AU2016226468B2 - TGF-beta inhibitors - Google Patents

TGF-beta inhibitors Download PDF

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Publication number
AU2016226468B2
AU2016226468B2 AU2016226468A AU2016226468A AU2016226468B2 AU 2016226468 B2 AU2016226468 B2 AU 2016226468B2 AU 2016226468 A AU2016226468 A AU 2016226468A AU 2016226468 A AU2016226468 A AU 2016226468A AU 2016226468 B2 AU2016226468 B2 AU 2016226468B2
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AU
Australia
Prior art keywords
imidazol
imidazo
fluorophenyl
pyridazine
carbonitrile
Prior art date
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Ceased
Application number
AU2016226468A
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English (en)
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AU2016226468A1 (en
Inventor
Robert M. Borzilleri
Chetan Darne
Ihab S. Darwish
Marina Gelman
Hui Hong
Todd Kinsella
Peiying Liu
Hasibur RAHAMAN
Rajinder Singh
Upender Velaparthi
Jayakumar Sankara WARRIER
Jiaxin Yu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Rigel Pharmaceuticals Inc
Original Assignee
Bristol Myers Squibb Co
Rigel Pharmaceuticals Inc
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Filing date
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Publication of AU2016226468A1 publication Critical patent/AU2016226468A1/en
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Publication of AU2016226468B2 publication Critical patent/AU2016226468B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
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    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Biochemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
AU2016226468A 2015-03-02 2016-02-26 TGF-beta inhibitors Ceased AU2016226468B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562127109P 2015-03-02 2015-03-02
US62/127,109 2015-03-02
PCT/US2016/019830 WO2016140884A1 (en) 2015-03-02 2016-02-26 TGF-β INHIBITORS

Publications (2)

Publication Number Publication Date
AU2016226468A1 AU2016226468A1 (en) 2017-08-03
AU2016226468B2 true AU2016226468B2 (en) 2020-10-22

Family

ID=55543068

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016226468A Ceased AU2016226468B2 (en) 2015-03-02 2016-02-26 TGF-beta inhibitors

Country Status (23)

