AR030563A1 - N- [5 - [[[5-ALQUIL-2-OXAZOLIL] METHYL] UNCLE] -2-TIAZOLIL] CARBOXAMIDS INHIBITING CYCLINE DEPENDENT KINASES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Google Patents

N- [5 - [[[5-ALQUIL-2-OXAZOLIL] METHYL] UNCLE] -2-TIAZOLIL] CARBOXAMIDS INHIBITING CYCLINE DEPENDENT KINASES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Info

Publication number
AR030563A1
AR030563A1 ARP010102516A ARP010102516A AR030563A1 AR 030563 A1 AR030563 A1 AR 030563A1 AR P010102516 A ARP010102516 A AR P010102516A AR P010102516 A ARP010102516 A AR P010102516A AR 030563 A1 AR030563 A1 AR 030563A1
Authority
AR
Argentina
Prior art keywords
compositions containing
alkyl
oxazolil
tiazolil
carboxamids
Prior art date
Application number
ARP010102516A
Other languages
Spanish (es)
Inventor
Raj Misra
Hai-Yun Xiao
Original Assignee
Bristol Myers Squibb Co
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
Priority claimed from US09/727,957 external-priority patent/US6515004B1/en
Priority claimed from US09/746,060 external-priority patent/US6414156B2/en
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR030563A1 publication Critical patent/AR030563A1/en

Links

Classifications

    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion describe compuestos de formula 1: y enantiomeros, diastereomeros, solvatos y sales farmacéutica-mente aceptables de los mismos, en donde: R es alquilo; R1 es hidrogeno o alquilo; X es NR2 o CHNR2R3; R2 y R3 son cada uno independientemente hidrogeno, alquilo, alquilo, sustituido, cicloalquilo o cicloalquilo sustituido; y n es 0, 1, 2, o 3. Los compuestos de formula 1 son inhibidores de la proteína cinasa y son utiles en el tratamiento de enfermedades proliferativas, por ejemplo cáncer, inflamacion y artritis. También pueden ser utiles en el tratamiento de la enfermedad de alzheimer, alopecia inducida por quimioterapia y enfermedad cardiovascular. También se describen las composiciones que contienen dichos compuestos.The present invention describes compounds of formula 1: and enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, wherein: R is alkyl; R1 is hydrogen or alkyl; X is NR2 or CHNR2R3; R2 and R3 are each independently hydrogen, alkyl, alkyl, substituted, cycloalkyl or substituted cycloalkyl; and n is 0, 1, 2, or 3. The compounds of formula 1 are protein kinase inhibitors and are useful in the treatment of proliferative diseases, for example cancer, inflammation and arthritis. They can also be useful in the treatment of Alzheimer's disease, chemotherapy-induced alopecia and cardiovascular disease. Compositions containing such compounds are also described.

ARP010102516A 2000-07-26 2001-05-24 N- [5 - [[[5-ALQUIL-2-OXAZOLIL] METHYL] UNCLE] -2-TIAZOLIL] CARBOXAMIDS INHIBITING CYCLINE DEPENDENT KINASES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AR030563A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US61662700A 2000-07-26 2000-07-26
US09/727,957 US6515004B1 (en) 1999-12-15 2000-12-01 N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US09/746,060 US6414156B2 (en) 1998-10-21 2000-12-22 Process for preparing azacycloalkanoylaminothiazoles

Publications (1)

Publication Number Publication Date
AR030563A1 true AR030563A1 (en) 2003-08-27

Family

ID=27417184

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010102516A AR030563A1 (en) 2000-07-26 2001-05-24 N- [5 - [[[5-ALQUIL-2-OXAZOLIL] METHYL] UNCLE] -2-TIAZOLIL] CARBOXAMIDS INHIBITING CYCLINE DEPENDENT KINASES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Country Status (26)

