JP5792799B2 - 核内受容体結合薬 - Google Patents

核内受容体結合薬 Download PDF

Info

Publication number
JP5792799B2
JP5792799B2 JP2013509219A JP2013509219A JP5792799B2 JP 5792799 B2 JP5792799 B2 JP 5792799B2 JP 2013509219 A JP2013509219 A JP 2013509219A JP 2013509219 A JP2013509219 A JP 2013509219A JP 5792799 B2 JP5792799 B2 JP 5792799B2
Authority
JP
Japan
Prior art keywords
compound
another embodiment
estrogen receptor
hydrogen
alk
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2013509219A
Other languages
English (en)
Japanese (ja)
Other versions
JP2013525494A (ja
JP2013525494A5 (enExample
Inventor
ナラヤナン、ラメシュ
イェプル、ムラリモハン
ダルトン、ジェームズ・ティー
Original Assignee
ジーティーエックス・インコーポレイテッド
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 ジーティーエックス・インコーポレイテッド filed Critical ジーティーエックス・インコーポレイテッド
Publication of JP2013525494A publication Critical patent/JP2013525494A/ja
Publication of JP2013525494A5 publication Critical patent/JP2013525494A5/ja
Application granted granted Critical
Publication of JP5792799B2 publication Critical patent/JP5792799B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2013509219A 2010-05-04 2011-05-04 核内受容体結合薬 Expired - Fee Related JP5792799B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/773,515 2010-05-04
US12/773,515 US9623021B2 (en) 2007-01-22 2010-05-04 Nuclear receptor binding agents
PCT/US2011/035206 WO2011140228A1 (en) 2010-05-04 2011-05-04 Nuclear receptor binding agents

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015155050A Division JP2016006095A (ja) 2010-05-04 2015-08-05 核内受容体結合薬

Publications (3)

Publication Number Publication Date
JP2013525494A JP2013525494A (ja) 2013-06-20
JP2013525494A5 JP2013525494A5 (enExample) 2014-06-26
JP5792799B2 true JP5792799B2 (ja) 2015-10-14

Family

ID=44904060

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2013509219A Expired - Fee Related JP5792799B2 (ja) 2010-05-04 2011-05-04 核内受容体結合薬
JP2015155050A Pending JP2016006095A (ja) 2010-05-04 2015-08-05 核内受容体結合薬

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2015155050A Pending JP2016006095A (ja) 2010-05-04 2015-08-05 核内受容体結合薬

Country Status (11)

Country Link
US (1) US9623021B2 (enExample)
EP (1) EP2566330A4 (enExample)
JP (2) JP5792799B2 (enExample)
KR (1) KR20130061151A (enExample)
CN (2) CN106420745A (enExample)
AU (1) AU2011248154B2 (enExample)
CA (1) CA2798259A1 (enExample)
IL (1) IL222823A0 (enExample)
MX (1) MX2012012777A (enExample)
RU (1) RU2604666C2 (enExample)
WO (1) WO2011140228A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016006095A (ja) * 2010-05-04 2016-01-14 ジーティーエックス・インコーポレイテッド 核内受容体結合薬

