EA200300205A1 - DERIVATIVES OF PYRAZOL AND THEIR APPLICATION AS PROTEINKINASE INHIBITORS - Google Patents

DERIVATIVES OF PYRAZOL AND THEIR APPLICATION AS PROTEINKINASE INHIBITORS

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Publication number
EA200300205A1
EA200300205A1 EA200300205A EA200300205A EA200300205A1 EA 200300205 A1 EA200300205 A1 EA 200300205A1 EA 200300205 A EA200300205 A EA 200300205A EA 200300205 A EA200300205 A EA 200300205A EA 200300205 A1 EA200300205 A1 EA 200300205A1
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EA
Eurasian Patent Office
Prior art keywords
formula
compounds
conditions
syndrome
pharmaceutical compositions
Prior art date
Application number
EA200300205A
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Russian (ru)
Inventor
Кристофер Блэйр Купер
Кристофер Джон Хелал
Марк Аллен Саннер
Трэвис Т. Уэйджер
Original Assignee
Пфайзер Продактс Инк.
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.)
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Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200300205A1 publication Critical patent/EA200300205A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C07D231/40—Acylated on said nitrogen atom
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Abstract

В данном изобретении представлены соединения формулы (1), в которой R, R, Rи Rтакие, как определены в описании, и их фармацевтически приемлемые соли. Соединения формулы (1) оказывают ингибирующее действие на cdk2 и GSK-3. Фармацевтические композиции и способы, включающие соединения формулы (1) для лечения и профилактики заболеваний и состояний, включающих аномальный рост клеток, такой как рак, и нейродегенеративные заболевания и состояния и состояния, на которые влияет нейтротрансмиссия допамина. Также описаны фармацевтические композиции и способы, включающие применение соединений формулы (1) для лечения мужского бесплодия и подвижности сперматозоидов; сахарного диабета; нарушения толерантности к глюкозе; метаболического синдрома или синдрома X; синдрома поликистоза яичников; липогенеза и ожирения; миогенеза и хрупкости, например возрастного снижения физической активности; острой саркопении, например атрофии мышц и/или кахексии, связанной с ожогами, постельным режимом, неподвижностью конечностей, или обширным торакальным, абдоминальным и/или ортопедическим хирургическим вмешательством; сепсиса; потери волос, истончения волос и облысения и иммунодефицита.Международная заявка была опубликована вместе с отчетом о международном поиске.The present invention provides compounds of formula (1) in which R, R, R and R are as defined in the specification, and their pharmaceutically acceptable salts. The compounds of formula (1) have an inhibitory effect on cdk2 and GSK-3. Pharmaceutical compositions and methods, including the compounds of formula (1) for the treatment and prevention of diseases and conditions, including abnormal cell growth, such as cancer, and neurodegenerative diseases and conditions and conditions that are affected by the neutrotransmission of dopamine. Pharmaceutical compositions and methods are also described, including the use of compounds of formula (1) for the treatment of male infertility and sperm motility; diabetes; impaired glucose tolerance; metabolic syndrome or syndrome X; polycystic ovary syndrome; lipogenesis and obesity; myogenesis and fragility, such as age-related decline in physical activity; acute sarcopenia, such as muscle atrophy and / or cachexia associated with burns, bed rest, immobility of the limbs, or extensive thoracic, abdominal and / or orthopedic surgery; sepsis; hair loss, thinning hair and alopecia and immunodeficiency. The international application was published along with an international search report.

EA200300205A 2000-08-31 2001-08-24 DERIVATIVES OF PYRAZOL AND THEIR APPLICATION AS PROTEINKINASE INHIBITORS EA200300205A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22941500P 2000-08-31 2000-08-31
PCT/IB2001/001540 WO2002018346A1 (en) 2000-08-31 2001-08-24 Pyrazole derivatives and their use as protein kinase inhibitors

Publications (1)

Publication Number Publication Date
EA200300205A1 true EA200300205A1 (en) 2003-06-26

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA200300205A EA200300205A1 (en) 2000-08-31 2001-08-24 DERIVATIVES OF PYRAZOL AND THEIR APPLICATION AS PROTEINKINASE INHIBITORS

Country Status (38)

