ZA200107204B - Cyclic Protein Tyrosine Kinase Inhibitors. - Google Patents

Cyclic Protein Tyrosine Kinase Inhibitors. Download PDF

Info

Publication number
ZA200107204B
ZA200107204B ZA200107204A ZA200107204A ZA200107204B ZA 200107204 B ZA200107204 B ZA 200107204B ZA 200107204 A ZA200107204 A ZA 200107204A ZA 200107204 A ZA200107204 A ZA 200107204A ZA 200107204 B ZA200107204 B ZA 200107204B
Authority
ZA
South Africa
Prior art keywords
thiazolecarboxamide
methyl
amino
trimethylphenyl
chloro
Prior art date
Application number
ZA200107204A
Other languages
English (en)
Inventor
Jagabandhu Das
Ping Chen
Arthur M P Doweyko
John Wityak
Ramesh Padmanabha
Derek J Norris
Joel C Barrish
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22440334&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200107204(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of ZA200107204B publication Critical patent/ZA200107204B/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • C07D277/56Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/65Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/40Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • C07D263/48Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ZA200107204A 1999-04-15 2001-08-30 Cyclic Protein Tyrosine Kinase Inhibitors. ZA200107204B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US12951099P 1999-04-15 1999-04-15

Publications (1)

Publication Number Publication Date
ZA200107204B true ZA200107204B (en) 2002-12-02

Family

ID=22440334

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200107204A ZA200107204B (en) 1999-04-15 2001-08-30 Cyclic Protein Tyrosine Kinase Inhibitors.

Country Status (27)

Country Link
US (12) US6596746B1 (ko)
EP (3) EP2308833A3 (ko)
JP (1) JP3989175B2 (ko)
KR (2) KR100710100B1 (ko)
CN (2) CN1348370A (ko)
AU (1) AU779089B2 (ko)
BR (2) BRPI0009721B8 (ko)
CA (1) CA2366932C (ko)
CY (2) CY1113312T1 (ko)
CZ (1) CZ302788B6 (ko)
DK (1) DK1169038T3 (ko)
ES (1) ES2391550T3 (ko)
FR (1) FR13C0003I2 (ko)
HK (2) HK1042433B (ko)
HU (1) HUP0202708A3 (ko)
ID (1) ID30460A (ko)
IL (2) IL144910A0 (ko)
LU (1) LU92146I2 (ko)
MX (1) MXPA01010292A (ko)
NO (3) NO322470B1 (ko)
NZ (1) NZ513639A (ko)
PL (1) PL215901B1 (ko)
PT (1) PT1169038E (ko)
RU (2) RU2260592C9 (ko)
TR (1) TR200102969T2 (ko)
WO (1) WO2000062778A1 (ko)
ZA (1) ZA200107204B (ko)

