JP2017503000A5 - - Google Patents

Download PDF

Info

Publication number
JP2017503000A5
JP2017503000A5 JP2016547026A JP2016547026A JP2017503000A5 JP 2017503000 A5 JP2017503000 A5 JP 2017503000A5 JP 2016547026 A JP2016547026 A JP 2016547026A JP 2016547026 A JP2016547026 A JP 2016547026A JP 2017503000 A5 JP2017503000 A5 JP 2017503000A5
Authority
JP
Japan
Prior art keywords
alkyl
amino
substituted
hydrogen
halo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
JP2016547026A
Other languages
English (en)
Japanese (ja)
Other versions
JP2017503000A (ja
JP6523303B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/IB2015/050343 external-priority patent/WO2015107493A1/en
Publication of JP2017503000A publication Critical patent/JP2017503000A/ja
Publication of JP2017503000A5 publication Critical patent/JP2017503000A5/ja
Application granted granted Critical
Publication of JP6523303B2 publication Critical patent/JP6523303B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2016547026A 2014-01-17 2015-01-16 Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物 Active JP6523303B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461928738P 2014-01-17 2014-01-17
US61/928,738 2014-01-17
PCT/IB2015/050343 WO2015107493A1 (en) 2014-01-17 2015-01-16 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2

Publications (3)

Publication Number Publication Date
JP2017503000A JP2017503000A (ja) 2017-01-26
JP2017503000A5 true JP2017503000A5 (enExample) 2018-02-22
JP6523303B2 JP6523303B2 (ja) 2019-05-29

Family

ID=52462361

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016547026A Active JP6523303B2 (ja) 2014-01-17 2015-01-16 Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物

Country Status (6)

Country Link
US (4) US10093646B2 (enExample)
EP (1) EP3094627B1 (enExample)
JP (1) JP6523303B2 (enExample)
CN (1) CN105899491B (enExample)
ES (1) ES2699351T3 (enExample)
WO (1) WO2015107493A1 (enExample)

Families Citing this family (128)

