PH12017501326A1 - Tgf-� inhibitors - Google Patents

Tgf-� inhibitors

Info

Publication number
PH12017501326A1
PH12017501326A1 PH12017501326A PH12017501326A PH12017501326A1 PH 12017501326 A1 PH12017501326 A1 PH 12017501326A1 PH 12017501326 A PH12017501326 A PH 12017501326A PH 12017501326 A PH12017501326 A PH 12017501326A PH 12017501326 A1 PH12017501326 A1 PH 12017501326A1
Authority
PH
Philippines
Prior art keywords
tgf
inhibitors
compound
disclosed
prodrugs
Prior art date
Application number
PH12017501326A
Other languages
English (en)
Inventor
Todd Kinsella
Marina Gelman
Hui Hong
Ihab S Darwish
Rajinder Singh
Jiaxin Yu
Robert M Borzilleri
Upender Velaparthi
Peiying Liu
Chetan Darne
Hasibur Rahaman
Jayakumar Sankara Warrier
Original Assignee
Rigel Pharmaceuticals Inc
Bristol Myers Squibb Co
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 Rigel Pharmaceuticals Inc, Bristol Myers Squibb Co filed Critical Rigel Pharmaceuticals Inc
Publication of PH12017501326A1 publication Critical patent/PH12017501326A1/en

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    • 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
    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • 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
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • 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
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • 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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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
PH12017501326A 2015-03-02 2017-07-21 Tgf-� inhibitors PH12017501326A1 (en)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
PH12017501326A1 true PH12017501326A1 (en) 2017-12-18