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9604931B2 (en) 2007-01-22 2017-03-28 Gtx, Inc. Nuclear receptor binding agents
EA026578B1 (ru) * 2007-01-22 2017-04-28 ДЖиТиЭкс, ИНК. Вещества, связывающие ядерные рецепторы
US8304413B2 (en) 2008-06-03 2012-11-06 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
US20140297314A1 (en) 2011-07-13 2014-10-02 Gino Tutera Systems and methods for calculating patient dosage
US9744149B2 (en) 2012-07-13 2017-08-29 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US9622992B2 (en) 2012-07-13 2017-04-18 Gtx, Inc. Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs)
US10314807B2 (en) 2012-07-13 2019-06-11 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
US10987334B2 (en) 2012-07-13 2021-04-27 University Of Tennessee Research Foundation Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs)
JP6226978B2 (ja) 2012-07-13 2017-11-08 ジーティーエックス・インコーポレイテッド 選択的アンドロゲン受容体モジュレーター（ｓａｒｍ）によりアンドロゲン受容体（ａｒ）陽性乳癌を処置する方法
US9969683B2 (en) 2012-07-13 2018-05-15 Gtx, Inc. Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS)
US10258596B2 (en) 2012-07-13 2019-04-16 Gtx, Inc. Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS)
JP6401702B2 (ja) 2012-09-07 2018-10-10 ザ・ガバナーズ・オブ・ザ・ユニバーシティー オブ・アルバータ 炎症性肝疾患の診断のための方法および組成物
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
EP3010587A4 (en) * 2013-06-18 2017-04-12 Salk Institute for Biological Studies Methods of treating muscular dystrophy
PL229743B1 (pl) * 2013-07-30 2018-08-31 Narodowy Instytut Zdrowia Publicznego Panstwowy Zakl Higieny Nowe pochodne kwasu 3,4-dihydroizochinolino-3- karboks ylowego o właściwościach przeciwnowotworowych, sposób ich syntezy, kompozycje farmaceutyczne zawierające te pochodne oraz ich zastosowanie
PT3043865T (pt) * 2013-09-11 2021-01-14 Univ Claude Bernard Lyon Métodos e composições farmacêuticas para o tratamento da infeção por vírus da hepatite b
RU2692485C2 (ru) 2014-04-02 2019-06-25 Интермьюн, Инк. Противофиброзные пиридиноны
LT3126330T (lt) 2014-04-04 2019-04-25 Pfizer Inc. Bicikliniai kondensuoti heteroarilo arba arilo junginiai, ir jų panaudojimas kaip irak4 inhibitorių
CN104776687B (zh) * 2014-09-05 2017-09-29 山东诚创医药技术开发有限公司 盐酸考来维仑聚合物的干燥方法
PT3206692T (pt) 2014-10-15 2024-04-30 Corcept Therapeutics Inc Tratamento da doença hepática gordurosa utilizando antagonistas dos recetores de glicocorticoides e mineralocorticoides
KR101647348B1 (ko) * 2014-12-30 2016-08-22 충남대학교산학협력단 Shp를 유효성분으로 하는 통풍 예방 및 치료용 조성물
WO2017003723A1 (en) 2015-07-01 2017-01-05 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
KR101800876B1 (ko) 2015-10-28 2017-11-27 전남대학교 산학협력단 신규한 디아릴이소퀴놀론 또는 디아릴이소퀴놀린 화합물 및 이를 포함하는 약제학적 조성물
AU2017312499B2 (en) 2016-08-19 2023-02-02 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Selective estrogen-receptor modulators (SERMs) confer protection against photoreceptor degeneration
US11529391B2 (en) * 2017-01-09 2022-12-20 The Board Of Trustees Of The Leland Stanford Junior University Reversing deficient hedgehog signaling restores deficient skeletal regeneration
WO2019023278A1 (en) 2017-07-25 2019-01-31 Crinetics Pharmaceuticals, Inc. MODULATORS OF SOMATOSTATIN AND USES THEREOF
AU2018379255B2 (en) 2017-12-04 2024-10-17 Alexion Pharma International Operations Unlimited Company Bis-choline tetrathiomolybdate for treating Wilson Disease
US11419832B2 (en) 2017-12-04 2022-08-23 Alexion Pharmaceuticals, Inc. Bis-choline tetrathiomolybdate for treating Wilson Disease

