MA26946A1 - Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases. - Google Patents

Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases.

Info

Publication number
MA26946A1
MA26946A1 MA27050A MA27050A MA26946A1 MA 26946 A1 MA26946 A1 MA 26946A1 MA 27050 A MA27050 A MA 27050A MA 27050 A MA27050 A MA 27050A MA 26946 A1 MA26946 A1 MA 26946A1
Authority
MA
Morocco
Prior art keywords
formula
compounds
syndrome
kinase inhibitors
pyrazole derivatives
Prior art date
Application number
MA27050A
Other languages
English (en)
Inventor
Christopher Blair Cooper
Christopher John Helal
Mark Allen Sanner
Travis T Wager
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of MA26946A1 publication Critical patent/MA26946A1/fr

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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

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  • 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

DEPOSANT Société dite : PFIZER PRODUCTS INC. REVENDICATION DE PRIORITES US 31 Aoét 2000 60/229,415 Voir en annexe le titre de l'invention et le texte de l'abrégé Dérivés de pyrazole nouveaux et leur utilisation comme inhibiteurs de protéine-kinases L'invention propose des composés de formule (1) dans laquelle R1, R2, R3 et R4 répondent aux définitions, et leurs sels pharmaceutiquement acceptables. Les composés de formule (1) sont indiqués en tant qu'agents ayant une activité inhibitrice de cdk2, et GSK-3. Des compositions pharmaceutiques et méthodes comprenant des composés de formule (1) pour le traitement et la prévention de maladies et d'affections comprenant une croissance cellulaire anormale, telle qu'un cancer, et des maladies et affections neuro-dégénératives ainsi que celles affectées par la neurotransmission de la dopamine. Il est décrit également des compositions et méthodes pharmaceutiques, comprenant des composés de formule (1) pour le traitement de la stérilité masculine et de la motilité du sperme ; du diabète sucré ; d'une tolérance entravée au glucose ; du syndrome métabolique ou syndrome X ; du syndrome d'ovaire polykystique ; de 1'adipogénèse et de l'obésité ; de la myogénèse et de la fragilité, par exemple du déclin des performances physiques dé à l'??ge ; de la sarcopénie aigue, par exemple de l'atrophie musculaire et/ou de la cachexie associées aux brélures, à l'état alité, à une immobilisation des membres ou à une intervention chirurgicale thoracique, abdominale et/ou orthopédique importante ; de la septicémie ; de la perte des cheveux, de l'éclaircissement capillaire et de la calvitie ; et d'une immunodéficience.
MA27050A 2000-08-31 2003-02-21 Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases. MA26946A1 (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22941500P 2000-08-31 2000-08-31

Publications (1)

Publication Number Publication Date
MA26946A1 true MA26946A1 (fr) 2004-12-20

Family

ID=22861151

Family Applications (1)

Application Number Title Priority Date Filing Date
MA27050A MA26946A1 (fr) 2000-08-31 2003-02-21 Derives de pyrazole nouveaux et leur utilisation comme inhibiteurs de proteine-kinases.

Country Status (39)

