CN102105459B - 作为蛋白激酶抑制剂的3,4-二芳基吡唑类 - Google Patents

作为蛋白激酶抑制剂的3,4-二芳基吡唑类 Download PDF

Info

Publication number
CN102105459B
CN102105459B CN200980128629.1A CN200980128629A CN102105459B CN 102105459 B CN102105459 B CN 102105459B CN 200980128629 A CN200980128629 A CN 200980128629A CN 102105459 B CN102105459 B CN 102105459B
Authority
CN
China
Prior art keywords
phenyl
pyridin
group
formula
amino
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.)
Active
Application number
CN200980128629.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN102105459A (zh
Inventor
M·普里茨
F·祖考图
A·巴达里
S·努沃罗尼
G·塞尔维
G·特拉昆迪
S·比昂达洛
P·特里菲罗
C·玛奇昂尼
M·莫度格诺
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Lsi Braafsap LLC
Original Assignee
Nerviano Medical Sciences SRL
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41059486&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102105459(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Nerviano Medical Sciences SRL filed Critical Nerviano Medical Sciences SRL
Publication of CN102105459A publication Critical patent/CN102105459A/zh
Application granted granted Critical
Publication of CN102105459B publication Critical patent/CN102105459B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D513/12—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 three hetero rings
    • C07D513/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN200980128629.1A 2008-07-24 2009-07-23 作为蛋白激酶抑制剂的3,4-二芳基吡唑类 Active CN102105459B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08161076.8 2008-07-24
EP08161076 2008-07-24
PCT/EP2009/059506 WO2010010154A1 (en) 2008-07-24 2009-07-23 3,4-diarylpyrazoles as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
CN102105459A CN102105459A (zh) 2011-06-22
CN102105459B true CN102105459B (zh) 2014-09-10

Family

ID=41059486

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980128629.1A Active CN102105459B (zh) 2008-07-24 2009-07-23 作为蛋白激酶抑制剂的3,4-二芳基吡唑类

Country Status (19)

Country Link
US (2) US8541575B2 (OSRAM)
EP (1) EP2324008B1 (OSRAM)
JP (1) JP5385382B2 (OSRAM)
CN (1) CN102105459B (OSRAM)
AT (1) ATE557015T1 (OSRAM)
AU (1) AU2009273197B2 (OSRAM)
BR (1) BRPI0916356B1 (OSRAM)
CA (1) CA2731146C (OSRAM)
CL (1) CL2011000124A1 (OSRAM)
CY (1) CY1117667T1 (OSRAM)
DK (1) DK2324008T3 (OSRAM)
EA (1) EA019722B1 (OSRAM)
ES (1) ES2386408T3 (OSRAM)
HR (1) HRP20120577T1 (OSRAM)
MX (1) MX2011000738A (OSRAM)
PL (1) PL2324008T3 (OSRAM)
PT (1) PT2324008E (OSRAM)
SI (1) SI2324008T1 (OSRAM)
WO (1) WO2010010154A1 (OSRAM)