Family Cites Families (147)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2848356A (en) * 1954-08-30 1958-08-19 Phillips Petroleum Co Fungicides, their preparation and use
CA1285951C (en) * 1985-10-28 1991-07-09 Raj N. Misra Naphthalenyl- and quinolinyl-amino substituted phenols
US4921941A (en) 1987-07-01 1990-05-01 Schering Corporation Orally active antiandrogens
KR890011876A (ko) 1988-01-27 1989-08-23 메이 앤드 베이커 리미팃드 신규한 이소퀴놀린 유도체 그의 제조방법 및 그를 함유하는 제약학적 조성물
US5177075A (en) * 1988-08-19 1993-01-05 Warner-Lambert Company Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
US4942163A (en) * 1989-03-07 1990-07-17 E. I. Du Pont De Nemours And Company 1(2H)-isoquinolinones and 1-isoquinolineamines as cancer chemotherapeutic agents
US5112869A (en) * 1989-04-04 1992-05-12 Sloan-Kettering Institute For Cancer Research Substituted 1-phenylnaphthalenes
KR920008026A (ko) 1990-10-24 1992-05-27 오노 화아마슈티칼 캄파니 리미팃드 이소퀴놀리논 유도체 또는 이의 무독성 산부가염 또는 이의 수화물, 이의 제조방법 및 이를 포함하는 약제 조성물
EP0502575A1 (en) 1991-03-06 1992-09-09 Merck & Co. Inc. Substituted 1-(2H)-isoquinolinones
ATE198328T1 (de) * 1992-09-28 2001-01-15 Hoechst Ag Antiarrhythmische und cardioprotektive substituierte 1(2h)-isochinoline, verfahren zu deren herstellung, diese enthaltende arzneimittel und ihre anwendung für die herstellung eines arzneimittels zur behandlung von herzinsuffizienzen
DE4345266C2 (de) 1993-10-04 1996-12-19 Luitpold Pharma Gmbh Heterocyclische Carbamate, Verfahren zu ihrer Herstellung und Arzneimittel
US5612359A (en) * 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
US5719144A (en) * 1995-02-22 1998-02-17 Merck & Co., Inc. Fibrinogen receptor antagonists
IT1307327B1 (it) * 1995-09-12 2001-10-30 Smithkline Beecham Spa Derivati idroisochinolinici sostituiti
AU1730497A (en) 1996-02-17 1997-09-02 Agrevo Uk Limited Fungicidal 1,2,4-oxadiazoles and analogues
SE9600769D0 (sv) 1996-02-28 1996-02-28 Astra Ab Compounds useful as analgesic
JP3065949B2 (ja) 1996-09-13 2000-07-17 日本アンテナ株式会社 多周波用アンテナ
BR9714189A (pt) 1996-12-27 2000-02-29 Hoechst Marion Roussel Inc N-(piridinilamino) isoindolinas e compostos relacionados
TW536540B (en) * 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
WO1998038168A1 (en) 1997-02-27 1998-09-03 Tanabe Seiyaku Co., Ltd. Isoquinolinone derivatives, process for preparing the same, and their use as phosphodiesterase inhibitors
JPH10259176A (ja) 1997-03-17 1998-09-29 Japan Tobacco Inc 血管新生阻害作用を有する新規アミド誘導体及びその用途
CN1198614C (zh) 1997-05-13 2005-04-27 奥科特默股份有限公司 pADPRT抑制剂在用于制备治疗炎症和炎性疾病的药物中的方法
KR20010083092A (ko) 1998-07-06 2001-08-31 스티븐 비. 데이비스 이중 안지오텐신 엔도텔린 수용체 길항제로서의 비페닐술폰아미드
JP2000072675A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd 医薬組成物
AU1199600A (en) 1998-10-02 2000-04-26 Board Of Trustees Of The University Of Illinois, The Estrogen receptor ligands
US6486155B1 (en) * 1998-11-24 2002-11-26 Cell Pathways Inc Method of inhibiting neoplastic cells with isoquinoline derivatives
US6593322B1 (en) * 1999-03-17 2003-07-15 Signal Pharmaceuticals, Inc. Compounds and methods for modulation of estrogen receptors
US6436923B1 (en) * 1999-03-17 2002-08-20 Signal Pharmaceuticals, Inc. Compounds and methods for modulation of estrogen receptors
JP2003506355A (ja) 1999-08-03 2003-02-18 アボット・ラボラトリーズ カリウムチャンネル開放剤
WO2001022960A1 (en) 1999-09-30 2001-04-05 Charlotte-Mecklenburg Hospital Authority Doing Business As Carolinas Medical Center Treatment of carbon monoxide poisoning