Families Citing this family (294)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU756699B2 (en) * 1996-12-03 2003-01-23 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
AU779089B2 (en) * 1999-04-15 2005-01-06 Bristol-Myers Squibb Holdings Ireland Unlimited Company Cyclic protein tyrosine kinase inhibitors
US7125875B2 (en) * 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
US6114365A (en) * 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
ES2250186T3 (es) * 1999-09-10 2006-04-16 MERCK & CO., INC. Inhibidores de tirosina quinasa.
EP1257536A1 (en) 2000-01-27 2002-11-20 Cytovia, Inc. Substituted nicotinamides and analogs as activators of caspases and inducers of apoptosis and the use thereof
GB0001930D0 (en) * 2000-01-27 2000-03-22 Novartis Ag Organic compounds
US7427689B2 (en) * 2000-07-28 2008-09-23 Georgetown University ErbB-2 selective small molecule kinase inhibitors
WO2002024200A1 (en) * 2000-09-21 2002-03-28 Bristol-Myers Squibb Company Substituted azole derivatives as inhibitors of corticotropin releasing factor
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
SI1347971T1 (sl) * 2000-12-21 2006-06-30 Bristol Myers Squibb Co Tiazolilni inhibitorji tirozin kinaz Tec druzine
DE60117605T2 (de) 2000-12-21 2006-12-07 Bristol-Myers Squibb Co. Thiazolyl-inhibitoren von tyrosinkinasen der tec-familie
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
FR2820136A1 (fr) * 2001-01-26 2002-08-02 Aventis Pharma Sa Nouveaux derives de l'uree, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation
JP2005500294A (ja) * 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
EP1404672B1 (en) 2001-06-22 2006-01-18 Merck & Co., Inc. Tyrosine kinase inhibitors
AUPR688101A0 (en) * 2001-08-08 2001-08-30 Luminis Pty Limited Protein domains and their ligands
CN1523991A (zh) 2001-08-10 2004-08-25 ��˹��ŵ�� 单独的c-Src抑制剂或其与STI571的组合用于治疗白血病的用途
US7638522B2 (en) 2001-08-13 2009-12-29 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile
US8101629B2 (en) 2001-08-13 2012-01-24 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US7265134B2 (en) * 2001-08-17 2007-09-04 Merck & Co., Inc. Tyrosine kinase inhibitors
US6677487B2 (en) 2001-08-30 2004-01-13 Pharmacia Corporation α-haloenamine reagents
CA2462441A1 (en) 2001-10-18 2003-04-24 Pier F. Cirillo 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
IL161662A0 (en) 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors)
HUP0402330A3 (en) 2001-11-01 2010-03-29 Janssen Pharmaceutica Nv Amide derivatives as glycogen synthase kinase 3-beta inhibitors, process for producing them, pharmaceutical compositions containing them and use thereof
US6693097B2 (en) 2001-11-30 2004-02-17 Synta Pharmaceuticals Corp. Pyrimidine compounds
NZ533437A (en) 2001-11-30 2007-05-31 Synta Pharmaceuticals Corp Pyrimidine compounds for treating interleukin-12 (IL12) related diseases
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
EA007987B1 (ru) * 2002-03-29 2007-02-27 Чирон Корпорейшн Замещённые бензазолы и их применение в качестве ингибиторов киназы raf
AUPS251402A0 (en) * 2002-05-23 2002-06-13 Cytopia Pty Ltd Kinase inhibitors
IL165262A0 (en) * 2002-05-23 2005-12-18 Cytopia Pty Ltd Kinase inhibitors
KR101169964B1 (ko) 2002-05-23 2012-08-06 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 키나아제 저해제
US7238717B2 (en) 2002-05-24 2007-07-03 Millennium Pharmaceuticals, Inc. CCR9 inhibitors and methods of use thereof
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
US6872724B2 (en) 2002-07-24 2005-03-29 Merck & Co., Inc. Polymorphs with tyrosine kinase activity
AU2003261354A1 (en) * 2002-08-02 2004-02-23 The Regents Of The University Of California New uses for inhibitors of inosine monophosphate dehydrogenase
AU2003282231A1 (en) * 2002-08-09 2004-02-25 Pfizer Inc. Antiproliferative 2-(heteroaryl)-aminothiazole compounds, pharmaceutical compositions and methods for their use
AU2003266413B2 (en) 2002-08-09 2009-04-02 Janssen Pharmaceutica N.V. Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
KR101173510B1 (ko) * 2002-08-23 2012-08-21 슬로안-케테링인스티튜트퍼캔서리서치 에포틸론, 이의 중간물질과 유사체의 합성 및 이들의 용도
US7504211B2 (en) 2002-08-27 2009-03-17 Bristol-Myers Squibb Company Methods of using EPHA2 for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells
US7537891B2 (en) * 2002-08-27 2009-05-26 Bristol-Myers Squibb Company Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in breast cells
WO2004041164A2 (en) * 2002-10-30 2004-05-21 Merck & Co., Inc. Kinase inhibitors
US7741519B2 (en) 2007-04-23 2010-06-22 Chemocentryx, Inc. Bis-aryl sulfonamides
CN101077867B (zh) 2002-11-18 2012-10-10 坎莫森特里克斯公司 芳基磺酰胺
US7227035B2 (en) 2002-11-18 2007-06-05 Chemocentryx Bis-aryl sulfonamides
US7420055B2 (en) 2002-11-18 2008-09-02 Chemocentryx, Inc. Aryl sulfonamides
EP1594854B1 (en) 2003-02-06 2010-09-01 Bristol-Myers Squibb Company Thiazolyl-based compounds useful as kinase inhibitors
MXPA05008364A (es) 2003-02-07 2005-11-04 Janssen Pharmaceutica Nv Derivados de pirimidina para la prevencion de una infeccion por vih.
JP2006517234A (ja) * 2003-02-10 2006-07-20 アムジエン・インコーポレーテツド バニロイド受容体リガンドおよび治療におけるこれらのリガンドの使用
CL2004000306A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa.
WO2004087153A2 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of organic compounds for immunopotentiation
US7427683B2 (en) 2003-04-25 2008-09-23 Ortho-Mcneil Pharmaceutical, Inc. c-fms kinase inhibitors
EP1631560A2 (en) * 2003-04-25 2006-03-08 3-Dimensional Pharmaceuticals, Inc. C-fms kinase inhibitors
US7790724B2 (en) 2003-04-25 2010-09-07 Janssen Pharmaceutica N.V. c-fms kinase inhibitors
US20050113566A1 (en) * 2003-04-25 2005-05-26 Player Mark R. Inhibitors of C-FMS kinase
AU2004251668B2 (en) 2003-06-03 2008-03-20 Triad Therapeutics, Inc 5-membered heterocycle-based p-38 inhibitors
PT1641764E (pt) 2003-06-26 2011-10-27 Novartis Ag Inibidores de p38 quinase a base de heterociclo de 5 elementos
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
US20050009891A1 (en) * 2003-07-09 2005-01-13 Lee Francis Y. Combination of SRC Kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
DE602004017654D1 (de) 2003-07-16 2008-12-18 Janssen Pharmaceutica Nv Triazolopyrimidin derivate als inhibitoren von glycogen synthase kinase-3
MXPA06000794A (es) 2003-07-22 2006-08-23 Astex Therapeutics Ltd Compuestos 1h-pirazola 3,4-disustituida y su uso como moduladores de quinasas dependientes de ciclina (cdk) y quinasa-3 de sintasa de glicogeno (gsr-3).
EP1697352B1 (en) * 2003-09-24 2012-06-27 Vertex Pharmceuticals Incorporated 4-azole substituted imidazole compositions useful as inhibitors or c-met receptor tyrosine kinase
EP1669348A4 (en) 2003-09-30 2009-03-11 Eisai R&D Man Co Ltd NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND
WO2005037273A1 (en) 2003-10-16 2005-04-28 Chiron Corporation Substituted benzazoles and use thereof as inhibitors of raf kinase
JP4851337B2 (ja) 2003-11-10 2012-01-11 シンタ ファーマシューティカルズ コーポレーション ヘテロアリールヒドラゾン化合物
CA2545258A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Pyridine compounds
CA2545340A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
CN1878767B (zh) * 2003-12-03 2010-05-05 西托匹亚研究有限公司 唑基激酶抑制剂
PT1689739T (pt) 2003-12-03 2016-07-13 Ym Biosciences Australia Pty Inibidores de cinases baseados em azol
CA2554201C (en) * 2004-01-21 2015-04-14 Emory University Compositions and use of tyrosine kinase inhibitors to treat pathogenic infection
WO2005075435A1 (en) * 2004-01-30 2005-08-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
KR20060129413A (ko) * 2004-01-30 2006-12-15 에이비 사이언스 티로신 키나제 억제제로서의2-(3-치환된-아릴)아미노-4-아릴-티아졸