* 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
WO2015092819A2 (en) * 2013-12-21 2015-06-25 Nektar Therapeutics (India) Pvt. Ltd. Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine
ES2699354T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2805232T3 (es) 2015-06-19 2021-02-11 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
ES2824576T3 (es) * 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
ES2846951T3 (es) * 2015-11-05 2021-07-30 Celgene Quanticel Res Inc Composiciones que comprenden un inhibidor de desmetilasa-1 específica para lisina, que tiene un anillo de pirimidina, y su uso en el tratamiento del cáncer
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
AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
EA202092442A3 (ru) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
CN109415360B (zh) 2016-06-14 2021-11-02 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
KR102598895B1 (ko) * 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
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
US20190343836A1 (en) 2017-01-10 2019-11-14 Novartis Ag Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
JP7240319B2 (ja) 2017-01-23 2023-03-15 レヴォリューション・メディスンズ,インコーポレイテッド アロステリックshp2阻害剤としての二環式化合物
AU2018239542C1 (en) 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
WO2018218133A1 (en) 2017-05-26 2018-11-29 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
TW202517628A (zh) 2017-09-11 2025-05-01 美商克魯松藥物公司 Shp2之八氫環戊烷并[c]吡咯別構抑制劑
US11701354B2 (en) 2017-09-29 2023-07-18 D. E. Shaw Research, Llc 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
CN108113984B (zh) * 2017-12-20 2021-05-07 中国科学院成都生物研究所 Shp2抑制剂在制备抗肿瘤的药物中的用途
CN110655520A (zh) * 2018-06-29 2020-01-07 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN110156786B (zh) * 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 嘧啶并环化合物及其制备方法和应用
SG11202007740TA (en) 2018-02-13 2020-09-29 Shanghai Blueray Biopharma Co Ltd Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
JP7326305B2 (ja) 2018-03-02 2023-08-15 大塚製薬株式会社 医薬化合物
TWI903299B (zh) 2018-03-08 2025-11-01 美商英塞特公司 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物
CN112368272B (zh) 2018-03-21 2023-04-21 苏州浦合医药科技有限公司 Shp2抑制剂及其用途
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
BR112020019385A2 (pt) 2018-03-21 2021-03-30 Relay Therapeutics, Inc. Inibidores de shp2 fosfatase e métodos de uso dos mesmos
CA3096535A1 (en) 2018-04-10 2019-10-17 Revolution Medicines, Inc. Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
HRP20230488T1 (hr) 2018-05-01 2023-08-04 Revolution Medicines, Inc. C40-, C28- I C-32-VEZANI ANALOZI RAPAMICINA KAO INHIBITORI mTOR
MX2020011528A (es) 2018-05-02 2021-02-09 Navire Pharma Inc Inhibidores heterociclicos sustituidos de ptpn11.
CN112409334B (zh) * 2018-05-09 2022-12-02 北京加科思新药研发有限公司 可用作shp2抑制剂的杂环衍生物
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
MX2021000795A (es) 2018-07-24 2021-04-12 Taiho Pharmaceutical Co Ltd Compuestos heterociclicos para inhibir la actividad de shp2.
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
CN112996795B (zh) 2018-09-18 2024-11-12 尼坎治疗公司 作为src同源-2磷酸酶抑制剂的稠合的三环衍生物
US20210393623A1 (en) 2018-09-26 2021-12-23 Jacobio Pharmaceuticals Co., Ltd. Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors
IL305106B2 (en) 2018-09-29 2025-08-01 Novartis Ag Process of manufacture of a compound for inhibiting the activity of shp2
KR20210068472A (ko) 2018-09-29 2021-06-09 노파르티스 아게 Shp2 활성의 억제를 위한 화합물 및 조성물의 제조
US11179397B2 (en) 2018-10-03 2021-11-23 Gilead Sciences, Inc. Imidazopyrimidine derivatives
WO2020076723A1 (en) 2018-10-08 2020-04-16 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
MA53921A (fr) 2018-10-17 2022-01-26 Array Biopharma Inc Inhibiteurs de protéine tyrosine phosphatase
CN117143079A (zh) * 2018-11-06 2023-12-01 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
WO2020094104A1 (zh) * 2018-11-07 2020-05-14 如东凌达生物医药科技有限公司 一类含氮稠杂环类shp2抑制剂化合物、制备方法和用途
CN111153899B (zh) * 2018-11-08 2023-12-01 四川科伦博泰生物医药股份有限公司 一种取代吡啶化合物、其制备方法和用途
CA3112129A1 (en) 2018-12-05 2020-06-11 Mirati Therapeutics, Inc. Combination therapies
CN111484491B (zh) * 2019-01-25 2022-09-02 四川科伦博泰生物医药股份有限公司 取代吡啶并环化合物、其制备方法和用途
WO2020165732A1 (en) 2019-02-12 2020-08-20 Novartis Ag Pharmaceutical combination comprising tno155 and a krasg12c inhibitor
KR20210146287A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
CA3127361A1 (en) 2019-03-07 2020-09-10 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
BR112021018664A2 (pt) 2019-04-02 2021-11-23 Array Biopharma Inc Inibidores de proteína tirosina fosfatase
US11001561B2 (en) 2019-04-08 2021-05-11 Merck Patent Gmbh Pyrimidinone derivatives as SHP2 antagonists
KR20220019017A (ko) * 2019-06-07 2022-02-15 레볼루션 메디슨즈, 인크. {6-[(2-아미노-3-클로로피리딘-4-일)설파닐]-3-[(3s,4s)-4-아미노-3-메틸-2-옥사-8-아자스피로[4.5]데칸-8-일]-5-메틸피라진-2-일}메탄올의 고체 형태인 shp2 저해제