Family

ID=55543068

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12017501326A PH12017501326A1 (en) 2015-03-02 2017-07-21 Tgf-� 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 (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6836998B2 (ja) 2015-03-02 2021-03-03 ライジェル ファーマシューティカルズ, インコーポレイテッド TGF−β阻害剤
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
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
CA3045947A1 (en) * 2016-12-08 2018-06-14 Michael J. Soth Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease
US10961239B2 (en) 2017-01-05 2021-03-30 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
ES3053505T3 (en) * 2017-03-23 2026-01-22 Clavius Pharmaceuticals Llc Tri-substituted imidazoles for the inhibition of tgf beta and methods of treatment
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
ES2918448T3 (es) 2018-03-29 2022-07-15 Univ Masarykova 4-(1H-Imidazol-5-il)-1H-pirrolo [2,3-b]piridinas para su uso en el tratamiento de leucemias, linfomas y tumores sólidos
KR102891320B1 (ko) 2018-07-11 2025-11-28 스칼러 락, 인크. 고친화도, 이소형-선택적 TGFβ1 억제제 및 그의 용도
WO2020041562A1 (en) 2018-08-22 2020-02-27 Clavius Pharmaceuticals, Llc Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
CA3117710A1 (en) * 2018-12-11 2020-06-18 Theravance Biopharma R&D Ip, Llc 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
KR20220104208A (ko) * 2019-11-22 2022-07-26 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 Alk5 억제제로서 치환된 1,5-나프티리딘 또는 퀴놀린
CN114981298B (zh) 2019-12-12 2024-08-20 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
WO2021138391A1 (en) 2019-12-30 2021-07-08 Tyra Biosciences, Inc. Indazole compounds
CN116323607A (zh) * 2020-06-10 2023-06-23 施万生物制药研发Ip有限责任公司 用作alk5抑制剂的萘啶衍生物
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
JP2024527978A (ja) * 2021-07-28 2024-07-26 ティウムバイオ カンパニー、リミテッド 腫瘍の予防または処置のための医薬組成物およびその使用
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
AU2023449764A1 (en) * 2023-05-22 2025-12-11 Iregene Therapeutics Co., Ltd. Pyrazolecarbonyl piperazinone compound, pharmaceutical composition and use thereof
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
WO2025063820A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN117899085A (zh) * 2023-12-27 2024-04-19 无锡市南京大学锡山应用生物技术研究所 用于提升全层皮肤移植成功率的药物组合物和药物制剂及其用途
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025193774A1 (en) * 2024-03-12 2025-09-18 The Regents Of The University Of California Methods of identifying and treating an immune poor cancer
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
KR20250174164A (ko) * 2024-06-04 2025-12-12 아주대학교산학협력단 신규 화합물 및 이를 포함하는 대사성 질환의 예방 또는 치료용 약학적 조성물
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026043823A2 (en) 2024-08-19 2026-02-26 Sutro Biopharma, Inc. Antibodies comprising site-specific non-natural amino acid residues, methods of preparation and uses thereof
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026080697A1 (en) 2024-10-09 2026-04-16 Sutro Biopharma, Inc. Antibody conjugates with high payload to antibody ratios, compositions comprising the same, and methods of their use
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003517580A (ja) 1999-01-21 2003-05-27 メタモーフイクス・インコーポレーテツド 増殖分化因子インヒビター及びそれらの用途
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
AU2003256297A1 (en) * 2002-08-09 2004-02-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
US7863310B2 (en) * 2004-02-03 2011-01-04 Eli Lilly And Company Kinase inhibitors
TWI309240B (en) 2004-09-17 2009-05-01 Hoffmann La Roche Anti-ox40l antibodies
JP5238936B2 (ja) 2005-03-25 2013-07-17 ジーアイティーアール,インク. Gitr結合分子およびその使用
DK1879573T3 (da) 2005-05-10 2013-02-25 Incyte Corp Modulatorer af indolamin 2,3-dioxygenase og fremgangsmåder til anvendelse deraf
KR101704734B1 (ko) 2005-07-01 2017-02-09 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
ES2540561T3 (es) 2005-12-20 2015-07-10 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa
WO2007076348A2 (en) * 2005-12-23 2007-07-05 Smithkline Beecham Corporation Azaindole inhibitors of aurora kinases
AU2007207743B2 (en) * 2006-01-18 2010-07-08 Amgen Inc. Thiazole compounds as protein kinase B (PKB) inhibitors
CA2663057C (en) 2006-09-19 2015-12-08 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
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.
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
CN101790526A (zh) * 2007-06-08 2010-07-28 雅培制药有限公司 用作激酶抑制剂的5-杂芳基取代的吲唑化合物
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
PT2175884T (pt) 2007-07-12 2016-09-21 Gitr Inc Terapias de combinação empregando moléculas de ligação a gitr
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
WO2009073620A2 (en) 2007-11-30 2009-06-11 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
MX356367B (es) 2008-12-09 2018-05-25 Genentech Inc Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t.
IN2015DN02826A (enExample) 2009-09-03 2015-09-11 Merck Sharp & Dohme
EP2493862B1 (en) 2009-10-28 2016-10-05 Newlink Genetics Corporation Imidazole derivatives as ido inhibitors
DK2510010T3 (en) 2009-12-10 2015-12-14 Hoffmann La Roche Antibodies that bind to human CSF1R extracellular domain 4 and their use
DK2542256T3 (da) 2010-03-04 2019-08-26 Macrogenics Inc Antistoffer reagerende med b7-h3, immunologisk aktive fragmenter deraf og anvendelser deraf
CN102918061B (zh) 2010-03-05 2016-06-08 霍夫曼-拉罗奇有限公司 针对人csf-1r的抗体及其用途
RU2617971C2 (ru) 2010-03-05 2017-04-28 Ф.Хоффманн-Ля Рош Аг Антитела против csf-1r человека и их применение
EP3943154A1 (en) 2010-05-04 2022-01-26 Five Prime Therapeutics, Inc. Antibodies that bind csf1r
WO2011138409A1 (en) * 2010-05-05 2011-11-10 Universität Bayreuth Combretastatin analogs for use in the treatment of cancer
NZ729044A (en) 2010-09-09 2020-07-31 Pfizer 4-1bb binding molecules
JP2014500277A (ja) 2010-12-09 2014-01-09 アムジエン・インコーポレーテツド Pim阻害剤としての二環式化合物
NO2694640T3 (enExample) 2011-04-15 2018-03-17
CA2833636A1 (en) 2011-04-20 2012-10-26 Amplimmune, Inc. Antibodies and other molecules that bind b7-h1 and pd-1
EP2729146B1 (en) * 2011-07-08 2017-03-08 Helmholtz-Zentrum für Infektionsforschung GmbH 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
CN103930424A (zh) 2011-09-01 2014-07-16 Irm责任有限公司 作为c-Kit激酶抑制剂的化合物和组合物
MX2014005304A (es) 2011-10-31 2015-03-20 Xenon Pharmaceuticals Inc Biaril eter sulfonamidas y su uso como agentes terapeuticos.
BR112014012819B1 (pt) 2011-11-28 2022-08-16 Merck Patent Gmbh Anticorpo anti-pd-l1 ou fragmento de ligação ao antígeno do mesmo e composição
US9428732B2 (en) * 2011-12-05 2016-08-30 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
MX356337B (es) 2011-12-15 2018-05-23 Hoffmann La Roche Anticuerpos contra csf-1r humano y sus usos.
MX2014008961A (es) 2012-02-06 2014-10-14 Genentech Inc Composiciones y metodos para utilizar inhibidores de csf1r.
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
KR20150018533A (ko) 2012-05-11 2015-02-23 파이브 프라임 테라퓨틱스, 인크. 콜로니 자극 인자 1 수용체(csf1r)에 결속하는 항체들에 의한 질병 상태의 치료 방법
AR091649A1 (es) 2012-07-02 2015-02-18 Bristol Myers Squibb Co Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos
CN107759690A (zh) 2012-08-31 2018-03-06 戊瑞治疗有限公司 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法
JP6457942B2 (ja) 2012-10-05 2019-01-23 ライジェル ファーマシューティカルズ, インコーポレイテッド Gdf−8阻害剤
JP6267231B2 (ja) * 2012-12-21 2018-01-24 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company カゼインキナーゼ1δ/ε阻害剤としての新規な置換イミダゾール
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
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
RU2015149937A (ru) * 2013-05-30 2017-07-06 Плексксикон Инк. Соединения для модулирования киназы и показания к их применению
EP3035921A1 (en) 2013-08-20 2016-06-29 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
JP6836998B2 (ja) 2015-03-02 2021-03-03 ライジェル ファーマシューティカルズ, インコーポレイテッド TGF−β阻害剤

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