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MX2021013683A - Derivados heterociclicos novedosos utiles como inhibidores de shp2. - Google Patents

Derivados heterociclicos novedosos utiles como inhibidores de shp2.

Info

Publication number
MX2021013683A
MX2021013683A MX2021013683A MX2021013683A MX2021013683A MX 2021013683 A MX2021013683 A MX 2021013683A MX 2021013683 A MX2021013683 A MX 2021013683A MX 2021013683 A MX2021013683 A MX 2021013683A MX 2021013683 A MX2021013683 A MX 2021013683A
Authority
MX
Mexico
Prior art keywords
shp2
derivatives useful
heterocyclic derivatives
novel heterocyclic
inhibitors
Prior art date
Application number
MX2021013683A
Other languages
English (en)
Inventor
Cunbo Ma
Panliang Gao
Xinping Wu
Di Kang
Shaojing Hu
Zilong Xu
Huifeng Han
Original Assignee
Jacobio Pharmaceuticals Co Ltd
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 Jacobio Pharmaceuticals Co Ltd filed Critical Jacobio Pharmaceuticals Co Ltd
Publication of MX2021013683A publication Critical patent/MX2021013683A/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D401/14—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 three or more hetero 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hematology (AREA)

Abstract

Esta invención se refiere a ciertos derivados de pirazina novedosos (Fórmula I) como inhibidores de SHP2 que se muestra como fórmula I, sus síntesis y sus usos para tratar un trastorno mediado por SHP2. De manera más particular, esta invención se dirige a derivados del grupo heterocíclico fusionado útiles como inhibidores de SHP2, métodos para producir estos compuestos y métodos para tratar un trastorno mediado por SHP2. (ver Fórmula).
MX2021013683A 2017-03-23 2019-09-23 Derivados heterociclicos novedosos utiles como inhibidores de shp2. MX2021013683A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IB2017051690 2017-03-23

Publications (1)

Publication Number Publication Date
MX2021013683A true MX2021013683A (es) 2021-12-10

Family

ID=63584301

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MX2019011330A MX387786B (es) 2017-03-23 2018-03-23 Derivados heterocíclicos novedosos útiles como inhibidores de shp2.
MX2021013685A MX2021013685A (es) 2017-03-23 2019-09-23 Derivados heterociclicos novedosos utiles como inhibidores de shp2.
MX2021013683A MX2021013683A (es) 2017-03-23 2019-09-23 Derivados heterociclicos novedosos utiles como inhibidores de shp2.
MX2021013686A MX2021013686A (es) 2017-03-23 2019-09-23 Derivados heterociclicos novedosos utiles como inhibidores de shp2.

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MX2019011330A MX387786B (es) 2017-03-23 2018-03-23 Derivados heterocíclicos novedosos útiles como inhibidores de shp2.
MX2021013685A MX2021013685A (es) 2017-03-23 2019-09-23 Derivados heterociclicos novedosos utiles como inhibidores de shp2.

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US (2) US10988466B2 (es)
EP (1) EP3601239B1 (es)
JP (3) JP6878615B2 (es)
KR (4) KR20210130254A (es)
AU (3) AU2018239542C1 (es)
CA (1) CA3057582C (es)
CL (2) CL2019002698A1 (es)
CO (1) CO2019011678A2 (es)
DK (1) DK3601239T3 (es)
EA (2) EA201992253A1 (es)
ES (1) ES2989888T3 (es)
FI (1) FI3601239T3 (es)
HR (1) HRP20241239T1 (es)
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MA (1) MA49013A (es)
MX (4) MX387786B (es)
NZ (1) NZ758458A (es)
PH (1) PH12019502175A1 (es)
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PT (1) PT3601239T (es)
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SI (1) SI3601239T1 (es)
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TW (1) TWI664175B (es)
WO (1) WO2018172984A1 (es)
ZA (1) ZA201906995B (es)

