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

DERIVATIVES OF PYRAZOL AND THEIR APPLICATION AS PROTEINKINASE INHIBITORS

Info

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
Authority
EA
Eurasian Patent Office
Prior art keywords
formula
compounds
conditions
syndrome
pharmaceutical compositions
Prior art date
Application number
EA200300205A
Other languages
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.)
Filing date
Publication date
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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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

ID=22861151

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)

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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 (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000041698A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
RU2319693C9 (en) 1999-01-13 2008-08-20 Байер Копэрейшн Derivatives of urea (variants), pharmaceutical composition (variants) and method for treatment of diseases associated with cancer cells growth (variants)
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
CA2422367C (en) 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 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
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
WO2002059111A2 (en) 2000-12-21 2002-08-01 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CA2458661A1 (en) * 2001-09-27 2003-04-03 Applied Research Systems Ars Holding N.V. Methods of increasing endogenous testosterone levels
WO2003068228A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
DE60320560T2 (en) * 2002-07-17 2008-12-11 Pfizer Italia S.R.L. Heterocyclic pyrazole derivatives as kinase inhibitors
JP4733388B2 (en) 2002-08-02 2011-07-27 バーテックス ファーマシューティカルズ インコーポレイテッド Pyrazole compositions useful as inhibitors of GSK-3
JP2006504725A (en) * 2002-10-09 2006-02-09 ファイザー・プロダクツ・インク Pyrazole compounds for the treatment of neurodegenerative disorders
US7582630B2 (en) * 2002-10-15 2009-09-01 Smithkline Beecham Corporation Pyradazine compounds as GSK-3 inhibitors
WO2004076414A2 (en) 2003-02-27 2004-09-10 Smithkline Beecham Corporation Novel compounds
DE602004007382T2 (en) 2003-05-20 2008-04-17 Bayer Pharmaceuticals Corp., West Haven DIARYL UREAS FOR PDGFR MEDIATED DISEASES
EP1633350B1 (en) * 2003-06-05 2012-10-03 Elan Pharmaceuticals, Inc. Acylated amino acid amidyl pyrazoles and related compounds
JP4681548B2 (en) 2003-07-22 2011-05-11 アステックス・セラピューティクス・リミテッド 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase (CDK) and glycogen synthetase kinase-3 (GSK-3) modulators
GB0317127D0 (en) * 2003-07-22 2003-08-27 Astex Technology Ltd Pharmaceutical compounds
NZ544920A (en) 2003-07-23 2009-11-27 Bayer Healthcare Llc 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide and metabolites for the treatment and prevention of diseases and conditions
JP2006528661A (en) * 2003-07-25 2006-12-21 ファイザー・インク Aminopyrazole compounds and use as CHK1 inhibitors
DE602004028150D1 (en) * 2003-11-26 2010-08-26 Pfizer Prod Inc AMINOPYRAZOL DERIVATIVES AS GSK-3 INHIBITORS
PT1696920E (en) 2003-12-19 2015-01-14 Plexxikon Inc Compounds and methods for development of ret modulators
US7244757B2 (en) 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
JP2007533717A (en) * 2004-04-21 2007-11-22 アストラゼネカ アクチボラグ Compound
WO2005110994A2 (en) 2004-04-30 2005-11-24 Bayer Pharmaceuticals Corporation Substituted pyrazolyl urea derivatives useful in the treatment of cancer
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
EP1781637A1 (en) * 2004-06-29 2007-05-09 Rigel Pharmaceuticals, Inc. 2-substituted quinoline compounds and their uses as inhibitors of the ige receptor signaling cascade
US7491720B2 (en) 2004-10-29 2009-02-17 Banyu Pharmaceutical Co., Ltd. Aminopyridine derivatives having Aurora A selective inhibitory action
BRPI0517737A (en) 2004-11-17 2008-10-21 Miikana Therapeutics Inc 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.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
ATE530545T1 (en) 2005-02-04 2011-11-15 Astrazeneca Ab PYRAZOLYLAMINOPYRIDINE DERIVATIVES SUITABLE AS KINASE INHIBITORS
US20090156582A1 (en) * 2005-02-09 2009-06-18 Tetsuya Tsukamoto Pyrazole Compound
RU2405780C2 (en) 2005-02-16 2010-12-10 Астразенека Аб Chemical compounds
WO2006123113A2 (en) 2005-05-16 2006-11-23 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
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
EP2275096A3 (en) 2005-08-26 2011-07-13 Braincells, Inc. Neurogenesis via modulation of the muscarinic receptors
