-13 2018-12-28 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
TW201808283A (zh) * 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 含氮三環化合物及其在藥物中的應用
CN108059607B (zh) * 2016-11-09 2020-11-17 中国科学院上海药物研究所 亚砜基乙酸或砜基乙酸类衍生物、其药物组合物、制备方法和用途
JP6906626B2 (ja) 2017-03-28 2021-07-21 ギリアード サイエンシーズ， インコーポレイテッド 肝疾患を処置するための治療的組み合わせ
WO2018178260A1 (en) 2017-03-30 2018-10-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses
IL305150B2 (en) 2017-03-31 2025-03-01 Aurigene Oncology Ltd Compounds and preparations for the treatment of hematological disorders
KR20240130818A (ko) 2017-10-31 2024-08-29 쿠리스 인코퍼레이션 혈액학적 장애를 치료하기 위한 화합물 및 조성물
BR112020008157A2 (pt) * 2017-11-01 2020-10-06 Bristol-Myers Squibb Company compostos espirocíclicos como moduladores do receptor farnesoide x
US11214536B2 (en) 2017-11-21 2022-01-04 Inspirna, Inc. Polymorphs and uses thereof
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
SG11202105175WA (en) * 2018-11-20 2021-06-29 Regeneron Pharma Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as lxr agonists
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
AU2019398198A1 (en) 2018-12-12 2021-07-08 Chemocentryx, Inc. CXCR7 inhibitors for the treatment of cancer
HUE065889T2 (hu) 2019-01-15 2024-06-28 Gilead Sciences Inc Izoxazol vegyület mint FXR agonista és az azt tartalmazó gyógyszerészeti készítmények
KR20240160667A (ko) 2019-02-19 2024-11-11 길리애드 사이언시즈, 인코포레이티드 Fxr 효능제의 고체 형태
CN114144185A (zh) 2019-05-30 2022-03-04 英特塞普特医药品公司 用于治疗胆汁淤积性肝病的包含fxr激动剂和贝特类的药物组合物
AU2020312735A1 (en) 2019-07-18 2021-12-16 Enyo Pharma Method for decreasing adverse-effects of interferon
CN110713460A (zh) * 2019-11-08 2020-01-21 南通大学 一种含吡唑苯基单元的吡唑酰胺衍生物的制备方法及其应用
PL4073025T3 (pl) 2019-12-13 2024-09-16 Inspirna, Inc. Sole metali i ich zastosowania
MX2022007686A (es) 2019-12-19 2022-07-19 Bayer Ag Acidos 1,5-difenilpirazolil-3-oxialquilicos y acidos 1-fenil-5-tienilpirazolil-3-oxialquilicos y su uso para el combate del crecimiento de plantas no deseado.
WO2021144330A1 (en) 2020-01-15 2021-07-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
WO2021219527A1 (de) 2020-04-29 2021-11-04 Bayer Aktiengesellschaft 1-pyrazinylpyrazolyl-3-oxyalkylsäuren sowie deren derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums
AU2021373985A1 (en) 2020-11-05 2023-06-08 Bayer Aktiengesellschaft [(1-phenyl-5-heteroaryl-1h-pyrazol-3-yl)oxy] acetic acid derivatives as safeners for the protection of useful plants and crop plants
CA3200696A1 (en) 2020-11-05 2022-05-12 Bayer Aktiengesellschaft Use of [(1,5-diphenyl-1h-pyrazol-3-yl)oxy] acetic acid derivatives and their salts and compositions containing them, for reducing phytotoxic effects of agrochemicals, in particular of herbicides, in useful plants and crop plants
CA3204800A1 (en) 2021-01-14 2022-07-21 Raphael Darteil Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CN117120054A (zh) 2021-04-08 2023-11-24 柯里斯公司 治疗癌症的组合疗法
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
CA2276946A1 (en) 1993-11-30 1995-06-08 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides and pharmaceutical compositions containing the same
US6492411B1 (en) 1993-11-30 2002-12-10 G. D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for the treatment of inflammation
ES2179254T3 (es) 1996-11-04 2003-01-16 Bayer Cropscience Sa 1-poliarilpirazoles plaguicidas.
AU5928898A (en) 1997-01-24 1998-08-18 Regents Of The University Of California, The Use of fxr, pparalpha and lxralpha activators to restore barrier function, promote epidermal differentiation and inhibit proliferation
US20020035156A1 (en) 1997-04-18 2002-03-21 Barbara Roniker Combination therapy in the prevention of cardiovascular disorders
US6294558B1 (en) 1999-05-31 2001-09-25 Pfizer Inc. Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
JP4221129B2 (ja) 1999-02-15 2009-02-12 富士フイルム株式会社 含窒素ヘテロ環化合物、有機発光素子材料、有機発光素子
US6071955A (en) 1999-02-25 2000-06-06 The Regents Of The University Of California FXR, PPARA and LXRA activators to treat acne/acneiform conditions
PT1177187E (pt) 1999-04-28 2007-09-03 Sanofi Aventis Deutschland Derivados ácidos de di-arilo como ligados do receptor ppar.
