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

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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
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phenyl
pyridin
group
formula
amino
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CN102105459A (zh
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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
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Lsi Braafsap LLC
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Nerviano Medical Sciences SRL
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (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)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 2008-07-24
EP08161076.8 2008-07-24
PCT/EP2009/059506 WO2010010154A1 (en) 2008-07-24 2009-07-23 3,4-diarylpyrazoles as protein kinase inhibitors

Publications (2)

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

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

Families Citing this family (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2008001943A1 (es) 2007-07-02 2009-09-11 Boehringer Ingelheim Int Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes.
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
EP2324008B1 (en) * 2008-07-24 2012-05-09 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
US8778929B2 (en) 2008-09-29 2014-07-15 Boehringer Ingelheim International Gmbh Substituted heteroaryl inhibitors of B-RAF
JP2011057661A (ja) * 2009-08-14 2011-03-24 Bayer Cropscience Ag 殺虫性カルボキサミド類
AR077975A1 (es) * 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
US8242260B2 (en) * 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
CA2786509C (en) * 2010-01-27 2016-01-05 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
EP2552905B1 (en) 2010-03-26 2016-10-05 Boehringer Ingelheim International GmbH B-Raf kinase inhibitors
JP5871897B2 (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 ピリジルトリアゾール
AR081810A1 (es) 2010-04-07 2012-10-24 Bayer Cropscience Ag Piridinilpirazoles biciclicos
EA201201676A1 (ru) * 2010-06-25 2013-06-28 Новартис Аг Гетероарильные соединения и композиции в качестве ингибиторов протеинкиназы
US9114137B2 (en) 2010-08-03 2015-08-25 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
US8691184B2 (en) 2011-01-25 2014-04-08 The Regents Of The University Of Michigan Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same
RU2606497C2 (ru) 2011-02-24 2017-01-10 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Тиазолилфенилбензолсульфонамидопроизводные в качестве ингибиторов киназ
KR101298651B1 (ko) * 2011-03-16 2013-08-21 연세대학교 산학협력단 효능이 강화된 혈관신생 억제용 약제학적 조성물
PL2763993T3 (pl) 2011-10-06 2017-09-29 Bayer Intellectual Property Gmbh Heterocyklilopiry(mi)dynylopirazol
EP2763987B1 (en) 2011-10-06 2018-07-18 Bayer CropScience AG Heterocyclylpyri(mi)dinylpyrazole as fungicidals
CN103917236A (zh) 2011-11-11 2014-07-09 诺华股份有限公司 治疗增生性疾病的方法
PE20141994A1 (es) 2011-11-23 2014-12-24 Novartis Ag Formulaciones farmaceuticas
SG11201502893WA (en) 2012-11-02 2015-05-28 Pfizer Bruton's tyrosine kinase inhibitors
US9096625B2 (en) 2013-01-16 2015-08-04 The Regents Of The University Of Michigan BCL-2/BCL-XL inhibitors and therapeutic methods using the same
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
US10822337B2 (en) 2015-04-01 2020-11-03 Rigel Pharmaceuticals, Inc. TGF-β inhibitorC
PT3331863T (pt) * 2015-08-03 2020-05-22 Glenmark Pharmaceuticals Sa Novos compostos como moduladores de ror gama
KR20180109842A (ko) 2015-09-16 2018-10-08 록쏘 온콜로지, 인코포레이티드 화합물
MX380907B (es) * 2015-12-16 2025-03-12 Loxo Oncology Inc Compuestos útiles como inhibidores de cinasa.
DK3463345T3 (da) 2016-06-03 2023-01-09 Array Biopharma Inc Farmaceutiske kombinationer
AU2017329090B9 (en) 2016-09-19 2019-09-05 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
US11266653B2 (en) 2017-05-02 2022-03-08 Novartis Ag Combination therapy
WO2019081477A1 (de) 2017-10-26 2019-05-02 Bayer Cropscience Aktiengesellschaft Substituierte pyrazole sowie deren salze und ihre verwendung als herbizide wirkstoffe
WO2019081485A1 (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
JP7186874B2 (ja) * 2018-10-26 2022-12-09 アーリーン ファーマシューティカルズ エルエルシー ピラゾリル化合物およびその使用方法
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
CA3138123A1 (en) 2019-05-13 2020-11-19 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
CN114071999B (zh) 2019-06-03 2024-08-27 拜耳公司 1-苯基-5-吖嗪基吡唑基-3-氧基烷基酸及其用于控制不需要的植物生长的用途
PH12022550361A1 (en) 2019-08-14 2023-02-27 Incyte Corp Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
JP7693656B2 (ja) 2019-10-11 2025-06-17 インサイト・コーポレイション Ｃｄｋ２阻害剤としての二環式アミン
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
AU2020409657A1 (en) 2019-12-19 2022-07-07 Bayer Aktiengesellschaft 1,5-diphenylpyrazolyl-3-oxyalkyl acids and 1-phenyl-5-thienylpyrazolyl-3-oxyalkyl acids and the use thereof for control of undesired plant growth
WO2021120890A1 (en) 2019-12-20 2021-06-24 Novartis Ag Pyrazolyl derivatives useful as anti-cancer agents
WO2021151976A1 (de) 2020-01-31 2021-08-05 Bayer Aktiengesellschaft [(1,4,5-trisubstituierte-1h-pyrazol-3-yl)sulfanyl]essigsäure derivate sowie deren salze und ihre verwendung als herbizide wirkstoffe
TW202204354A (zh) * 2020-04-02 2022-02-01 美商普雷辛肯公司 用於ｃｓｋ調節之化合物及方法以及其說明
EP4143181A1 (de) 2020-04-29 2023-03-08 Bayer Aktiengesellschaft 1-pyrazinylpyrazolyl-3-oxyalkylsäuren sowie deren derivate und deren verwendung zur bekämpfung unerwünschten pflanzenwachstums
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US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2022268933A1 (de) 2021-06-25 2022-12-29 Bayer Aktiengesellschaft (1,4,5-trisubstituierte-1h-pyrazol-3-yl)oxy-2-alkoxy-alkylsäuren und -alkylsäure-derivate, deren salze und ihre verwendung als herbizide wirkstoffe
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US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
JP2025509886A (ja) 2022-03-28 2025-04-11 ニカング セラピューティクス， インコーポレイテッド サイクリン依存性キナーゼ２阻害剤としてのスルホンアミド誘導体
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
HUP0001880A3 (en) 1997-05-22 2002-03-28 G D Searle & Co Chicago Substituted pyrazoles as p38 kinase inhibitors
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
JP2009506040A (ja) 2005-08-26 2009-02-12 スミスクライン・ビーチャム・コーポレイション オーロラキナーゼのピリミジニル−ピラゾール阻害剤
EP2324008B1 (en) * 2008-07-24 2012-05-09 Nerviano Medical Sciences S.R.L. 3,4-diarylpyrazoles as protein kinase inhibitors
CA2786509C (en) * 2010-01-27 2016-01-05 Nerviano Medical Sciences S.R.L. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
US9114137B2 (en) 2010-08-03 2015-08-25 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

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