RU2350618C2 - ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ - Google Patents
ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ Download PDFInfo
- Publication number
- RU2350618C2 RU2350618C2 RU2005117337/04A RU2005117337A RU2350618C2 RU 2350618 C2 RU2350618 C2 RU 2350618C2 RU 2005117337/04 A RU2005117337/04 A RU 2005117337/04A RU 2005117337 A RU2005117337 A RU 2005117337A RU 2350618 C2 RU2350618 C2 RU 2350618C2
- Authority
- RU
- Russia
- Prior art keywords
- ethoxy
- propoxy
- group
- piperazin
- chloro
- Prior art date
Links
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title claims 2
- 102000009076 src-Family Kinases Human genes 0.000 title 1
- 108010087686 src-Family Kinases Proteins 0.000 title 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- -1 tetrahydropyran-4-yloxy Chemical group 0.000 claims abstract 40
- 150000003839 salts Chemical class 0.000 claims abstract 12
- 125000001309 chloro group Chemical group Cl* 0.000 claims abstract 7
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims abstract 6
- 206010028980 Neoplasm Diseases 0.000 claims abstract 5
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims abstract 5
- 230000001740 anti-invasion Effects 0.000 claims abstract 4
- 239000003795 chemical substances by application Substances 0.000 claims abstract 4
- 239000003085 diluting agent Substances 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims abstract 2
- 150000003246 quinazolines Chemical class 0.000 claims 10
- 239000002253 acid Substances 0.000 claims 8
- 125000001246 bromo group Chemical group Br* 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 claims 3
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 claims 3
- XQGNSUGMUSXKKB-UHFFFAOYSA-N 1-[4-[2-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-(oxan-4-yloxy)quinazolin-7-yl]oxyethyl]piperazin-1-yl]ethanone Chemical compound C1CN(C(=O)C)CCN1CCOC1=CC(OC2CCOCC2)=C(C(NC=2C(=CN=C3OCOC3=2)Cl)=NC=N2)C2=C1 XQGNSUGMUSXKKB-UHFFFAOYSA-N 0.000 claims 1
- CETXQBFLIVLDTF-UHFFFAOYSA-N 1-[4-[2-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-propan-2-yloxyquinazolin-7-yl]oxyethyl]piperazin-1-yl]-2-(dimethylamino)ethanone Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCN(C(=O)CN(C)C)CC1 CETXQBFLIVLDTF-UHFFFAOYSA-N 0.000 claims 1
- MVWATCATLSSVBH-UHFFFAOYSA-N 1-[4-[2-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-propan-2-yloxyquinazolin-7-yl]oxyethyl]piperazin-1-yl]ethanone Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCN(C(C)=O)CC1 MVWATCATLSSVBH-UHFFFAOYSA-N 0.000 claims 1
- XACGJHGLWHFNKU-UHFFFAOYSA-N 2-[4-[2-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-5-propan-2-yloxyquinazolin-7-yl]oxyethyl]piperazin-1-yl]ethanol Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCN(CCO)CC1 XACGJHGLWHFNKU-UHFFFAOYSA-N 0.000 claims 1
- SDYDJNLCQKFKIL-UHFFFAOYSA-N 6-chloro-n-[5-(oxan-4-yloxy)-7-[2-(4-prop-2-ynylpiperazin-1-yl)ethoxy]quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound ClC1=CN=C2OCOC2=C1NC(C1=C(OC2CCOCC2)C=2)=NC=NC1=CC=2OCCN1CCN(CC#C)CC1 SDYDJNLCQKFKIL-UHFFFAOYSA-N 0.000 claims 1