Families Citing this family (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP7044375B2 (ja) 2016-05-31 2022-03-30 ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム Ｐｔｐｎ１１の複素環式阻害剤
PT3464272T (pt) * 2016-06-07 2022-03-11 Jacobio Pharmaceuticals Co Ltd Novos derivados heterocíclicos úteis como inibidores de shp2
MX383856B (es) 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CA3051206A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
WO2018172984A1 (en) * 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
HUE069643T2 (hu) 2017-03-27 2025-03-28 Hydro Quebec Elektrolitkeverékekben vagy elektródaadalékként való felhasználásra szánt sók
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
WO2019051084A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
TWI879728B (zh) * 2018-03-21 2025-04-11 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
JP7265275B2 (ja) 2018-03-21 2023-04-26 スージョウ プーヘー バイオファーマ カンパニー リミテッド Ｓｈｐ２阻害剤およびその使用
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
US11104675B2 (en) 2018-08-10 2021-08-31 Navire Pharma, Inc. PTPN11 inhibitors
CA3113233A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
WO2020063760A1 (en) * 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
KR20210068472A (ko) * 2018-09-29 2021-06-09 노파르티스 아게 Shp2 활성의 억제를 위한 화합물 및 조성물의 제조
KR102820455B1 (ko) * 2018-09-29 2025-06-16 노파르티스 아게 Shp2 활성 억제용 화합물의 제조 방법
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
TW202028183A (zh) * 2018-10-10 2020-08-01 大陸商江蘇豪森藥業集團有限公司 含氮雜芳類衍生物調節劑、其製備方法和應用
AU2019359885B2 (en) 2018-10-17 2024-01-18 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN111138412B (zh) * 2018-11-06 2023-09-15 上海奕拓医药科技有限责任公司 一种螺芳环化合物及其应用
KR20210089716A (ko) 2018-11-07 2021-07-16 상하이 린진 바이오파마 씨오., 엘티디. 질소 함유 축합 헤테로고리 shp2억제제 화합물, 제조방법 및 용도
KR20210097144A (ko) 2018-11-30 2021-08-06 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피리미딘 및 5-원 질소 헤테로사이클 유도체, 이의 제조 방법, 및 이의 의학적 용도
WO2020156242A1 (zh) * 2019-01-31 2020-08-06 贝达药业股份有限公司 Shp2抑制剂及其应用
CN113365988B (zh) * 2019-01-31 2023-10-03 贝达药业股份有限公司 Shp2抑制剂及其应用
EP3930845A1 (en) 2019-03-01 2022-01-05 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
AU2020232242A1 (en) 2019-03-01 2021-09-09 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
CN111647000B (zh) 2019-03-04 2021-10-12 勤浩医药（苏州）有限公司 吡嗪类衍生物及其在抑制shp2中的应用
AU2020232026A1 (en) 2019-03-07 2021-09-02 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
KR102698608B1 (ko) 2019-04-02 2024-08-27 어레이 바이오파마 인크. 단백질 티로신 포스파타제 억제제
AU2020271838A1 (en) 2019-04-08 2021-08-19 Merck Patent Gmbh Pyrimidinone derivatives as SHP2 antagonists
CN110003049A (zh) * 2019-05-13 2019-07-12 苏州山青竹生物医药有限公司 一种制备4-氰基-1-茚酮的方法
CN114126620B (zh) 2019-05-13 2024-12-31 传达治疗有限公司 Fgfr抑制剂和其使用方法
TWI826690B (zh) 2019-05-23 2023-12-21 美商基利科學股份有限公司 經取代之烯吲哚酮化物及其用途
TW202112761A (zh) 2019-06-14 2021-04-01 中國商北京盛諾基醫藥科技股份有限公司 Shp2磷酸酶變構抑制劑
PH12021553256A1 (en) 2019-06-25 2022-08-08 Gilead Sciences Inc Flt3l-fc fusion proteins and methods of use
EP3991731A4 (en) * 2019-06-28 2022-07-20 Tuojie Biotech (Shanghai) Co., Ltd. FIVE-MEMBERED NITROGEN-CONTAINING HETEROCYCLIC PYRIMIDINE DERIVATIVE, PROCESS FOR ITS PREPARATION AND ITS PHARMACEUTICAL USE
CN111704611B (zh) * 2019-07-25 2022-01-14 上海凌达生物医药有限公司 一类芳基螺环类shp2抑制剂化合物、制备方法和用途
EP3772513A1 (en) 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
CN114450287A (zh) 2019-09-24 2022-05-06 传达治疗有限公司 Shp2磷酸酶抑制剂及其制备和使用方法
CN112574212B (zh) * 2019-09-30 2022-04-19 上海拓界生物医药科技有限公司 一种嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用