TWI338004B (en) * 2004-02-06 2011-03-01 Bristol Myers Squibb Co Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
US7491725B2 (en) 2004-02-06 2009-02-17 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
CN1980909B (zh) * 2004-02-06 2010-08-25 布里斯托尔-迈尔斯·斯奎布公司 作为激酶抑制剂的2-氨基噻唑-5-芳香族甲酰胺的制备方法
US20050215795A1 (en) * 2004-02-06 2005-09-29 Bang-Chi Chen Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
US7652146B2 (en) * 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
US7534798B2 (en) 2004-02-11 2009-05-19 Amgen Inc. Vanilloid receptor ligands and their use in treatments
US7384968B2 (en) * 2004-04-01 2008-06-10 Pfizer Inc. Thiazole-amine compounds for the treatment of neurodegenerative disorders
US7820704B2 (en) * 2004-04-20 2010-10-26 Transtech Pharma, Inc. Substituted heteroaryl derivatives, compositions, and methods of use
US7550499B2 (en) * 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US20110104186A1 (en) 2004-06-24 2011-05-05 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
SG156650A1 (en) * 2004-07-16 2009-11-26 Sunesis Pharmaceuticals Inc Thienopyrimidines useful as aurora kinase inhibitors
ES2401138T3 (es) 2004-08-13 2013-04-17 Genentech, Inc. Inhibidores basados en tiazol de enzimas que usan ATP
US7910613B2 (en) 2004-09-22 2011-03-22 H. Lundbeck A/S 2-acylaminothiazole derivatives
US20060069101A1 (en) * 2004-09-27 2006-03-30 Kim Kyoung S Prodrugs of protein tyrosine kinase inhibitors
NZ555289A (en) * 2004-10-22 2010-10-29 Janssen Pharmaceutica Nv Inhibitors of c-fms kinase
US7645755B2 (en) * 2004-10-22 2010-01-12 Janssen Pharmaceutical N.V. Inhibitors of c-fms kinase
TW200628156A (en) * 2004-11-04 2006-08-16 Bristol Myers Squibb Co Combination of a SRC kinase inhibitor and a BCR-ABL inhibitor for the treatment of proliferative diseases
WO2006053112A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Process for preparing trisubstituted pyrimidine compounds
WO2006053227A2 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Il-12 modulatory compounds
TW200628463A (en) 2004-11-10 2006-08-16 Synta Pharmaceuticals Corp Heteroaryl compounds
SE0402763D0 (sv) * 2004-11-11 2004-11-11 Astrazeneca Ab Nitro indazole derivatives
SE0402762D0 (sv) * 2004-11-11 2004-11-11 Astrazeneca Ab Indazole sulphonamide derivatives
US7851466B2 (en) 2004-11-19 2010-12-14 Synta Pharmaceuticals Corp. Pyrimidine compounds and uses thereof
JP2008521862A (ja) * 2004-12-01 2008-06-26 デブジェン エヌブイ イオンチャンネル、特にkvファミリーのイオンチャンネルと相互作用する5−カルボキサミド置換チアゾール誘導体
BRPI0519759A2 (pt) 2004-12-30 2009-03-10 Astex Therapeutics Ltd composiÇÕes farmacÊuticas
AU2006206611A1 (en) * 2005-01-19 2006-07-27 Bristol-Myers Squibb Company 2-phenoxy-N- (1, 3 , 4-thiadizol-2-yl) pyridin-3-amine derivatives and related compounds as P2Y1 receptor inhibitors for the treatment of thromboembolic disorders
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
WO2006077424A1 (en) 2005-01-21 2006-07-27 Astex Therapeutics Limited Pharmaceutical compounds
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.
MX2007008781A (es) 2005-01-21 2007-09-11 Astex Therapeutics Ltd Compuestos farmaceuticos.
PE20061394A1 (es) * 2005-03-15 2006-12-15 Bristol Myers Squibb Co Metabolitos de n-(2-cloro-6-metilfenil)-2-[[6-[4-(2-hidroxietil)-1-piperazinil]-2-metil-4-pirimidinil]amino]-5-tiazolcarboxamidas
EP1864980A4 (en) 2005-03-30 2010-08-18 Eisai R&D Man Co Ltd A PYRIDINE DERIVATIVE ANTIPILIC AGENT
US20060235006A1 (en) * 2005-04-13 2006-10-19 Lee Francis Y Combinations, methods and compositions for treating cancer
US7674912B2 (en) 2005-04-25 2010-03-09 H. Lundbeck A/S Pro-drugs of N-thiazol-2-yl-benzamide derivatives
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
EP1885339B1 (en) 2005-05-05 2015-07-29 Bristol-Myers Squibb Holdings Ireland Formulations of a src/abl inhibitor
US20060281788A1 (en) * 2005-06-10 2006-12-14 Baumann Christian A Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor
EP1896072A4 (en) 2005-06-24 2013-01-09 Univ Duke SYSTEM FOR DIRECT HEALTH MANAGEMENT BASED ON HEAT-CONTROLLED BIOPOLYMERS
DE602006021306D1 (ko) * 2005-06-27 2011-05-26 Bristol Myers Squibb Co
WO2007002634A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
ES2360818T3 (es) 2005-06-27 2011-06-09 Bristol-Myers Squibb Company Miméticos de urea lineal antagonistas del receptor p2y, útiles en el tratamiento de afecciones trombóticas.
WO2007002635A2 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
DE602006014001D1 (de) * 2005-08-05 2010-06-10 Bristol Myers Squibb Co Herstellung von 2-aminothiazol-5-carbonsäurederivaten
EP1937270A1 (en) * 2005-09-21 2008-07-02 Brystol-Myers Squibb Company Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof
WO2007047919A2 (en) 2005-10-20 2007-04-26 University Of South Florida Treatment of restenosis and stenosis with dasatinib
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
EP1948652B1 (en) 2005-11-01 2011-08-24 Array Biopharma, Inc. Glucokinase activators
PT1951684T (pt) * 2005-11-01 2016-10-13 Targegen Inc Inibidores de cinases de tipo biaril-meta-pirimidina
EP1948820A2 (en) * 2005-11-04 2008-07-30 Bristol-Myers Squibb Pharma Company T315a and f317i mutations of bcr-abl kinase domain
DE602006019128D1 (de) * 2005-11-10 2011-02-03 Bristol Myers Squibb Pharma Co Moesin, caveolin 1 und yes-assoziiertes protein 1 als prädiktive marker der reaktion auf dasatinib bei brustkrebs
US20100286090A1 (en) * 2005-11-14 2010-11-11 Bristol-Myers Squibb Company Treatment of Multiple Myeloma
US20070149523A1 (en) * 2005-11-14 2007-06-28 Jan Ehlert Thiazole Analogues and Uses Thereof
US20090099197A1 (en) * 2005-11-15 2009-04-16 Bristol-Myers Squibb Company Methods of Identifying and Treating Individuals Exhibiting MDR-1 Overexpression With Protein Tyrosine Kinase Inhibitors and Combinations Thereof
US7705009B2 (en) * 2005-11-22 2010-04-27 Hoffman-La Roche Inc. 4-aminopyrimidine-5-thione derivatives
CA2630860A1 (en) 2005-11-25 2007-05-31 Galapagos Sas Urea derivatives useful as calcium receptor modulators
WO2007065124A2 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Methods of identifying and treating individuals exhibiting complex karyotypes
EP1976839A4 (en) * 2006-01-26 2011-06-15 Foldrx Pharmaceuticals Inc COMPOUNDS AND METHOD FOR MODULATING A PROTEIN TRANSPORT
CN101379060B (zh) 2006-02-10 2012-05-23 转化技术制药公司 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
WO2007106391A1 (en) * 2006-03-10 2007-09-20 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
US20070219370A1 (en) * 2006-03-15 2007-09-20 Bristol-Myers Squibb Company Process for preparing n-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino] -5-thiazolecarboxamide and related metabolites thereof
WO2007109527A1 (en) * 2006-03-17 2007-09-27 Bristol-Myers Squibb Company Methods of identifying and treating individuals exhibiting mutant bcr/abl kinase polypeptides
TW200808788A (en) 2006-04-19 2008-02-16 Astellas Pharma Inc Azolecarboxamide derivative
NZ572073A (en) 2006-04-20 2011-09-30 Janssen Pharmaceutica Nv Heterocyclic compounds as inhibitors of c-fms kinase
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
JP5331681B2 (ja) 2006-04-20 2013-10-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ c−fmsキナーゼの阻害剤
DK2016067T3 (da) * 2006-04-28 2012-10-22 Syngenta Participations Ag Insecticidforbindelser
WO2007138110A2 (en) * 2006-06-01 2007-12-06 Devgen N.V. Compounds that interact with ion channels, in particular with ion channels from the kv family
MX2009000110A (es) * 2006-06-28 2009-01-23 Glaxo Group Ltd Derivados de piperazinilo utiles en el tratamiento de enfermedades mediadas por el receptor grp38.
GB0613674D0 (en) * 2006-07-10 2006-08-16 Proskelia Sas Derivatives of urea and related diamines, methods for their manufacture, and uses therefor