Country Link
EP (1) EP1313710A1 (fr)
JP (1) JP2004507526A (fr)
KR (1) KR20030027093A (fr)
CN (1) CN1518543A (fr)
AP (1) AP2001002266A0 (fr)
AR (1) AR035345A1 (fr)
AU (1) AU2001280009A1 (fr)
BG (1) BG107455A (fr)
BR (1) BR0113574A (fr)
CA (1) CA2420363A1 (fr)
CR (1) CR6881A (fr)
CZ (1) CZ2003468A3 (fr)
DO (1) DOP2001000243A (fr)
DZ (1) DZ3398A1 (fr)
EA (1) EA200300205A1 (fr)
EC (1) ECSP034480A (fr)
EE (1) EE200300085A (fr)
GT (1) GT200100179A (fr)
HN (1) HN2001000192A (fr)
HR (1) HRP20030140A2 (fr)
HU (1) HUP0302669A3 (fr)
IL (1) IL154016A0 (fr)
IS (1) IS6687A (fr)
MA (1) MA26946A1 (fr)
MX (1) MXPA03001785A (fr)
NO (1) NO20030958D0 (fr)
NZ (1) NZ523656A (fr)
OA (1) OA12368A (fr)
PA (1) PA8528101A1 (fr)
PE (1) PE20020470A1 (fr)
PL (1) PL360742A1 (fr)
PY (1) PY0121331A (fr)
SK (1) SK2002003A3 (fr)
SV (1) SV2002000618A (fr)
TN (1) TNSN01132A1 (fr)
UY (1) UY26909A1 (fr)
WO (1) WO2002018346A1 (fr)
YU (1) YU14703A (fr)
ZA (1) ZA200301064B (fr)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2298311B1 (fr) 1999-01-13 2012-05-09 Bayer HealthCare LLC Urées de diphényle à substitution omega-carboxyaryle en tant qu'inhibiteurs de la p38 kinase
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
US7351834B1 (en) 1999-01-13 2008-04-01 Bayer Pharmaceuticals Corporation ω-Carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
AU2001290912A1 (en) 2000-09-15 2002-03-26 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
US6660731B2 (en) 2000-09-15 2003-12-09 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
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
BR0116493A (pt) 2000-12-21 2003-09-30 Vertex Pharma Compostos de pirazol úteis como inibidores de proteìna cinase
PT1441724E (pt) * 2001-09-27 2007-10-15 Serono Lab Métodos para aumentar os níveis endógenos de testosterona
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
WO2003068229A1 (fr) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation N-oxydes de pyridine, de quinoline, et d'isoquinoline en tant qu'inhibiteurs de kinase
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004007504A1 (fr) * 2002-07-17 2004-01-22 Pharmacia Italia S.P.A. Derives de pyrazole heterobicycliques utilises comme inhibiteurs de kinase
MXPA05001367A (es) 2002-08-02 2005-04-28 Vertex Pharma Composiciones de pirazol utiles como inhibidores de gsk-3.
JP2006504725A (ja) 2002-10-09 2006-02-09 ファイザー・プロダクツ・インク 神経変性障害治療用ピラゾール化合物
WO2004035588A1 (fr) * 2002-10-15 2004-04-29 Smithkline Beecham Corporation Composes de pyradazine utiles comme inhibiteurs de gsk-3
EP1597234B1 (fr) * 2003-02-27 2008-10-08 Smithkline Beecham Corporation Nouveaux composes
EP1636585B2 (fr) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl-urees presentant une activite d'inhibition des kinases
AU2004258841B8 (en) * 2003-06-05 2010-01-07 Elan Pharmaceuticals, Inc. Acylated amino acid amidyl pyrazoles and related compounds
EP2256106B1 (fr) * 2003-07-22 2015-05-06 Astex Therapeutics Limited Composes 1H-pyrazole 3,4-disubstitues et leur utilisation en tant que kinases dependant des cyclines (CDK) et modulateurs de la glycogene synthase kinase-3 (GSK-3)
GB0317127D0 (en) * 2003-07-22 2003-08-27 Astex Technology Ltd Pharmaceutical compounds
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
JP2006528661A (ja) * 2003-07-25 2006-12-21 ファイザー・インク アミノピラゾール化合物およびchk1阻害剤としての使用
CA2547283C (fr) * 2003-11-26 2010-11-09 Pfizer Products Inc. Derives d'aminopyrazole en tant qu'inhibiteurs de la gsk-3
JP5138938B2 (ja) 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Ret調節剤の開発のための化合物および方法
US7244757B2 (en) * 2004-04-01 2007-07-17 Pfizer Inc Pyrazole-amine compounds for the treatment of neurodegenerative disorders
EP1742921A2 (fr) * 2004-04-21 2007-01-17 AstraZeneca AB Derives de pyrazole pour le traitement du cancer
US7838524B2 (en) 2004-04-30 2010-11-23 Bayer Healthcare Llc 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