Country Link
EP (1) EP1303513A1 (en)
JP (1) JP2004509857A (en)
KR (1) KR20030016429A (en)
CN (1) CN100457753C (en)
AR (1) AR030563A1 (en)
AU (1) AU2001259704A1 (en)
BG (1) BG65132B1 (en)
BR (1) BR0112674A (en)
CA (1) CA2417254A1 (en)
CZ (1) CZ2003237A3 (en)
EE (1) EE200300041A (en)
EG (1) EG24409A (en)
GE (1) GEP20043367B (en)
HR (1) HRP20030116A2 (en)
HU (1) HUP0303698A2 (en)
IL (2) IL153591A0 (en)
LV (1) LV13037B (en)
MX (1) MXPA03000774A (en)
MY (1) MY129635A (en)
NO (1) NO20030394L (en)
PL (1) PL365170A1 (en)
SI (1) SI21099A (en)
SK (1) SK18392002A3 (en)
TW (1) TWI302533B (en)
WO (1) WO2002010162A1 (en)
YU (1) YU4903A (en)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6414156B2 (en) 1998-10-21 2002-07-02 Bristol-Myers Squibb Company Process for preparing azacycloalkanoylaminothiazoles
MY156407A (en) 2002-02-28 2016-02-26 Novartis Ag 5-phenylthiazole derivatives and use as p13 kinase inhibitors
EP2311818B1 (en) * 2002-02-28 2013-01-16 Novartis AG Combination of a 5-phenylthiazole compound as PI3 kinase inhibitor with an antiinflammatory, bronchodilatory or antihistamine drug
KR20050057072A (en) 2002-09-04 2005-06-16 쉐링 코포레이션 Pyrazolopyrimidines as cyclin dependent kinase inhibitors
RU2380369C9 (en) 2002-09-04 2011-07-10 Шеринг Корпорейшн Novel pyrazolopyrimidines as inhibitors of cyclin-dependant kinase
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
JP2006503838A (en) 2002-09-23 2006-02-02 シェーリング　コーポレイション A novel imidazopyrazine as a cyclin-dependent kinase inhibitor
PE20050081A1 (en) 2002-09-23 2005-03-01 Schering Corp NEW IMIDAZOPYRAZINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASES
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
EP1555264A1 (en) * 2004-01-15 2005-07-20 Sireen AG Five-membered heterocyclic compounds as inhibitors of SRC family protein kinase.
DE102005008310A1 (en) * 2005-02-17 2006-08-24 Schering Ag Use of CDKII inhibitors for fertility control
WO2007022258A1 (en) * 2005-08-17 2007-02-22 Schering Corporation Novel high affinity thiophene-based and furan-based kinase ligands
JP2009507843A (en) 2005-09-09 2009-02-26 シェーリング コーポレイション Aza-fused cyclin-dependent kinase inhibitors
CN101321760A (en) 2005-10-06 2008-12-10 先灵公司 Pyrazolopyrimidines as protein kinase inhibitors
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
JP2009539846A (en) * 2006-06-06 2009-11-19 ブリストル−ミエルス スクイッブ カンパニー Crystalline form of N- [5-[[[5- (1,1-dimethylethyl) -2-oxazolyl] methyl] thio] -2-thiazolyl] -4-piperidinecarboxamide
US9206142B2 (en) 2006-10-31 2015-12-08 Merck Sharp & Dohme Corp. Anilinopiperazine derivatives and methods of use thereof
US8318735B2 (en) 2006-10-31 2012-11-27 Merck Sharp & Dohme Corp. 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
CN101678002A (en) 2007-05-08 2010-03-24 先灵公司 Methods of treatment using intravenous formulations comprising temozolomide
TW200922564A (en) 2007-09-10 2009-06-01 Curis Inc CDK inhibitors containing a zinc binding moiety
WO2010075542A1 (en) 2008-12-23 2010-07-01 Curis, Inc. Cdk inhibitors
WO2011025706A2 (en) 2009-08-26 2011-03-03 Schering Corporation Heterocyclic amide compounds as protein kinase inhibitors
EP2831282B1 (en) 2012-03-30 2018-07-04 Merck Sharp & Dohme Corp. Predictive biomarker useful for cancer therapy mediated by a cdk inhibitor
WO2015081867A1 (en) * 2013-12-04 2015-06-11 杭州民生药物研究院有限公司 Gemcitabine derivative, composition containing the derivative and pharmaceutical use of the derivative

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6040321A (en) * 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6262096B1 (en) * 1997-11-12 2001-07-17 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
EP1087951B9 (en) * 1998-06-18 2006-09-13 Bristol-Myers Squibb Company Carbon substituted aminothiazole inhibitors of cyclin dependent kinases
US6414156B2 (en) * 1998-10-21 2002-07-02 Bristol-Myers Squibb Company Process for preparing azacycloalkanoylaminothiazoles
MY125768A (en) * 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases

Also Published As

Publication number Publication date
TWI302533B (en) 2008-11-01
BG65132B1 (en) 2007-03-30
LV13037B (en) 2003-11-20
EG24409A (en) 2009-05-20
CA2417254A1 (en) 2002-02-07
PL365170A1 (en) 2004-12-27
SI21099A (en) 2003-06-30
WO2002010162A1 (en) 2002-02-07
AU2001259704A1 (en) 2002-02-13
GEP20043367B (en) 2004-06-10
IL153591A0 (en) 2003-07-06
SK18392002A3 (en) 2003-09-11
MXPA03000774A (en) 2003-09-10
NO20030394D0 (en) 2003-01-24
KR20030016429A (en) 2003-02-26
CZ2003237A3 (en) 2003-06-18
JP2004509857A (en) 2004-04-02
YU4903A (en) 2006-03-03
NO20030394L (en) 2003-03-03
BG107468A (en) 2004-01-30
HRP20030116A2 (en) 2005-02-28
EE200300041A (en) 2005-04-15
HUP0303698A2 (en) 2004-04-28
CN100457753C (en) 2009-02-04
MY129635A (en) 2007-04-30
EP1303513A1 (en) 2003-04-23
IL153591A (en) 2009-07-20
BR0112674A (en) 2003-12-30
CN1444584A (en) 2003-09-24

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