SG174790A1 (en) * 2006-09-11 2011-10-28 Curis Inc Tyrosine kinase inhibitors containing a zinc binding moiety
AU2007296744A1 (en) * 2006-09-11 2008-03-20 Curis, Inc. Multi-functional small molecules as anti-proliferative agents
DK2068938T3 (da) 2006-09-22 2011-04-04 Novartis Ag Optimering af behandlingen af Philadelphia-positiv leukæmi med ABL-tyrosinkinaseinhibitor imatinib
EP2073803B1 (en) 2006-10-12 2018-09-19 Astex Therapeutics Limited Pharmaceutical combinations
EP2073807A1 (en) 2006-10-12 2009-07-01 Astex Therapeutics Limited Pharmaceutical combinations
US7960569B2 (en) * 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
CA2668210C (en) 2006-10-31 2013-03-12 Schering Corporation Anilinopiperazine derivatives and methods of use thereof
CN101573345A (zh) 2006-10-31 2009-11-04 先灵公司 作为蛋白激酶抑制剂的2-氨基噻唑-4-甲酰胺
AU2007314305B2 (en) 2006-10-31 2013-01-24 Merck Sharp & Dohme Corp. 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors
JP5622393B2 (ja) 2006-12-15 2014-11-12 アブラクシスバイオサイエンス リミテッド ライアビリティー カンパニー トリアジン誘導体類及びそれらの治療応用
CN101265274B (zh) * 2007-02-16 2013-09-04 中国医学科学院药物研究所 嘧啶噻唑胺衍生物、及其制法和药物组合物与用途
TW200906825A (en) * 2007-05-30 2009-02-16 Scripps Research Inst Inhibitors of protein kinases
US9062023B2 (en) * 2007-06-07 2015-06-23 Intra-Cellular Therapies, Inc. Heterocycle compounds and uses thereof
JP5710251B2 (ja) 2007-06-07 2015-04-30 イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. 新規ヘテロ環化合物およびその使用
WO2009012482A2 (en) 2007-07-19 2009-01-22 H.Lundbeck A/S 5-membered heterocyclic amides and related compounds
US20090076025A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched dasatinib
EP3078662A1 (en) 2007-09-21 2016-10-12 Array Biopharma, Inc. Pyridin-2-yl-amino-1,2,4-thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
JO3240B1 (ar) * 2007-10-17 2018-03-08 Janssen Pharmaceutica Nv c-fms مثبطات كيناز
JP2010539156A (ja) * 2007-10-23 2010-12-16 テバ ファーマシューティカル インダストリーズ リミティド ダサチニブ多形体およびその調製プロセス
EP2206707B1 (en) * 2007-10-24 2014-07-23 Astellas Pharma Inc. Azolecarboxamide compound or salt thereof
EP2062578A1 (en) 2007-11-12 2009-05-27 Institut National De La Sante Et De La Recherche Medicale (Inserm) Novel use of chemical compounds for the treatment of AIDS
WO2009076373A1 (en) * 2007-12-10 2009-06-18 Concert Pharmaceuticals Inc. Heterocyclic kinase inhibitors
WO2009094556A2 (en) * 2008-01-25 2009-07-30 Bristol-Myers Squibb Pharma Company Identification of predictive markers of response to dasatinib in human colon cancer
ES2694103T3 (es) * 2008-03-27 2018-12-18 Grünenthal GmbH Derivados de 4-aminociclohexano sustituidos
DE102008031036A1 (de) 2008-06-30 2009-12-31 Dömling, Alexander, Priv.-Doz. Dr. Dasatinib zur Anwendung in der Organtransplantation
EP2323693B1 (en) * 2008-07-30 2017-11-08 Nitto Denko Corporation Drug carriers
CA2731442A1 (en) * 2008-08-29 2010-03-04 Transtech Pharma, Inc. Substituted aminothiazole derivatives, pharmaceutical compositions, and methods of use
WO2010056539A1 (en) 2008-10-29 2010-05-20 E. I. Du Pont De Nemours And Company Treatment of tailings streams
US20100113520A1 (en) * 2008-11-05 2010-05-06 Principia Biopharma, Inc. Kinase knockdown via electrophilically enhanced inhibitors
WO2010065444A1 (en) * 2008-12-01 2010-06-10 University Of Central Florida Research Foundation, Inc. Drug composition cytotoxic for pancreatic cancer cells
WO2010120386A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
US8816077B2 (en) 2009-04-17 2014-08-26 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
WO2010139981A2 (en) * 2009-06-03 2010-12-09 Generics [Uk] Limited Processes for preparing crystalline forms
KR20120026612A (ko) 2009-06-09 2012-03-19 아브락시스 바이오사이언스, 엘엘씨 벤질 치환 트리아진 유도체와 이들의 치료적 용도
CN102573480B (zh) 2009-06-09 2015-06-10 加利福尼亚资本权益有限责任公司 三嗪衍生物及其治疗应用
US10640457B2 (en) 2009-12-10 2020-05-05 The Trustees Of Columbia University In The City Of New York Histone acetyltransferase activators and uses thereof
CN101812060B (zh) * 2010-02-02 2011-08-17 南京卡文迪许生物工程技术有限公司 一种简捷制备高纯度达沙替尼的新方法以及中间体化合物
CN101845045A (zh) * 2010-02-02 2010-09-29 南京卡文迪许生物工程技术有限公司 一种新的达沙替尼合成方法
EP2359813A1 (en) 2010-02-04 2011-08-24 Ratiopharm GmbH Pharmaceutical composition comprising N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamid
CN101973989B (zh) * 2010-05-17 2012-07-18 苏州波锐生物医药科技有限公司 一种噻唑酰胺类化合物及其在治疗恶性肿瘤中的药物用途
MX2012013274A (es) 2010-05-21 2013-05-28 Chemilia Ab Novedosos derivados de la pirimidina.
EP2598147A1 (en) 2010-07-30 2013-06-05 Ranbaxy Laboratories Limited N-methylformamide solvate of dasatinib
AU2010363329A1 (en) 2010-11-07 2013-05-09 Targegen, Inc. Compositions and methods for treating myelofibrosis
CA2822621C (en) * 2010-12-22 2020-12-15 The Trustees Of Columbia University In The City Of New York Histone acetyltransferase modulators and uses thereof
CA2825367C (en) 2011-01-21 2018-09-25 Sun Pharma Advanced Research Company Ltd. Diarylacetylene hydrazide containing tyrosine kinase inhibitors
WO2012118599A1 (en) 2011-02-28 2012-09-07 Emory University C-abl tyrosine kinase inhibitors useful for inhibiting filovirus replication
DK2683643T3 (da) 2011-03-09 2019-08-12 Richard G Pestell Prostatacancercellelinjer, gensignaturer og anvendelser deraf
US9006241B2 (en) 2011-03-24 2015-04-14 Noviga Research Ab Pyrimidine derivatives
LT2717883T (lt) 2011-05-02 2017-04-25 Stichting Vumc Apsauga nuo endotelio barjero disfunkcijos, slopinant su abl susijusio geno (arg) tirozino kinazę
JP2014513687A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Syk阻害薬としてのピリジルアミノピリジン
US9145391B2 (en) 2011-05-10 2015-09-29 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as Syk inhibitors
JP2014513686A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Syk阻害薬としてのアミノピリミジン
CN102898424A (zh) * 2011-07-29 2013-01-30 江苏奥赛康药业股份有限公司 达沙替尼新的多晶型物及其制备方法
WO2013065063A1 (en) 2011-11-03 2013-05-10 Cadila Healthcare Limited Anhydrous form of dasatinib, process for its preparation and its use
WO2013082458A1 (en) 2011-12-02 2013-06-06 The Regents Of The University Of California Reperfusion protection solution and uses thereof
WO2013157019A2 (en) 2012-04-20 2013-10-24 Shilpa Medicare Ltd. Process for preparing dasatinib monohydrate
EP2850081A1 (en) * 2012-05-11 2015-03-25 AbbVie Inc. Thiazolecarboxamide derivatives for use as nampt inhibitors
US9453836B2 (en) 2012-05-14 2016-09-27 Richard G. Pestell Use of modulators of CCR5 in the treatment of cancer and cancer metastasis
AU2013276138B2 (en) * 2012-06-15 2017-02-23 Basf Se Multicomponent crystals comprising Dasatinib and selected cocrystal formers
CA2880236C (en) 2012-07-27 2022-09-13 Antonius Martinus Gustave Bunt Efflux inhibitor compositions and methods of treatment using the same
JOP20180012A1 (ar) 2012-08-07 2019-01-30 Janssen Pharmaceutica Nv عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد
WO2014025675A1 (en) 2012-08-07 2014-02-13 Janssen Pharmaceutica Nv Process for the preparation of heterocyclic ester derivatives
WO2014031784A1 (en) 2012-08-23 2014-02-27 Alios Biopharma, Inc. Compounds for the treatment of paramoxyvirus viral infections
ES2731833T3 (es) 2012-09-10 2019-11-19 Principia Biopharma Inc Compuestos pirazolopirimidínicos comos inhibidores de cinasas
CN103788085B (zh) * 2012-10-31 2016-09-07 复旦大学 2-(喹唑啉-4-氨基)-5-噻唑甲酰胺类衍生物及其生物药物用途
CZ306598B6 (cs) 2012-12-06 2017-03-22 Zentiva, K.S. Způsob přípravy a čištění nových i známých polymorfů a solvátů dasatinibu
WO2014102759A2 (en) 2012-12-31 2014-07-03 Ranbaxy Laboratories Limited Process for the preparation of dasatinib and its intermediates
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