EP2258359A3 (en) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenesis by muscarinic receptor modulation with sabcomelin
BRPI0616630B8 (en) 2005-09-30 2021-05-25 Miikana Therapeutics Inc substituted pyrazole compounds
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
TW200800963A (en) 2005-10-28 2008-01-01 Astrazeneca Ab Chemical compounds
JP2009513672A (en) 2005-10-31 2009-04-02 ブレインセルス，インコーポレイティド GABA receptor-mediated regulation of neurogenesis
BRPI0619706A2 (en) 2005-11-03 2011-10-11 Vertex Pharma compound, composition, method for inhibiting aurora kinase activity in a biological sample, method for treating a proliferative disorder in a patient, method for treating cancer in an individual
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
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
BRPI0717439A2 (en) * 2006-10-18 2013-11-19 Periness Ltd PHARMACEUTICAL COMPOSITION, AND METHODS FOR TREATING MALE SUBFERTILITY, FOR DETERMINING A FERTLITY STATUS IN A MALE SEX, FOR ASSISTED REPRODUCTION TECHNIQUE FOR A SPECULAR SPULLET REPRODUCTION FOR CULLED SPLIT USE IN AN AUXILIARY REPRODUCTION TECHNIQUE.
US8642598B2 (en) 2006-10-21 2014-02-04 Abbvie Inc. 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
AU2008208920A1 (en) 2007-01-24 2008-07-31 Glaxo Group Limited 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
MX2010002772A (en) 2007-09-21 2010-03-31 Array Biopharma Inc Pyridin-2 -yl-amino-i, 2, 4 -thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus.
WO2009130900A1 (en) * 2008-04-24 2009-10-29 日本曹達株式会社 Oxime derivative, intermediate compound, and plant disease control agent
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
AU2010232670B2 (en) 2009-04-03 2015-07-09 F. Hoffmann-La Roche Ag 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
JP2013506691A (en) * 2009-10-02 2013-02-28 バーテックス ファーマシューティカルズ インコーポレイテッド 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
CN103119035B (en) 2010-09-27 2015-09-30 雅培股份有限两合公司 Heterogeneous ring compound and they are as the purposes of GSK-3 inhibitor
US9090592B2 (en) 2010-12-30 2015-07-28 AbbVie Deutschland GmbH & Co. KG Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors
CN103517710B (en) 2011-02-07 2017-05-31 普莱希科公司 For the compound of kinases regulation
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
CA2921265C (en) * 2013-08-16 2021-03-23 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
AU2019417833B2 (en) 2018-12-31 2024-11-07 Biomea Fusion, Inc. Irreversible inhibitors of menin-MLL interaction
EP3906029A4 (en) 2018-12-31 2022-09-21 Biomea Fusion, LLC 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
US12479816B2 (en) 2019-02-08 2025-11-25 University of Pittsburgh—of the Commonwealth System of Higher Education 20-HETE formation inhibitors
CA3194868A1 (en) * 2020-10-16 2022-04-21 Georg Winter Heterocyclic cullin ring ubiquitin ligase compounds and uses thereof
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
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
UY39832A (en) 2021-06-28 2023-01-31 Blueprint Medicines Corp CDK2 INHIBITORS
WO2023274397A1 (en) * 2021-07-01 2023-01-05 上海拓界生物医药科技有限公司 Cdk2 inhibitor, preparation method therefor and use thereof
EP4384179A1 (en) 2021-08-11 2024-06-19 Biomea Fusion, Inc. Covalent inhibitors of menin-mll interaction for diabetes mellitus
CN119816500A (en) 2021-08-20 2025-04-11 拜欧米富士恩公司 Crystalline forms of the irreversible menin-MLL inhibitor N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide for the treatment of cancer
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
WO2024155719A1 (en) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Crystalline forms of n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-piperidinyl]methyl]-2- pyridinecarboxamide as a covalentinhibitor of menin-mll interaction
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2315717C (en) * 1997-12-22 2011-02-01 Bayer Corporation Inhibition of raf kinase using substituted heterocyclic ureas
KR100579792B1 (en) * 1998-05-13 2006-05-12 동화약품공업주식회사 New 2,5-pyridinedicarboxylic acid derivatives
GB9811427D0 (en) * 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
CA2380389A1 (en) * 1999-07-26 2001-02-01 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
US7034049B1 (en) * 1999-08-12 2006-04-25 Pharmacia Italia S.P.A. 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents
OA12097A (en) * 1999-11-30 2006-05-04 Pfizer Prod Inc 2,4-Diaminopyrimidine compounds useful as immunosuppressants.
WO2001079198A1 (en) * 2000-04-18 2001-10-25 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinase

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