EA201992253A1 - Новые гетероциклические производные, применимые в качестве ингибиторов shp2 - Google Patents

Новые гетероциклические производные, применимые в качестве ингибиторов shp2

Info

Publication number
EA201992253A1
EA201992253A1 EA201992253A EA201992253A EA201992253A1 EA 201992253 A1 EA201992253 A1 EA 201992253A1 EA 201992253 A EA201992253 A EA 201992253A EA 201992253 A EA201992253 A EA 201992253A EA 201992253 A1 EA201992253 A1 EA 201992253A1
Authority
EA
Eurasian Patent Office
Prior art keywords
shp2
shp2 inhibitors
heterocyclic derivatives
new heterocyclic
derivatives applicable
Prior art date
Application number
EA201992253A
Other languages
English (en)
Inventor
Цуньбо МА
Паньлян Гао
Шаоцзин Ху
Цзылун Сюй
Хуэйфэн Хань
Синьпин У
Ди Кан
Original Assignee
Джакобио Фармасьютикалс Ко., Лтд.
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 Джакобио Фармасьютикалс Ко., Лтд. filed Critical Джакобио Фармасьютикалс Ко., Лтд.
Publication of EA201992253A1 publication Critical patent/EA201992253A1/ru

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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 System
    • 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

Abstract

Настоящее изобретение относится к определенным новым производным пиразина (формула I) в качестве ингибиторов SHP2, которые представлены формулой I, к их синтезу и их применению для лечения SHP2-опосредованного нарушения. Более конкретно, настоящее изобретение направлено на производные в виде конденсированных гетероциклических групп, применимые в качестве ингибиторов SHP2, на способы получения таких соединений и способы лечения SHP2-опосредованного нарушения.
EA201992253A 2017-03-23 2018-03-23 Новые гетероциклические производные, применимые в качестве ингибиторов shp2 EA201992253A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IB2017051690 2017-03-23
PCT/IB2018/051973 WO2018172984A1 (en) 2017-03-23 2018-03-23 Novel heterocyclic derivatives useful as shp2 inhibitors

Publications (1)

Publication Number Publication Date
EA201992253A1 true EA201992253A1 (ru) 2020-03-31

Family

ID=63584301

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201992253A EA201992253A1 (ru) 2017-03-23 2018-03-23 Новые гетероциклические производные, применимые в качестве ингибиторов shp2
EA202190196A EA202190196A1 (ru) 2017-03-23 2018-03-23 Новые гетероциклические производные, применимые в качестве ингибиторов shp2

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA202190196A EA202190196A1 (ru) 2017-03-23 2018-03-23 Новые гетероциклические производные, применимые в качестве ингибиторов shp2

Country Status (16)

Country Link
US (1) US10988466B2 (ru)
EP (1) EP3601239A4 (ru)
JP (3) JP6878615B2 (ru)
KR (4) KR20240026521A (ru)
AU (3) AU2018239542C1 (ru)
CA (1) CA3057582C (ru)
CL (2) CL2019002698A1 (ru)
CO (1) CO2019011678A2 (ru)
EA (2) EA201992253A1 (ru)
MA (1) MA49013A (ru)
MX (4) MX2019011330A (ru)
NZ (1) NZ758458A (ru)
PH (1) PH12019502175A1 (ru)
SG (1) SG11201908820VA (ru)
TW (1) TWI664175B (ru)
WO (1) WO2018172984A1 (ru)