Country Link
US (3) US9884868B2 (enExample)
EP (1) EP3265454B1 (enExample)
JP (1) JP6836998B2 (enExample)
KR (1) KR20170122799A (enExample)
CN (1) CN107406412B (enExample)
AR (1) AR103828A1 (enExample)
AU (1) AU2016226468B2 (enExample)
BR (1) BR112017017135A2 (enExample)
CA (1) CA2973602A1 (enExample)
CL (1) CL2017002207A1 (enExample)
CO (1) CO2017009891A2 (enExample)
EA (1) EA037112B1 (enExample)
ES (1) ES2789331T3 (enExample)
IL (1) IL254187A0 (enExample)
MX (1) MX371167B (enExample)
MY (1) MY186133A (enExample)
PE (1) PE20171789A1 (enExample)
PH (1) PH12017501326A1 (enExample)
SG (1) SG11201705821XA (enExample)
TN (1) TN2017000374A1 (enExample)
TW (1) TW201639827A (enExample)
WO (1) WO2016140884A1 (enExample)
ZA (1) ZA201705527B (enExample)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017017135A2 (pt) 2015-03-02 2018-04-03 Rigel Pharmaceuticals, Inc. inibidores de tgf-beta
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
EA201991375A1 (ru) 2016-12-08 2020-01-20 Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем Бицикло[1.1.1]пентановые ингибиторы киназы, содержащей домен с двумя лейциновыми "застежками-молниями" (dlk), для лечения заболевания
WO2018132279A1 (en) 2017-01-05 2018-07-19 Bristol-Myers Squibb Company Tgf beta receptor antagonists
US11040027B2 (en) 2017-01-17 2021-06-22 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
JP2020512400A (ja) * 2017-03-23 2020-04-23 クラヴィウス ファーマシューティカルズ，エルエルシー ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法
CN109293652B (zh) * 2017-07-24 2021-10-22 四川科伦博泰生物医药股份有限公司 一种取代的噻唑衍生物及其用途
GB201718285D0 (en) 2017-11-03 2017-12-20 Discuva Ltd Antibacterial Compounds
WO2019185631A1 (en) 2018-03-29 2019-10-03 Masarykova Univerzita 4—(1h— imidazol— 5— yl) -1h-pyrrolo [2, 3-b] pyridines for use in the treatment of leukaemias, lymphomas and solid tumors
US12252531B2 (en) 2018-07-11 2025-03-18 Scholar Rock, Inc. Methods of screening for high-affinity, isoform-selective TGFβ1 inhibitors
WO2020041562A1 (en) 2018-08-22 2020-02-27 Clavius Pharmaceuticals, Llc Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
EP3894401A2 (en) * 2018-12-11 2021-10-20 Theravance Biopharma R&D IP, LLC Naphthyridine and quinoline derivatives useful as alk5 inhibitors
CN111825658B (zh) * 2019-04-18 2024-11-08 华东理工大学 Egfr三突变抑制剂及其应用
US11560366B2 (en) 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
WO2021102468A1 (en) * 2019-11-22 2021-05-27 Theravance Biopharma R&D Ip, Llc Substituted 1,5-naphthyridines or quinolines as alk5 inhibitors
CN118767143A (zh) 2019-12-12 2024-10-15 听治疗有限责任公司 用于预防和治疗听力损失的组合物和方法
US12441707B2 (en) 2019-12-30 2025-10-14 Tyra Biosciences, Inc. Indazole compounds
TW202214623A (zh) * 2020-06-10 2022-04-16 美商施萬生物製藥研發 Ip有限責任公司 結晶型alk5抑制劑及其用途
CN112321592B (zh) * 2020-11-12 2022-03-04 山东省科学院菏泽分院 一种6-氯咪唑并[1,2-b]哒嗪-3-甲腈的合成方法
WO2022251359A1 (en) * 2021-05-26 2022-12-01 Theravance Biopharma R&D Ip, Llc Bicyclic inhibitors of alk5 and methods of use
CA3227334A1 (en) * 2021-07-28 2023-02-02 Tiumbio Co., Ltd. Pharmaceutical composition for preventing or treating tumor, and use thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024239186A1 (zh) * 2023-05-22 2024-11-28 睿健医药科技(苏州)有限公司 吡唑甲酰基哌嗪酮类化合物、药物组合物及其应用
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025063820A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
KR20250144822A (ko) * 2024-03-27 2025-10-13 동국대학교 산학협력단 신규 옥사졸 유도체 및 이를 포함하는 암 예방 또는 치료용 조성물
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005075478A1 (en) * 2004-01-30 2005-08-18 Eli Lilly And Company Kinase inhibitors
WO2007076348A2 (en) * 2005-12-23 2007-07-05 Smithkline Beecham Corporation Azaindole inhibitors of aurora kinases
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
CN103936730A (zh) * 2013-01-22 2014-07-23 通化济达医药有限公司 苯磺酰胺噻唑激酶抑制剂
US20140357612A1 (en) * 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE322681T1 (de) 1999-01-21 2006-04-15 Metamorphix Inc Inhibitoren für wachstumdifferenzierungsfaktor und ihre anwendungen
EP1349851A4 (en) * 2000-11-16 2004-09-08 Smithkline Beecham Corp COMPOUNDS
WO2002072576A1 (en) 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
US7320789B2 (en) 2001-09-26 2008-01-22 Wyeth Antibody inhibitors of GDF-8 and uses thereof
DE60309342T2 (de) * 2002-08-09 2007-05-16 Eli Lilly And Co., Indianapolis Benzimidazole und benzothiazole als inhibitoren der map-kinase
EP1720862A1 (en) * 2004-02-03 2006-11-15 Eli Lilly And Company Kinase inhibitors
TWI309240B (en) 2004-09-17 2009-05-01 Hoffmann La Roche Anti-ox40l antibodies
EP1866339B8 (en) 2005-03-25 2021-12-01 GITR, Inc. Gitr binding molecules and uses therefor
ME02461B (me) 2005-05-10 2017-02-20 Incyte Holdings Corp Modulatori indoleamina 2,3-dioksigenaze i metode za upotrebu istih
KR101607288B1 (ko) 2005-07-01 2016-04-05 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체