Country Link
EP (1) EP1313710A1 (en)
JP (1) JP2004507526A (en)
KR (1) KR20030027093A (en)
CN (1) CN1518543A (en)
AP (1) AP2001002266A0 (en)
AR (1) AR035345A1 (en)
AU (1) AU2001280009A1 (en)
BG (1) BG107455A (en)
BR (1) BR0113574A (en)
CA (1) CA2420363A1 (en)
CR (1) CR6881A (en)
CZ (1) CZ2003468A3 (en)
DO (1) DOP2001000243A (en)
DZ (1) DZ3398A1 (en)
EA (1) EA200300205A1 (en)
EC (1) ECSP034480A (en)
EE (1) EE200300085A (en)
GT (1) GT200100179A (en)
HN (1) HN2001000192A (en)
HR (1) HRP20030140A2 (en)
HU (1) HUP0302669A3 (en)
IL (1) IL154016A0 (en)
IS (1) IS6687A (en)
MA (1) MA26946A1 (en)
MX (1) MXPA03001785A (en)
NO (1) NO20030958L (en)
NZ (1) NZ523656A (en)
OA (1) OA12368A (en)
PA (1) PA8528101A1 (en)
PE (1) PE20020470A1 (en)
PL (1) PL360742A1 (en)
SK (1) SK2002003A3 (en)
SV (1) SV2002000618A (en)
TN (1) TNSN01132A1 (en)
UY (1) UY26909A1 (en)
WO (1) WO2002018346A1 (en)
YU (1) YU14703A (en)
ZA (1) ZA200301064B (en)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE556713T1 (en) 1999-01-13 2012-05-15 Bayer Healthcare Llc OMEGA-CARBOXYARYL SUBSTITUTED DIPHENYL UREAS AS P38 KINASE INHIBITORS
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317452B1 (en) 2000-09-15 2006-05-17 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6653301B2 (en) 2000-12-21 2003-11-25 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20040198799A1 (en) * 2001-09-27 2004-10-07 Brondyk William H. Methods of increasing endogenous testosterone levels
EP2324825A1 (en) 2002-02-11 2011-05-25 Bayer Healthcare LLC Aryl ureas with angiogenesis inhibiting activity
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
JP2006501191A (en) * 2002-07-17 2006-01-12 ファルマシア・イタリア・エス・ピー・エー Heterobicyclic pyrazole derivatives as kinase inhibitors
BR0315158A (en) 2002-10-09 2005-08-16 Pfizer Prod Inc Pyrazole Compounds for the Treatment of Neurodegenative Disorders
EP1551842A1 (en) * 2002-10-15 2005-07-13 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
ATE410415T1 (en) 2003-02-27 2008-10-15 Smithkline Beecham Corp NEW CONNECTIONS
PT1626714E (en) 2003-05-20 2007-08-24 Bayer Pharmaceuticals Corp Diaryl ureas for diseases mediated by pdgfr
CA2528496C (en) * 2003-06-05 2011-04-12 Elan Pharmaceuticals, Inc. Acylated amino acid amidyl pyrazoles and related compounds
EP2256106B1 (en) * 2003-07-22 2015-05-06 Astex Therapeutics Limited 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
SI1663978T1 (en) 2003-07-23 2008-02-29 Bayer Pharmaceuticals Corp Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
MXPA06000933A (en) * 2003-07-25 2006-03-30 Pfizer Aminopyrazole compounds and use as chk1 inhibitors.
ATE473967T1 (en) * 2003-11-26 2010-07-15 Pfizer Prod Inc AMINOPYRAZOLE DERIVATIVES AS GSK-3 INHIBITORS
US7244757B2 (en) 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
EP1742921A2 (en) * 2004-04-21 2007-01-17 AstraZeneca AB Pyrazole derivatives useful for the treatment of cancer
ATE517885T1 (en) 2004-04-30 2011-08-15 Bayer Healthcare Llc SUBSTITUTED PYRAZOLYL UREA DERIVATIVES FOR THE TREATMENT OF CANCER
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
US7521560B2 (en) 2004-06-29 2009-04-21 Rigel Pharmaceuticals, Inc. 2-substituted quinoline compounds and their uses
US7491720B2 (en) 2004-10-29 2009-02-17 Banyu Pharmaceutical Co., Ltd. Aminopyridine derivatives having Aurora A selective inhibitory action
WO2006055831A2 (en) 2004-11-17 2006-05-26 Miikana Therapeutics, Inc. Kinase inhibitors
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (en) 2005-01-21 2007-06-27 Astex Therapeutics Ltd PIPERIDIN ADDITION SALTS 4-IL-ACID AMID 4- (2,6-DICLORO-BENZOILAMINO) 1H-PIRAZOL-3-CARBOXILICO.
CN101155800B (en) 2005-02-04 2012-05-23 阿斯利康(瑞典)有限公司 Pyrazolylaminopyridine derivatives useful as kinase inhibitors
WO2006085685A1 (en) * 2005-02-09 2006-08-17 Takeda Pharmaceutical Company Limited Pyrazole compound
DK1853588T3 (en) 2005-02-16 2008-09-15 Astrazeneca Ab Chemical compounds
BRPI0610184A2 (en) 2005-05-16 2012-09-25 Astrazeneca Ab compound, pharmaceutically acceptable salt of a compound, process for preparing a compound or a pharmaceutically acceptable salt thereof, use of a compound or a pharmaceutically acceptable salt thereof, methods for inhibiting trk activity, for cancer treatment or prophylaxis and for producing an antiproliferative effect on a warm-blooded animal, and, pharmaceutical composition
EP1741708A1 (en) * 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals
US7678363B2 (en) 2005-08-26 2010-03-16 Braincells Inc Methods of treating psychiatric conditions comprising administration of muscarinic agents in combination with SSRIs
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
CA2622352C (en) 2005-09-30 2014-05-27 Miikana Therapeutics, Inc. Substituted pyrazole compounds