CO5271709A1 (es) * 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos
US6906063B2 (en) * 2000-02-04 2005-06-14 Portola Pharmaceuticals, Inc. Platelet ADP receptor inhibitors
JP4331913B2 (ja) * 2000-02-14 2009-09-16 メルク エンド カムパニー インコーポレーテッド エストロゲンレセプターモデュレーター
PE20011077A1 (es) * 2000-03-01 2001-12-12 Akzo Nobel Nv Derivados de cromano que tiene afinidad por receptores de estrogenos
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
JP2004506712A (ja) * 2000-08-23 2004-03-04 アクゾ・ノベル・エヌ・ベー 医療に使用するための１０−アリール−１１Ｈ−ベンゾ［ｂ］フルオレン誘導体および類似体
EP1322619B1 (en) * 2000-09-20 2008-01-23 Merck & Co., Inc. Isoquinolinone potassium channel inhibitors
CA2321406A1 (en) 2000-09-29 2002-03-29 The Regents Of The University Of California Restoration of perturbed barrier function by application of antiandrogens
JP2004511501A (ja) 2000-10-19 2004-04-15 メルク　エンド　カムパニー　インコーポレーテッド エストロゲン受容体モジュレーター
CA2428019C (en) 2000-11-27 2010-09-21 Merck & Co., Inc. Estrogen receptor modulators
EP1341768A1 (en) 2000-12-07 2003-09-10 AstraZeneca AB Therapeutic benzimidazole compounds
EP1341765A1 (en) * 2000-12-07 2003-09-10 AstraZeneca AB Therapeutic compounds
US7045539B2 (en) 2000-12-22 2006-05-16 Astrazeneca Ab Therapeutic benzoxazole compounds
WO2002058639A2 (en) 2001-01-23 2002-08-01 Merck & Co., Inc. Pyranoflavonoid compounds and their use as estrogen receptor modulators
WO2002072561A1 (en) * 2001-01-26 2002-09-19 Smithkline Beecham Corporation Piperazinyltriazines as estrogen receptor modulators
HUP0400058A2 (hu) 2001-02-02 2004-04-28 Takeda Chemical Industries, Ltd. Kondenzált heterogyűrűs vegyületek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
US20040171006A1 (en) * 2001-04-27 2004-09-02 Yonghong Xiao Regulation of human prostaglandin-f synthase 1-like protein
ES2282410T3 (es) 2001-05-08 2007-10-16 Kudos Pharmaceuticals Limited Derivados de isoquinolinona como inhibidores de parp.
WO2002091993A2 (en) 2001-05-10 2002-11-21 Merck & Co., Inc. Estrogen receptor modulators
EP1396488A1 (en) * 2001-05-23 2004-03-10 Mitsubishi Pharma Corporation Fused heterocyclic compound and medicinal use thereof
EP1392287B8 (en) * 2001-05-25 2007-01-10 Schering Corporation Use of substituted azetidinone derivatives in the treatment of Alzheimer's disease
US20030119800A1 (en) * 2001-06-18 2003-06-26 Manolagas Stavros C. Bone anabolic compounds and methods of use
ES2274986T3 (es) * 2001-08-01 2007-06-01 MERCK & CO., INC. Derivados de benzimidazo 4,5-f/isoquinolinona.
WO2003015761A1 (en) 2001-08-13 2003-02-27 Merck & Co., Inc. Selective estrogen receptor modulators
SE0103644D0 (sv) * 2001-11-01 2001-11-01 Astrazeneca Ab Therapeutic isoquinoline compounds
JP4381810B2 (ja) 2001-11-19 2009-12-09 イーライ リリー アンド カンパニー 選択的エストロゲン受容体βアゴニストとしての置換ベンゾピラン
EP1478631A1 (en) 2001-11-28 2004-11-24 AstraZeneca AB Therapeutic compounds
UA83620C2 (ru) * 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
TWI306450B (en) * 2001-12-13 2009-02-21 Wyeth Corp Substituted phenyl naphthalenes as estrogenic agents
US6960607B2 (en) * 2001-12-13 2005-11-01 Wyeth Naphthyl benzoxazoles and benzisoxazoles as estrogenic agents
US6903238B2 (en) * 2001-12-13 2005-06-07 Wyeth Substituted indenones as estrogenic agents
TW200301107A (en) * 2001-12-13 2003-07-01 Wyeth Corp Substituted 6H-dibenzo[c,h]chromenes as estrogenic agents
EP1454898A4 (en) 2001-12-13 2006-12-13 Ajinomoto Kk NEW PHENYL ALANIDE DERIVATIVES