CN104151321B (zh) * 2013-05-15 2016-09-07 复旦大学 N-(2-氯-6-甲基苯基)-2[(2-甲基嘧啶-4-基)氨基]噻唑-5-甲酰胺化合物及其制备方法和用途
HUE034829T2 (en) * 2013-05-23 2018-03-28 Kalvista Pharmaceuticals Ltd Heterocyclic derivatives
CN104225611B (zh) * 2013-06-18 2017-06-30 天津键凯科技有限公司 达沙替尼与非线性构型聚乙二醇的结合物
TW201534597A (zh) * 2013-06-20 2015-09-16 Ab Science 作為選擇性蛋白質激酶抑制劑之苯并咪唑衍生物
WO2015011578A1 (en) * 2013-07-22 2015-01-29 Shilpa Medicare Limited Dasatinib glucuronate salt and process for preparation thereof
EP3024831A2 (en) 2013-07-25 2016-06-01 Basf Se Salts of dasatinib in amorphous form
JP6501773B2 (ja) 2013-07-25 2019-04-17 ビーエーエスエフ ソシエタス・ヨーロピアBasf Se 結晶形態のダサチニブの塩
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
CN103588758A (zh) * 2013-11-04 2014-02-19 南京大学 一类含1,4-苯并二噁烷骨架的硝基咪唑衍生物的合成、制备及其在抗癌药物中的应用
US9636340B2 (en) 2013-11-12 2017-05-02 Ayyappan K. Rajasekaran Kinase inhibitors
IN2013MU03610A (ko) 2013-12-18 2015-04-24 Dharmesh Mahendrabhai Shah
CZ306732B6 (cs) 2013-12-19 2017-05-31 Zentiva, K.S. Způsob přípravy bezvodé polymorfní formy N-6 Dasatinibu
WO2015116735A1 (en) 2014-01-28 2015-08-06 Mayo Foundation For Medical Education And Research Methods and combinations for killing senescent cells and for treating senescence-associated diseases and disorders
CA2939186C (en) 2014-02-21 2023-03-07 Principia Biopharma Inc. Salts and solid form of a btk inhibitor
AU2015200822A1 (en) 2014-03-11 2015-10-01 Cerbios-Pharma Sa Process and intermediates for the preparation of dasatinib
HU231013B1 (hu) 2014-05-26 2019-11-28 Egis Gyógyszergyár Zrt. Dasatinib sók
US20180230140A1 (en) 2014-06-30 2018-08-16 Basf Se Multicomponent crystals of dasatinib with menthol or vanillin
CN104119292A (zh) * 2014-07-23 2014-10-29 天津市炜杰科技有限公司 一种达沙替尼中间体的制备方法
US9844549B2 (en) 2014-08-26 2017-12-19 Astellas Pharma Inc. 2-aminothiazole derivative or salt thereof
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
EA036269B1 (ru) 2014-12-18 2020-10-21 Принсипиа Биофарма Инк. Лечение пузырчатки
EA201792028A1 (ru) 2015-03-13 2018-04-30 Форма Терапьютикс, Инк. Альфа-цинамидные соединения и композиции как ингибиторы hdac8
CN104788445B (zh) * 2015-04-10 2017-06-23 山东新时代药业有限公司 一种达沙替尼中间体的合成方法
CN104974222B (zh) * 2015-06-14 2020-06-02 深圳市康尔诺生物技术有限公司 作为蛋白酪氨酸激酶抑制剂的偶联肽化合物
EP3313839A1 (en) 2015-06-24 2018-05-02 Principia Biopharma Inc. Tyrosine kinase inhibitors
CN106749223B (zh) * 2015-11-25 2019-12-20 中国科学院广州生物医药与健康研究院 酪氨酸激酶抑制剂及其制备方法和用途
CN106866684B (zh) * 2015-12-10 2020-06-09 吴耀东 用于治疗肿瘤的大环衍生物
WO2017108605A1 (en) 2015-12-22 2017-06-29 Synthon B.V. Pharmaceutical composition comprising amorphous dasatinib
TWI620748B (zh) * 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
WO2017168454A2 (en) * 2016-04-02 2017-10-05 Sun Pharma Advanced Research Company Limited Novel compounds as btk inhibitors
AU2017275820B2 (en) 2016-05-31 2020-10-22 Kalvista Pharmaceuticals Limited Pyrazole derivatives as plasma kallikrein inhibitors
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
KR102391693B1 (ko) 2016-06-29 2022-04-29 프린시피아 바이오파마, 인코퍼레이티드 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴의 변형 방출 제제
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
MA45656A (fr) 2016-07-14 2021-03-24 Pfizer Nouveaux pyrimidine carboxamides utilisées comme inhibiteurs de l'enzyme vanin-1
WO2018051306A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
US20190270735A1 (en) 2016-10-29 2019-09-05 Cipla Limited Polymorphs of Dasatinib
WO2018100585A1 (en) 2016-12-01 2018-06-07 Natco Pharma Limited An improved process for the preparation of dasatinib polymorph
CN108473487B (zh) * 2016-12-13 2021-08-03 普林斯顿药物研发公司 一种蛋白激酶抑制剂
CN106674150A (zh) * 2016-12-28 2017-05-17 上海应用技术大学 具有抗肿瘤活性的达沙替尼衍生物及其应用
IT201700006157A1 (it) 2017-01-20 2018-07-20 Cerbios Pharma Sa Co-cristalli di un composto antitumorale
IT201700006145A1 (it) 2017-01-20 2018-07-20 Cerbios Pharma Sa Co-cristallo di un composto antitumorale
JP2020523282A (ja) * 2017-03-29 2020-08-06 パデュー リサーチ ファウンデイション キナーゼネットワークの阻害剤およびその使用
EP3388430A1 (en) 2017-04-10 2018-10-17 Technische Universität München Compound, compound for use in the treatment of a pathological condition, a pharmaceutical composition and a method for preparing said compound
DK3391907T3 (da) 2017-04-20 2020-03-09 Iomx Therapeutics Ag Intracellulær kinase sik3, der er associeret med resistens over for antitumorimmunresponser, og anvendelser deraf
CN111108104A (zh) 2017-07-07 2020-05-05 拜康有限公司 达沙替尼的多晶形式
RU2674443C1 (ru) * 2017-11-16 2018-12-10 Федеральное государственное автономное образовательное учреждение высшего образования "Белгородский государственный национальный исследовательский университет" (НИУ "БелГУ") Способ ингибирования нуклеарного фактора каппа В с использованием 5-гидрокисиникотинат 3-(2,2,2-триметилгидразиний) пропионата калия в культуре клеток
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
HRP20220367T1 (hr) 2017-11-29 2022-05-27 Kalvista Pharmaceuticals Limited Oblici za doziranje koji sadrže plazmatski kalikrein inhibitor
CA3090545A1 (en) 2018-02-28 2019-09-06 University Of Southern California Compositions and methods for modulating inflammatory and degenerative disorder
WO2019238816A1 (en) * 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting uchl5
WO2019238886A1 (en) * 2018-06-13 2019-12-19 University Of Dundee Bifunctional molecules for targeting usp14
JP2021527137A (ja) * 2018-06-13 2021-10-11 アンフィスタ セラピューティクス リミテッド Rpn11を標的化するための二機能性分子
CN116808044A (zh) 2018-06-15 2023-09-29 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物
CN108929273A (zh) * 2018-06-27 2018-12-04 合肥医工医药有限公司 一种咪唑乙基香草酸醚钠盐的制备方法
WO2020092650A1 (en) * 2018-10-30 2020-05-07 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods for modulating t cell exhaustion
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
CN109438437B (zh) * 2018-12-24 2020-07-17 深圳市第二人民医院 一类含噻唑环的抗癌化合物
US11434291B2 (en) 2019-05-14 2022-09-06 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
WO2021018195A1 (en) * 2019-07-29 2021-02-04 Ascentage Pharma (Suzhou) Co., Ltd. Novel tricyclic compounds as bcr-abl inhibitors
CN114206852A (zh) 2019-08-09 2022-03-18 卡尔维斯塔制药有限公司 血浆激肽释放酶抑制剂
CN112402422A (zh) * 2019-08-20 2021-02-26 湖南华纳大药厂股份有限公司 氟取代的2-氨基噻唑-5-芳香族甲酰胺的用途
CN112409349A (zh) * 2019-08-20 2021-02-26 湖南华纳大药厂股份有限公司 激酶抑制剂及其制备、药物组合物和用途
GB201913124D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913121D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913122D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
GB201913123D0 (en) 2019-09-11 2019-10-23 Seald As Compositions and methods for treatment of cholangiocarcinoma
AU2021210974A1 (en) 2020-01-24 2022-09-22 Nanocopoeia, Llc Amorphous solid dispersions of dasatinib and uses thereof
WO2021228983A1 (en) 2020-05-13 2021-11-18 INSERM (Institut National de la Santé et de la Recherche Médicale) A pharmaceutical composition comprising an arsenic compound, an inductor of type-1 ifn and a protein kinase inhibitor for treating cancer
KR20230092863A (ko) 2020-06-11 2023-06-26 프로벤션 바이오, 인코포레이티드 제1형 당뇨병을 예방하기 위한 방법 및 조성물
KR20220054066A (ko) * 2020-10-23 2022-05-02 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
US11980619B2 (en) 2021-07-28 2024-05-14 Nanocopoeia, Llc Pharmaceutical compositions and crushable tablets including amorphous solid dispersions of dasatinib and uses
WO2023081923A1 (en) 2021-11-08 2023-05-11 Frequency Therapeutics, Inc. Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof
WO2023204642A1 (ko) * 2022-04-20 2023-10-26 (주)메디톡스 단백질 키나제 저해제 및 그의 용도
US20230355678A1 (en) 2022-05-05 2023-11-09 Immatics US, Inc. Methods for improving t cell efficacy
CN117820251B (zh) * 2024-03-01 2024-05-03 南京桦冠生物技术有限公司 双α-酮酸酰胺类化合物及其组合物