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
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
GB201911928D0 (en) 2019-08-20 2019-10-02 Otsuka Pharma Co Ltd Pharmaceutical compounds
CN114127053B (zh) * 2019-09-06 2023-06-13 四川科伦博泰生物医药股份有限公司 一种取代吡嗪化合物、其制备方法和用途
WO2021061706A1 (en) 2019-09-24 2021-04-01 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
CN112724145A (zh) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
JP7823816B2 (ja) 2019-11-04 2026-03-04 レヴォリューション・メディスンズ,インコーポレイテッド Ras阻害剤
EP4054719B1 (en) 2019-11-04 2026-02-11 Revolution Medicines, Inc. Ras inhibitors
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
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
CN114761394B (zh) * 2020-01-16 2024-03-29 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
US20230348467A1 (en) 2020-01-16 2023-11-02 Zhejiang Hisun Pharmaceutical Co., Ltd. Heteroaryl Derivative, Preparation Method Therefor, And Use Thereof
TW202146021A (zh) 2020-02-28 2021-12-16 瑞士商諾華公司 包含達拉菲尼、erk抑制劑和shp2抑制劑之三重藥物組合
WO2021247836A1 (en) 2020-06-03 2021-12-09 Board Of Regents, The University Of Texas System Methods for targeting shp-2 to overcome resistance
CN113754683A (zh) 2020-06-05 2021-12-07 上海奕拓医药科技有限责任公司 同位素取代的螺芳环化合物及其应用
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
JP2023530838A (ja) * 2020-06-22 2023-07-20 スーチュアン・コールン-バイオテック・バイオファーマシューティカル・カンパニー・リミテッド 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用
TW202216723A (zh) 2020-07-08 2022-05-01 瑞士商諾華公司 用於抑制shp2活性的化合物及組成物之製造
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
CN117396472A (zh) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 Sos1抑制剂及其用途
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
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
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
CA3216220A1 (en) 2021-06-09 2022-12-15 F. Hoffmann-La Roche Ag Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
KR102699226B1 (ko) 2021-06-09 2024-08-27 에프. 호프만-라 로슈 아게 암 치료를 위한 병용요법
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
TW202327569A (zh) 2021-09-01 2023-07-16 瑞士商諾華公司 包含tead抑制劑的藥物組合及其用於癌症治療之用途
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023078881A1 (en) 2021-11-04 2023-05-11 F. Hoffmann-La Roche Ag Novel use of quinazolinone compound for the treatment of cancer
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
CN116903581A (zh) * 2022-04-14 2023-10-20 山东大学 Shp2/hdac双靶点抑制剂及其制备方法和应用
CN115611869B (zh) * 2022-05-11 2024-08-09 山东大学 杂环吡嗪衍生物与其在制备shp2抑制剂中的应用
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
CN115677828B (zh) * 2022-11-02 2024-10-18 四川大学 一种抗肿瘤的间二氯苯酚衍生物及其制备方法
WO2024126660A1 (en) 2022-12-15 2024-06-20 F. Hoffmann-La Roche Ag Combination therapy for cancer treatment
CN116332908B (zh) * 2023-03-21 2024-07-02 杭州医学院 一种shp2变构抑制剂及其制备方法和应用
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
PE20260039A1 (es) 2023-04-07 2026-01-09 Revolution Medicines Inc Inhibidores macrociclicos de ras
TW202448897A (zh) 2023-04-14 2024-12-16 美商銳新醫藥公司 Ras抑制劑之結晶形式、含有其之組合物及其使用方法
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025034919A1 (en) 2023-08-08 2025-02-13 Quanta Therapeutics, Inc. Combination therapies with kras modulators
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
WO2025106901A1 (en) 2023-11-17 2025-05-22 Quanta Therapeutics, Inc. Combination cancer therapies with a kras modulator and an rtk-mapk pathway inhibitor
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025261943A1 (en) 2024-06-18 2025-12-26 F. Hoffmann-La Roche Ag Anti-cancer combinations comprising mosperafenib and folfox or folfiri
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH445129A (fr) 1964-04-29 1967-10-15 Nestle Sa Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453259A (en) 1967-03-22 1969-07-01 Corn Products Co Cyclodextrin polyol ethers and their oxidation products
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
FR2567518B1 (fr) 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
US4737323A (en) 1986-02-13 1988-04-12 Liposome Technology, Inc. Liposome extrusion method
WO1987004928A1 (fr) 1986-02-24 1987-08-27 Mitsui Petrochemical Industries, Ltd. Agents therapeutiques de la neuropathie
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9012316D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
DK169008B1 (da) 1990-06-01 1994-07-25 Holec Lk A S Fremgangsmåde og skærm til afskærmning af en strømtransformer samt strømtransformer med en sådan afskærmning
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL115849A0 (en) 1994-11-03 1996-01-31 Merz & Co Gmbh & Co Tangential filtration preparation of liposomal drugs and liposome product thereof
WO2000059893A1 (en) 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