SI1285908T1 (sl) 2000-05-29 2008-12-31 Kyorin Seiyaku Kk Substituirani fenilpropionski kislinski derivati
RU2341513C2 (ru) 2001-06-12 2008-12-20 Веллстат Терапьютикс Корпорейшн Соединения для лечения метаболических заболеваний
US7482366B2 (en) * 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
US20040248956A1 (en) 2002-01-29 2004-12-09 Hagmann William K Substituted imidazoles as cannabinoid receptor modulators
JP2005528384A (ja) 2002-04-08 2005-09-22 ザ オハイオ ステート ユニバーシティー リサーチ ファウンデーション 増殖性細胞においてアポトーシスを誘導するための化合物および方法
WO2003090732A1 (en) * 2002-04-23 2003-11-06 Chugai Seiyaku Kabushiki Kaisha Lxr modulators for the treatment of cardiovascular diseases
WO2004011446A1 (en) 2002-07-26 2004-02-05 Bayer Pharmaceuticals Corporation Indane, dihydrobenzofuran, and tetrahydronaphthalene carboxylic acid derivatives and their use as antidiabetics
US7109227B2 (en) 2002-08-26 2006-09-19 National Health Research Institutes Imidazolamino compounds
EP1398029A1 (en) 2002-09-10 2004-03-17 LION Bioscience AG NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives
JP4631259B2 (ja) 2002-10-03 2011-02-16 コニカミノルタホールディングス株式会社 有機エレクトロルミネッセンス素子及び表示装置
WO2004033432A1 (ja) 2002-10-09 2004-04-22 Ssp Co., Ltd. 抗真菌活性を有する新規ピラゾール化合物
JP2006510687A (ja) 2002-12-20 2006-03-30 ノボ　ノルディスク　アクティーゼルスカブ 新規化合物、その調製および使用
EP1572693A1 (en) 2002-12-20 2005-09-14 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
WO2004063165A1 (en) 2003-01-06 2004-07-29 Eli Lilly And Company A pyrazole derivative as ppar modulator
WO2004069158A2 (en) 2003-01-27 2004-08-19 Merck & Co., Inc. Substituted pyrazoles, compositions containing such compounds and methods of use
CN1747936A (zh) 2003-02-12 2006-03-15 特兰斯泰克制药公司 作为治疗试剂的取代吡咯衍生物
EP1601657A1 (en) 2003-03-12 2005-12-07 Vertex Pharmaceuticals Incorporated Pyrazole modulators of atp-binding cassette transporters
AU2004228057A1 (en) 2003-04-03 2004-10-21 Merck & Co., Inc. Di-aryl substituted pyrazole modulators of metabotropic glutamate receptor-5
DE10315571A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
DE10315569A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
DE10315573A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
WO2004106307A2 (fr) 2003-05-27 2004-12-09 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Nouveaux derives d’imidazoles, leur preparation et leur utilisation en tant que medicament
WO2005012263A1 (en) 2003-07-24 2005-02-10 Pharmagene Laboratories Limited 5-ht2b receptor antagonists
JP2006528661A (ja) 2003-07-25 2006-12-21 ファイザー・インク アミノピラゾール化合物およびｃｈｋ１阻害剤としての使用
JP4745971B2 (ja) 2003-10-03 2011-08-10 ザ オハイオ ステート ユニバーシティー リサーチ ファウンデーション ＰＤＫ−１／Ａｋｔシグナル伝達インヒビター
WO2005037199A2 (en) * 2003-10-10 2005-04-28 Bristol-Myers Squibb Company Pyrazole derivatives as cannabinoid receptor modulators
WO2005037763A1 (en) 2003-10-14 2005-04-28 Eli Lilly And Company Phenoxyether derivatives as ppar modulators
WO2005037271A2 (en) 2003-10-17 2005-04-28 Tanabe Seiyaku Co., Ltd. Large conductance calcium-activated k channel opener
CA2545942C (en) 2003-11-14 2012-07-10 Lorus Therapeutics Inc. Aryl imidazoles and their use as anti-cancer agents
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
CA2547212A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company Peroxisome proliferator activated receptor modulators
US20050148601A1 (en) 2003-12-19 2005-07-07 Maynard George D. Neurokinin-3 receptor modulators: diaryl imidazole derivatives
EP1799673A1 (en) 2004-10-15 2007-06-27 Memory Pharmaceuticals Corporation Pyrazole derivatives as phosphodiesterase 4 inhibitors
AU2005297984B2 (en) * 2004-10-27 2009-11-12 Daiichi Sankyo Company, Limited Benzene compound having 2 or more substituents
CA2593156C (en) 2005-01-10 2015-05-05 Exelixis, Inc. Heterocyclic carboxamide compounds as steroid nuclear receptors ligands
AU2006250354A1 (en) 2005-05-23 2006-11-30 Japan Tobacco Inc. Pyrazole compound and therapeutic agent for diabetes comprising the same
JP5237799B2 (ja) 2005-06-27 2013-07-17 エグゼリクシス パテント カンパニー エルエルシー ピラゾールベースのｌｘｒモジュレーター
US20080090834A1 (en) * 2006-07-06 2008-04-17 Pfizer Inc Selective azole pde10a inhibitor compounds