PL4045083T3 (pl) 2019-10-18 2024-05-13 Forty Seven, Inc. Terapie skojarzone do leczenia zespołów mielodysplastycznych i ostrej białaczki szpikowej
EP4052040A1 (en) 2019-10-31 2022-09-07 Forty Seven, Inc. Anti-cd47 and anti-cd20 based treatment of blood cancer
CR20220241A (es) 2019-11-04 2022-08-03 Revolution Medicines Inc Inhibidores de ras
CN114867735A (zh) 2019-11-04 2022-08-05 锐新医药公司 Ras抑制剂
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂
BR112022008858A2 (pt) 2019-11-08 2022-09-06 Revolution Medicines Inc Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer
TW202120488A (zh) 2019-11-08 2021-06-01 大陸商南京聖和藥業股份有限公司 作為shp2抑制劑的化合物及其應用
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
SI4081305T1 (sl) 2019-12-24 2025-03-31 Carna Biosciences, Inc. Spojine, ki modulirajo diacilglicerol kinazo
CN113072499B (zh) * 2020-01-03 2024-02-20 南京药石科技股份有限公司 一种4-氧代-8-氮杂螺[4．5]癸-2-烯-8-羧酸叔丁酯（苄酯）的制备方法
WO2021147879A1 (zh) * 2020-01-21 2021-07-29 贝达药业股份有限公司 Shp2抑制剂及其应用
CN115087488A (zh) 2020-02-14 2022-09-20 震动疗法股份有限公司 与ccr8结合的抗体和融合蛋白及其用途
EP4110338A1 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
CN113493440B (zh) * 2020-04-03 2024-08-23 上海翰森生物医药科技有限公司 含氮杂芳类衍生物的盐及其晶型
TW202144334A (zh) * 2020-04-03 2021-12-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜芳類衍生物游離鹼的晶型
BR112022020769A2 (pt) 2020-05-01 2022-12-20 Gilead Sciences Inc Compostos de 2,4-dioxopirimidina de inibição de cd73
WO2021236775A1 (en) * 2020-05-19 2021-11-25 The Regents Of The University Ofmichigan Small molecule degraders of shp2 protein
AU2021293228A1 (en) 2020-06-18 2023-02-09 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
CN116348466B (zh) * 2020-09-23 2025-05-30 上海齐鲁制药研究中心有限公司 吡嗪硫联苯基类化合物及其应用
TW202233625A (zh) 2020-11-18 2022-09-01 美商傳達治療有限公司 Ｆｇｆｒ抑制劑及其製造及使用方法
TW202241885A (zh) 2020-12-22 2022-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Ｓｏｓ１抑制劑及其用途
WO2022156765A1 (zh) * 2021-01-22 2022-07-28 南京明德新药研发有限公司 吡唑并吡嗪联三环类化合物及其应用
CA3206933A1 (en) * 2021-02-05 2022-08-11 Guangxiu Dai Tricyclic compounds and uses thereof
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
JP7599039B2 (ja) * 2021-03-23 2024-12-12 上海海雁医薬科技有限公司 複素環置換ケトン類誘導体、その組成物および医薬における使用
EP4067358A1 (en) 2021-04-02 2022-10-05 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening (s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo[1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
TW202302145A (zh) 2021-04-14 2023-01-16 美商基利科學股份有限公司 ＣＤ４７／ＳＩＲＰα結合及ＮＥＤＤ８活化酶Ｅ１調節次單元之共抑制以用於治療癌症
CA3217920A1 (en) 2021-05-05 2022-11-10 Andreas BUCKL Ras inhibitors for the treatment of cancer
JP2024516037A (ja) 2021-05-05 2024-04-11 フヤバイオ インターナショナル，エルエルシー Ｓｈｐ２阻害剤とｐｄ－１阻害剤とを含む併用療法
CN118234731A (zh) 2021-05-05 2024-06-21 锐新医药公司 Ras抑制剂
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ｒａｓ阻害剤及びその使用
WO2022245671A1 (en) 2021-05-18 2022-11-24 Gilead Sciences, Inc. Methods of using flt3l-fc fusion proteins
JP2024519098A (ja) * 2021-05-21 2024-05-08 石薬集団中奇制薬技術（石家庄）有限公司 スピロ系化合物およびその使用
TW202313041A (zh) 2021-06-09 2023-04-01 瑞士商諾華公司 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合
CN117396478A (zh) 2021-06-23 2024-01-12 吉利德科学公司 二酰基甘油激酶调节化合物
KR20240023629A (ko) 2021-06-23 2024-02-22 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
KR20240023628A (ko) 2021-06-23 2024-02-22 길리애드 사이언시즈, 인코포레이티드 디아실글리세롤 키나제 조절 화합물
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途
US11932634B2 (en) 2021-06-23 2024-03-19 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
US20240383908A1 (en) * 2021-07-07 2024-11-21 Hinova Pharmaceuticals Inc. Synthesis and application of phosphatase degrader