Families Citing this family (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10280171B2 (en) 2016-05-31 2019-05-07 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
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
EP4108659A1 (en) * 2016-06-07 2022-12-28 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
EA036446B1 (ru) 2016-06-14 2020-11-11 Новартис Аг Соединения и композиции для подавления активности shp2
CN116478132A (zh) 2016-07-12 2023-07-25 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
TW201819386A (zh) 2016-10-24 2018-06-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
MX2019008696A (es) 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
AU2018239542C1 (en) 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
US11591336B2 (en) 2017-05-26 2023-02-28 D. E. Shaw Research, Llc Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
US11701354B2 (en) 2017-09-29 2023-07-18 D. E. Shaw Research, Llc Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors
EP3694848A1 (en) 2017-10-12 2020-08-19 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
EP3724189B1 (en) 2017-12-15 2023-10-04 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
US10561655B2 (en) 2018-03-21 2020-02-18 Synblia Therapeutics, Inc. SHP2 inhibitors and uses thereof
EP3768668A1 (en) 2018-03-21 2021-01-27 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
BR112020022224A2 (pt) 2018-05-02 2021-06-08 Navire Pharma, Inc. inibidores heterocíclicos substituídos de ptpn11
SG11202100199UA (en) 2018-08-10 2021-02-25 Navire Pharma Inc 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer
US11459340B2 (en) 2018-09-18 2022-10-04 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as Src homology-2 phosphatase inhibitors
CN112839935A (zh) * 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
EP4282416A3 (en) * 2018-09-29 2024-03-06 Novartis AG Process of manufacture of a compound for inhibiting the activity of shp2
JP7386855B2 (ja) 2018-09-29 2023-11-27 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための化合物及び組成物の製造
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine 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
PE20211465A1 (es) 2018-10-17 2021-08-05 Array Biopharma Inc Inhibidores de la proteina tirosina fosfatasa
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
US20220127271A1 (en) 2018-11-07 2022-04-28 Shanghai Ringene Biopharma Co., Ltd. Nitrogen-containing fused heterocyclic shp2 inhibitor compound, preparation method, and use
TW202039498A (zh) 2018-11-30 2020-11-01 大陸商上海拓界生物醫藥科技有限公司 嘧啶並五員氮雜環類衍生物、其製備方法及其在醫藥上的應用
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
WO2020156243A1 (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
SG11202109036WA (en) 2019-03-01 2021-09-29 Revolution Medicines Inc Bicyclic heteroaryl compounds and uses thereof
MX2021010323A (es) 2019-03-01 2021-12-10 Revolution Medicines Inc Compuestos bicíclicos de heterociclilo y usos de este.
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
CN113795483A (zh) 2019-03-07 2021-12-14 默克专利有限公司 作为shp2拮抗剂的甲酰胺-嘧啶衍生物
CA3135555C (en) * 2019-04-02 2023-09-19 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN113646049A (zh) 2019-04-08 2021-11-12 默克专利有限公司 作为shp2拮抗剂的嘧啶酮衍生物
KR20220007889A (ko) 2019-05-13 2022-01-19 릴레이 테라퓨틱스, 인크. Fgfr 저해제 및 이의 사용 방법
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
EP3972695A1 (en) 2019-05-23 2022-03-30 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
EP3984999A4 (en) * 2019-06-14 2023-11-22 Beijing Shenogen Pharma Group Ltd. ALLOSTERIC INHIBITOR OF SHP2 PHOSPHATASE
CA3142513A1 (en) 2019-06-25 2020-12-30 Gilead Sciences, Inc. Flt3l-fc fusion proteins and methods of use
AU2020306124A1 (en) 2019-06-28 2022-02-03 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine five-membered nitrogen heterocyclic derivative, preparation method thereof and pharmaceutical use thereof
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
CA3154862A1 (en) * 2019-09-24 2021-04-01 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
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
AU2020365113A1 (en) 2019-10-18 2022-04-07 Forty Seven, Inc. Combination therapies for treating myelodysplastic syndromes and acute myeloid leukemia