US6774248B2 (en) * 2001-12-18 2004-08-10 Wyeth Substituted 2-phenyl benzofurans as estrogenic agents
US7015219B2 (en) * 2001-12-19 2006-03-21 Bristol-Myers Squibb Company 3-aryl-hydroxybenzoxazines and 3, 4-dihydro-3-aryl-hydroxybenzoxazines as selective estrogen receptor beta modulators
TW200408385A (en) 2001-12-21 2004-06-01 Akzo Nobel Nv Tetrahydrobenzfluorene derivatives
US6835745B2 (en) * 2002-01-15 2004-12-28 Wyeth Phenyl substituted thiophenes as estrogenic agents
US6630508B1 (en) * 2002-02-11 2003-10-07 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor β agonists
US7402595B2 (en) * 2002-02-13 2008-07-22 Takeda Pharmaceutical Company Limited JNK inhibitor
US7214693B2 (en) * 2002-10-15 2007-05-08 University Of Tennessee Research Foundation Heterocyclic selective androgen receptor modulators and methods of use thereof
AU2003212856A1 (en) 2002-03-01 2003-09-16 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
US7381730B2 (en) * 2002-03-15 2008-06-03 Bristol-Myers Squibb Company 3-arylquinazoline derivatives as selective estrogen receptor beta modulators
US7138426B2 (en) * 2002-04-24 2006-11-21 Merck & Co., Inc. Estrogen receptor modulators
US20030220377A1 (en) * 2002-05-08 2003-11-27 Richard Chesworth Indole compounds and their use as estrogen agonists/antagonists
CA2489906A1 (en) * 2002-06-06 2003-12-18 University Of Rochester Androgen receptor coregulators
DE10230381A1 (de) * 2002-07-05 2004-01-22 Institut für Medizintechnologie Magdeburg GmbH, IMTM Verwendung von Inhibitoren der Alanyl-Aminopeptidasen und diese umfassende pharmazeutischen Zubereitungen
WO2004006906A2 (en) 2002-07-15 2004-01-22 Combinatorx, Incorporated Methods for the treatment of neoplasms
US6893191B2 (en) 2002-07-19 2005-05-17 Creative Pultrusions, Inc. Wale and retaining wall system
MXPA05000983A (es) * 2002-07-24 2005-08-18 Kyorin Seiyaku Kk Derivados de 4-(aril substituido)-5-hidroxiisoquinolinona.
WO2004014378A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 3-isoquinolinone derivatives as matrix metalloproteinase inhiitors
JPWO2004024694A1 (ja) 2002-09-10 2006-01-05 杏林製薬株式会社 ４−置換アリール−５−ヒドロキシイソキノリノン誘導体
US20060039974A1 (en) 2002-09-11 2006-02-23 Takeda Pharmaceutical Company Limited Sustained release preparation
WO2004026290A1 (en) * 2002-09-19 2004-04-01 Merck & Co., Inc. Method for treating depression and/or anxiety
MXPA05003054A (es) 2002-09-20 2005-05-27 Pfizer Prod Inc Ligandos de amida y sulfonamida para el receptor de estrogenos.
US7501412B2 (en) 2002-11-22 2009-03-10 Mitsubishi Tanabe Pharma Corporation Isoquinoline compounds and medicinal use thereof
AU2003301020A1 (en) * 2002-12-20 2004-07-22 Sankyo Company, Limited Isoquinolinone derivatives and their use as therapeutic agents
US7199110B2 (en) * 2002-12-30 2007-04-03 Purdue Research Foundation Method of treatment for spinal cord injury
WO2004073612A2 (en) 2003-02-13 2004-09-02 Merck & Co. Inc. Estrogen receptor modulators
WO2004083184A1 (ja) 2003-03-17 2004-09-30 Takeda Pharmaceutical Company Limited 受容体拮抗剤
US20060111318A1 (en) * 2003-04-18 2006-05-25 Advanced Medicine Research Institute Agent for treating eye diseases
WO2004094400A2 (en) 2003-04-21 2004-11-04 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
WO2004094401A1 (en) * 2003-04-21 2004-11-04 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