Family Cites Families (130)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3709992A (en) 1966-12-07 1973-01-09 Us Rubber Co Fungicidal use of certain carboxamidothiazoles
US3725427A (en) 1966-12-07 1973-04-03 Uniroyal Ltd Certain 2,4-dimethyl-5-carboxamido-thiazoles
US3505055A (en) * 1966-12-07 1970-04-07 Uniroyal Inc Method of controlling plant growth with carboxamidothiazoles
DE2128699A1 (de) 1971-06-09 1973-01-25 Bayer Ag Thiazylharnstoffe, verfahren zu ihrer herstellung und ihre fungizide verwendung
US3896223A (en) 1971-11-22 1975-07-22 Uniroyal Inc Anti-inflammatory thiazole compositions and methods for using same
US3796800A (en) * 1971-11-22 1974-03-12 Uniroyal Inc Anti-inflammatory triazole compositions and methods for using same
US3879531A (en) * 1972-07-17 1975-04-22 Uniroyal Inc 2-aminothiazoles compositions and methods for using them as psychotherapeutic agents
US3932633A (en) 1972-12-04 1976-01-13 Uniroyal Inc. Novel o-triazenobenzamides, in treating aggressive behavior
JPS57183768A (en) 1981-05-06 1982-11-12 Kanto Ishi Pharma Co Ltd 4-methyl-5-(o-carboxyphenyl)carbamoylthiazole derivative and its preparation
DE3205638A1 (de) 1982-02-17 1983-08-25 Hoechst Ag, 6230 Frankfurt Trisubstituierte pyrimidin-5-carbonsaeuren und deren derivate, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel
DE3220118A1 (de) * 1982-05-28 1983-12-01 Bayer Ag, 5090 Leverkusen Alkylenverbrueckte guanidinothiazolderivate, verfahren zu ihrer herstellung sowie ihre verwendung als arzneimittel
US4649146A (en) 1983-01-31 1987-03-10 Fujisawa Pharmaceutical Co., Ltd. Thiazole derivatives and pharmaceutical composition comprising the same
US4727073A (en) 1984-10-01 1988-02-23 Fujisawa Pharmaceutical Co., Ltd. Pyrimidine derivatives and composition of the same
JPS62123180A (ja) * 1985-11-21 1987-06-04 Otsuka Pharmaceut Factory Inc p−アミノフエノ−ル誘導体
JPS6339868A (ja) * 1986-08-04 1988-02-20 Otsuka Pharmaceut Factory Inc ジ低級アルキルフエノ−ル誘導体
US4837242A (en) * 1987-01-20 1989-06-06 Sumitomo Chemical Company, Limited Thiazoles and pyrazoles as fungicides
JP2552494B2 (ja) 1987-04-08 1996-11-13 ヘキストジャパン株式会社 イミダゾチアジアジン誘導体及びその製造法
GB8717068D0 (en) * 1987-07-20 1987-08-26 Fujisawa Pharmaceutical Co Nitric ester derivative
US4877441A (en) * 1987-11-06 1989-10-31 Sumitomo Chemical Company Ltd. Fungicidal substituted carboxylic acid derivatives
HU202728B (en) 1988-01-14 1991-04-29 Eszakmagyar Vegyimuevek Synergetic fungicide and acaricide compositions containing two or three active components
US4970318A (en) 1988-05-24 1990-11-13 Pfizer Inc. Aromatic and heterocyclic carboxamide derivatives as antineoplastic agents
JPH02129171A (ja) 1988-11-08 1990-05-17 Nissan Chem Ind Ltd ピラゾールカルボキサニリド誘導体及び有害生物防除剤
JPH02275857A (ja) 1989-01-13 1990-11-09 Yoshitomi Pharmaceut Ind Ltd ピリジン誘導体
US5696270A (en) 1989-05-23 1997-12-09 Abbott Laboratories Intermediate for making retroviral protease inhibiting compounds
US5064825A (en) 1989-06-01 1991-11-12 Merck & Co., Inc. Angiotensin ii antagonists
AU644802B2 (en) 1989-06-30 1993-12-23 E.I. Du Pont De Nemours And Company Substituted imidazoles
TW205041B (ko) 1989-08-07 1993-05-01 Fujisawa Pharmaceutical Co
DE3934197A1 (de) 1989-10-13 1991-04-18 Bayer Ag Thiazolcarbonsaeureamid-derivate
JPH04316559A (ja) 1990-11-28 1992-11-06 Nissan Chem Ind Ltd ピラゾールカルボキサニリド誘導体及び殺菌剤
PL170837B1 (pl) 1991-10-18 1997-01-31 Monsanto Co S rod ek g r zybobó j c zy PL PL PL PL PL PL
DE4138042C2 (de) 1991-11-19 1993-10-14 Biotechnolog Forschung Gmbh Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel
JPH05345780A (ja) 1991-12-24 1993-12-27 Kumiai Chem Ind Co Ltd ピリミジンまたはトリアジン誘導体及び除草剤
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
HUT63941A (en) 1992-05-15 1993-11-29 Hoechst Ag Process for producing 4-alkyl-substituted pyrimidine-5-carboxanilide derivatives, and fungicidal compositions comprising same
IL105939A0 (en) 1992-06-11 1993-10-20 Rhone Poulenc Agriculture Herbicidal compounds and compositions
DE4231517A1 (de) 1992-09-21 1994-03-24 Basf Ag Carbonsäureanilide, Verfahren zu ihrer Herstellung und sie enthaltende Mittel zur Bekämpfung von Schadpilzen
HRP921338B1 (en) 1992-10-02 2002-04-30 Monsanto Co Fungicides for the control of take-all disease of plants
EP0603595A1 (de) 1992-12-04 1994-06-29 Hoechst Aktiengesellschaft Faserreaktive Farbstoffe, Verfahren zu deren Herstellung und ihre Verwendung
US5721264A (en) 1993-04-07 1998-02-24 Nissan Chemical Industries, Ltd. Pyrazole derivatives
US5514643A (en) * 1993-08-16 1996-05-07 Lucky Ltd. 2-aminothiazolecarboxamide derivatives, processes for preparing the same and use thereof for controlling phytopathogenic organisms
US5728693A (en) 1993-12-29 1998-03-17 E. I. Du Pont De Nemours And Company Arthropodicidal oxadiazine-thiadiazine-or triazine-carboxanilides
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5582167A (en) * 1994-03-02 1996-12-10 Thomas Jefferson University Methods and apparatus for reducing tracheal infection using subglottic irrigation, drainage and servoregulation of endotracheal tube cuff pressure
US5922751A (en) 1994-06-24 1999-07-13 Euro-Celtique, S.A. Aryl pyrazole compound for inhibiting phosphodiesterase IV and methods of using same
CA2193725A1 (en) 1994-06-24 1996-01-04 David Cavalla Aryl derivative compounds and uses to inhibit phosphodiesterase iv acti vity
US6080772A (en) * 1995-06-07 2000-06-27 Sugen, Inc. Thiazole compounds and methods of modulating signal transduction
US5811428A (en) 1995-12-18 1998-09-22 Signal Pharmaceuticals, Inc. Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions
JPH11512399A (ja) 1995-09-01 1999-10-26 シグナル ファーマシューティカルズ,インコーポレイテッド ピリミジンカルボキサミドおよび関連化合物ならびに炎症状態を処置するための方法
EP1440973A3 (de) 1995-11-17 2004-10-20 Gesellschaft für biotechnologische Forschung mbH (GBF) Epothilonderivate, Herstellung und Mittel
US5677097A (en) 1996-01-18 1997-10-14 Fuji Xerox Co., Ltd. Electrophotographic photoreceptor
US6011029A (en) 1996-02-26 2000-01-04 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
AU716123B2 (en) 1996-04-03 2000-02-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE59711647D1 (de) 1996-11-18 2004-06-24 Biotechnolog Forschung Gmbh Epothilon d, dessen herstellung und dessen verwendung als cytostatisches mittel bzw. als pflanzenschutzmittel
AU756699B2 (en) 1996-12-03 2003-01-23 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US6380394B1 (en) 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6187797B1 (en) * 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
ATE236890T1 (de) * 1996-12-23 2003-04-15 Bristol Myers Squibb Pharma Co Sauerstoff oder schwefel enthaltende 5-gliedrige heteroaromatishe derivative als factor xa hemmer
ES2183338T3 (es) 1997-02-25 2003-03-16 Biotechnolog Forschung Gmbh Epotilona modificada en la cadena lateral.
CA2302438A1 (en) 1997-05-19 1998-11-26 Sugen, Inc. Heteroarylcarboxamide compounds active against protein tyrosine kinase related disorders