MX2022005123A (es) 2019-10-31 2022-05-30 Forty Seven Inc Tratamiento basado en anti-cd47 y anti-cd20 para cancer hematologico.
CN115873020A (zh) 2019-11-04 2023-03-31 锐新医药公司 Ras抑制剂
CA3160142A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021088945A1 (zh) 2019-11-08 2021-05-14 南京圣和药业股份有限公司 作为shp2抑制剂的化合物及其应用
MX2022005525A (es) 2019-11-08 2022-06-08 Revolution Medicines Inc Compuestos de heteroarilo bicíclicos y usos de estos.
TWI778443B (zh) 2019-11-12 2022-09-21 美商基利科學股份有限公司 Mcl1抑制劑
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CA3165735A1 (en) 2019-12-24 2021-07-01 Carna Biosciences, Inc. Diacylglycerol kinase modulating compounds
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
BR112022014623A2 (pt) 2020-02-14 2022-09-13 Jounce Therapeutics Inc Anticorpos e proteínas de fusão que se ligam a ccr8 e usos dos mesmos
EP4110338A1 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
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
CN113493440A (zh) * 2020-04-03 2021-10-12 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
US20230039553A1 (en) 2020-05-01 2023-02-09 Gilead Sciences, Inc. Cd73 compounds
WO2021236775A1 (en) * 2020-05-19 2021-11-25 The Regents Of The University Ofmichigan Small molecule degraders of shp2 protein
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
EP4208261A1 (en) 2020-09-03 2023-07-12 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
CA3203111A1 (en) 2020-12-22 2022-06-30 Kailiang Wang Sos1 inhibitors and uses thereof
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
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
JP2024509243A (ja) * 2021-03-23 2024-02-29 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
KR20240004960A (ko) 2021-05-05 2024-01-11 레볼루션 메디슨즈, 인크. Ras 억제제
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
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
TW202313094A (zh) 2021-05-18 2023-04-01 美商基利科學股份有限公司 使用ＦＬＴ３Ｌ—Ｆｃ融合蛋白之方法
CN115368373A (zh) 2021-05-21 2022-11-22 石药集团中奇制药技术（石家庄）有限公司 螺环类化合物及其用途
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
US11976072B2 (en) 2021-06-23 2024-05-07 Gilead Sciences, Inc. Diacylglycerol kinase modulating compounds
US11926628B2 (en) 2021-06-23 2024-03-12 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
AU2022298639A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
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
CA3220923A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023280237A1 (zh) * 2021-07-07 2023-01-12 海创药业股份有限公司 一种磷酸酶降解剂的合成和应用
AU2022309195A1 (en) * 2021-07-09 2024-01-25 Kanaph Therapeutics Inc. Shp2 inhibitor and use thereof
CA3224341A1 (en) 2021-09-01 2023-03-09 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
WO2023076983A1 (en) 2021-10-28 2023-05-04 Gilead Sciences, Inc. Pyridizin-3(2h)-one derivatives
AU2022376954A1 (en) 2021-10-29 2024-05-02 Gilead Sciences, Inc. Cd73 compounds
WO2023107956A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Proteins binding nkg2d, cd16 and 5t4
WO2023107954A1 (en) 2021-12-08 2023-06-15 Dragonfly Therapeutics, Inc. Antibodies targeting 5t4 and uses thereof
US20230242508A1 (en) 2021-12-22 2023-08-03 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
WO2023122581A2 (en) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Ikaros zinc finger family degraders and uses thereof
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
TW202346277A (zh) 2022-03-17 2023-12-01 美商基利科學股份有限公司 Ｉｋａｒｏｓ鋅指家族降解劑及其用途
US20230355796A1 (en) 2022-03-24 2023-11-09 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
TW202345901A (zh) 2022-04-05 2023-12-01 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
TW202400138A (zh) 2022-04-21 2024-01-01 美商基利科學股份有限公司 Ｋｒａｓ ｇ１２ｄ調節化合物
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
US20240116928A1 (en) 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
WO2024035830A1 (en) 2022-08-11 2024-02-15 Relay Therapeutics, Inc. Solid forms of a cdk inhibitor
US20240091351A1 (en) 2022-09-21 2024-03-21 Gilead Sciences, Inc. FOCAL IONIZING RADIATION AND CD47/SIRPa DISRUPTION ANTICANCER COMBINATION THERAPY
WO2024061298A1 (zh) * 2022-09-22 2024-03-28 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