Also Published As

Publication number Publication date
AU2007333194A1 (en) 2008-06-19
US7998995B2 (en) 2011-08-16
US20100069367A1 (en) 2010-03-18
JP2010512342A (ja) 2010-04-22
WO2008073825A1 (en) 2008-06-19
EP2121621A1 (en) 2009-11-25
JP5399262B2 (ja) 2014-01-29
CN101679297B (zh) 2012-01-11
EP2121621B1 (en) 2014-05-07
KR20090094125A (ko) 2009-09-03
CN101679297A (zh) 2010-03-24

Similar Documents

Publication Publication Date Title
NO20092587L (no) LXR og FXR modulatorer
NO20084382L (no) Sykloalkylaminosyrederivater og farmasoytiske sammensetninger derav
NO20080391L (no) Pyrazolbaserte LXR modulatorer
NO20080865L (no) Spirokromanonderivater som acetyl-koenzym-A-karboksylase(ACC)inhibitorer
EA200900135A1 (ru) Производные пиразола в качестве ингибиторов цитохрома р450
NO20081554L (no) Isoindollmidforbindelser og sammensetninger omfattende samme, og anvendelse derav
WO2010138598A3 (en) Lxr modulators
UY32156A (es) Derivados sustituidos de la n2 - [1-(5 - fluoropirimidin -2-il) etil] - n4 - (1-metil - 1h-imidazol - 4 - il)) - pirimidina - 2,4 - diaminas y sus sales farmacéuticamente aceptables, proceso de preparación, composiciones conteniéndolos y aplicaciones.
NO20083434L (no) Benzamid- og heteroarenderivater
EA201000805A1 (ru) Бис-(сульфониламино)производные в терапии 066
ECSP10010272A (es) Derivados bis-(sulfonilamino) para uso en terapia
DK3133070T3 (da) Eliglustat (genz 112638) som inhibitor af glucosylceramidsyntase til anvendelse i en fremgangsmåde til behandling af fabrys eller gauchers sygdom, hvilken fremgangsmåde omfatter justering af den individuelle terapeutiske dosis i forhold til patientens p-450-metabolisme
AR056873A1 (es) Derivados de pirazolopirimidinas como inhibidores de quinasa dependientes de ciclina, composiciones farmaceuticas
NO20090835L (no) Nye HIV-reverstranskriptaseinhibitorer
NO20082124L (no) Bifenyloksyeddiksyrederivater for behandling av respiratorisk sykdom
UY33075A (es) Derivados de ciclohexano y usos de los mismos
MX2009008540A (es) Inhibidores de virus de hepatitis c macrociclicos sustituidos con pirimidina.
ECSP078053A (es) Nuevos derivados de 2-azetidinona útiles en el tratamiento de condiciones de hiperlipidemia
ECSP088854A (es) Moduladores bencimidazolicos de vr1
UY29607A1 (es) Compuestos quimicos
SE0400284D0 (sv) Novel compounds
NI200900052A (es) Heterocíclicos derivados de los inhibidores de metaloproteasa
CR9268A (es) Nuevo derivado de diazabiciclononeno
CO6361855A2 (es) Derivados de 7-hidroxi-benzoimidazol-4-il-,etanona e inhibidores de cinasa que enlaza pdz que contienen los mismos
CR9391A (es) Derivados de indanil-piperazinas, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen

Legal Events

Date Code Title Description
FC2A Withdrawal, rejection or dismissal of laid open patent application