KR20170122799A - TGF-β 억제제 - Google Patents

TGF-β 억제제 Download PDF

Info

Publication number
KR20170122799A
KR20170122799A KR1020177027381A KR20177027381A KR20170122799A KR 20170122799 A KR20170122799 A KR 20170122799A KR 1020177027381 A KR1020177027381 A KR 1020177027381A KR 20177027381 A KR20177027381 A KR 20177027381A KR 20170122799 A KR20170122799 A KR 20170122799A
Authority
KR
South Korea
Prior art keywords
alkyl
imidazol
imidazo
haloalkyl
pyridine
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.)
Ceased
Application number
KR1020177027381A
Other languages
English (en)
Korean (ko)
Inventor
토드 킨셀라
마리나 젤먼
후이 홍
이하브 에스. 다르위쉬
라진데르 싱
지아신 유
로버트 엠. 보르질레리
우펜더 벨라파르티
페이잉 리우
체탄 다르네
하시부르 라하만
자야쿠마르 산카라 와리에르
Original Assignee
리겔 파마슈티칼스, 인크.
브리스톨-마이어스 스큅 컴퍼니
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 리겔 파마슈티칼스, 인크., 브리스톨-마이어스 스큅 컴퍼니 filed Critical 리겔 파마슈티칼스, 인크.
Publication of KR20170122799A publication Critical patent/KR20170122799A/ko
Ceased legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (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)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
KR1020177027381A 2015-03-02 2016-02-26 TGF-β 억제제 Ceased KR20170122799A (ko)

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 (1)

Publication Number Publication Date
KR20170122799A true KR20170122799A (ko) 2017-11-06

Family

ID=55543068

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020177027381A Ceased KR20170122799A (ko) 2015-03-02 2016-02-26 TGF-β 억제제

Country Status (23)

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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023008936A1 (ko) * 2021-07-28 2023-02-02 주식회사 티움바이오 종양 예방 또는 치료용 약학 조성물 및 이의 용도
WO2025063820A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물
WO2025206749A1 (ko) * 2024-03-27 2025-10-02 동국대학교 산학협력단 신규 옥사졸 유도체 및 이를 포함하는 암 예방 또는 치료용 조성물

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta
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
JP7128816B2 (ja) 2016-12-08 2022-08-31 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム 疾患の治療のための二重ロイシンジッパー(dlk)キナーゼのビシクロ[1.1.1]ペンタン阻害剤
US10961239B2 (en) 2017-01-05 2021-03-30 Bristol-Myers Squibb Company TGF beta receptor antagonists
ES2928773T3 (es) 2017-01-17 2022-11-22 Heparegenix Gmbh Inhibidores de proteína cinasas para fomentar la regeneración hepática o reducir o prevenir la muerte de hepatocitos
US11124509B2 (en) 2017-03-23 2021-09-21 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
SI3774795T1 (sl) 2018-03-29 2022-07-29 Masarykova Univerzita 4-(1H-imidazol-5-il)-1H-pirolo (2,3-B) piridini za uporabo pri zdravljenju levkemij, limfomov in trdnih tumorjev
MX2021000347A (es) 2018-07-11 2021-04-19 Scholar Rock Inc Inhibidores de tgf?1 selectivos de isoforma, de alta afinidad y usos de los mismos.
US12077548B2 (en) 2018-08-22 2024-09-03 Clavius Pharmaceuticals, LLC. Substituted imidazoles for the inhibition of TGF-β and methods of treatment
SG11202104331YA (en) * 2018-12-11 2021-05-28 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
CN114728941A (zh) * 2019-11-22 2022-07-08 施万生物制药研发Ip有限责任公司 作为alk5抑制剂的经取代的1,5-萘啶或喹啉
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
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
EP4717694A1 (en) * 2023-05-22 2026-04-01 Iregene Therapeutics Co., Ltd. Pyrazolformyl piperazinone compound, pharmaceutical composition and use thereof
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
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
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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (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
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