CA3226206A1 (en) 2021-07-09 2023-01-12 Kanaph Therapeutics Inc. Shp2 inhibitor and use thereof
IL309086A (en) 2021-09-01 2024-02-01 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
US20230183216A1 (en) 2021-10-28 2023-06-15 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
CR20240173A (es) 2021-10-29 2024-06-20 Gilead Sciences Inc Compuestos de cd73
CN116063307A (zh) * 2021-10-29 2023-05-05 中国药科大学 Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用
WO2023107954A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Antibodies targeting 5t4 and uses thereof
US20230203202A1 (en) 2021-12-08 2023-06-29 Dragonfly Therapeutics, Inc. Proteins binding nkg2d, cd16 and 5t4
EP4452414A2 (en) 2021-12-22 2024-10-30 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
WO2023122615A1 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
CN116332794B (zh) * 2021-12-24 2024-10-15 上海合全药物研发有限公司 一种芳基腈类化合物的制备方法
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Ｐａｒｐ７抑制劑
CN114524772B (zh) * 2022-02-28 2023-07-11 中国药科大学 一种含杂环串联类化合物及其制备方法与应用
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
HUE069263T2 (hu) 2022-03-17 2025-02-28 Gilead Sciences Inc Ikarosz cink-ujj család degradálói és azok alkalmazása
US20230355796A1 (en) 2022-03-24 2023-11-09 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TWI876305B (zh) 2022-04-05 2025-03-11 美商基利科學股份有限公司 用於治療結腸直腸癌之組合療法
IL316058A (en) 2022-04-21 2024-11-01 Gilead Sciences Inc Compounds modulate KRAS G12D
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
KR20250022133A (ko) 2022-06-10 2025-02-14 레볼루션 메디슨즈, 인크. 거대고리 ras 억제제
IL317958A (en) 2022-07-01 2025-02-01 Gilead Sciences Inc CD73 compounds
WO2024035830A1 (en) 2022-08-11 2024-02-15 Relay Therapeutics, Inc. Solid forms of a cdk inhibitor
WO2024064668A1 (en) 2022-09-21 2024-03-28 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPα DISRUPTION ANTICANCER COMBINATION THERAPY
CN119923402A (zh) * 2022-09-22 2025-05-02 上海海雁医药科技有限公司 杂环取代的甲酮类衍生物的固体形式及其应用
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
WO2024113194A1 (en) * 2022-11-30 2024-06-06 Canwell Biotech Limited Shp2 inhibitors, compositions and methods thereof
CN118206550A (zh) * 2022-12-15 2024-06-18 江苏威凯尔医药科技有限公司 Shp2抑制剂及其应用
CN120225509A (zh) 2022-12-22 2025-06-27 吉利德科学公司 Prmt5抑制剂及其用途
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024215754A1 (en) 2023-04-11 2024-10-17 Gilead Sciences, Inc. Kras modulating compounds
US20240352036A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024220917A1 (en) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025006720A1 (en) 2023-06-30 2025-01-02 Gilead Sciences, Inc. Kras modulating compounds
US20250066328A1 (en) 2023-07-26 2025-02-27 Gilead Sciences, Inc. Parp7 inhibitors
WO2025024811A1 (en) 2023-07-26 2025-01-30 Gilead Sciences, Inc. Parp7 inhibitors
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
US20250101042A1 (en) 2023-09-08 2025-03-27 Gilead Sciences, Inc. Kras g12d modulating compounds
WO2025054530A1 (en) 2023-09-08 2025-03-13 Gilead Sciences, Inc. Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025081291A1 (en) * 2023-10-16 2025-04-24 Canwell Biotech Limited Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof
WO2025096589A1 (en) 2023-11-03 2025-05-08 Gilead Sciences, Inc. Prmt5 inhibitors and uses thereof
US20250230168A1 (en) 2023-12-22 2025-07-17 Gilead Sciences, Inc. Azaspiro wrn inhibitors
WO2025137507A1 (en) 2023-12-22 2025-06-26 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof

Family Cites Families (167)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3377826B2 (ja) 1993-05-06 2003-02-17 ヘキスト・アクチェンゲゼルシャフト 液晶組成物に使用するための新規化合物
WO1997025033A1 (en) 1995-10-31 1997-07-17 Eli Lilly And Company Antithrombotic diamines
EP1154997A4 (en) 1999-01-26 2002-11-04 Dana Farber Cancer Inst Inc PHARMACEUTICALLY ACTIVE COMPOUNDS AND METHODS OF USE
US7375125B2 (en) 1999-08-04 2008-05-20 Ore Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
CN1308310C (zh) 2000-10-20 2007-04-04 卫材R&D管理有限公司 含氮芳环衍生物
MXPA04005561A (es) 2001-12-21 2004-12-06 Bayer Pharmaceuticals Corp Terapias de combinacion anti-angiogenesis que comprenden derivados de piridazina o piridina.
JP4467307B2 (ja) 2002-02-22 2010-05-26 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ５−ｈｔ受容体アンタゴニストとしてのピリジルスルホン誘導体
DE10246657A1 (de) 2002-10-07 2004-04-15 Merck Patent Gmbh Chirales Phenolderivat, dieses enthaltendes Flüssigkristallmedium, Verfahren zur Herstellung eines Flüssigkristallmediums und elektrooptische Flüssigkristallanzeige
KR100866456B1 (ko) 2002-11-18 2008-10-31 케모센트릭스 아릴 술폰아마이드
SE0203712D0 (sv) 2002-12-13 2002-12-13 Astrazeneca Ab Novel compounds
CN102503903A (zh) 2003-02-07 2012-06-20 詹森药业有限公司 抑制hiv的1,2,4-三嗪
EP1594512A4 (en) 2003-02-11 2007-07-11 Kemia Inc COMPOUNDS FOR THE TREATMENT OF VIRUS INFECTIONS
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
WO2004099158A1 (en) 2003-04-30 2004-11-18 Ricerca Biosciences, Llc. Monocyclic diazodioxide based bcl-2 protein antagonists
WO2005004810A2 (en) 2003-07-02 2005-01-20 Merck & Co., Inc. Arylsulfonamide derivatives
CA2531510A1 (en) 2003-07-08 2005-01-20 Astrazeneca Ab Spiro '1-azabicyclo '2.2.2!octan-3,5'-oxazolidin-2'one! derivatives with affinity to the alpha7 nicotinic acetylcholine receptor
CA2540640A1 (en) 2003-09-30 2005-04-14 Amgen Inc. Vanilloid receptor ligands and their use in treatments
GB0325956D0 (en) 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
TW200528459A (en) 2004-01-06 2005-09-01 Achillion Pharmaceuticals Inc Azabenzofuran substituted thioureas; inhibitors of viral replication
WO2005066156A1 (en) 2004-01-12 2005-07-21 Cytopia Research Pty Ltd Selective kinase inhibitors
EP1720545B1 (en) 2004-03-03 2014-10-29 ChemoCentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
JPWO2005090332A1 (ja) 2004-03-23 2008-01-31 萬有製薬株式会社 置換キナゾリン又はピリドピリミジン誘導体
EP1745036A2 (en) 2004-05-03 2007-01-24 Boehringer Ingelheim Pharmaceuticals Inc. Cytokine inhibitors
MXPA06014574A (es) 2004-06-24 2007-03-12 Incyte Corp Piperidinas n-sustituidas y su uso como farmaceuticos.
US20070043057A1 (en) 2005-02-09 2007-02-22 Threshold Pharmaceuticals, Inc. Lonidamine analogs
BRPI0517272A (pt) 2004-10-29 2008-10-07 Tibotec Pharm Ltd derivados de pirimidina bicìclicos de inibição de hiv
GB0428082D0 (en) 2004-12-22 2005-01-26 Welcome Trust The Ltd Therapeutic compounds
CN101087767A (zh) 2004-12-23 2007-12-12 马林克罗特公司 荧光吡嗪衍生物及其在评估肾功能中的使用方法
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
TWI375521B (en) 2005-02-04 2012-11-01 Senomyx Inc Compounds comprising linked heteroaryl moieties and their use as novel umami flavor modifiers, tastants and taste enhancers for comestible compositions
JP2008530171A (ja) 2005-02-16 2008-08-07 ノイロサーチ アクティーゼルスカブ 新規なジアザ二環系アリール誘導体及びそれらの医療上の使用
WO2007046867A2 (en) 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
BRPI0610580B8 (pt) 2005-05-30 2021-05-25 Banyu Pharma Co Ltd composto derivado de piperidina
JP2007013804A (ja) 2005-07-01 2007-01-18 Mitsubishi Electric Corp 属性指定通信方法および通信装置
PL1940821T3 (pl) 2005-10-19 2013-08-30 Gruenenthal Gmbh Nowe ligandy receptora waniloidowego i ich zastosowanie do wytwarzania leków
WO2007057742A2 (en) 2005-11-18 2007-05-24 Pfizer Products Inc. Novel piperazinone derivatives
WO2007057775A1 (en) * 2005-11-21 2007-05-24 Pfizer Limited Spiropiperidine derivatives
CA2636314A1 (en) 2005-11-29 2007-06-07 Toray Industries, Inc. Arylmethylene urea derivative and use thereof
US20080269251A1 (en) 2005-12-21 2008-10-30 Jose Ignacio Andre-Gil Substituted Pyrazinone Derivatives as Alpha2C-Adrenoreceptor Antagonists
CA2637674A1 (en) 2006-01-19 2007-07-26 Abbott Laboratories 2-imino-benzimidazoles