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20090837A1 (es) 2007-07-02 2009-07-24 Boehringer Ingelheim Int Nuevos compuestos quimicos
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
DK2324008T3 (da) * 2008-07-24 2012-07-23 Nerviano Medical Sciences Srl Diarylpyrazol som protein kinase inhibitorer
JP5603869B2 (ja) 2008-09-29 2014-10-08 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
JP2011057661A (ja) * 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
JO3002B1 (ar) 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
AU2011209234B2 (en) * 2010-01-27 2015-05-07 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
JP5871896B2 (ja) 2010-03-26 2016-03-01 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 Ｂ−ｒａｆキナーゼインヒビター
US8865703B2 (en) 2010-03-26 2014-10-21 Boehringer Ingelheim International Gmbh Pyridyltriazoles
AR081810A1 (es) 2010-04-07 2012-10-24 Bayer Cropscience Ag Piridinilpirazoles biciclicos
CA2803055A1 (en) * 2010-06-25 2011-12-29 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
WO2012016993A1 (en) 2010-08-03 2012-02-09 Nerviano Medical Sciences S.R.L. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
TWI480276B (zh) * 2010-08-27 2015-04-11 Irm Llc 作為蛋白質激酶抑制劑之化合物及組合物
US8710055B2 (en) * 2010-12-21 2014-04-29 Boehringer Ingelheim International Gmbh Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
KR101762724B1 (ko) * 2011-01-25 2017-07-28 더 리젠츠 오브 더 유니버시티 오브 미시건 Bcl-2/bcl-xl 억제제 및 이를 이용한 치료 방법
EP2678336B1 (en) 2011-02-24 2016-04-20 Nerviano Medical Sciences S.r.l. Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors
KR101298651B1 (ko) * 2011-03-16 2013-08-21 연세대학교 산학협력단 효능이 강화된 혈관신생 억제용 약제학적 조성물
PL2763987T3 (pl) 2011-10-06 2019-01-31 Bayer Cropscience Ag Heterocyklilopiry(mi)dynylopirazole jako środki grzybobójcze
US9314026B2 (en) 2011-10-06 2016-04-19 Bayer Intellectual Property Gmbh Heterocyclylpyri(mi)dinylpyrazole
WO2013070996A1 (en) 2011-11-11 2013-05-16 Novartis Ag Method of treating a proliferative disease
EP2782557B1 (en) 2011-11-23 2018-09-12 Array Biopharma, Inc. Pharmaceutical formulations
WO2014068527A1 (en) 2012-11-02 2014-05-08 Pfizer Inc. Bruton's tyrosine kinase inhibitors
CN105246882A (zh) 2013-01-16 2016-01-13 密执安大学评议会 BCL-2/Bcl-xL抑制剂和使用所述抑制剂的治疗方法
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3277673B1 (en) 2015-04-01 2022-05-04 Rigel Pharmaceuticals, Inc. Tgf-beta inhibitors
PE20180686A1 (es) * 2015-08-03 2018-04-23 Glenmark Pharmaceuticals Sa Compuestos nuevos como moduladores de ror gamma
EP4116303A1 (en) 2015-09-16 2023-01-11 Loxo Oncology, Inc. Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer
EP3782994B1 (en) 2015-12-16 2025-07-16 Loxo Oncology, Inc. Compounds useful as kinase inhibitors
MX387795B (es) 2016-06-03 2025-03-19 Array Biopharma Inc Combinaciones farmaceuticas.
CA3037456A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
CN106883266B (zh) * 2017-01-23 2020-03-17 江苏七洲绿色化工股份有限公司 一种1-(4-氯苯基)-2-环丙基-1-丙酮的制备方法及其中间体
IL270224B1 (en) 2017-05-02 2024-04-01 Novartis Ag Combination therapy employing trametinib and a defined raf inhibitor
WO2019081485A1 (de) 2017-10-26 2019-05-02 Bayer Cropscience Aktiengesellschaft Substituierte pyrazole sowie deren salze und ihre verwendung als herbizide wirkstoffe
WO2019081477A1 (de) 2017-10-26 2019-05-02 Bayer Cropscience Aktiengesellschaft Substituierte pyrazole sowie deren salze und ihre verwendung als herbizide wirkstoffe
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN113226321B (zh) * 2018-10-26 2024-12-17 阿利安制药有限责任公司 吡唑基化合物及其使用方法
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
EP4563150A3 (en) 2019-05-13 2025-07-23 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
BR112021020565A2 (pt) 2019-06-03 2021-12-21 Bayer Ag Ácidos 1-fenil-5-azinil pirazolil-3-oxialquílicos e seu uso para o controle do crescimento indesejado de plantas