CL2004000985A1 (es) * 2003-05-16 2005-01-14 Wyeth Corp Compuestos derivados de fenilquinolinas; composicion farmaceutica, proceso de preparacion; y uso para tratar osteoporosis, enfermedad de paget, dano vascular, osteoartritis, cancer oseo, cancer ovarico, cancer prostatico, hipercolesterolemia, aterosc
DE602004004124T2 (de) * 2003-05-16 2007-04-26 Wyeth Aryl-carbaldehyd oxime-verbindungen und deren verwendung als oestrogenwirksame substanzen
US7250440B2 (en) * 2003-08-12 2007-07-31 Wyeth (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents
WO2005030727A1 (en) * 2003-09-23 2005-04-07 Merck & Co., Inc. Isoquinolinone potassium channel inhibitors
US7741322B2 (en) * 2003-09-23 2010-06-22 Merck Sharp & Dohme Corp. Isoquinolinone potassium channel inhibitors
CN1856476A (zh) * 2003-09-23 2006-11-01 默克公司 异喹啉酮钾通道抑制剂
ATE534404T1 (de) * 2003-10-03 2011-12-15 Takeda Pharmaceutical Dipeptidylpeptidase-iv-inhibitoren zur behandlung von diabetes-patienten mit sekundärversagen durch sulfonylharnstoffe
CN1863789B (zh) * 2003-10-03 2010-06-09 博尔托拉制药公司 取代的异喹啉酮
JP2007512344A (ja) * 2003-11-24 2007-05-17 メルク　エンド　カムパニー　インコーポレーテッド エストロゲン受容体調節剤
WO2005097141A2 (en) * 2003-11-24 2005-10-20 Merck & Co., Inc. Estrogen receptor modulators
EP1689410B1 (en) * 2003-11-26 2008-05-21 Bayer Schering Pharma Aktiengesellschaft Prevention and treatment of hypertensive heart diseases by the selective estrogens 8beta-vinyl-estra-1,3,5(10)-trien-3,17beta-diol and 17beta-fluor-9alpha-vinyl-estra-1,3,5(10)-trien-3,16alpha-diol
AU2005212092B2 (en) * 2004-02-13 2011-01-20 Msd K.K. Fused-ring 4-oxopyrimidine derivative
US7157492B2 (en) * 2004-02-26 2007-01-02 Wyeth Dibenzo chromene derivatives and their use as ERβ selective ligands
WO2005099700A1 (en) 2004-04-06 2005-10-27 Merck & Co., Inc. Methods for the treatment of hypertension
BRPI0510639A (pt) * 2004-05-04 2007-11-13 Acadia Pharm Inc composto ou um sal ou uma pró-droga farmaceuticamente aceitável do mesmo, composição farmacêutica, métodos de tratar ou prevenir distúrbios, de terapia de reposição hormonal, de abaixar nìveis de colesterol, triglicerìdeos ou ldl, de tratar cognição prejudicada ou prover neuroproteção, de prevenir concepção, de modular ou agonizar especificamente um ou mais receptores de estrogênio e, uso de um composto
CN1968960A (zh) 2004-06-10 2007-05-23 默克公司 雌激素受体调节剂
WO2006009912A1 (en) 2004-06-23 2006-01-26 Merck & Co., Inc. Estrogen receptor modulators
JP2008505079A (ja) * 2004-06-30 2008-02-21 メルク　エンド　カムパニー　インコーポレーテッド エストロゲン受容体調節剤
EP1761513A1 (en) * 2004-07-01 2007-03-14 Wyeth Tetracyclic compounds as estrogen ligands
US20060205733A1 (en) 2004-08-26 2006-09-14 Encysive Pharmaceuticals Endothelin a receptor antagonists in combination with phosphodiesterase 5 inhibitors and uses thereof
CN101072564A (zh) 2004-08-26 2007-11-14 恩希赛弗制药公司 内皮缩血管肽a受体(eta)拮抗剂与磷酸二酯酶5(pde5)抑制剂的联合及其用途
RU2007106870A (ru) * 2004-09-07 2008-10-20 Вайет (Us) 6Н-[1]БЕНЗОПИРАНО[4,3-b]ХИНОЛИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЭСТРОГЕННЫХ АГЕНТОВ
ES2361031T3 (es) * 2004-10-18 2011-06-13 Eli Lilly And Company Benzopiranos sustituidos como agonistas selectivos del receptor beta de estrógenos.
AR051597A1 (es) 2004-11-01 2007-01-24 Merck & Co Inc Moduladores de los receptores de estrogeno
US7511152B2 (en) 2004-12-09 2009-03-31 Merck & Co., Inc. Estrogen receptor modulators
US20060183652A1 (en) 2004-12-10 2006-08-17 Takashi Fujitsu Lubricating oil composition