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
GB9801231D0 (en) 1997-06-05 1998-03-18 Merck & Co Inc A method of treating cancer
US5896223A (en) * 1997-06-13 1999-04-20 Tigliev; George S. Optical system having an unlimited depth of focus
AU8071698A (en) * 1997-06-13 1998-12-30 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme relatedcellular signal transduction
EP0991625B1 (en) * 1997-06-19 2005-06-01 Bristol-Myers Squibb Pharma Company Inhibitors of factor xa with a neutral p1 specificity group
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
WO1999002224A1 (en) 1997-07-07 1999-01-21 Lewis Robert D Statistical analysis and feedback system for sports employing a projectile
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
JPH1180137A (ja) 1997-07-10 1999-03-26 Nissan Chem Ind Ltd カルバモイルテトラゾールおよび除草剤
WO1999003848A1 (de) 1997-07-16 1999-01-28 Schering Aktiengesellschaft Thiazolderivate, verfahren zur herstellung und verwendung
PT1005465E (pt) 1997-08-09 2007-10-18 Bayer Schering Pharma Ag Novos derivados da epotilona, processo para a sua preparação e sua utilização farmacêutica
HUP0004512A3 (en) * 1997-10-27 2003-01-28 Agouron Pharmaceuticals Inc La 4-aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases
US6022884A (en) 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
NZ503491A (en) * 1997-11-10 2002-08-28 Bristol Myers Squibb Co 2-substituted amino-1,3-benzothiazole derivatives useful as protein tyrosine kinase inhibitors
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
US6365749B1 (en) 1997-12-04 2002-04-02 Bristol-Myers Squibb Company Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
HUP0100582A3 (en) 1997-12-04 2003-03-28 Bristol Myers Squibb Co A process for the reduction of oxiranyl epothilones to olefinic epothilones
JP4135318B2 (ja) 1997-12-15 2008-08-20 アステラス製薬株式会社 新規なピリミジン−5−カルボキサミド誘導体
JPH11180965A (ja) 1997-12-24 1999-07-06 Nissan Chem Ind Ltd 新規カルバモイルテトラゾリノンおよび除草剤
SI0928793T1 (en) 1998-01-02 2002-10-31 F. Hoffmann-La Roche Ag Thiazole derivatives
SI0928790T1 (en) * 1998-01-02 2003-06-30 F. Hoffmann-La Roche Ag Thiazole derivatives
IL138113A0 (en) 1998-02-25 2001-10-31 Sloan Kettering Inst Cancer Synthesis of epothilones, intermediates thereto and analogues thereof
EP1064289A1 (en) 1998-03-18 2001-01-03 Ariad Pharmaceuticals, Inc. Heterocyclic signal transduction inhibitors, compositions containing them
US6498257B1 (en) 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
US6380395B1 (en) 1998-04-21 2002-04-30 Bristol-Myers Squibb Company 12, 13-cyclopropane epothilone derivatives
AU765030B2 (en) 1998-05-05 2003-09-04 F. Hoffmann-La Roche Ag Pyrazole derivatives as p-38 map kinase inhibitors
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
DE19826988A1 (de) 1998-06-18 1999-12-23 Biotechnolog Forschung Gmbh Epothilon-Nebenkomponenten
WO1999067253A2 (en) 1998-06-22 1999-12-29 Novartis Ag Desmethyl epothilones
AU5036999A (en) 1998-06-30 2000-01-17 Schering Aktiengesellschaft Epothilon derivatives, their preparation process, intermediate products and their pharmaceutical use
AU747427B2 (en) 1998-07-10 2002-05-16 Merck & Co., Inc. Novel angiogenesis inhibitors
GB2323595A (en) 1998-07-29 1998-09-30 Zeneca Ltd Preparation of 2-Mercaptothiazole
CA2337755C (en) 1998-09-18 2008-07-29 Vertex Pharmaceuticals Incorporated Inhibitors of p38
JP3244672B2 (ja) 1998-10-13 2002-01-07 住友製薬株式会社 イソキサゾール誘導体からなる医薬
AU760219B2 (en) * 1998-10-22 2003-05-08 F. Hoffmann-La Roche Ag Thiazole-derivatives
GB9823871D0 (en) 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
GB9823873D0 (en) 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
DE69926542T2 (de) 1998-12-25 2006-04-27 Teikoku Hormone Mfg. Co., Ltd. Aminopyrazolderivate
KR100659007B1 (ko) 1999-02-10 2007-02-28 미츠비시 웰파마 가부시키가이샤 아미드 화합물 및 그 의약으로서의 용도
KR100342044B1 (ko) 1999-04-14 2002-06-27 김순택 녹색발광 형광체 조성물 및 이를 이용하여 제조된 음극선관
AU779089B2 (en) 1999-04-15 2005-01-06 Bristol-Myers Squibb Holdings Ireland Unlimited Company Cyclic protein tyrosine kinase inhibitors
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
US6962933B1 (en) 1999-08-06 2005-11-08 Takeda Pharmaceutical Company Limited Method for inhibiting p38 MAP kinase or TNF-α production using a 1,3-thiazole
KR20020030791A (ko) 1999-08-12 2002-04-25 버텍스 파마슈티칼스 인코포레이티드 c-JUN N-말단 키나제(JNK) 및 기타의 단백질키나제 억제제
US6114365A (en) 1999-08-12 2000-09-05 Pharmacia & Upjohn S.P.A. Arylmethyl-carbonylamino-thiazole derivatives, process for their preparation, and their use as antitumor agents
ES2250186T3 (es) 1999-09-10 2006-04-16 MERCK & CO., INC. Inhibidores de tirosina quinasa.
WO2001052847A1 (en) 2000-01-19 2001-07-26 Alteon, Inc. Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging
WO2001056567A1 (en) * 2000-02-04 2001-08-09 Novo Nordisk A/S 2,4-diaminothiazole derivatives and their use as glycogen synthase kinase-3 (gsk-3) inhibitors
AU2002213466A1 (en) 2000-10-11 2002-04-22 Chemocentryx, Inc. Compounds and methods for modulating ccr4 function
AU2002213467A8 (en) 2000-10-11 2009-07-30 Chemocentryx Inc Modulation of ccr4 function
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
EP1353676A4 (en) 2000-12-29 2006-05-31 Alteon Inc METHOD FOR THE TREATMENT OF FIBROUS OR OTHER INDICATIONS
JP2002338537A (ja) 2001-05-16 2002-11-27 Mitsubishi Pharma Corp アミド化合物およびその医薬用途
WO2002094798A1 (fr) 2001-05-23 2002-11-28 Nippon Soda Co.,Ltd. Preparation de composes thiazole
US7144903B2 (en) * 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
JP4011359B2 (ja) 2002-02-15 2007-11-21 株式会社ニフコ カップホルダ装置
US20050009891A1 (en) 2003-07-09 2005-01-13 Lee Francis Y. Combination of SRC Kinase inhibitors and chemotherapeutic agents for the treatment of proliferative diseases
US7491725B2 (en) * 2004-02-06 2009-02-17 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
US7652146B2 (en) * 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
TW200628156A (en) * 2004-11-04 2006-08-16 Bristol Myers Squibb Co Combination of a SRC kinase inhibitor and a BCR-ABL inhibitor for the treatment of proliferative diseases
US20060235006A1 (en) 2005-04-13 2006-10-19 Lee Francis Y Combinations, methods and compositions for treating cancer
EP1885339B1 (en) * 2005-05-05 2015-07-29 Bristol-Myers Squibb Holdings Ireland Formulations of a src/abl inhibitor
EP1937270A1 (en) * 2005-09-21 2008-07-02 Brystol-Myers Squibb Company Oral administration of n-(2-chloro-6-methylphenyl)-2-[[6-4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof
JP4316559B2 (ja) 2005-11-30 2009-08-19 株式会社ナノクリエート 導光板及びその製造方法
US8554512B2 (en) 2006-06-13 2013-10-08 Nike, Inc. Athletic performance data system and method
US7678998B2 (en) 2007-05-21 2010-03-16 Cicoil, Llc Cable assembly
US8897586B2 (en) 2012-06-15 2014-11-25 Comcast Cable Communications, Llc Dynamic generation of a quantization matrix for compression of a digital object

