AR035345A1 - Compuestos derivados de pirazol, composicion farmaceutica, compuestos intermediarios - Google Patents

Compuestos derivados de pirazol, composicion farmaceutica, compuestos intermediarios

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Publication number
AR035345A1
AR035345A1 ARP010104115A ARP010104115A AR035345A1 AR 035345 A1 AR035345 A1 AR 035345A1 AR P010104115 A ARP010104115 A AR P010104115A AR P010104115 A ARP010104115 A AR P010104115A AR 035345 A1 AR035345 A1 AR 035345A1
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Argentina
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straight
members
branched chain
independently selected
nr7r8
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ARP010104115A
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English (en)
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Pfizer Prod Inc
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Publication of AR035345A1 publication Critical patent/AR035345A1/es

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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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (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

Compuestos de la fórmula (1) donde R1 es un alquilo C1-8 de cadena lineal o ramificada, un alquenilo C2-8 de cadena lineal o ramificada, un alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, o heterobicicloalquilo (5-11 miembros); y donde R1 está opcionalmente sustituido con 1 a 6 sustituyentes R5 independientemente seleccionados de F, Cl, Br, I, nitro, ciano, -CF3, -NR7R8, -NR7C(=O)R8, -NR7C(=O)OR8, -NR7C(=O)NR8R9, -NR7S(=O)2R8, -NR7S(=O)2NR8R9, -OR7, OC(=O)R7, -OC(=O)OR7, -C(=O)OR7, -C(=O)R7, -C(=O)NR7R8, -OC(=O)NR7R8, -OC(=O)SR7, -SR7, -S(=O)R7, -S(=O)2R7, -S(=O)2NR7R8, y R7; R2 es H, -CH3, -CN o -C(=O)OR7; R3 es -C(=O)NR9-, -C(=O)O-, -C(=O)(CR10R11)n-, o -(CR10R11)n-; R4 es un alquilo C1-8 de cadena lineal o ramificada, un alquenilo C2-8 de cadena lineal o ramificada, un alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo (5-11 miembros), arilo C6-14, o heteroarilo (5-14 miembros); y donde R4 está opcionalmente sustituido con 1 a 3 sustituyentes R6 independientemente seleccionados de F, Cl, Br, I, nitro, ciano, -CF3, -NR7R8, -NR7C(=O)R8, NR7C(=O)OR8, -NR7C(=O)NR8R9, -NR7S(=O)2R8, -NR7S(=O)2NR8R9, -OR7, OC(=O)R7, -OC(=O)OR7, -C(=O)OR7, -C(=O)R7, -C(=O)NR7R8, -OC(=O)NR7R8, -OC(=O)SR7, -SR7, -S(=O)R7, -S(=O)2R7, -S(=O)2NR7R8, y R7; cada uno de R7, R8 y R9 se selecciona independientemente de H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo (5-11 miembros), arilo C6-14, y heteroarilo (5-14 miembros), donde R7, R8 y R9 están cada uno independientemente opcionalmente sustituidos con 1 a 6 sustituyentes independientemente seleccionados de F, Cl, Br, I, -NO2, -CN, -CF3, -NR10R11, -NR10C(=O)R11, -NR10C(=O)OR11, -NR10C(=O)NR11R12, -NR10S(=O)2R11, NR10S(=O)2NR11R12, -OR10, OC(=O)R10, -OC(=O)OR10, -OC(=O)NR10R11, -OC(=O)SR10, -SR10, -S(=O)R10, -S(=O)2R10, -S(=O)2NR10R11, -C(=O)R10, -C(=O)OR10, -C(=O)NR10R11 y R10; o, cuando R7 y R8 están como en NR7R8, ellos pueden, por el contrario, estar opcionalmente conectados para formar con el nitrógeno de NR7R8 al que está unido un resto