JP2009512711A (en) 2005-10-21 2009-03-26 ブレインセルス，インコーポレイティド Regulation of neurogenesis by PDE inhibition
CA2626375A1 (en) 2005-10-28 2007-05-03 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
AU2006308889A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. GABA receptor mediated modulation of neurogenesis
ES2533241T3 (en) 2005-11-03 2015-04-08 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
US7572809B2 (en) * 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
EP2377531A2 (en) 2006-05-09 2011-10-19 Braincells, Inc. Neurogenesis by modulating angiotensin
WO2008047364A2 (en) 2006-10-18 2008-04-24 Periness Ltd. Method and pharmacological composition for the diagnosis and treatment of male sub-fertility
MX2009004140A (en) 2006-10-21 2009-07-10 Abbott Gmbh & Co Kg Heterocyclic compounds and their use as glycogen synthase kinase 3 inhibitors.
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US7737149B2 (en) * 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
MX2009007916A (en) 2007-01-24 2009-07-31 Glaxo Group Ltd Pharmaceutical compositions comprising 3, 5-diamin0-6- (2, 3-dichl0phenyl) -l, 2, 4-triazine or r (-) -2, 4-diamino-5- (2, 3-dichlorophenyl) -6-fluoromethyl pyrimidine and an nk1.
SG183036A1 (en) 2007-07-17 2012-08-30 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
WO2009017453A1 (en) * 2007-07-30 2009-02-05 Astrazeneca Ab New therapeutic combination of an antipsychotic and a gsk3 inhibitor 958
MY180558A (en) 2007-09-21 2020-12-02 Array Biopharma Inc Pyridin-2-yl-amino-1,2,4- theiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
JPWO2009130900A1 (en) * 2008-04-24 2011-08-11 日本曹達株式会社 Oxime derivatives, intermediate compounds and plant disease control agents
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
MX349923B (en) 2009-04-03 2017-08-21 Hoffmann La Roche Propane- i-sulfonic acid {3- [5- (4 -chloro-phenyl) -1h-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof.
EP2488511A1 (en) * 2009-10-02 2012-08-22 Vertex Pharmaceuticals Incorporated Pyrazole inhibitors of phosphatidylinositol 3-kinase
ES2633317T3 (en) 2009-11-06 2017-09-20 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications for it
JP5998142B2 (en) 2010-09-27 2016-09-28 アボット ゲーエムベーハー ウント カンパニー カーゲー Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
MY162950A (en) 2011-02-07 2017-07-31 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
TWI558702B (en) 2011-02-21 2016-11-21 普雷辛肯公司 Solid forms of a pharmaceutically active substance
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
MX2016001934A (en) 2013-08-16 2016-06-10 Merck Patent Gmbh 3-substituted cyclopentylamine derivatives.
CN106580986B (en) * 2016-11-28 2017-09-15 王保亮 A kind of pharmaceutical composition for treating teen bra
CA3125353A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
CA3125350A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Irreversible inhibitors of menin-mll interaction
AU2020213761C1 (en) * 2019-01-31 2023-08-10 Pfizer Inc. 3-carbonylamino-5-cyclopentyl-1 Fi-pyrazole compounds having inhibitory activity on CDK2
TW202229268A (en) * 2020-12-22 2022-08-01 大陸商上海拓界生物醫藥科技有限公司 Cdk2 inhibitor and preparation method thereof
UY39832A (en) 2021-06-28 2023-01-31 Blueprint Medicines Corp CDK2 INHIBITORS
TW202317564A (en) * 2021-07-01 2023-05-01 大陸商上海拓界生物醫藥科技有限公司 Cdk2 inhibitor, a preparation method and a use thereof
WO2023083201A1 (en) * 2021-11-09 2023-05-19 上海拓界生物医药科技有限公司 Aminopyrazole derivative, and preparation method therefor and use thereof
WO2023092088A1 (en) * 2021-11-19 2023-05-25 Blueprint Medicines Corporation Cdk2 inhibitors and methods of making and using same
WO2023239629A1 (en) * 2022-06-06 2023-12-14 Plexium, Inc. Compounds and pharmaceutical compositions that degrade cdk2

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ID26620A (en) * 1997-12-22 2001-01-25 Bayer Ag OBSTACLES IN RAF KINASE USING SUBSTITUTED HETEROSICLIC URES
KR100579792B1 (en) * 1998-05-13 2006-05-12 동화약품공업주식회사 Novel 2,5-pyridinedicarboxylic acid derivatives
GB9811427D0 (en) * 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
EP1199306B1 (en) * 1999-07-26 2005-12-07 Banyu Pharmaceutical Co., Ltd. Biarylurea derivatives
US6387900B1 (en) * 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
AU4971400A (en) * 1999-08-12 2001-03-13 Pharmacia & Upjohn Company 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
EE200200275A (en) * 1999-11-30 2003-10-15 Pfizer Products Inc. 2,4-Diaminopyrimidine compounds used as immunosuppressants
JP2004501083A (en) * 2000-04-18 2004-01-15 アゴーロン・ファーマシューティカルズ・インコーポレイテッド Pyrazole for inhibiting protein kinases

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