- ZBQDUFLGPNBYCE-UHFFFAOYSA-N 6-chloro-n-[5-(oxan-4-yloxy)-7-[3-(4-prop-2-ynylpiperazin-1-yl)propoxy]quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound ClC1=CN=C2OCOC2=C1NC(C1=C(OC2CCOCC2)C=2)=NC=NC1=CC=2OCCCN1CCN(CC#C)CC1 ZBQDUFLGPNBYCE-UHFFFAOYSA-N 0.000 claims 1
- FJNMDDYFEUEVLJ-UHFFFAOYSA-N 6-chloro-n-[5-propan-2-yloxy-7-(2-pyrrolidin-1-ylethoxy)quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCCC1 FJNMDDYFEUEVLJ-UHFFFAOYSA-N 0.000 claims 1
- AMXMRGRLUQUEDG-UHFFFAOYSA-N 6-chloro-n-[5-propan-2-yloxy-7-[2-(4-prop-2-ynylpiperazin-1-yl)ethoxy]quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCN(CC#C)CC1 AMXMRGRLUQUEDG-UHFFFAOYSA-N 0.000 claims 1
- LHNUBGOLVVVBFV-UHFFFAOYSA-N 6-chloro-n-[7-(2-morpholin-4-ylethoxy)-5-(oxan-4-yloxy)quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound ClC1=CN=C2OCOC2=C1NC(C1=C(OC2CCOCC2)C=2)=NC=NC1=CC=2OCCN1CCOCC1 LHNUBGOLVVVBFV-UHFFFAOYSA-N 0.000 claims 1
- CIYSACKPZCOGHC-UHFFFAOYSA-N 6-chloro-n-[7-(2-morpholin-4-ylethoxy)-5-propan-2-yloxyquinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCOCC1 CIYSACKPZCOGHC-UHFFFAOYSA-N 0.000 claims 1
- LXWLEHANZSZKOO-UHFFFAOYSA-N 6-chloro-n-[7-(2-piperazin-1-ylethoxy)-5-propan-2-yloxyquinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCNCC1 LXWLEHANZSZKOO-UHFFFAOYSA-N 0.000 claims 1
- CMSYDWDIPDBPGZ-UHFFFAOYSA-N 6-chloro-n-[7-(2-piperidin-1-ylethoxy)-5-propan-2-yloxyquinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCCCC1 CMSYDWDIPDBPGZ-UHFFFAOYSA-N 0.000 claims 1
- STMAOZDCKQKDGH-UHFFFAOYSA-N 6-chloro-n-[7-(3-morpholin-4-ylpropoxy)-5-(oxan-4-yloxy)quinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound ClC1=CN=C2OCOC2=C1NC(C1=C(OC2CCOCC2)C=2)=NC=NC1=CC=2OCCCN1CCOCC1 STMAOZDCKQKDGH-UHFFFAOYSA-N 0.000 claims 1
- QOCFWLMWEMNAJO-UHFFFAOYSA-N 6-chloro-n-[7-(3-morpholin-4-ylpropoxy)-5-propan-2-yloxyquinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCCN1CCOCC1 QOCFWLMWEMNAJO-UHFFFAOYSA-N 0.000 claims 1
- NPLQFGONSPDLQX-UHFFFAOYSA-N 6-chloro-n-[7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-propan-2-yloxyquinazolin-4-yl]-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound C=1C2=NC=NC(NC=3C(=CN=C4OCOC4=3)Cl)=C2C(OC(C)C)=CC=1OCCN1CCN(C)CC1 NPLQFGONSPDLQX-UHFFFAOYSA-N 0.000 claims 1
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- DANWDGOLHZFHLA-UHFFFAOYSA-N n-[7-[2-(3a,4,6,6a-tetrahydro-[1,3]dioxolo[4,5-c]pyrrol-5-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-yl]-6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-amine Chemical compound ClC1=CN=C2OCOC2=C1NC(C=12)=NC=NC2=CC(OCCN2CC3OCOC3C2)=CC=1OC1CCOCC1 DANWDGOLHZFHLA-UHFFFAOYSA-N 0.000 claims 1
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 abstract 4
- 201000011510 cancer Diseases 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 239000000460 chlorine Substances 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 239000000654 additive Substances 0.000 abstract 1
- 230000000118 anti-neoplastic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic 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
- C07D491/02—Heterocyclic 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
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
- 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