heterocicloalquilo de 3 a 7 miembros en el anillo, comprendiendo dicho resto heterocicloalquilo opcionalmente 1 o 2 heteroátomos adicionales independientemente seleccionados de N, O y S; cada uno de R10, R11 y R12 se selecciona independientemente de H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo (5-11 miembros), arilo C6-14, y heteroarilo (5-14 miembros), donde R10, R11 y R12 están cada uno independientemente opcionalmente sustituidos con 1 a 6 sustituyentes independientemente seleccionados de F, Cl, Br, I, NO2, -CN, -CF3, -NR13R14, -NR13C(=O)R14, -NR13C(=O)OR14, -NR13C(=O)NR14R15, -NR13S(=O)2R14, -NR13S(=O)2NR14R15, -OR13, -OC(=O)R13, -OC(=O)OR13, -OC(=O)NR13R14, -OC(=O)SR13, -SR13, -S(=O)R13, -S(=O)2R13, -S(=O)2NR13R14, -C(=O)R13, -C(=O)OR13, -C(=O)NR13R14, y R13; cada uno de R13, R14 y R15 se selecciona independientemente de H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobiciciloalquilo (5-11 miembros), arilo C6-14, y heteroarilo (5-14 miembros), donde R13, R14 y R15 están cada uno independientemente opcionalmente sustituidos con 1 a 6 sustituyentes independientemente seleccionados de F, Cl, Br, I, NO2, -CN, -CF3, -NR16R17, -NR16C(=O)R17, -NR16C(=O)OR17, -NR16C(=O)NR17R18, -NR16S(=O)2R17, -NR16S(=O)2NR17R18, -OR16, -OC(=O)R16, -OC(=O)OR16, -OC(=O)NR16R17, -OC(=O)SR16, -SR16, -S(=O)R16, -(=O)2R16, -S(=O)2NR16R17, -C(=O)R16, - C(=O)OR16, -C(=O)NR16R17, y R16; cada uno de R16, R17 y R18 se selecciona independientemente de H, alquilo C1-8 de cadena lineal o ramificada, alquenilo C2-8 de cadena lineal o ramificada, alquinilo C2-8 de cadena lineal o ramificada, cicloalquilo C3-8, cicloalquenilo C4-8, heterocicloalquilo (3-8 miembros), bicicloalquilo C5-11, bicicloalquenilo C7-11, heterobicicloalquilo (5-11 miembros), arilo C6-14, y heteroarilo (5-14 miembros), n es 0, 1, 2 o 3; donde R10 y R11 en -C(=O)(CR10R11)n- y -(CR10R11)n- se definen independientemente para cada valor de n como se ha detallado antes; y sus sales farmacéuticamente aceptables. Se indica que los compuestos de la fórmula (1) tienen actividad para inhibir las cdk5, cdk2, GSK-3. Proporciona composiciones farmacéuticas y métodos que comprenden compuestos de la fórmula (1) para tratar y prevenir enfermedades y condiciones que implican crecimiento celular anormal, tales como el cáncer, y enfermedades y condiciones neurodegenerativas y las afectadas por la neurotransmisión de la dopamina. También se describen composiciones farmacéuticas y métodos que comprenden compuestos de la fórmula (1) para tratar la fertilidad masculina y la motilidad espermática; diabetes mellitus; deterioro de la tolerancia a la glucosa; síndrome metabólico o síndrome X; síndrome de poliquistosis ovárica, adipogénesis y obesidad; miogénesis y fragilidad, por ejemplo el deterioro de las características físicas relacionado con la edad; sarcopenia aguda, por ejemplo atrofia muscular y/o caquexia asociada con la quemaduras, reposo en cama, inmovilización de miembros, o importante cirugía torácica, abdominal y/o ortopédica; sepsis; caída del cabello, cabello ralo y calvicie; e inmunodeficiencia.
ARP010104115A 2000-08-31 2001-08-29 Compuestos derivados de pirazol, composicion farmaceutica, compuestos intermediarios AR035345A1 (es)