Also Published As

Publication number Publication date
HK1042433A1 (en) 2002-08-16
US6979694B2 (en) 2005-12-27
CY2013005I2 (el) 2015-11-04
CA2366932A1 (en) 2000-10-26
BRPI0009721B8 (pt) 2021-11-23
HUP0202708A2 (hu) 2002-12-28
EP1169038A1 (en) 2002-01-09
NO20014970D0 (no) 2001-10-12
US20050261305A1 (en) 2005-11-24
CY1113312T1 (el) 2015-11-04
RU2260592C9 (ru) 2017-04-07
HUP0202708A3 (en) 2004-12-28
NO20014970L (no) 2001-12-10
US9382219B2 (en) 2016-07-05
BR0009721A (pt) 2002-02-13
RU2312860C2 (ru) 2007-12-20
US20040073026A1 (en) 2004-04-15
US20060079563A1 (en) 2006-04-13
EP2308833A3 (en) 2011-09-28
US8716323B2 (en) 2014-05-06
CA2366932C (en) 2009-08-25
US20140206691A1 (en) 2014-07-24
US7091223B2 (en) 2006-08-15
FR13C0003I1 (ko) 2013-02-01
NO322470B1 (no) 2006-10-09
US20190210986A1 (en) 2019-07-11
ID30460A (id) 2001-12-06
NO2019016I1 (no) 2019-04-05
JP3989175B2 (ja) 2007-10-10
FR13C0003I2 (fr) 2015-11-20
MXPA01010292A (es) 2002-10-23
US20160264537A1 (en) 2016-09-15
IL144910A0 (en) 2002-06-30
LU92146I2 (fr) 2013-04-05
BRPI0009721B1 (pt) 2018-11-21
HK1244797A1 (zh) 2018-08-17
US20050288303A1 (en) 2005-12-29
DK1169038T3 (da) 2012-11-26
EP1169038B1 (en) 2012-08-08
KR20010108500A (ko) 2001-12-07
HK1042433B (zh) 2012-12-14
IL144910A (en) 2007-07-24
KR100722344B1 (ko) 2007-05-29
KR20070020153A (ko) 2007-02-16
NO2007005I1 (no) 2007-03-27
TR200102969T2 (tr) 2002-08-21
US20040077875A1 (en) 2004-04-22
US7189854B2 (en) 2007-03-13
RU2005107463A (ru) 2006-08-27
US8993567B2 (en) 2015-03-31
ES2391550T3 (es) 2012-11-27
US6596746B1 (en) 2003-07-22
PL215901B1 (pl) 2014-02-28
US20180016247A1 (en) 2018-01-18
CN1348370A (zh) 2002-05-08
CN101481359A (zh) 2009-07-15
PL351126A1 (en) 2003-03-24
EP1169038B9 (en) 2013-07-10
CY2013005I1 (el) 2015-11-04
NZ513639A (en) 2004-02-27
CZ302788B6 (cs) 2011-11-09
EP1169038A4 (en) 2004-10-13
JP2002542193A (ja) 2002-12-10
RU2260592C2 (ru) 2005-09-20
AU779089B2 (en) 2005-01-06
AU4233800A (en) 2000-11-02
US20150158830A1 (en) 2015-06-11
CZ20013677A3 (cs) 2002-06-12
PT1169038E (pt) 2012-10-26
EP3222619A1 (en) 2017-09-27
EP2308833A2 (en) 2011-04-13
US20040024208A1 (en) 2004-02-05
WO2000062778A1 (en) 2000-10-26
KR100710100B1 (ko) 2007-04-23
US7153856B2 (en) 2006-12-26
NO2007005I2 (ko) 2008-12-01

Similar Documents

Publication Publication Date Title
CA2366932C (en) Cyclic protein tyrosine kinase inhibitors
CA2519898C (en) Oral administration of cyclic protein tyrosine kinase inhibitors