ATE493131T1 - Chinazolin-4-one als inhibitoren der humanen phosphatidylinositol-3-kinase delta - Google Patents
Chinazolin-4-one als inhibitoren der humanen phosphatidylinositol-3-kinase deltaInfo
- Publication number
- ATE493131T1 ATE493131T1 AT02757407T AT02757407T ATE493131T1 AT E493131 T1 ATE493131 T1 AT E493131T1 AT 02757407 T AT02757407 T AT 02757407T AT 02757407 T AT02757407 T AT 02757407T AT E493131 T1 ATE493131 T1 AT E493131T1
- Authority
- AT
- Austria
- Prior art keywords
- pi3kδ
- methods
- activity
- inhibit
- compounds
- Prior art date
Links
- 108091007960 PI3Ks Proteins 0.000 title abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title abstract 2
- QMNUDYFKZYBWQX-UHFFFAOYSA-N 1H-quinazolin-4-one Chemical compound C1=CC=C2C(=O)N=CNC2=C1 QMNUDYFKZYBWQX-UHFFFAOYSA-N 0.000 title 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000002401 inhibitory effect Effects 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 3
- 102000038030 PI3Ks Human genes 0.000 abstract 2
- 102000001708 Protein Isoforms Human genes 0.000 abstract 2
- 108010029485 Protein Isoforms Proteins 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000010261 cell growth Effects 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000036039 immunity Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 210000000265 leukocyte Anatomy 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
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- A61P11/06—Antiasthmatics
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- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
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- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- C07D233/54—Heterocyclic 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
- C07D233/66—Heterocyclic 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
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- C07D—HETEROCYCLIC COMPOUNDS
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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- C—CHEMISTRY; METALLURGY
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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/24—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one nitrogen and one sulfur atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/28—Oxygen atom
- C07D473/30—Oxygen atom attached in position 6, e.g. hypoxanthine
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
-
- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/36—Sulfur atom
- C07D473/38—Sulfur atom attached in position 6
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/40—Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
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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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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
- C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
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- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/99—Enzyme inactivation by chemical treatment
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- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/01—Phosphotransferases with an alcohol group as acceptor (2.7.1)
- C12Y207/01137—Phosphatidylinositol 3-kinase (2.7.1.137)
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Genetics & Genomics (AREA)
- General Engineering & Computer Science (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Endocrinology (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/027,591 US6667300B2 (en) | 2000-04-25 | 2001-10-19 | Inhibitors of human phosphatidylinositol 3-kinase delta |
| PCT/US2002/027240 WO2003035075A1 (en) | 2001-10-19 | 2002-08-27 | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE493131T1 true ATE493131T1 (de) | 2011-01-15 |
Family
ID=21838603
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT02757407T ATE493131T1 (de) | 2001-10-19 | 2002-08-27 | Chinazolin-4-one als inhibitoren der humanen phosphatidylinositol-3-kinase delta |
Country Status (11)
| Country | Link |
|---|---|
| US (12) | US6667300B2 (de) |
| EP (1) | EP1438052B1 (de) |
| JP (1) | JP4945060B2 (de) |
| CN (1) | CN1606444B (de) |
| AT (1) | ATE493131T1 (de) |
| AU (1) | AU2002323426B2 (de) |
| CA (1) | CA2463294C (de) |
| DE (1) | DE60238779D1 (de) |
| DK (1) | DK1438052T3 (de) |
| NZ (1) | NZ532206A (de) |
| WO (1) | WO2003035075A1 (de) |
Families Citing this family (187)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| EP1158985B1 (de) | 1999-01-13 | 2011-12-28 | Bayer HealthCare LLC | GAMMA CARBOXYARYLSUBSTITUIERTE DIPHENYLHARNSTOFFVERBINDUNGEN ALS p38 KINASEHEMMER |
| US6667300B2 (en) * | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| US20030133939A1 (en) | 2001-01-17 | 2003-07-17 | Genecraft, Inc. | Binding domain-immunoglobulin fusion proteins |
| US7754208B2 (en) | 2001-01-17 | 2010-07-13 | Trubion Pharmaceuticals, Inc. | Binding domain-immunoglobulin fusion proteins |
| US20070129334A1 (en) * | 2001-10-30 | 2007-06-07 | Conforma Therapeutics Corporation | Orally Active Purine-Based Inhibitors of Heat Shock Protein 90 |
| WO2003037860A2 (en) * | 2001-10-30 | 2003-05-08 | Conforma Therapeutics Corporation | Purine analogs having hsp90-inhibiting activity |
| SI1478358T1 (sl) | 2002-02-11 | 2013-09-30 | Bayer Healthcare Llc | Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi |
| US7879621B2 (en) * | 2003-05-08 | 2011-02-01 | Phynexus, Inc. | Open channel solid phase extraction systems and methods |
| CA2491555C (en) * | 2002-07-10 | 2012-09-11 | Massachusetts Institute Of Technology | Solid-phase and solution-phase synthesis of glycosylphosphatidylinositol glycans |
| US7435419B2 (en) * | 2002-07-19 | 2008-10-14 | Beth Israel Deaconess Medical Center | Methods of diagnosing and treating pre-eclampsia or eclampsia |
| US7335362B2 (en) * | 2002-07-19 | 2008-02-26 | Beth Israel Deaconess Medical Center | Methods of treating pre-eclampsia or eclampsia |
| KR101215701B1 (ko) * | 2002-07-19 | 2012-12-26 | 베스 이스라엘 데코니스 메디칼 센터 | 자간전증 또는 자간의 진단 및 치료 방법 |
| ATE488231T1 (de) * | 2002-12-23 | 2010-12-15 | Icagen Inc | Quinazolinone als kaliumkanalmodulatoren |
| US7557129B2 (en) | 2003-02-28 | 2009-07-07 | Bayer Healthcare Llc | Cyanopyridine derivatives useful in the treatment of cancer and other disorders |
| EP1636585B2 (de) | 2003-05-20 | 2012-06-13 | Bayer HealthCare LLC | Diaryl-harnstoffe mit kinasehemmender wirkung |
| 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 |
| EP1663978B1 (de) | 2003-07-23 | 2007-11-28 | Bayer Pharmaceuticals Corporation | Fluorsubstituierter omega-carboxyaryldiphenylharnstoff zur behandlung und prävention von krankheiten und leiden |
| US20080146562A1 (en) * | 2003-08-08 | 2008-06-19 | Ulysses Pharmaceutical Products Inc., | Halogenated quinazolinyl nitrofurans as antibacterial agents |
| EP1660486A4 (de) * | 2003-08-08 | 2006-12-13 | Ulysses Pharmaceutical Product | Halogenierte chinazolinylnitrofurane als antibakterielle mittel |
| WO2005016348A1 (en) * | 2003-08-14 | 2005-02-24 | Icos Corporation | Method of inhibiting immune responses stimulated by an endogenous factor |
| US20050054614A1 (en) * | 2003-08-14 | 2005-03-10 | Diacovo Thomas G. | Methods of inhibiting leukocyte accumulation |
| GB0320197D0 (en) * | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
| MXPA06002997A (es) * | 2003-09-18 | 2007-02-08 | Conforma Therapeutics Corp | Novedosos compuestos heterociclicos como inhibidores- hsp90. |
| CA2552664A1 (en) * | 2004-01-08 | 2005-07-28 | Michigan State University | Methods for treating and preventing hypertension and hypertension-related disorders |
| RU2358969C2 (ru) * | 2004-02-13 | 2009-06-20 | Баниу Фармасьютикал Ко., Лтд. | Конденсированное 4-оксопиримидиновое производное |
| NZ551004A (en) * | 2004-04-02 | 2010-07-30 | Prana Biotechnology Ltd | Neurologically-active compounds |
| CA2566436C (en) * | 2004-05-13 | 2011-05-10 | Vanderbilt University | Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis |
| WO2005113556A1 (en) * | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| WO2005117889A1 (en) * | 2004-05-25 | 2005-12-15 | Icos Corporation | Methods for treating and/or preventing aberrant proliferation of hematopoietic |
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