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
JP2002500618A (ja) 1995-10-31 2002-01-08 イーライ・リリー・アンド・カンパニー 抗血栓性ジアミン
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
EP1415987B1 (en) 2000-10-20 2007-02-28 Eisai R&D Management Co., Ltd. Nitrogenous aromatic ring compounds as anti cancer agents
US20050019424A1 (en) 2001-12-21 2005-01-27 Adams Paul E. Anti-angiogenesis combination therapies comprising pyridazine or pyridine derivatives
US6855709B2 (en) 2002-02-22 2005-02-15 Pharmacia & Upjohn Company Pyridyl sulfone derivatives
DE10246657A1 (de) 2002-10-07 2004-04-15 Merck Patent Gmbh Chirales Phenolderivat, dieses enthaltendes Flüssigkristallmedium, Verfahren zur Herstellung eines Flüssigkristallmediums und elektrooptische Flüssigkristallanzeige
EP2256116A3 (en) 2002-11-18 2011-11-16 ChemoCentryx, Inc. Aryl sulfonamides
SE0203712D0 (sv) 2002-12-13 2002-12-13 Astrazeneca Ab Novel compounds
WO2004074266A1 (en) 2003-02-07 2004-09-02 Janssen Pharmaceutica N.V. Hiv inhibiting 1,2,4-triazines
CA2515544A1 (en) 2003-02-11 2004-08-26 Kemia Inc. Compounds for the treatment of viral infection
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US20040242886A1 (en) 2003-04-30 2004-12-02 Sandeep Gupta Monocyclic diazodioxide based Bcl-2 protein antagonists related applications
US7393873B2 (en) 2003-07-02 2008-07-01 Merck & Co., Inc. Arylsulfonamide derivatives
BRPI0412382A (pt) 2003-07-08 2006-09-19 Astrazeneca Ab composto , método para a verificação de novos compostos medicinais que se ligam a e modulam a atividade, por agonismo , agonismo parcial, ou antagonismo, do receptor de acetilcolina nicotìnico alfa7, método de tratamento ou profilaxia de uma doença ou condição humana, método para tratamento de jetlag, induzindo interrupção de fumar, vìcio em nicotina, abstinência, dor, e para colite ulcerativa, composição farmacêutica, e, método de tratamento ou prevenção de uma condição ou distúrbio que surge da disfunção de neurotransmissão do receptor de acetilcolina nicotìnico em um mamìfero, e, uso de um composto
AU2004278382B2 (en) 2003-09-30 2008-09-18 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
EP1704145B1 (en) 2004-01-12 2012-06-13 YM BioSciences Australia Pty Ltd Selective kinase inhibitors
JP4845873B2 (ja) 2004-03-03 2011-12-28 ケモセントリックス インコーポレーティッド 二環式および架橋した窒素複素環
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
CA2560286A1 (en) 2004-03-23 2005-09-29 Banyu Pharmaceutical Co., Ltd. Substituted quinazoline or pyridopyrimidine derivative
JP4865702B2 (ja) 2004-05-03 2012-02-01 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害剤
BRPI0512535A (pt) 2004-06-24 2008-03-25 Incyte Corp compostos de piperidinas n-substituìdas, suas composições e métodos de modulações
US20070043057A1 (en) 2005-02-09 2007-02-22 Threshold Pharmaceuticals, Inc. Lonidamine analogs
CA2577588C (en) 2004-10-29 2013-09-10 Tibotec Pharmaceuticals Ltd. Hiv inhibiting bicyclic pyrimidine derivatives
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
CA2597134C (en) 2005-02-04 2015-05-26 Senomyx, Inc. Compounds comprising linked heteroaryl moieties and their use as novel umami flavor modifiers, tastants and taste enhancers for comestible compositions
ATE481407T1 (de) 2005-02-16 2010-10-15 Neurosearch As Neue diazabicyclische arylderivate und medizinische verwendung dafür
WO2007046867A2 (en) 2005-05-19 2007-04-26 Xenon Pharmaceuticals Inc. Piperidine derivatives and their uses as therapeutic agents
ES2574014T3 (es) 2005-05-30 2016-06-14 Msd K.K. Derivado de piperidina novedoso
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
AU2006303437B2 (en) 2005-10-19 2012-06-28 Grunenthal Gmbh Novel vanilloid receptor ligands and their use for producing medicaments
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
EP1970375A4 (en) 2005-11-29 2010-06-02 Toray Industries ARYLMETHYLENE UREE DERIVATIVE AND USE THEREOF