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- 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
-
- 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
-
- 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
- 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
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02292736 | 2002-11-04 | ||
| EP02292736.2 | 2002-11-04 | ||
| EP03290900 | 2003-04-10 | ||
| EP03290900.4 | 2003-04-10 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2005117337A RU2005117337A (ru) | 2006-01-20 |
| RU2350618C2 true RU2350618C2 (ru) | 2009-03-27 |
Family
ID=32313852
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005117337/04A RU2350618C2 (ru) | 2002-11-04 | 2003-10-29 | ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US7462623B2 (https=) |
| EP (1) | EP1562955B1 (https=) |
| JP (2) | JP4593464B2 (https=) |
| KR (1) | KR101089462B1 (https=) |
| AR (1) | AR041884A1 (https=) |
| AT (1) | ATE387451T1 (https=) |
| AU (1) | AU2003278383B2 (https=) |
| BR (1) | BR0315756A (https=) |
| CA (1) | CA2503371C (https=) |
| CO (1) | CO5560578A2 (https=) |
| CY (1) | CY1108061T1 (https=) |
| DE (1) | DE60319410T2 (https=) |
| DK (1) | DK1562955T3 (https=) |
| EG (1) | EG24957A (https=) |
| ES (1) | ES2300619T3 (https=) |
| IL (1) | IL168013A (https=) |
| IS (1) | IS2568B (https=) |
| MX (1) | MXPA05004858A (https=) |
| MY (1) | MY137835A (https=) |
| NO (1) | NO331951B1 (https=) |
| NZ (1) | NZ539408A (https=) |
| PL (1) | PL215161B1 (https=) |
| PT (1) | PT1562955E (https=) |
| RU (1) | RU2350618C2 (https=) |
| SI (1) | SI1562955T1 (https=) |
| TW (1) | TWI320786B (https=) |
| WO (1) | WO2004041829A1 (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2280003B1 (en) | 2002-07-15 | 2014-04-02 | Symphony Evolution, Inc. | Process for preparing receptor-type kinase modulators |
| PT2213661E (pt) | 2003-09-26 | 2011-12-15 | Exelixis Inc | Moduladores de c-met e métodos de uso |
| GB0406445D0 (en) * | 2004-03-23 | 2004-04-28 | Astrazeneca Ab | Combination therapy |
| GB0427697D0 (en) * | 2004-12-17 | 2005-01-19 | Astrazeneca Ab | Chemical process |
| ES2364495T3 (es) * | 2005-02-03 | 2011-09-05 | The General Hospital Corporation | Método para tratar cáncer resistente a gefitinib. |
| WO2009068906A2 (en) * | 2007-11-26 | 2009-06-04 | Astrazeneca Ab | Combinations comprising zd4054 and a src family kinase inhibitor 172 |
| SG173014A1 (en) | 2009-01-16 | 2011-08-29 | Exelixis Inc | Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quin0lin-4-yl] oxy}phenyl)-n' - (4 -fluorophenyl) cyclopropane-1,1-dicarboxamide, and crystalline forms therof for the treatment of cancer |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| CA2812750C (en) | 2010-09-27 | 2020-10-06 | Exelixis, Inc. | Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases |
| TWI577671B (zh) * | 2011-11-14 | 2017-04-11 | Sunshine Lake Pharma Co Ltd | Aminoquinazoline derivatives and salts thereof and methods of use thereof |