RU2007129150A (ru) * 2004-12-31 2009-02-10 Авентис Фармасьютикалз Инк. (Us) Применение ряда фенилнафтильных соединений, которые не проявляют значительной аффинности в отношениях эстрогеновых рецепторов (er)
WO2006081152A2 (en) 2005-01-24 2006-08-03 Merck & Co., Inc. Estrogen receptor modulators
EP1853578A1 (en) 2005-02-15 2007-11-14 Eli Lilly And Company Substituted tetralins as selective estrogen receptor-beta agonists
KR20070103456A (ko) * 2005-02-16 2007-10-23 와이어쓰 방사선- 또는 화학요법-유발 점막염 및 방사선 방광염용에스트로겐 수용체-β 선택적 아고니스트의 용도
US7482029B2 (en) * 2005-04-01 2009-01-27 Bionovo, Inc. Composition for treatment of menopause
CN101184395A (zh) 2005-04-06 2008-05-21 Irm责任有限公司 包含二芳基胺的化合物和组合物及其作为类固醇激素核受体调节剂的用途
US9763961B2 (en) * 2005-04-13 2017-09-19 City Of Hope Compositions that modulate the activity of estrogen receptors and estrogen-related receptors and methods for use
US7456188B1 (en) 2005-04-28 2008-11-25 Bristol-Myers Squibb Company C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators
AU2005334672A1 (en) * 2005-07-21 2007-01-25 Reliance Life Sciences Pvt Ltd Compounds for treatment of lipase-mediated diseases
US20070021495A1 (en) * 2005-07-25 2007-01-25 Katzenellenbogen John A Sulfonamides as selective estrogen receptor
NI200800025A (es) * 2005-07-26 2009-03-03 Derivados de isoquinolona sustituidos con piperidinilo en calidad de inhibidores de rho-quinasa
ATE517871T1 (de) 2005-10-05 2011-08-15 Merck Sharp & Dohme Östrogenrezeptormodulatoren
WO2007053353A2 (en) * 2005-10-28 2007-05-10 Wyeth Pyrrolo[2,3-f] and [3,2-f]isoquinolinone derivatives as 5-hydroxytryptamine-6 ligands
US20070197488A1 (en) * 2005-11-29 2007-08-23 Olaf Peters Prodrugs of ERbeta-selective substances, process for their production, and pharmaceutical compositions that contain these compounds
EP1981539B1 (en) * 2006-02-09 2014-07-23 Amgen Research (Munich) GmbH Treatment of metastatic breast cancer
WO2007093364A1 (en) 2006-02-15 2007-08-23 Sanofi-Aventis Azacyclyl-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
CA2636617A1 (en) 2006-02-15 2007-08-23 Lothar Schwink Novel aminoalcohol-substituted aryldihydroisoquinolinones, process for their preparation and their use as medicaments
EP1990335A4 (en) * 2006-03-02 2009-11-11 Astellas Pharma Inc 17-BETA-HSD-type-5 INHIBITOR
US8481529B2 (en) 2006-05-16 2013-07-09 The Arizona Board Of Regents On Behalf Of The University Of Arizona Combination cancer chemotherapy
JP2009541310A (ja) 2006-06-19 2009-11-26 アストラゼネカ・アクチエボラーグ イソキノリン誘導体およびサイトカイン仲介疾患の阻害剤としてのそれらの使用
US8318941B2 (en) * 2006-07-06 2012-11-27 Bristol-Myers Squibb Company Pyridone/hydroxypyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors
JP2009545605A (ja) 2006-08-02 2009-12-24 ユニバーシティ オブ サザン カリフォルニア フィトエストロゲン製剤およびその使用
US8058243B2 (en) * 2006-10-13 2011-11-15 Hsc Research And Development Limited Partnership Method for treating a brain cancer with ifenprodil
EA026578B1 (ru) 2007-01-22 2017-04-28 ДЖиТиЭкс, ИНК. Вещества, связывающие ядерные рецепторы
US9623021B2 (en) * 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
GB0722779D0 (en) * 2007-11-20 2008-01-02 Sterix Ltd Compound
US20100029734A1 (en) * 2008-05-06 2010-02-04 Ore Pharmaceuticals Inc. Methods for breast cancer screening and treatment
WO2010096801A1 (en) 2009-02-23 2010-08-26 Gtx, Inc. Estrogen receptor ligands and methods of use thereof
WO2012006634A2 (en) 2010-07-09 2012-01-12 The Board Of Trustees Of The University Of Illiniois Prostate specific antigen (psa) peptide therapy