CN101346368A (zh) 2005-12-21 2009-01-14 詹森药业有限公司 作为α2C－肾上腺素受体拮抗剂的取代的吡嗪酮衍生物
EP1983992A4 (en) 2006-01-19 2010-08-18 Abbott Lab 2-IMINO-BENZIMIDAZOLES
CN101374835B (zh) 2006-01-30 2012-04-25 转化技术制药公司 作为PTPase抑制剂的取代的咪唑衍生物、组合物和使用方法
EP2001880A2 (en) 2006-03-07 2008-12-17 Array Biopharma, Inc. 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
CA2649707A1 (en) 2006-05-22 2007-11-29 Janssen Pharmaceutica N.V. Substituted pyrazinone derivatives for use as a medicine
AR063707A1 (es) 2006-09-11 2009-02-11 Cgi Pharmaceuticals Inc Determinadas amidas sustituidas, el uso de las mismas para el tratamiento de enfermedades mediadas por la inhibicion de la actividad de btk y composiciones farmacéuticas que las comprenden.
US7838523B2 (en) 2006-09-11 2010-11-23 Cgi Pharmaceuticals, Inc. Certain substituted amides, method of making, and method of use thereof
DE602007006531D1 (de) 2006-10-04 2010-06-24 Hoffmann La Roche Pyrazin-2-carboxamid-derivate als cb2-rezeptormodulatoren
DE102007018150A1 (de) 2007-04-16 2008-10-23 Grünenthal GmbH VR1-Rezeptor-Liganden und µ-Opioid-Rezeptor-Liganden zur Behandlung von Schmerz
WO2008100412A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
WO2008104077A1 (en) 2007-02-28 2008-09-04 Methylgene Inc. Small molecule inhibitors of protein arginine methyltransferases (prmts)
EP2131861A2 (en) 2007-03-01 2009-12-16 Mallinckrodt Inc. Integrated photoactive small molecules and uses thereof
MX2009009304A (es) 2007-03-01 2009-11-18 Novartis Ag Inhibidores de cinasa pim y metodos para su uso.
WO2008112674A1 (en) 2007-03-12 2008-09-18 Irm Llc Compounds and compositions as inhibitors of cannabinoid receptor 1 activity
CN101918403A (zh) 2007-09-06 2010-12-15 阵列生物制药公司 作为酪氨酸激酶抑制剂的吡唑并吡啶类化合物
WO2009036066A1 (en) 2007-09-10 2009-03-19 Curis, Inc. Vegfr inhibitors containing a zinc binding moiety
BRPI0817211A2 (pt) 2007-09-20 2017-05-16 Irm Llc composto composições como moduladores da atividade de gpr119
BRPI0817835A2 (pt) 2007-10-18 2015-03-31 Boehringer Ingelheim Int Antagonistas cgrp
CA2703471A1 (en) 2007-10-24 2009-04-30 Merck Sharp & Dohme Corp. Pyrazinyl amide t-type calcium channel antagonists
CA2716747A1 (en) 2008-02-29 2009-09-03 Schering Corporation Gamma secretase modulators for the treatment of alzheimer's disease
MX2010010975A (es) 2008-04-07 2010-11-01 Amgen Inc Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular.
AR071619A1 (es) 2008-05-07 2010-06-30 Galapagos Nv Compuestos de pirazina fusionados utiles para el tratamiento de enfermedades degenerativas e inflamatorias y composiciones farmaceuticas que los contienen.
EP2328586A2 (en) 2008-05-20 2011-06-08 Cephalon, Inc. Substituted pyridazinone derivatives as histamine-3 (h3) receptor ligands
JP2011524917A (ja) 2008-06-20 2011-09-08 メタボレックス， インコーポレイテッド アリールｇｐｒ１１９作動薬およびその使用
PL2331547T3 (pl) 2008-08-22 2015-01-30 Novartis Ag Związki pirolopirymidynowe jako inhibitory CDK
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
ES2397934T3 (es) 2008-12-17 2013-03-12 Amgen Inc. Compuestos de aminopiridina y carboxipiridina como inhibidores de fosfodiesterasa 10
EP2379529B1 (de) 2008-12-19 2015-06-10 Boehringer Ingelheim International Gmbh Cgrp-antagonisten
EP2377851A4 (en) 2008-12-25 2012-06-20 Taisho Pharmaceutical Co Ltd isoquinoline
CA2750035C (en) 2009-01-22 2018-02-27 Unigene Laboratories Inc. Treatment for obesity
WO2010086613A1 (en) 2009-01-30 2010-08-05 Betagenon Ab Compounds useful as inhibitors as ampk
WO2010103547A2 (en) 2009-03-13 2010-09-16 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
CN102596923B (zh) 2009-07-08 2015-04-29 波罗的海生物公司 1,2,4-噻唑烷-3-酮衍生物及其在癌症治疗中的用途
MX353747B (es) 2009-08-17 2018-01-26 Memorial Sloan Kettering Cancer Center Star Compuesto de union a proteina de choque termico, composiciones, y metodos para producir y usar los mismos.