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
PE20221905A1 (es) 2019-10-11 2022-12-23 Incyte Corp Aminas biciclicas como inhibidoras de la cdk2
KR102323820B1 (ko) * 2019-10-31 2021-11-08 한국화학연구원 돌연변이형 idh 억제제, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
CN112979613B (zh) * 2019-12-16 2022-04-26 四川大学华西医院 2-(1h-吡唑-3-基)吡啶衍生物及其制备方法和用途
WO2021122728A1 (de) 2019-12-19 2021-06-24 Bayer Aktiengesellschaft 1,5-diphenylpyrazolyl-3-oxyalkylsäuren und 1-phenyl-5-thienylpyrazolyl-3-oxyalkylsäuren und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums
WO2021120890A1 (en) * 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
US20230126893A1 (en) 2020-01-31 2023-04-27 Bayer Aktiengesellschaft [(1,4,5-trisubstituted-1h-pyrazol-3-yl)sulfanyl]acetic acid derivatives, salts thereof, and use thereof as active herbicidal ingredients
WO2021202900A1 (en) * 2020-04-02 2021-10-07 Plexxikon Inc. 1,6-naphthyridine compounds and methods for csk modulation and indications therefor
EP4143181A1 (de) 2020-04-29 2023-03-08 Bayer Aktiengesellschaft 1-pyrazinylpyrazolyl-3-oxyalkylsäuren sowie deren derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums
US12303509B2 (en) 2020-06-09 2025-05-20 Pfizer Inc. Compounds for the treatment of BRAF-associated diseases and disorders
EP4232443B1 (de) 2020-10-23 2024-12-18 Bayer Aktiengesellschaft 1-(pyridyl)-5-azinylpyrazol derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums
BR112023007912A2 (pt) * 2020-10-30 2024-01-02 Novartis Ag Formas cristalinas de um composto inibidor de kras g12c
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CN117615652A (zh) 2021-06-25 2024-02-27 拜耳公司 (1,4,5-三取代-1h-吡唑-3-基)氧基-2-烷氧基烷基酸及其衍生物、其盐及其作为除草剂的用途
US20250051300A1 (en) * 2021-11-19 2025-02-13 The Board Of Trustees Of The University Of Illinois Gram-negative specific antibiotics sparing effect on gut microbiome
US20250026724A1 (en) 2021-12-01 2025-01-23 Bayer Aktiengesellschaft (1,4,5-trisubstituted 1h-pyrazol-3-yl)oxy-2-alkylthioalkyl acids and -alkyl acid derivatives, salts thereof and use thereof as active herbicidal ingredients
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12331026B2 (en) 2022-03-28 2025-06-17 Nikang Therapeutics, Inc. Sulfonamido derivatives as cyclin-dependent kinase 2 inhibitors
WO2024078871A1 (de) 2022-10-14 2024-04-18 Bayer Aktiengesellschaft 1-pyridyl-5-phenylpyrazolyl-3-oxy- und -3-thioalkylsäuren und derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005068452A1 (en) * 2004-01-09 2005-07-28 Novartis Ag Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives as igf-ir inhibitors
WO2007105058A2 (en) * 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
WO2008042639A1 (en) * 2006-10-02 2008-04-10 Irm Llc Compounds and compositions as protein kinase inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR200000235T2 (tr) 1997-05-22 2000-05-22 G.D. Searle &Co. p38 kinaz inhibitörleri olarak ikame edilmiş pirazoller.
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
JP4399265B2 (ja) 2001-12-21 2010-01-13 ヴァーナリス（ケンブリッジ）リミテッド ３，４−ジアリールピラゾール、および癌の治療におけるそれらの使用
WO2007024843A2 (en) 2005-08-26 2007-03-01 Smithkline Beecham Corporation Pyrimidinyl-pyrazole inhibitors of aurora kinases
DK2324008T3 (da) * 2008-07-24 2012-07-23 Nerviano Medical Sciences Srl Diarylpyrazol som protein kinase inhibitorer
AU2011209234B2 (en) * 2010-01-27 2015-05-07 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
WO2012016993A1 (en) 2010-08-03 2012-02-09 Nerviano Medical Sciences S.R.L. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005068452A1 (en) * 2004-01-09 2005-07-28 Novartis Ag Phenyl-[4-(3-phenyl-1h-pyrazol-4-yl)-pyrimidin-2-yl]-amine derivatives as igf-ir inhibitors
WO2007105058A2 (en) * 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazole compounds
WO2008042639A1 (en) * 2006-10-02 2008-04-10 Irm Llc Compounds and compositions as protein kinase inhibitors