WO2006004865A1 (fr) * 2004-06-29 2006-01-12 Rigel Pharmaceuticals, Inc. Composés de quinoléine de substitution et leurs utilisations comme inhibiteurs de la cascade de signalement du récepteur d'immunoglobuline (ige)
US7491720B2 (en) 2004-10-29 2009-02-17 Banyu Pharmaceutical Co., Ltd. Aminopyridine derivatives having Aurora A selective inhibitory action
MX2007005857A (es) 2004-11-17 2007-10-10 Mikana Therapeutics Inc Inhibidores de cinasa.
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 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
DK2383268T3 (en) 2005-02-04 2015-09-14 Astrazeneca Ab PYRAZOLYLAMINOPYRIDINDERIVATER useful as kinase inhibitors
EP1847531A4 (fr) * 2005-02-09 2009-04-22 Takeda Pharmaceutical Derive de pyrazole
KR101362621B1 (ko) 2005-02-16 2014-02-13 아스트라제네카 아베 화합물
CA2608009A1 (fr) 2005-05-16 2006-11-23 Astrazeneca Ab Composes chimiques
EP1741708A1 (fr) 2005-06-28 2007-01-10 Sanofi-Aventis Deutschland GmbH Amides heterocycliques substitués contenant un linker cyclique ou insaturé, et leur utilisation comme agent pharmaceutique
EP2275096A3 (fr) 2005-08-26 2011-07-13 Braincells, Inc. Neurogenese par modulation des recepteurs muscariniques
EP2258357A3 (fr) 2005-08-26 2011-04-06 Braincells, Inc. Neurogenèse avec inhibiteur de l'acetylcholinestérase
BRPI0616630B8 (pt) 2005-09-30 2021-05-25 Miikana Therapeutics Inc compostos de pirazol substituídos
WO2007047978A2 (fr) 2005-10-21 2007-04-26 Braincells, Inc. Modulation de la neurogenese par inhibition de la pde
BRPI0618011A2 (pt) 2005-10-28 2011-08-16 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, métodos para produzir um efeito anti-proliferativo e um efeito pró-apoptósico em um animal de sangue quente, para tratar doença e para produzir um efeito inibidor de jak em um animal de sangue quente
EP2314289A1 (fr) 2005-10-31 2011-04-27 Braincells, Inc. Modulation de la neurogenese dont la médiation est assurée par récepteur gaba
JP5249770B2 (ja) 2005-11-03 2013-07-31 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 キナーゼインヒビターとして有用なアミノピリジン
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
EP2021000A2 (fr) 2006-05-09 2009-02-11 Braincells, Inc. Neurogenèse par modulation de l'angiotensine
DK2086642T3 (da) * 2006-10-18 2014-09-29 Periness Ltd Dnase til behandling af subfertilitet hos mænd
WO2008046919A2 (fr) * 2006-10-21 2008-04-24 Abbott Gmbh & Co. Kg Composés hétérocycliques et leur utilisation comme inhibiteurs de la glycogène synthase kinase 3
WO2008063888A2 (fr) 2006-11-22 2008-05-29 Plexxikon, Inc. Composés modulant l'activité de c-fms et/ou de c-kit et utilisations associées
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
US8093268B2 (en) 2007-01-24 2012-01-10 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)
JP2010533729A (ja) 2007-07-17 2010-10-28 プレキシコン,インコーポレーテッド キナーゼ調節のための化合物と方法、及びそのための適応
WO2009017453A1 (fr) * 2007-07-30 2009-02-05 Astrazeneca Ab Nouvelle combinaison thérapeutique d'antipsychotique et d'inhibiteur de gsk3 958
EA019104B1 (ru) 2007-09-21 2014-01-30 Эррей Биофарма Инк. Активаторы глюкокиназы
JPWO2009130900A1 (ja) * 2008-04-24 2011-08-11 日本曹達株式会社 オキシム誘導体、中間体化合物および植物病害防除剤
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CA2738573C (fr) 2009-04-03 2013-02-19 F. Hoffmann-La Roche Ag Compositions et utilisations associees
JP2013506691A (ja) * 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 ホスファチジルイノシトール3−キナーゼのピラゾール阻害薬
JP2013510166A (ja) 2009-11-06 2013-03-21 プレキシコン インコーポレーテッド キナーゼ調節のための化合物、方法およびその適用
US9266855B2 (en) 2010-09-27 2016-02-23 AbbVie Deutschland GmbH & Co. KG 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
PE20141360A1 (es) 2011-02-07 2014-10-13 Plexxikon Inc Compuestos y metodos para la modulacion de quinasas e indicaciones para los mismos.
TWI558702B (zh) 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