US20120157471A1 (en) 2009-09-01 2012-06-21 Pfizer Inc. Benzimidazole derivatives
KR20120092629A (ko) 2009-10-09 2012-08-21 아이알엠 엘엘씨 Ｇｐｒ119 활성의 조절제로서의 화합물 및 조성물
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
MX2012006776A (es) 2009-12-14 2012-10-05 Merck Patent Gmbh Inhibidores de la esfingosina quinasa.
CN102791687B (zh) 2009-12-18 2015-02-11 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
US8431575B2 (en) 2010-02-18 2013-04-30 Transtech Pharma, Inc. Phenyl-heteroaryl derivatives and methods of use thereof
MX2012011912A (es) 2010-04-13 2012-11-16 Novartis Ag Combinacion que comprende un inhibidor de cinasa 4 dependiente de ciclina o cinasa dependiente de ciclia (cdk4/6) y un inhibidor de mtor para tratar cancer.
CN102947295B (zh) 2010-04-29 2016-01-20 爱丁堡大学 作为11β-HSD1抑制剂的3,3-二取代的-(8-氮杂双环[3.2.1]辛烷-8-基)-[5-(1H-吡唑-4基)-噻吩-3-基]-甲酮
WO2011146401A1 (en) 2010-05-17 2011-11-24 Intermune, Inc. Novel inhibitors of hepatitis c virus replication
US8969349B2 (en) 2010-05-26 2015-03-03 Sunovion Pharmaceuticals Inc. Substituted quinoxalines and quinoxalinones as PDE-10 inhibitors
AU2011283684B2 (en) 2010-07-29 2015-08-27 Rigel Pharmaceuticals, Inc. AMPK-activating heterocyclic compounds and methods for using the same
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
CA2818903C (en) 2010-12-14 2021-03-23 Electrophoretics Limited 5-(1,3-benzoxazol-2-yl)-4-(pyridin-4-yl)pyrimidin-2-amine and its use as a casein kinase 1delta inhibitor
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
US10280171B2 (en) 2016-05-31 2019-05-07 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
AU2012249240A1 (en) 2011-04-29 2013-11-07 Icahn School Of Medicine At Mount Sinai Kinase inhibitors
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
JP6061949B2 (ja) 2011-12-12 2017-01-18 レセプトス エルエルシー 糖尿病などの疾患の治療のためのｇｌｐ−１受容体モジュレーターとして作用する４つの環を含むカルボン酸誘導体
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
RU2632899C2 (ru) 2012-04-25 2017-10-11 Раквалиа Фарма Инк. Амидопроизводные как блокаторы ttx-s
WO2013167633A1 (en) 2012-05-09 2013-11-14 Basf Se Acrylamide compounds for combating invertebrate pests
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
RU2665462C2 (ru) 2012-06-27 2018-08-30 Ф. Хоффманн-Ля Рош Аг Соединения 5-азаиндазола и способы их применения
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
MA37975B2 (fr) 2012-09-11 2021-03-31 Genzyme Corp Inhibiteurs de synthase de glucosylcéramide
US9527857B2 (en) 2013-03-15 2016-12-27 GI Therapeutics, Inc. HSPC-sparing treatments for RB-positive abnormal cellular proliferation
KR20150128863A (ko) 2013-03-15 2015-11-18 에프. 호프만-라 로슈 아게 RORc 조절제로서 아릴 설파미드 및 설파메이트 유도체
WO2014184014A1 (en) 2013-05-15 2014-11-20 Basf Se N-(1,2,5-oxadiazol-3-yl)carboxamide compounds and their use as herbicides
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
GB201309508D0 (en) 2013-05-28 2013-07-10 Redx Pharma Ltd Compounds
EA030857B1 (ru) 2013-06-11 2018-10-31 Селджин Интернэшнл Ii Сарл Новые модуляторы рецептора glp-1
CA2953482A1 (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
US20160159773A1 (en) 2013-07-30 2016-06-09 Takeda Pharmaceutical Company Limited Heterocyclic compound
EP3027625B1 (en) 2013-07-31 2018-05-30 Merck Sharp & Dohme Corp. Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure
US20150087673A1 (en) 2013-09-26 2015-03-26 Rigel Pharmaceuticals, Inc. Methods for using and biomarkers for ampk-activating compounds
CA2926571C (en) 2013-10-08 2022-05-17 Qing-bin LU Non-platinum-based anti-cancer compounds for use in targeted chemotherapy
AU2014340318B2 (en) 2013-10-21 2019-01-17 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
EP2883934B1 (en) 2013-12-16 2019-11-13 Merck Patent GmbH Liquid-crystalline medium
JP2017503778A (ja) 2013-12-19 2017-02-02 バイエル ファーマ アクチエンゲゼルシャフト アドレナリン受容体α２Ｃ拮抗薬としての置換されたビピペリジニル誘導体
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
US10093646B2 (en) 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
JP6473457B2 (ja) 2014-01-17 2019-02-20 ノバルティス アーゲー Ｓｈｐ２の活性を阻害するための１−（トリアジン−３−イル／ピリダジン−３−イル）−ピペリジン／ピペラジン誘導体およびその組成物
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
MA39337B1 (fr) 2014-02-14 2019-11-29 Takeda Pharmaceuticals Co Modulateurs de pyrazines de gpr6
WO2015148714A1 (en) 2014-03-25 2015-10-01 Duke University Heat shock protein 70 (hsp-70) receptor ligands
AU2015243694B2 (en) 2014-04-07 2019-01-17 Netherlands Translational Research Center B.V. (5,6-dihydro)pyrimido(4,5-e)indolizines
JP2017521480A (ja) 2014-05-23 2017-08-03 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ベンゼンスルホンアミド誘導体及びｒｏｒｃモデュレーターとしてのその使用
CN105294683B (zh) 2014-07-26 2018-01-23 广东东阳光药业有限公司 Cdk类小分子抑制剂的化合物及其用途
WO2016022645A1 (en) 2014-08-06 2016-02-11 Merck Sharp & Dohme Corp. Heterocyclic cgrp receptor antagonists
WO2016022644A1 (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
TWI788655B (zh) 2015-02-27 2023-01-01 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
US9969719B2 (en) 2015-03-11 2018-05-15 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Substituted 2-hydrogen-pyrazole derivative serving as anticancer drug
WO2016151501A1 (en) 2015-03-25 2016-09-29 Novartis Ag Pharmaceutical combinations
AR104020A1 (es) 2015-06-04 2017-06-21 Kura Oncology Inc Métodos y composiciones para inhibir la interacción de menina con proteínas mill
WO2016197027A1 (en) 2015-06-04 2016-12-08 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
CN112625028A (zh) * 2015-06-19 2021-04-09 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
WO2016203405A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
RU2604047C1 (ru) 2015-07-10 2016-12-10 Фортис Аксис, Закрытое Акционерное Общество Массажёр для воздействия на мышцы спины трех отделов позвоночника
CA2998375A1 (en) 2015-09-17 2017-03-23 Marvin J. Miller Benzyl amine-containing heterocyclic compounds and compositions useful against mycobacterial infection
CN113549069A (zh) 2015-12-27 2021-10-26 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
EP4108659A1 (en) 2016-06-07 2022-12-28 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
EA036446B1 (ru) 2016-06-14 2020-11-11 Новартис Аг Соединения и композиции для подавления активности shp2
CN116478132A (zh) * 2016-07-12 2023-07-25 锐新医药公司 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪
EP3290412A1 (en) 2016-08-31 2018-03-07 Università degli Studi di Siena Hiv-1 nucleocapsid inhibitors
EP3515916B1 (en) 2016-09-22 2023-06-07 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
JP2020503352A (ja) 2017-01-03 2020-01-30 ヴィーブ ヘルスケア ユーケー（ナンバー５）リミテッド ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−３−イル酢酸誘導体
AU2018239542C1 (en) * 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
CN114213421A (zh) 2017-04-01 2022-03-22 晟科药业（江苏）有限公司 1h-咪唑[4,5-h]喹唑啉类化合物作为蛋白激酶抑制剂
JP2020526557A (ja) 2017-07-12 2020-08-31 ヴァンダービルト ユニバーシティー ムスカリン性アセチルコリン受容体ｍ４のアンタゴニスト
EP3694848A1 (en) 2017-10-12 2020-08-19 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors
EP3697759A4 (en) 2017-10-20 2021-05-12 Vanderbilt University MUSCARINIAN ACETYLCHOLINE RECEPTOR ANTAGONISTS M4
AU2018392805A1 (en) 2017-12-22 2020-05-07 Dana-Farber Cancer Institute, Inc. NEK inhibitors and methods of use
KR20200116481A (ko) 2018-01-29 2020-10-12 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
SG11202006832YA (en) 2018-01-29 2020-08-28 Merck Patent Gmbh Gcn2 inhibitors and uses thereof
WO2019152454A1 (en) 2018-01-30 2019-08-08 Research Development Foundation Shp2 inhibitors and methods of use thereof
AU2019216793B2 (en) 2018-02-08 2023-02-02 Enyo Pharma Fused thiophene derivatives and their uses
US11466016B2 (en) 2018-03-02 2022-10-11 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
JP7462951B2 (ja) 2018-03-21 2024-04-08 リャオ，シビン Ｊａｋ阻害剤