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016006095A (ja) * 2010-05-04 2016-01-14 ジーティーエックス・インコーポレイテッド 核内受容体結合薬

Also Published As

Publication number Publication date
RU2604666C2 (ru) 2016-12-10
EP2566330A4 (en) 2013-11-06
US20100267767A1 (en) 2010-10-21
JP2016006095A (ja) 2016-01-14
KR20130061151A (ko) 2013-06-10
EP2566330A1 (en) 2013-03-13
AU2011248154A1 (en) 2012-11-29
JP2013525494A (ja) 2013-06-20
RU2012151846A (ru) 2014-06-10
US9623021B2 (en) 2017-04-18
IL222823A0 (en) 2012-12-31
CA2798259A1 (en) 2011-11-10
MX2012012777A (es) 2013-04-24
CN102970870A (zh) 2013-03-13
AU2011248154B2 (en) 2016-03-03
WO2011140228A1 (en) 2011-11-10
CN106420745A (zh) 2017-02-22

Similar Documents

Publication Publication Date Title
JP5792799B2 (ja) 核内受容体結合薬
JP6122055B2 (ja) 核内受容体結合剤
US20170014401A1 (en) Nuclear receptor binding agents
JP5913400B2 (ja) 核内受容体結合剤
AU2006318400C1 (en) Nuclear receptor binding agents
JP2009543872A (ja) 選択的アンドロゲン受容体調節薬、その類似体及び誘導体とそれらの使用
JP2014518848A (ja) 糖尿病を治療するための選択的アンドロゲン受容体調節因子
US9604931B2 (en) Nuclear receptor binding agents
AU2013219238C1 (en) Nuclear receptor binding agents
HK1124337A (en) Nuclear receptor binding agents

Legal Events

Date Code Title Description
A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20140430

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140430

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20150324

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150619

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20150619

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20150714

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20150806

R150 Certificate of patent or registration of utility model

Ref document number: 5792799

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees