HUP0400267A2 - Pirazolo[3,4-d]pirimidinek mint terápiás szerek - Google Patents
Pirazolo[3,4-d]pirimidinek mint terápiás szerekInfo
- Publication number
- HUP0400267A2 HUP0400267A2 HU0400267A HUP0400267A HUP0400267A2 HU P0400267 A2 HUP0400267 A2 HU P0400267A2 HU 0400267 A HU0400267 A HU 0400267A HU P0400267 A HUP0400267 A HU P0400267A HU P0400267 A2 HUP0400267 A2 HU P0400267A2
- Authority
- HU
- Hungary
- Prior art keywords
- cra
- alkyl
- heteroaryl
- aryl
- nitrogen
- Prior art date
Links
- QUKPALAWEPMWOS-UHFFFAOYSA-N 1h-pyrazolo[3,4-d]pyrimidine Chemical class C1=NC=C2C=NNC2=N1 QUKPALAWEPMWOS-UHFFFAOYSA-N 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 229940124597 therapeutic agent Drugs 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000003287 optical effect Effects 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
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- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
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- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P17/06—Antipsoriatics
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- 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
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- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- 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
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- 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
- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Transplantation (AREA)
Abstract
A találmány az (I) általános képletű vegyületekre, racém-diasztereomerkeverékeikre, optikai izomerjeikre, gyógyászatilag elfogadható sóikra,p-rodrugjaikra vagy biológiailag aktív metabolitjaikra vonatkozik,ahol a képletben a helyettesítők jellemző jelentése: G jelentése (A)általános képletű csoport, ahol Z100 jelentése (B) általános képletűcsoport vagy egy R1 helyettesítővel szubsztituált alkil-, cikloalkil-,pirrolidinil-, vagy biciklusos aromás nitrogéntartalmú heterociklus;Z110 és Z111 jelentése kovalens kötés vagy adott esetben szubsztituáltszénhidrogéncsoport; Ra és R1 jelentése többek között hidrogénatom, -C(O)O-aril, -C(O)O-heteroaril, -C(O)-a1kil, -C(O)-aril, -C(O)-heteroaril; szubsztituált vagy szubsztituálatlan cikloalkil-,heteroaril-, heteroarilalkoxi-, arilalkoxi-, alkil-S(O)p-, alkil-S-,aril-S(O)p,-, heteroaril-S(O)p- képletű csoport; ahol p értéke 1 vagy2; A jelentése többek között - (1-6 szénatomos szénhidrogéncsoport)-,-O-; -S-; vagy Z110-A-Z111 együtt kovalens kötést alkot; R3 jelentésehidrogénatom, hidroxil-, szubsztituált vagy szubsztituálatlan alkil-,-C(O)-alkil, -C(O)-aril, -C(O)-heteroaril vagy alkoxicsoport; R2jelentése többek között hidrogénatom, tritil-, cikloalkenil-,azaheteroaril- vagy azacikloalkilcsoport, a értéke 1 és D1, G1, J1 ésL1 és Ml jelentése CRa vagy nitrogénatom; vagy a értéke 0 és D1, Gl,L1 és M1 közül az egyik jelentése NRa; Dl, Gl, L1 és M1 egyikénekjelentése CRa és a többi jelentése CRa vagy nitrogénatom; b értéke 1és D2, G2, J2, L2 és M2 jelentése egymástól függetlenül CRa vagynitrogénatom; vagy b értéke 0 és D2 G2, L2 és M2 közül az egyikjelentése NRa; D2, G2, L2 és M2 egyikének jelentése CRa, és a többijelentése CRa vagy nitrogénatom. A találmány szerinti vegyületekalkalmasak egy betegben protein-kinázok gátlására, ezáltal többekközött hiperproliferatív betegségek és angiogenezis befolyásolására. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US27804701P | 2001-03-22 | 2001-03-22 | |
PCT/US2002/008996 WO2002076986A1 (en) | 2001-03-22 | 2002-03-22 | Pyrazolopyrimidines as therapeutic agents |
Publications (1)
Publication Number | Publication Date |
---|---|
HUP0400267A2 true HUP0400267A2 (hu) | 2004-08-30 |
Family
ID=23063472