Also Published As

Publication number Publication date
JP2023011889A (ja) 2023-01-24
MA49013A (fr) 2021-05-05
CL2019002698A1 (es) 2020-07-24
PH12019502175A1 (en) 2020-06-08
MX2019011330A (es) 2020-02-05
KR20240026521A (ko) 2024-02-28
AU2022204681B2 (en) 2024-02-22
EA202190196A1 (ru) 2021-08-31
WO2018172984A1 (en) 2018-09-27
TW201840553A (zh) 2018-11-16
EP3601239A4 (en) 2020-05-13
MX2021013685A (es) 2021-12-10
MX2021013686A (es) 2021-12-10
KR20220113545A (ko) 2022-08-12
CO2019011678A2 (es) 2020-01-17
US20200392128A1 (en) 2020-12-17
AU2020267305A1 (en) 2020-12-10
JP6878615B2 (ja) 2021-05-26
AU2022204681A1 (en) 2022-07-21
KR20210130254A (ko) 2021-10-29
JP2020515538A (ja) 2020-05-28
AU2018239542C1 (en) 2021-02-11
MX2021013683A (es) 2021-12-10
NZ758458A (en) 2022-07-29
CL2020003425A1 (es) 2021-07-19
US10988466B2 (en) 2021-04-27
KR20190140931A (ko) 2019-12-20
CA3057582A1 (en) 2018-09-27
CA3057582C (en) 2024-01-09
KR102317480B1 (ko) 2021-10-25
EP3601239A1 (en) 2020-02-05
AU2018239542A1 (en) 2019-11-14
SG11201908820VA (en) 2019-10-30
JP2021121592A (ja) 2021-08-26
TWI664175B (zh) 2019-07-01
AU2018239542B2 (en) 2020-08-20

Similar Documents

Publication Publication Date Title
EA201992253A1 (ru) Новые гетероциклические производные, применимые в качестве ингибиторов shp2
EA201990001A1 (ru) Новые гетероциклические производные, применимые в качестве ингибиторов shp2
EA201992601A1 (ru) Конденсированное имидазопиперидиновое соединение, являющееся ингибитором jak
MX2018010374A (es) Inhibidores del enlace proteína-proteína de wdr5.
EA201992322A2 (ru) Соединения и композиции для лечения гематологических расстройств
EA201992126A1 (ru) Ингибиторы jak, содержащие 4-членный гетероциклический амид
EA201591382A1 (ru) Ингибиторы гистондеметилаз
EA201690094A1 (ru) Ингибиторы syk
EA201692418A1 (ru) Замещенные индазольные соединения в качестве irak4 ингибиторов
EA202090256A1 (ru) 5-членные и бициклические гетероциклические амиды в качестве ингибиторов rock
MX2020001757A (es) Compuestos, sales de los mismos y metodos para el tratamiento de enfermedades.
EA201592033A1 (ru) 3-(2-АМИНОПИРИМИДИН-4-ИЛ)-5-(3-ГИДРОКСИПРОПИНИЛ)-1H-ПИРРОЛО[2,3-c]ПИРИДИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ NIK ДЛЯ ЛЕЧЕНИЯ РАКА
EA201591889A1 (ru) 6-(5-гидрокси-1h-пиразол-1-ил)никотинамидные ингибиторы phd
EA202091803A1 (ru) Производные триазолопиримидина для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat)
EA202091016A1 (ru) Пиримидиновое соединение в качестве ингибитора jak киназы
MX2020002399A (es) Inhibidores del enlace proteína-proteína de wdr5.
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA202190464A1 (ru) Замещенные бензимидазолы в качестве ингибиторов pad4
EA201891379A1 (ru) Ингибиторы тирозинкиназы брутона и способы их применения
EA201790206A1 (ru) Новые 2,5-замещенные пиримидины в качестве ингибиторов pde4
EA202091804A1 (ru) Гетероциклил-замещенные оксадиазолопиридиновые производные для применения в качестве ингибиторов грелин-о-ацилтрансферазы (goat)
EA201790800A1 (ru) Замещенные производные бензотиофенила в качестве агонистов gpr40 для лечения диабета ii типа
EA201990418A1 (ru) Производные оксадиазолопиридина для применения в качестве ингибиторов грелин-о-ацилтрасферазы (goat)
EA202190055A1 (ru) Производные пиразола в качестве ингибиторов malt1
MX2019013979A (es) Metodos para la preparacion de compuestos heterociclicos de 1,3-benzodioxol.