BRPI0707338A2 (pt) 2006-01-30 2011-05-03 Transtech Pharma Inc derivados de imidazol, composições, e métodos substituìdos de uso como inibidores de ptpase
CA2645137A1 (en) 2006-03-07 2007-09-13 James F. Blake Heterobicyclic pyrazole compounds and methods of use
CN101426788A (zh) 2006-04-20 2009-05-06 詹森药业有限公司 用作药物的取代吡嗪酮衍生物
RU2008150485A (ru) 2006-05-22 2010-06-27 Янссен Фармацевтика Н.В. (Be) Замещенные производные пиразинона для применения в качестве лекарственного средства
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
PE20081370A1 (es) 2006-09-11 2008-11-28 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
BRPI0717822A2 (pt) 2006-10-04 2013-11-12 Hoffmann La Roche Composto, processo de fabricação de composto da fórmula i, composição farmacêutica, método de tratamento e/ou profilaxia de doenças que são associadas à modulação de receptores de cb2 e uso de composto.
DE102007018150A1 (de) 2007-04-16 2008-10-23 Grünenthal GmbH VR1-Rezeptor-Liganden und µ-Opioid-Rezeptor-Liganden zur Behandlung von Schmerz
CA2676920A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
US8338437B2 (en) 2007-02-28 2012-12-25 Methylgene Inc. Amines as small molecule inhibitors
CN101687040A (zh) 2007-03-01 2010-03-31 马林克罗特公司 整合光活性的小分子及其用途
AU2008221263B2 (en) 2007-03-01 2012-02-23 Novartis Ag Pim kinase inhibitors and methods of their use
WO2008112674A1 (en) 2007-03-12 2008-09-18 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
US20110130406A1 (en) 2007-09-06 2011-06-02 Array Biopharma Inc. Pyrazolo-pyridines as tyrosine kinase inhibitors
WO2009036066A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Vegfr inhibitors containing a zinc binding moiety
WO2009038974A1 (en) 2007-09-20 2009-03-26 Irm Llc Compounds and compositions as modulators of gpr119 activity
NZ585347A (en) 2007-10-18 2011-09-30 Boehringer Ingelheim Int Cgrp antagonists
AU2008317351A1 (en) 2007-10-24 2009-04-30 Merck Sharp & Dohme Corp. Pyrazinyl amide T-type calcium channel antagonists
JP2011513323A (ja) 2008-02-29 2011-04-28 シェーリング コーポレイション アルツハイマー病の治療のためのγ−セクレターゼモジュレーター
CA2719538C (en) 2008-04-07 2014-03-18 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
CL2009001064A1 (es) 2008-05-07 2009-10-09 Galapagos Nv Compuestos derivados de imidazol-pirazina o triazol-pirazina fusionados, inhibidores de mapkapk5; composicion farmaceutica que comprende dichos compuestos; y uso para preparar un medicamento destinado al tratamiento de inflamacion, especialmente en la artritis reumatoide.
EP2328586A2 (en) 2008-05-20 2011-06-08 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
KR20110026481A (ko) 2008-06-20 2011-03-15 메타볼렉스, 인코포레이티드 아릴 ｇｐｒ１１９ 작동약 및 이의 용도
GEP20135785B (en) 2008-08-22 2013-03-11 Novartis Ag Pyrrolopyrimidine compounds as cdk inhibitors
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
MX2011006575A (es) 2008-12-17 2011-10-06 Amgen Inc Compuestos de aminopiridina y carboxipiridina como inhibidores de la fosfodiesterasa 10.
JP5599815B2 (ja) 2008-12-19 2014-10-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規化合物
SG172383A1 (en) 2008-12-25 2011-07-28 Taisho Pharmaceutical Co Ltd Isoquinoline derivative
WO2010085700A2 (en) 2009-01-22 2010-07-29 Unigene Laboratories Inc. Treatment for obesity
WO2010086613A1 (en) 2009-01-30 2010-08-05 Betagenon Ab Compounds useful as inhibitors as ampk
EP2405917B1 (en) 2009-03-13 2014-04-23 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
JP5982281B2 (ja) 2009-07-08 2016-08-31 バルティック バイオ アーベー 医薬として有用な化合物
CA2771190C (en) 2009-08-17 2020-01-21 Memorial Sloan-Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
EP2473500A2 (en) 2009-09-01 2012-07-11 Pfizer Inc. Benzimidazole derivatives
WO2011044001A1 (en) 2009-10-09 2011-04-14 Irm Llc Compounds and compositions as modulators of gpr119 activity
US8759377B2 (en) 2009-11-23 2014-06-24 Vanderbilt University Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
EP2513057B1 (de) 2009-12-14 2013-09-04 Merck Patent GmbH Inhibitoren der sphingosinkinase
CN104341401B (zh) 2009-12-18 2017-02-15 北京凯因科技股份有限公司 C型肝炎病毒复制的新型抑制剂
JP5894540B2 (ja) 2010-02-18 2016-03-30 ブイティーブイ・セラピューティクス・エルエルシー フェニル−ヘテロアリール誘導体とその使用の方法
CA2800327A1 (en) 2010-04-13 2011-10-20 Novartis Ag Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase 6 (cdk4/6) inhibitor and an mtor inhibitor for treating cancer