EP1438053B1 (de) 2001-10-17 2008-09-10 Boehringer Ingelheim Pharma GmbH & Co.KG Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
SI1482924T1 (sl) 2002-03-05 2008-12-31 Merck Frosst Canada Ltd Katepsin cistein proteazni inhibitorji
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
GB0300783D0 (en) * 2003-01-14 2003-02-12 Btg Int Ltd Treatment of neurodegenerative conditions
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
CA2562126A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
JP5213229B2 (ja) * 2004-04-23 2013-06-19 エグゼリクシス, インコーポレイテッド キナーゼ調節因子および使用方法
KR20170001725A (ko) 2004-09-02 2017-01-04 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
WO2007031529A1 (en) 2005-09-13 2007-03-22 Palau Pharma, S.A. 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity
US7515405B2 (en) 2006-07-25 2009-04-07 Hewlett-Packard Development Company, L.P. Anti-rotation mechanism for an electronic device
US20090137549A1 (en) 2006-11-09 2009-05-28 Paul John Edward Novel compounds useful for the treatment of degenerative & inflamatory diseases
EP2120573A4 (en) 2007-02-12 2011-05-25 Merck Sharp & Dohme piperidine
JP5550352B2 (ja) * 2007-03-15 2014-07-16 ノバルティス アーゲー 有機化合物およびその使用
CA2699202C (en) 2007-09-12 2016-09-27 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
EP2214675B1 (en) 2007-10-25 2013-11-20 Genentech, Inc. Process for making thienopyrimidine compounds
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
KR20110031318A (ko) 2008-06-13 2011-03-25 노파르티스 아게 Ia 심부전 및 암 치료에 유용한 단백질 키나제 d 억제제로서의 2,4'-비피리디닐 화합물
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
CN102203074A (zh) 2008-06-20 2011-09-28 麦它波莱克斯股份有限公司 芳基gpr119激动剂及其用途
SG10201510696RA (en) 2008-06-27 2016-01-28 Celgene Avilomics Res Inc Heteroaryl compounds and uses thereof
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
EP2394993A4 (en) 2008-12-10 2012-05-30 Dong Wha Pharm Co Ltd A NEW 2,6-SUBSTITUTED 3-NITROPYRIDINE DERIVATIVE, METHOD FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF
FR2941696B1 (fr) 2009-02-05 2011-04-15 Sanofi Aventis Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique
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
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
PL2589592T3 (pl) 2010-06-30 2019-03-29 Fujifilm Corporation Nowe pochodne nikotynamidu lub ich sole
AU2011279509A1 (en) 2010-07-13 2013-01-10 Merck Sharp & Dohme Corp. Spirocyclic compounds
CA2806341C (en) 2010-07-29 2020-03-24 Rigel Pharmaceuticals, Inc. Ampk-activating heterocyclic compounds and methods for using the same
US8609672B2 (en) * 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
WO2012052948A1 (en) 2010-10-20 2012-04-26 Pfizer Inc. Pyridine- 2- derivatives as smoothened receptor modulators
JP5727276B2 (ja) 2011-03-04 2015-06-03 協同油脂株式会社 グリース組成物及びグリース封入転がり軸受
EA028057B1 (ru) 2011-09-12 2017-10-31 Мерк Патент Гмбх Производные аминопиримидина для применения в качестве модуляторов киназной активности
WO2013096093A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Compounds as dgat-1 inhibitors
WO2013182546A1 (en) 2012-06-07 2013-12-12 F. Hoffmann-La Roche Ag Pyrazolopyrimidone and pyrazolopyridone inhibitors of tankyrase
JP6099753B2 (ja) 2012-10-03 2017-03-22 アドビナス セラピューティクス リミテッド スピロ環化合物、その組成物及びその医薬応用
WO2014160521A1 (en) * 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
WO2015092819A2 (en) * 2013-12-21 2015-06-25 Nektar Therapeutics (India) Pvt. Ltd. Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2699354T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2
PE20161438A1 (es) 2014-05-01 2017-01-18 Celgene Quanticel Res Inc Inhibidores de desmetilasa 1 especifica a lisina
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
ES2805232T3 (es) 2015-06-19 2021-02-11 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2

Similar Documents

Publication Publication Date Title
JP2017503000A5 (enExample)
JP2017502994A5 (enExample)
JP2017502993A5 (enExample)
JP2018517746A5 (enExample)
JP2017509586A5 (enExample)
JP2010538003A5 (enExample)
RU2019100295A (ru) Соединения и композиции для подавления активности shp2
JP2018507877A5 (enExample)
JP2016040288A5 (enExample)
JP2018517752A5 (enExample)
JP2014518544A5 (enExample)
JP2016505637A5 (enExample)
JP2015517574A5 (enExample)
JP2014515406A5 (enExample)
RU2018105614A (ru) Производное 1,3,5-триазина и способ его применения
JP2018525441A5 (enExample)
JP2016515561A5 (enExample)
RU2018107668A (ru) Пиразолпиримидиновое производное и его применение
JP2014528467A5 (enExample)
JP2013533879A5 (enExample)
JP2016513130A5 (enExample)
JP2016503797A5 (enExample)
RU2015126015A (ru) Новые улавливатели в лечении макулодистрофии
RU2016126503A (ru) Аналоги кортистатина, их синтез и применения
RU2012140185A (ru) Ингибирование ангиогенеза