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU772694B2 (en) 1999-01-21 2004-05-06 Metamorphix International, Inc. Growth differentiation factor inhibitors and uses therefor
JP2004517068A (ja) * 2000-11-16 2004-06-10 スミスクライン・ビーチャム・コーポレイション 化合物
CA2440211A1 (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
WO2004014900A1 (en) * 2002-08-09 2004-02-19 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
WO2005080380A1 (en) * 2004-02-03 2005-09-01 Eli Lilly And Company Kinase inhibitors
TWI309240B (en) 2004-09-17 2009-05-01 Hoffmann La Roche Anti-ox40l antibodies
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
PL1879573T3 (pl) 2005-05-10 2013-05-31 Incyte Holdings Corp Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania
CN104356236B (zh) 2005-07-01 2020-07-03 E.R.施贵宝&圣斯有限责任公司 抗程序性死亡配体1(pd-l1)的人单克隆抗体
US7473784B2 (en) * 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
CA2634198C (en) 2005-12-20 2014-06-03 Incyte Corporation N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase
SI1962830T1 (sl) * 2005-12-23 2013-07-31 Glaxosmithkline Llc Azaindolni inhibitorji kinaz Aurora
MY149143A (en) * 2006-01-18 2013-07-15 Amgen Inc Thiazole compounds as protien kinase b (pkb) inhibitors
ES2444574T3 (es) 2006-09-19 2014-02-25 Incyte Corporation N-hidroxiamidinoheterociclos como moduladores de la indolamina 2,3-dioxigenasa
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
JP5451602B2 (ja) 2007-06-08 2014-03-26 アッヴィ・インコーポレイテッド キナーゼ阻害薬としての5−ヘテロアリール置換インダゾール類
WO2009005675A1 (en) * 2007-06-28 2009-01-08 Abbott Laboratories Novel triazolopyridazines
ES2776406T3 (es) 2007-07-12 2020-07-30 Gitr Inc Terapias de combinación que emplean moléculas de enlazamiento 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
JP5583592B2 (ja) 2007-11-30 2014-09-03 ニューリンク ジェネティクス コーポレイション Ido阻害剤
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
AU2009333580B2 (en) 2008-12-09 2016-07-07 Genentech, Inc. Anti-PD-L1 antibodies and their use to enhance T-cell function
EP2473531A4 (en) 2009-09-03 2013-05-01 Merck Sharp & Dohme Anti-gitr antibodies
US8722720B2 (en) 2009-10-28 2014-05-13 Newlink Genetics Corporation Imidazole derivatives as IDO inhibitors
PH12012500881A1 (en) 2009-12-10 2017-07-26 Hoffmann La Roche Antibodies binding preferentially human csf1r extracellular domain 4 and their use
JP5998060B2 (ja) 2010-03-04 2016-09-28 マクロジェニクス,インコーポレーテッド B7−h3と反応性のある抗体、その免疫学的に活性なフラグメントおよびその使用
CA2789076C (en) 2010-03-05 2017-11-21 F. Hoffmann-La Roche Ag Antibodies against human colony stimulating factor-1 receptor and uses thereof
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
MX378336B (es) 2010-05-04 2025-03-10 Five Prime Therapeutics Inc Anticuerpos que se unen a factor estimulante de colonias 1 (csf1r).
CN102985410B (zh) * 2010-05-05 2015-05-27 拜罗伊特大学 在癌症的治疗中使用的考布他汀类似物
PT2614082T (pt) 2010-09-09 2018-12-03 Pfizer Moléculas de ligação a 4-1bb
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
NO2694640T3 (https=) 2011-04-15 2018-03-17
KR101970025B1 (ko) 2011-04-20 2019-04-17 메디뮨 엘엘씨 B7-h1 및 pd-1과 결합하는 항체 및 다른 분자들
EP2543372A1 (en) 2011-07-08 2013-01-09 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for the treatment of liver cancer
ES2627120T3 (es) * 2011-07-08 2017-07-26 Helmholtz-Zentrum für Infektionsforschung GmbH Medicamento para el tratamiento del cáncer de hígado
US20150051206A1 (en) 2011-09-01 2015-02-19 Irm Llc Compounds and compositions as c-kit kinase inhibitors
JP6014155B2 (ja) 2011-10-31 2016-10-25 ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用
HRP20201595T1 (hr) 2011-11-28 2020-12-11 Merck Patent Gmbh Anti-pd-l1 protutijela i njihova uporaba
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
WO2013086397A1 (en) 2011-12-08 2013-06-13 Array Biopharma Inc. Urea compounds as gka activators
BR112014012624A2 (pt) 2011-12-15 2018-10-09 F Hoffmann-La Roche Ag anticorpos, composição farmacêutica, ácido nucleico, vetores de expressão, célula hospedeira, método para a produção de um anticorpo recombinante e uso do anticorpo
RU2014136332A (ru) 2012-02-06 2016-03-27 Дженентек, Инк. Композиции и способы применения ингибиторов 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
EP2847220A1 (en) 2012-05-11 2015-03-18 Five Prime Therapeutics, Inc. Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r)
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
KR20150072412A (ko) 2012-10-05 2015-06-29 리겔 파마슈티칼스, 인크. Gdf-8 억제제
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
EP3004060B1 (en) * 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
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
ES2789331T3 (es) 2015-03-02 2020-10-26 Rigel Pharmaceuticals Inc Inhibidores de TGF-beta