MX344142B (es) 2010-04-29 2016-12-07 The Univ Of Edinburgh (8-aza-biciclico[3.2.1]oct-8-il)-[5-(1h-pirazol-4-il)-tiofen-3-il ]-metanonas 3, 3-disubstituidas como inhibidores de 1(beta)-hsd1.
WO2011146401A1 (en) 2010-05-17 2011-11-24 Intermune, Inc. Novel inhibitors of hepatitis c virus replication
CN103038229B (zh) 2010-05-26 2016-05-11 桑诺维恩药品公司 杂芳基化合物及其使用方法
JP5889895B2 (ja) 2010-07-29 2016-03-22 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 Ａｍｐｋ活性化複素環化合物およびその使用方法
JP2013230986A (ja) 2010-08-25 2013-11-14 Kyorin Pharmaceutical Co Ltd 新規ヒダントイン誘導体及びそれらを有効成分とする医薬
CN102432598A (zh) 2010-09-29 2012-05-02 江苏恒瑞医药股份有限公司 三环化合物、其制备方法及其在医药上的应用
GB201020161D0 (en) 2010-11-26 2011-01-12 Almac Discovery Ltd Pharmaceutical compounds
WO2012080727A2 (en) 2010-12-14 2012-06-21 Electrophoretics Limited Casein kinase 1delta (ck1delta) inhibitors
WO2012088438A1 (en) 2010-12-22 2012-06-28 Eutropics Pharmaceuticals, Inc. Compositions and methods useful for treating diseases
US20120184572A1 (en) 2011-01-13 2012-07-19 Metabolex, Inc. Aryl gpr119 agonists and uses thereof
CN103619854A (zh) 2011-04-29 2014-03-05 西奈山伊坎医学院 激酶抑制剂
WO2012158784A2 (en) 2011-05-16 2012-11-22 Theodore Mark Kamenecka Modulators of the nuclear hormone receptor ror
EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
WO2013039851A1 (en) 2011-09-12 2013-03-21 Mallinckrodt Llc Optical agents for imaging and visualization of matrix metalloproteinase enzymes
MX365923B (es) 2011-12-12 2019-06-20 Celgene Int Ii Sarl Derivados de acido carboxilico que comprenden cuatro ciclos, que actuan como moduladores del receptor del peptido 1 similar al glucagon (glp-1) para terapia de enfermedades como la diabetes.
US10934487B2 (en) 2012-02-22 2021-03-02 Merck Patent Gmbh Liquid crystalline medium
GB201204985D0 (en) 2012-03-21 2012-05-02 Genentech Inc Compounds
US8889730B2 (en) 2012-04-10 2014-11-18 Pfizer Inc. Indole and indazole compounds that activate AMPK
ES2743402T3 (es) 2012-04-25 2020-02-19 Raqualia Pharma Inc Derivados de amidas como bloqueadores TTX-S
BR112014027133A2 (pt) 2012-05-09 2017-06-27 Basf Se compostos, composição agrícola ou veterinária, método para o controle das pragas de invertebrados, material de propagação dos vegetais e método para o tratamento ou proteção de um animal.
EP2867232B1 (en) 2012-06-27 2018-08-08 F.Hoffmann-La Roche Ag 5-azaindazole compounds and methods of use
WO2014000178A1 (en) 2012-06-27 2014-01-03 Merck Sharp & Dohme Corp. Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug
JP6254163B2 (ja) 2012-08-16 2017-12-27 ザ スクリプス リサーチ インスティテュート 新規カッパオピオイドリガンド
JOP20130273B1 (ar) 2012-09-11 2021-08-17 Genzyme Corp مثبطات انزيم (سينثاز) غلوكوسيل سيراميد
CA2902252A1 (en) 2013-03-15 2014-09-18 Monique Bodil Van Niel Aryl sulfamide and sulfamate derivatives as rorc modulators
EP2968290B1 (en) 2013-03-15 2019-09-25 G1 Therapeutics, Inc. Transient protection of normal cells during chemotherapy
WO2014184074A1 (en) 2013-05-15 2014-11-20 Basf Se Substituted n-(tetrazol-5-yl)- and n-(triazol-5-yl)hetarylcarboxamide compounds and their use as herbicides
WO2014184014A1 (en) 2013-05-15 2014-11-20 Basf Se N-(1,2,5-oxadiazol-3-yl)carboxamide compounds and their use as herbicides
GB201309508D0 (en) 2013-05-28 2013-07-10 Redx Pharma Ltd Compounds
KR102271179B1 (ko) 2013-06-11 2021-07-01 셀진 인터내셔널 Ii 에스에이알엘 신규의 glp-1 수용체 조절제
WO2015003094A2 (en) 2013-07-03 2015-01-08 Indiana University Research & Technology Corporation Shp2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using shp2 inhibitors
JPWO2015016206A1 (ja) 2013-07-30 2017-03-02 武田薬品工業株式会社 複素環化合物
US9751881B2 (en) 2013-07-31 2017-09-05 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2015048547A2 (en) 2013-09-26 2015-04-02 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
US10463662B2 (en) 2013-10-08 2019-11-05 Qing-Bin Lu Non-platinum-based anti-cancer compounds for use in targeted chemotherapy
AR098136A1 (es) 2013-10-21 2016-05-04 Merck Patent Gmbh Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
KR20150070027A (ko) 2013-12-16 2015-06-24 메르크 파텐트 게엠베하 액정 매질
EP3083610A1 (de) 2013-12-19 2016-10-26 Bayer Pharma Aktiengesellschaft Substituierte bipiperidinyl-derivate als adrenrezeptor alpha 2c antagonisten