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US22941500P 2000-08-31 2000-08-31

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AR035345A1 true AR035345A1 (es) 2004-05-12

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

Families Citing this family (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP2298311B1 (en) 1999-01-13 2012-05-09 Bayer HealthCare LLC w-Carboxy aryl substituted diphenyl ureas as p38 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
MXPA03002294A (es) 2000-09-15 2005-09-08 Vertex Pharma Compuestos de pirazol utiles como inhibidores de proteina cinasa.
EP1345922B1 (en) 2000-12-21 2006-05-31 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE372114T1 (de) * 2001-09-27 2007-09-15 Applied Research Systems Verfahren zur erhöhung des testosteronspiegels
AU2003209119A1 (en) 2002-02-11 2003-09-04 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
WO2003068228A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Aryl ureas with angiogenesis inhibiting activity
DE60320560T2 (de) * 2002-07-17 2008-12-11 Pfizer Italia S.R.L. Heterobicyclische pyrazolderivate als kinaseinhibitoren
AU2003263518A1 (en) 2002-10-09 2004-05-04 Pfizer Products Inc. Pyrazole compounds for treatment of neurodegenerative disorders
AU2003301302A1 (en) * 2002-10-15 2004-05-04 Smithkline Beecham Corporation Pyradazine compounds as gsk-3 inhibitors
JP2006519234A (ja) * 2003-02-27 2006-08-24 スミスクライン ビーチャム コーポレーション 新規化合物
EP1636585B2 (en) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl ureas with kinase inhibiting activity
AU2004258841B8 (en) * 2003-06-05 2010-01-07 Elan Pharmaceuticals, Inc. Acylated amino acid amidyl pyrazoles and related compounds
KR101204247B1 (ko) 2003-07-22 2012-11-22 아스텍스 테라퓨틱스 리미티드 3,4-이치환된 1ｈ-피라졸 화합물 및 그의 시클린 의존성키나제 (ｃｄｋ) 및 글리코겐 합성효소 키나제-3(ｇｓｋ-3) 조정제로서 용도
ME00294B (me) 2003-07-23 2011-05-10 Bayer Pharmaceuticals Corp Fluoro supstituisana omega-karaboksiaril difenil urea za liječenje i prevenciju bolesti i stanja bolesti
WO2005009435A1 (en) * 2003-07-25 2005-02-03 Pfizer Inc. Aminopyrazole compounds and use as chk1 inhibitors
US7671072B2 (en) * 2003-11-26 2010-03-02 Pfizer 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
CA2564325A1 (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
WO2006004865A1 (en) * 2004-06-29 2006-01-12 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
JP2008520713A (ja) 2004-11-17 2008-06-19 ミイカナ セラピューティクス インコーポレイテッド キナーゼ阻害剤
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
WO2006082392A1 (en) 2005-02-04 2006-08-10 Astrazeneca Ab Pyrazolylaminopyridine derivatives useful as kinase inhibitors
JPWO2006085685A1 (ja) * 2005-02-09 2008-06-26 武田薬品工業株式会社 ピラゾール化合物
ES2308731T3 (es) 2005-02-16 2008-12-01 Astrazeneca Ab Compuestos quimicos.
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
WO2007025177A2 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
ES2535854T3 (es) 2005-09-30 2015-05-18 Miikana Therapeutics, Inc. Compuestos de pirazol sustituidos
EP2377530A3 (en) 2005-10-21 2012-06-20 Braincells, Inc. Modulation of neurogenesis by PDE inhibition
PT1945631E (pt) 2005-10-28 2012-10-15 Astrazeneca Ab Derivados de 4-(3-aminopirazole)pirimidina para utilização como inibidores da tirosina-cinase no tratamento do cancro
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
RU2427578C2 (ru) 2005-11-03 2011-08-27 Вертекс Фармасьютикалз Инкорпорейтед Аминопиримидины в качестве ингибиторов киназ
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
ES2524458T3 (es) 2006-10-18 2014-12-09 Periness Ltd. DNasa para el tratamiento de la subfertilidad masculina
JP5406030B2 (ja) 2006-10-21 2014-02-05 アボット ゲーエムベーハー ウント カンパニー カーゲー 複素環化合物およびそれらのグリコーゲンシンターゼキナーゼ３阻害薬としての使用
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
BRPI0807972A2 (pt) 2007-01-24 2014-06-10 Glaxo Group Ltd Composições farmacêuticas compreendendo 3,5-diamino-6-(2,3-diclofenil)-l,2,4-triazina ou r(-)-2,4-diamino-5-(2,3-diclorofenil)-6-fluorometilpirim idina e uma nk1
WO2009012283A1 (en) 2007-07-17 2009-01-22 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
BRPI0816881A2 (pt) 2007-09-21 2015-03-17 Array Biopharma Inc Composto, composição farmacêutica, uso de um composto, e, métodos para tratar doenças ou distúrbios e para preparar um composto.
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
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
MX349923B (es) 2009-04-03 2017-08-21 Hoffmann La Roche Composiciones del ácido propano-1-sulfónico {3-[5-(4-cloro-fenil)- 1h-pirrolo [2,3-b]-piridina-3-carbonil]-2,4-difluoro-fenil]-amida y el uso de las mismas.
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
ES2633317T3 (es) 2009-11-06 2017-09-20 Plexxikon, Inc. Compuestos y métodos para la modulación de quinasas, e indicaciones para ello
CA2810954A1 (en) 2010-09-27 2012-04-05 Abbott 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
PT2672967T (pt) 2011-02-07 2018-12-07 Plexxikon Inc Compostos e métodos de modulação da quinase e suas indicações
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
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
WO2020142559A1 (en) 2018-12-31 2020-07-09 Biomea Fusion, Llc Inhibitors of menin-mll interaction
CN114040760A (zh) 2018-12-31 2022-02-11 拜欧米富士恩公司 Menin-mll相互作用的不可逆抑制剂
KR20210121186A (ko) * 2019-01-31 2021-10-07 화이자 인코포레이티드 Cdk2에 대한 억제 활성을 갖는 3-카본일아미노-5-사이클로펜틸-1h-피라졸 화합물
WO2022135442A1 (zh) * 2020-12-22 2022-06-30 上海拓界生物医药科技有限公司 Cdk2抑制剂及其制备方法
CA3223223A1 (en) 2021-06-28 2023-01-05 Blueprint Medicines Corporation Cdk2 inhibitors
WO2023274397A1 (zh) * 2021-07-01 2023-01-05 上海拓界生物医药科技有限公司 Cdk2抑制剂及其制备方法和用途
CA3229150A1 (en) 2021-08-20 2023-02-23 Biomea Fusion, Inc. Crystalline form of 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, an irreversible menin-mll inhibitor for the treatment of cance
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 (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
AU2198999A (en) * 1997-12-22 1999-07-12 Bayer Corporation Inhibition of raf kinase using substituted heterocyclic ureas
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
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
OA12046A (en) * 1999-08-12 2006-05-02 Pharmacia Italia Spa 3(5)-Amino-pyrazole derivatives, process for theirpreparation and their use as antitumor agents.
AU1047601A (en) * 1999-11-30 2001-06-12 Pfizer Products 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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