| KR20180086187A (ko) | 2015-10-05 | 2018-07-30 | 더 트러스티이스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 | 자가포식 유동의 활성체 및 포스포리파제 d 및 타우를 포함하는 단백질 응집물의 클리어런스 및 단백질질환의 치료 |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| RS66727B1 (sr) | 2018-09-10 | 2025-05-30 | Mirati Therapeutics Inc | Kombinacija dasatiniba i adagrasiba za primenu u lečenju nesitnoćelijskog kancera pluća |
| CN119504612B (zh) * | 2024-11-18 | 2026-04-07 | 中国海洋大学 | 一种喹唑啉茋类衍生物及其制备方法和应用 |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5409930A (en) * | 1991-05-10 | 1995-04-25 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| WO1995015758A1 (en) * | 1993-12-10 | 1995-06-15 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit csf-1r receptor tyrosine kinase |
| US5580870A (en) * | 1992-12-10 | 1996-12-03 | Zeneca Limited | Quinazoline derivatives |
| WO1997030034A1 (en) * | 1996-02-14 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as antitumor agents |
| WO1998013354A1 (en) * | 1996-09-25 | 1998-04-02 | Zeneca Limited | Quinazoline derivatives and pharmaceutical compositions containing them |
| RU2111209C1 (ru) * | 1992-03-11 | 1998-05-20 | Зенека Лимитед | Производные хиназолина, способ их получения и фармацевтическая композиция на их основе |
| RU2127263C1 (ru) * | 1992-01-20 | 1999-03-10 | Зенека Лимитед | Производные хиназолина или их фармацевтически приемлемые соли, способ их получения и фармацевтическая композиция на их основе |
| RU2153495C2 (ru) * | 1995-04-27 | 2000-07-27 | Зенека Лимитед | Производные хиназолина, способ их получения, фармацевтическая композиция и способ достижения антипролиферативного эффекта |
| WO2000047212A1 (en) * | 1999-02-10 | 2000-08-17 | Astrazeneca Ab | Quinazoline derivatives as angiogenesis inhibitors |
Family Cites Families (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5721237A (en) | 1991-05-10 | 1998-02-24 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties |
| US5480883A (en) * | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| PT100905A (pt) * | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| GB9510757D0 (en) | 1994-09-19 | 1995-07-19 | Wellcome Found | Therapeuticaly active compounds |
| US6046206A (en) * | 1995-06-07 | 2000-04-04 | Cell Pathways, Inc. | Method of treating a patient having a precancerous lesions with amide quinazoline derivatives |
| GB9514265D0 (en) | 1995-07-13 | 1995-09-13 | Wellcome Found | Hetrocyclic compounds |
| GB9624482D0 (en) * | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| BR9707495A (pt) * | 1996-02-13 | 1999-07-27 | Zeneca Ltd | Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente |
| US6291455B1 (en) | 1996-03-05 | 2001-09-18 | Zeneca Limited | 4-anilinoquinazoline derivatives |
| EP0888310B1 (en) * | 1996-03-15 | 2005-09-07 | AstraZeneca AB | Cinnoline derivatives and use as medicine |
| GB9707800D0 (en) | 1996-05-06 | 1997-06-04 | Zeneca Ltd | Chemical compounds |
| ID19609A (id) | 1996-07-13 | 1998-07-23 | Glaxo Group Ltd | Senyawa-senyawa heterosiklik |
| KR100567649B1 (ko) | 1996-09-25 | 2006-04-05 | 아스트라제네카 유케이 리미티드 | 혈관 내피 성장 인자와 같은 성장 인자의 효과를 억제하는 퀴놀린 유도체 |
| WO1999010349A1 (en) | 1997-08-22 | 1999-03-04 | Zeneca Limited | Oxindolylquinazoline derivatives as angiogenesis inhibitors |