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023008936A1 (ko) * 2021-07-28 2023-02-02 주식회사 티움바이오 종양 예방 또는 치료용 약학 조성물 및 이의 용도
WO2025063820A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물
WO2025206749A1 (ko) * 2024-03-27 2025-10-02 동국대학교 산학협력단 신규 옥사졸 유도체 및 이를 포함하는 암 예방 또는 치료용 조성물

Also Published As

Publication number Publication date
US10287295B2 (en) 2019-05-14
IL254187A0 (en) 2017-10-31
ES2789331T3 (es) 2020-10-26
CA2973602A1 (en) 2016-09-09
WO2016140884A1 (en) 2016-09-09
CN107406412A (zh) 2017-11-28
SG11201705821XA (en) 2017-08-30
EA201791955A1 (ru) 2018-01-31
AR103828A1 (es) 2017-06-07
TN2017000374A1 (en) 2019-01-16
CN107406412B (zh) 2021-07-16
PE20171789A1 (es) 2017-12-28
ZA201705527B (en) 2019-08-28
EP3265454B1 (en) 2020-02-26
CL2017002207A1 (es) 2018-06-01
JP6836998B2 (ja) 2021-03-03
PH12017501326A1 (en) 2017-12-18
TW201639827A (zh) 2016-11-16
CO2017009891A2 (es) 2018-02-20
US20180127426A1 (en) 2018-05-10
HK1244785A1 (en) 2018-08-17
US20160257690A1 (en) 2016-09-08
US11352360B2 (en) 2022-06-07
US20200031832A1 (en) 2020-01-30
EP3265454A1 (en) 2018-01-10
EA037112B1 (ru) 2021-02-08
JP2018510857A (ja) 2018-04-19
BR112017017135A2 (pt) 2018-04-03
US9884868B2 (en) 2018-02-06
AU2016226468A1 (en) 2017-08-03
MY186133A (en) 2021-06-24
MX2017010735A (es) 2017-12-04
MX371167B (es) 2020-01-21
AU2016226468B2 (en) 2020-10-22

Similar Documents

Publication Publication Date Title
JP6836998B2 (ja) TGF−β阻害剤
JP7311654B2 (ja) Retキナーゼ阻害剤としての置換ピラゾロ[1,5-a]ピリジン化合物
JP6789941B2 (ja) Tgf−ベータ阻害剤としての縮合イミダゾール誘導体
ES2759240T3 (es) Compuestos de piridina 2,3-disustituidos como inhibidores de TGF-beta
WO2024233776A1 (en) Small molecule inhibitors of kras g12d mutant
JP2023538060A (ja) 二環化合物、それを含む組成物、及びそれらの使用
JP6800158B2 (ja) Gdf−8阻害剤
EP3503891A1 (en) Inhibitors of indoleamine 2,3-dioxygenase and methods of their use
AU2019390863B2 (en) Heterocyclic compound
WO2016106266A1 (en) TGFβ RECEPTOR ANTAGONISTS
CN117295737A (zh) Hpk1拮抗剂和其用途
CN119768403A (zh) 作为ddr抑制剂用于治疗纤维化病症和癌症的吡啶并吡唑类
WO2025199379A1 (en) Novel fak degrader compounds and uses thereof
WO2018132279A1 (en) Tgf beta receptor antagonists
HK1244785B (en) Tgf-beta inhibitors

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20170927

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20210226

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20230428

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20230810

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20230428

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I