US7473784B2 (en) * 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
EP1971583B1 (en) 2005-12-20 2015-03-25 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
EA200801716A1 (ru) * 2006-01-18 2009-04-28 Амген Инк. Тиазольные соединения и их применение
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.
US20080125470A1 (en) 2006-09-19 2008-05-29 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
SG182187A1 (en) * 2007-06-08 2012-07-30 Abbott Gmbh & Co Kg 5-heteroaryl substituted indazoles as kinase inhibitors
EP2175884B8 (en) 2007-07-12 2017-02-22 GITR, Inc. Combination therapies employing gitr binding molecules
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
EP2227233B1 (en) 2007-11-30 2013-02-13 Newlink Genetics Ido inhibitors
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
TWI729512B (zh) 2008-12-09 2021-06-01 美商建南德克公司 抗pd-l1抗體及其於增進t細胞功能之用途
CN102574924A (zh) 2009-09-03 2012-07-11 先灵公司 抗-gitr抗体
EP2493862B1 (en) 2009-10-28 2016-10-05 Newlink Genetics Corporation Imidazole derivatives as ido inhibitors
PT2949670T (pt) 2009-12-10 2019-05-20 Hoffmann La Roche Anticorpos que se ligam preferencialmente ao domínio extracelular 4 do csf1r e respetiva utilização
NZ705128A (en) 2010-03-04 2015-04-24 Macrogenics Inc Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof
WO2011107553A1 (en) 2010-03-05 2011-09-09 F. Hoffmann-La Roche Ag Antibodies against human csf-1r and uses thereof
CA2789071C (en) 2010-03-05 2018-03-27 F. Hoffmann-La Roche Ag Antibodies against human csf-1r and uses thereof
CN107011438B (zh) 2010-05-04 2020-11-20 戊瑞治疗有限公司 结合csf1r的抗体
EP2566851B1 (en) * 2010-05-05 2015-01-14 Universität Bayreuth Combretastatin analogs for use in the treatment of cancer
SG10201912092VA (en) 2010-09-09 2020-02-27 Pfizer 4-1bb binding molecules
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
NO2694640T3 (enExample) 2011-04-15 2018-03-17
DK2699264T3 (en) 2011-04-20 2018-06-25 Medimmune Llc ANTIBODIES AND OTHER MOLECULES BINDING B7-H1 AND PD-1
US10441577B2 (en) * 2011-07-08 2019-10-15 Helmholtz Zentrum Fuer Infektionsforschung Medicament for treatment of liver cancer
EP2543372A1 (en) * 2011-07-08 2013-01-09 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for the treatment of liver cancer
WO2013033203A1 (en) 2011-09-01 2013-03-07 Irm Llc Compounds and compositions as c-kit kinase inhibitors
RU2014121983A (ru) 2011-10-31 2015-12-10 Ксенон Фармасьютикалз Инк. Биарильные простоэфирные сульфонамиды и их применение в качестве терапевтических средств
KR101981873B1 (ko) 2011-11-28 2019-05-23 메르크 파텐트 게엠베하 항-ｐｄ-ｌ1 항체 및 그의 용도
EP2788475A1 (en) * 2011-12-05 2014-10-15 Primorigen Biosciences Inc. Compositions and methods for differentiating pluripotent stem cells into primitive blood cells and uses thereof
TW201329067A (zh) 2011-12-08 2013-07-16 Amgen Inc 作為ｇｋａ活化劑之脲化合物
RU2658603C2 (ru) 2011-12-15 2018-06-21 Ф.Хоффманн-Ля Рош Аг Антитела против человеческого csf-1r и их применения
CA2861122A1 (en) 2012-02-06 2013-08-15 Genentech, Inc. Compositions and methods for using csf1r inhibitors
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
US10280168B2 (en) 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
AU2012374617B2 (en) 2012-05-11 2015-09-17 Five Prime Therapeutics, Inc. Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (CSF1R)
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
SG10201906328RA (en) 2012-08-31 2019-08-27 Five Prime Therapeutics Inc Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r)
CN104837832B (zh) 2012-10-05 2019-04-26 里格尔药品股份有限公司 Gdf-8抑制剂
WO2014100533A1 (en) * 2012-12-21 2014-06-26 Bristol-Myers Squibb Company NOVEL SUBSTITUTED IMIDAZOLES AS CASEIN KINASE 1 δ/ε INHIBITORS
CN103275112A (zh) 2013-05-11 2013-09-04 济南韶远医药技术有限公司 一种利用微反应器连续合成芳基硼酸酯的方法
US20160199372A1 (en) 2013-08-20 2016-07-14 Bristol-Myers Squibb Company Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by aak1, such as alzheimer's disease, bipolar disorder, pain, schizophrenia
BR112017017135A2 (pt) 2015-03-02 2018-04-03 Rigel Pharmaceuticals, Inc. inibidores de tgf-beta

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005075478A1 (en) * 2004-01-30 2005-08-18 Eli Lilly And Company Kinase inhibitors
WO2007076348A2 (en) * 2005-12-23 2007-07-05 Smithkline Beecham Corporation Azaindole inhibitors of aurora kinases
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
CN103936730A (zh) * 2013-01-22 2014-07-23 通化济达医药有限公司 苯磺酰胺噻唑激酶抑制剂
US20140357612A1 (en) * 2013-05-30 2014-12-04 Plexxikon Inc. Compounds for kinase modulation, and indications therefor

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Gellibert, Françoise, et al. "Identification of 1, 5-naphthyridine derivatives as a novel series of potent and selective TGF-β type I receptor inhibitors." Journal of medicinal chemistry 47.18 (2004): 4494-4506. *

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