RU2016109243A (ru) 2013-08-16 2017-09-20 Мерк Патент Гмбх 3-замещенные производные циклопентиламина
CN106580986B (zh) * 2016-11-28 2017-09-15 王保亮 一种治疗少弱精子症的药物组合物
TW202043205A (zh) 2018-12-31 2020-12-01 美商拜歐米富士恩有限公司 Menin-mll相互作用之抑制劑
WO2020142557A1 (fr) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibiteurs irréversibles de l'interaction ménine-mll
CA3128155C (fr) * 2019-01-31 2023-09-19 Pfizer Inc. Composes 3-carbonylamino-5-cyclopentyl-1h-pyrazole ayant une activite inhibitrice sur cdk2
US12479816B2 (en) 2019-02-08 2025-11-25 University of Pittsburgh—of the Commonwealth System of Higher Education 20-HETE formation inhibitors
US20240132485A1 (en) * 2020-10-16 2024-04-25 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh Heterocyclic cullin ring ubiquitin ligase compounds and uses thereof
TW202229268A (zh) * 2020-12-22 2022-08-01 大陸商上海拓界生物醫藥科技有限公司 Cdk2抑制劑及其製備方法
CA3217792A1 (fr) 2021-05-07 2022-11-10 Kymera Therapeutics, Inc Agents de degradation de cdk2 et leurs utilisations
EP4347582A4 (fr) * 2021-05-27 2025-05-07 Boundless Bio, Inc. Inhibiteurs de la checkpoint kinase 1 (chk1) et leurs utilisations
WO2022266190A1 (fr) 2021-06-16 2022-12-22 Blueprint Medicines Corporation Pyrimidinyl-pyrazoles substitués utiles en tant qu'inhibiteurs de cdk2
CN117897384A (zh) 2021-06-28 2024-04-16 缆图药品公司 Cdk2抑制剂
TW202317564A (zh) * 2021-07-01 2023-05-01 大陸商上海拓界生物醫藥科技有限公司 Cdk2抑制劑及其製備方法和用途
JP7891524B2 (ja) 2021-08-11 2026-07-16 バイオメア フュージョン,インコーポレイテッド 真性糖尿病に対するメニン-mll相互作用の共有結合性阻害剤
MX2024002189A (es) 2021-08-20 2024-06-11 Biomea Fusion Inc Forma cristalina de n-[4-[4-(4-morfolinil)-7h-pirrolo[2,3-d]pirimi din-6-il]fenil]-4-[[3(r)-[(1-oxo)-2-propen-1-il)amino]-1-piperidi nil]metil]-2-piridinacarboxamida, un inhibidor irreversible de menina-mll para el tratamiento del cancer.
TW202325280A (zh) * 2021-11-09 2023-07-01 大陸商上海拓界生物醫藥科技有限公司 一種胺基吡唑衍生物及其製備方法和用途
WO2023092088A1 (fr) * 2021-11-19 2023-05-25 Blueprint Medicines Corporation Inhibiteurs de cdk2 et leurs procédés de fabrication et d'utilisation
WO2023239629A1 (fr) * 2022-06-06 2023-12-14 Plexium, Inc. Composés et compositions pharmaceutiques qui dégradent cdk2
WO2024155719A1 (fr) 2023-01-18 2024-07-25 Biomea Fusion, Inc. Formes cristallines de n-[4-[4-(4-morpholinyl)-7h-pyrrolo[2,3-d]pyrimidin-6-yl]phényl]-4-[[3(r)-[(l-oxo-2-propen-l-yl)amino]-l-pipéridinyl]méthyl]-2- pyridinecarboxamide en tant qu'inhibiteur covalent de l'interaction ménine-mll
WO2026024674A1 (fr) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Méthodes de traitement de cancers associés à skp2
TW202613099A (zh) * 2024-08-08 2026-04-01 大陸商上海美悅生物科技發展有限公司 取代的苯基化合物、及其藥物組合物和用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4437270B2 (ja) * 1997-12-22 2010-03-24 バイエル コーポレイション 置換複素環式尿素を用いたrafキナーゼの阻害
KR100579792B1 (ko) * 1998-05-13 2006-05-12 동화약품공업주식회사 신규 2,5-피리딘디카복실산 유도체
GB9811427D0 (en) * 1998-05-29 1998-07-22 Zeneca Ltd Chemical compounds
EP1199306B1 (fr) * 1999-07-26 2005-12-07 Banyu Pharmaceutical Co., Ltd. Derives de biaryluree
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
MXPA02001498A (es) * 1999-08-12 2003-07-21 Pharmacia & Italia S P A Derivados de 3(5)-amino-pirazol, procedimiento para la preparacion de los mismos y usos como agentes antitumorales.
BR0015995A (pt) * 1999-11-30 2002-08-06 Pfizer Prod Inc Compostos 2,4-diaminopirimidina úteis como imunossupressores
BR0110302A (pt) * 2000-04-18 2003-01-14 Agouron Pharma Compostos de pirazol para inibição de proteìnas cinase, sal e pró-droga farmaceuticamente aceitável, metabólito farmaceuticamente ativo ou sal farmaceuticamente aceitável de metabólito, composição farmacêutica, método de tratamento de condição doentia em mamìferos mediada pela atividade de proteìna cinase, método de modulação ou inibição da atividade de um receptor de proteìna cinase

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