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 THEMInfo
- 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
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.
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)
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)
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 |
-
2001
- 2001-05-09 CA CA002417254A patent/CA2417254A1/en not_active Abandoned
- 2001-05-09 MX MXPA03000774A patent/MXPA03000774A/en unknown
- 2001-05-09 GE GE5063A patent/GEP20043367B/en unknown
- 2001-05-09 HU HU0303698A patent/HUP0303698A2/en unknown
- 2001-05-09 SK SK1839-2002A patent/SK18392002A3/en unknown
- 2001-05-09 YU YU4903A patent/YU4903A/en unknown
- 2001-05-09 JP JP2002515891A patent/JP2004509857A/en not_active Withdrawn
- 2001-05-09 CZ CZ2003237A patent/CZ2003237A3/en unknown
- 2001-05-09 IL IL15359101A patent/IL153591A0/en unknown
- 2001-05-09 WO PCT/US2001/015081 patent/WO2002010162A1/en not_active Application Discontinuation
- 2001-05-09 CN CNB018133673A patent/CN100457753C/en not_active Expired - Fee Related
- 2001-05-09 AU AU2001259704A patent/AU2001259704A1/en not_active Abandoned
- 2001-05-09 KR KR10-2003-7001141A patent/KR20030016429A/en not_active Application Discontinuation
- 2001-05-09 PL PL01365170A patent/PL365170A1/en not_active Application Discontinuation
- 2001-05-09 BR BR0112674-1A patent/BR0112674A/en not_active Application Discontinuation
- 2001-05-09 EP EP01933266A patent/EP1303513A1/en not_active Withdrawn
- 2001-05-09 SI SI200120051A patent/SI21099A/en not_active IP Right Cessation
- 2001-05-09 EE EEP200300041A patent/EE200300041A/en unknown
- 2001-05-16 TW TW090111741A patent/TWI302533B/en not_active IP Right Cessation
- 2001-05-22 MY MYPI20012414A patent/MY129635A/en unknown
- 2001-05-23 EG EG20010550A patent/EG24409A/en active
- 2001-05-24 AR ARP010102516A patent/AR030563A1/en unknown
-
2002
- 2002-12-23 IL IL153591A patent/IL153591A/en not_active IP Right Cessation
-
2003
- 2003-01-16 BG BG107468A patent/BG65132B1/en unknown
- 2003-01-24 NO NO20030394A patent/NO20030394L/en not_active Application Discontinuation
- 2003-02-19 HR HR20030116A patent/HRP20030116A2/en not_active Application Discontinuation
- 2003-02-26 LV LVP-03-24A patent/LV13037B/en unknown
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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