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0400267A HUP0400267A2 (hu) | 2001-03-22 | 2002-03-22 | Pirazolo[3,4-d]pirimidinek mint terápiás szerek |
Country Status (21)
Country | Link |
---|---|
US (1) | US7332497B2 (hu) |
EP (1) | EP1379528A4 (hu) |
JP (1) | JP4319412B2 (hu) |
KR (1) | KR20030088114A (hu) |
CN (1) | CN101426792A (hu) |
BG (1) | BG108268A (hu) |
BR (1) | BR0205890A (hu) |
CA (1) | CA2440714C (hu) |
CO (1) | CO5570669A2 (hu) |
CZ (1) | CZ20032837A3 (hu) |
EC (1) | ECSP034773A (hu) |
HU (1) | HUP0400267A2 (hu) |
IL (1) | IL157640A0 (hu) |
MX (1) | MXPA03008560A (hu) |
NO (1) | NO20034177L (hu) |
PE (1) | PE20030047A1 (hu) |
PL (1) | PL363946A1 (hu) |
SK (1) | SK13122003A3 (hu) |
UY (1) | UY27222A1 (hu) |
WO (1) | WO2002076986A1 (hu) |
ZA (1) | ZA200306887B (hu) |
Families Citing this family (133)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6921763B2 (en) * | 1999-09-17 | 2005-07-26 | Abbott Laboratories | Pyrazolopyrimidines as therapeutic agents |
AU8473401A (en) * | 2000-08-04 | 2002-02-18 | Human Genome Sciences, Inc. | Vascular endothelial growth factor 2 |
CA2444632A1 (en) * | 2001-04-13 | 2002-10-24 | Human Genome Sciences, Inc. | Vascular endothelial growth factor 2 |
CA2444624A1 (en) * | 2001-04-13 | 2002-10-24 | Human Genome Sciences, Inc. | Vascular endothelial growth factor 2 |
US20050232921A1 (en) * | 2001-04-13 | 2005-10-20 | Rosen Craig A | Vascular endothelial growth factor 2 |
US20030199525A1 (en) * | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
AU2003246972A1 (en) | 2002-08-06 | 2004-02-23 | Astrazeneca Ab | Condensed pyridines and pyrimidines with tie2 (tek) activity |
WO2004100868A2 (en) * | 2003-04-23 | 2004-11-25 | Abbott Laboratories | Method of treating transplant rejection |
US7429596B2 (en) * | 2003-06-20 | 2008-09-30 | The Regents Of The University Of California | 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof |
DE10344223A1 (de) * | 2003-09-24 | 2005-04-21 | Merck Patent Gmbh | 1,3-Benzoxazolylderivate als Kinase-Inhibitoren |
CN1898240B (zh) * | 2003-10-15 | 2011-08-03 | Osi制药公司 | 咪唑并吡嗪类酪氨酸激酶抑制剂 |
JP2007520559A (ja) * | 2004-02-03 | 2007-07-26 | アボット・ラボラトリーズ | 治療薬としてのアミノベンゾオキサゾール類 |
BRPI0509576A (pt) | 2004-04-02 | 2007-05-29 | Osi Pharm Inc | composto, método de tratamento de um paciente tendo uma condição que é mediada pela atividade de proteìna quinase, e, composição farmacêutica |
US20080287405A1 (en) * | 2004-05-14 | 2008-11-20 | Thannickal Victor J | Compositions and Methods Relating to Protein Kinase Inhibitors |
MXPA06013250A (es) * | 2004-05-14 | 2007-02-28 | Abbott Lab | Inhibidores de quinasa como agentes terapeuticos. |
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JP2008520744A (ja) * | 2004-11-19 | 2008-06-19 | ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア | 抗炎症性ピラゾロピリミジン |
US8575164B2 (en) * | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
NZ571182A (en) * | 2006-04-04 | 2010-09-30 | Univ California | Pyrazolo[3,4-d]pyrimidines |
BRPI0622054B8 (pt) | 2006-09-22 | 2021-05-25 | Oxford Amherst Llc | composto e composição farmacêutica |
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US7998688B2 (en) * | 2008-03-07 | 2011-08-16 | OSI Pharmaceuticals, LLC | Inhibition of EMT induction in tumor cells by anti-cancer agents |
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UY27222A1 (es) | 2002-10-31 |
NO20034177D0 (no) | 2003-09-19 |
CA2440714C (en) | 2010-08-10 |
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SK13122003A3 (sk) | 2004-04-06 |
US7332497B2 (en) | 2008-02-19 |
CA2440714A1 (en) | 2002-10-03 |
BG108268A (en) | 2005-04-30 |
JP4319412B2 (ja) | 2009-08-26 |
MXPA03008560A (es) | 2004-06-30 |
CN101426792A (zh) | 2009-05-06 |
EP1379528A4 (en) | 2005-12-07 |
ZA200306887B (en) | 2004-09-13 |
CO5570669A2 (es) | 2005-10-31 |
ECSP034773A (es) | 2003-12-24 |
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