US9815813B2 (en) 2014-01-17 2017-11-14 Novartis Ag 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EP3094627B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
EA033861B1 (ru) 2014-02-14 2019-12-03 Такеда Фармасьютикал Компани Лимитед Пиразины в качестве модуляторов gpr6
US10000469B2 (en) 2014-03-25 2018-06-19 Duke University Heat shock protein 70 (hsp-70) receptor ligands
WO2015155042A1 (en) 2014-04-07 2015-10-15 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido[4,5-e]indolizines
CA2949229A1 (en) 2014-05-23 2015-11-26 F. Hoffmann-La Roche Ag Benzene sulfonamide derivatives and their use as rorc modulators
WO2016015605A1 (en) 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. Compounds as cdk small-molecule inhibitors and uses thereof
WO2016022644A1 (en) 2014-08-06 2016-02-11 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
WO2016022645A1 (en) 2014-08-06 2016-02-11 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
EP2985334B1 (en) 2014-08-15 2018-06-20 Merck Patent GmbH Liquid-crystalline medium
US9866893B2 (en) 2014-08-19 2018-01-09 Comcast Cable Communications, Llc Methods and systems for accessing content
WO2016040449A1 (en) 2014-09-10 2016-03-17 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
TWI744225B (zh) 2015-02-27 2021-11-01 美商林伯士拉克許米公司 酪胺酸蛋白質激酶２（ｔｙｋ２）抑制劑及其用途
JP6726677B2 (ja) 2015-03-11 2020-07-22 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. 抗がん剤としての置換２−ｈ−ピラゾール誘導体
JP2018509448A (ja) 2015-03-25 2018-04-05 ノバルティス アーゲー 組合せ医薬
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制ｍｅｎｉｎ及ｍｌｌ蛋白之交互作用的方法及組合物
HK1246593A1 (zh) 2015-06-04 2018-09-14 Kura Oncology, Inc. 用於抑制menin蛋白與mll蛋白的相互作用的方法及組合物
CN107922388B (zh) 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
CN107787323B (zh) 2015-06-19 2020-09-01 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
RU2604047C1 (ru) 2015-07-10 2016-12-10 Фортис Аксис, Закрытое Акционерное Общество Массажёр для воздействия на мышцы спины трех отделов позвоночника
BR112018005208B1 (pt) 2015-09-17 2023-12-12 Marvin J. Miller Compostos heterocíclicos que contêm benzilamina e composições úteis contra infecção micobacteriana
CN108779117B (zh) 2015-12-27 2021-08-31 重庆复创医药研究有限公司 一类激酶抑制剂
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
US10570141B2 (en) 2016-03-25 2020-02-25 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Substituted pyrrolopyrimidine CDK inhibitor, pharmaceutical composition containing same and use thereof
CN107286150B (zh) 2016-04-11 2020-07-07 中国科学院上海有机化学研究所 N-杂环类化合物、其中间体、制备方法、药物组合物和应用
JP7044375B2 (ja) 2016-05-31 2022-03-30 ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム Ｐｔｐｎ１１の複素環式阻害剤
PT3464272T (pt) 2016-06-07 2022-03-11 Jacobio Pharmaceuticals Co Ltd Novos derivados heterocíclicos úteis como inibidores de shp2
MX383856B (es) 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
EP3290412A1 (en) 2016-08-31 2018-03-07 Università degli Studi di Siena Hiv-1 nucleocapsid inhibitors
US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
WO2018089433A1 (en) 2016-11-08 2018-05-17 Navitor Pharmaceuticals, Inc. PHENYL mTORC INHIBITORS AND USES THEREOF
EP3565810A1 (en) 2017-01-03 2019-11-13 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
JP7175026B2 (ja) 2017-04-01 2022-11-18 晟科薬業（江蘇）有限公司 プロテインキナーゼ阻害剤としての１ｈ－イミダゾ［４，５－ｈ］キナゾリン系化合物
KR20200027992A (ko) 2017-07-12 2020-03-13 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 길항제
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
KR102776114B1 (ko) 2017-10-20 2025-03-07 반더빌트유니버시티 무스카린성 아세틸콜린 수용체 m4의 길항제
AU2018392805A1 (en) 2017-12-22 2020-05-07 Dana-Farber Cancer Institute, Inc. NEK inhibitors and methods of use
BR112020015396A2 (pt) 2018-01-29 2020-12-08 Merck Patent Gmbh Inididores de gcn2 e usos dos mesmos
TWI816742B (zh) 2018-01-29 2023-10-01 美商維泰克斯製藥公司 Gcn2抑制劑及其用途
WO2019152454A1 (en) 2018-01-30 2019-08-08 Research Development Foundation Shp2 inhibitors and methods of use thereof
JP7399109B2 (ja) 2018-02-08 2023-12-15 ウエヌイグレックオ・ファーマ 縮合チオフェン誘導体及びそれらの使用
EP3759111A1 (en) 2018-03-02 2021-01-06 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
EP3768272A4 (en) 2018-03-21 2021-08-11 Xibin Liao JAK INHIBITORS

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