Also Published As

Publication number Publication date
MX2011000738A (es) 2011-02-23
JP2011528698A (ja) 2011-11-24
CA2731146A1 (en) 2010-01-28
AU2009273197A1 (en) 2010-01-28
CA2731146C (en) 2016-05-03
ES2386408T3 (es) 2012-08-20
EA201170249A1 (ru) 2011-10-31
BRPI0916356B1 (pt) 2022-08-23
US20140005150A1 (en) 2014-01-02
EP2324008A1 (en) 2011-05-25
AU2009273197A2 (en) 2011-03-10
US8946250B2 (en) 2015-02-03
JP5385382B2 (ja) 2014-01-08
CY1117667T1 (el) 2017-05-17
ATE557015T1 (de) 2012-05-15
US20110144068A1 (en) 2011-06-16
US8541575B2 (en) 2013-09-24
CL2011000124A1 (es) 2011-05-06
AU2009273197B2 (en) 2014-01-16
HK1157337A1 (en) 2012-06-29
DK2324008T3 (da) 2012-07-23
SI2324008T1 (sl) 2012-08-31
PT2324008E (pt) 2012-06-25
PL2324008T3 (pl) 2012-09-28
CN102105459A (zh) 2011-06-22
EA019722B1 (ru) 2014-05-30
EP2324008B1 (en) 2012-05-09
BRPI0916356A2 (OSRAM) 2018-08-21
WO2010010154A1 (en) 2010-01-28
HRP20120577T1 (hr) 2012-08-31

Similar Documents

Publication Publication Date Title
CN102105459B (zh) 作为蛋白激酶抑制剂的3,4-二芳基吡唑类
CN103153980B (zh) 吡唑并苯基苯磺酰胺化合物的衍生物及其作为抗肿瘤药的用途
CN103797006B (zh) 用作端锚聚合酶抑制剂的4-哌啶基化合物
CN106535890A (zh) 5‑取代的吲唑‑3‑羧酰胺及其制备和应用
CN102015660A (zh) 2-氨基喹唑啉衍生物
US12233065B2 (en) Inhibitors of RNA helicase DHX9 and uses thereof
CN103781776A (zh) 用作端锚聚合酶抑制剂的新的2-哌啶-1-基-乙酰胺化合物
KR20050098286A (ko) 사이클릭 우레아 유도체, 이의 제조방법 및 키나제억제제로서의 이의 약제학적 용도
JP6921877B2 (ja) Ａｌｋ５抑制剤としての新規ピラゾール誘導体およびその用途
US20250179013A1 (en) Inhibitors of rna helicase dhx9 and uses thereof
CN120712252A (zh) 包含sos1抑制剂和抗癌药物的用于治疗癌症的药物组合物
HK1157337B (en) 3,4-diarylpyrazoles as protein kinase inhibitors
HK1186178A (en) Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
TW201524969A (zh) 葡萄糖轉運抑制劑
HK1230502B (zh) 治疗性抑制性化合物

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
TR01 Transfer of patent right
TR01 Transfer of patent right

Effective date of registration: 20241230

Address after: Ai Erlandubailin

Patentee after: LSI Financial 1 Design Activity Co.

Country or region after: Ireland

Address before: Italy, Milan

Patentee before: NERVIANO MEDICAL SCIENCES S.R.L.

Country or region before: Italy

TR01 Transfer of patent right
TR01 Transfer of patent right

Effective date of registration: 20250114

Address after: New York, United States

Patentee after: LSI Braafsap LLC

Country or region after: U.S.A.

Address before: Ai Erlandubailin

Patentee before: LSI Financial 1 Design Activity Co.

Country or region before: Ireland