| BR9914167B1 (pt) | 1998-09-29 | 2011-03-09 | compostos e composições farmacêuticas compreendendo 3-ciano quinolinas substituìdas. | |
| KR100860295B1 (ko) * | 1998-10-08 | 2008-09-25 | 아스트라제네카 아베 | 퀴나졸린 유도체 |
| GB9922171D0 (en) | 1999-09-21 | 1999-11-17 | Zeneca Ltd | Chemical compounds |
| KR20020032608A (ko) | 1999-09-21 | 2002-05-03 | 다비드 에 질레스 | 퀴나졸린 화합물 및 이를 함유하는 제약 조성물 |
| CZ301689B6 (cs) | 1999-11-05 | 2010-05-26 | Astrazeneca Ab | Derivát chinazolinu a farmaceutický prostredek, který ho obsahuje |
| AU2001235804A1 (en) | 2000-03-06 | 2001-09-17 | Astrazeneca Ab | Therapy |
| GB0008269D0 (en) | 2000-04-05 | 2000-05-24 | Astrazeneca Ab | Combination chemotherapy |
| ES2267748T3 (es) * | 2000-04-07 | 2007-03-16 | Astrazeneca Ab | Compuestos de quinazolina. |
| UA73993C2 (uk) * | 2000-06-06 | 2005-10-17 | Астразенека Аб | Хіназолінові похідні для лікування пухлин та фармацевтична композиція |
| ES2317923T3 (es) * | 2000-08-09 | 2009-05-01 | Astrazeneca Ab | Compuestos de cinolina. |
| CA2416525A1 (en) | 2000-08-09 | 2002-02-14 | Astrazeneca Ab | Indole, azaindole and indazole derivatives having vegf inhibiting activity |
| WO2002012226A1 (en) | 2000-08-09 | 2002-02-14 | Astrazeneca Ab | Quinoline derivatives having vegf inhibiting activity |
| CA2419301C (en) | 2000-08-21 | 2009-12-08 | Astrazeneca Ab | Quinazoline derivatives |
| WO2002030926A1 (en) | 2000-10-13 | 2002-04-18 | Astrazeneca Ab | Quinazoline derivatives |
| US6849625B2 (en) * | 2000-10-13 | 2005-02-01 | Astrazeneca Ab | Quinazoline derivatives with anti-tumour activity |
| US20040063733A1 (en) | 2000-10-25 | 2004-04-01 | Lambert Christine Marie Paul | Quinazoline derivatives |
| DE60229046D1 (de) | 2001-04-19 | 2008-11-06 | Astrazeneca Ab | Chinazolin derivate |
| WO2002092578A1 (en) | 2001-05-14 | 2002-11-21 | Astrazeneca Ab | Quinazoline derivatives |
| WO2002092577A1 (en) | 2001-05-14 | 2002-11-21 | Astrazeneca Ab | Quinazoline derivatives |
| WO2002092579A1 (en) | 2001-05-14 | 2002-11-21 | Astrazeneca Ab | 4-anilinoquinazoline derivatives |
| US7501516B2 (en) | 2001-07-16 | 2009-03-10 | Astrazeneca Ab | Quinoline derivatives and their use as tyrosine kinase inhibitors |
| GB0126879D0 (en) | 2001-11-08 | 2002-01-02 | Astrazeneca Ab | Combination therapy |
| AU2002365664A1 (en) | 2001-12-05 | 2003-06-17 | Astrazeneca Ab | Quinoline derivatives as antitumour agents |
| JP4608215B2 (ja) | 2002-02-01 | 2011-01-12 | アストラゼネカ アクチボラグ | キナゾリン化合物 |
| GB0215823D0 (en) | 2002-07-09 | 2002-08-14 | Astrazeneca Ab | Quinazoline derivatives |
| WO2004004732A1 (en) | 2002-07-09 | 2004-01-15 | Astrazeneca Ab | Quinazoline derivatives for use in the treatment of cancer |
| GB0218526D0 (en) | 2002-08-09 | 2002-09-18 | Astrazeneca Ab | Combination therapy |
| KR20050056190A (ko) | 2002-08-09 | 2005-06-14 | 아스트라제네카 아베 | 암의 치료에서의 방사선 요법과 함께 혈관 내피 성장 인자수용체의 억제제인 ｚｄ6474의 병행 치료 |
| GB0223380D0 (en) | 2002-10-09 | 2002-11-13 | Astrazeneca Ab | Combination therapy |
| GB0226434D0 (en) * | 2002-11-13 | 2002-12-18 | Astrazeneca Ab | Combination product |
| PT1592423E (pt) | 2003-02-13 | 2011-06-16 | Astrazeneca Ab | Terapia de combinação de zd6474 com 5-fu e/ou cpt-11 |
| GB0310401D0 (en) * | 2003-05-07 | 2003-06-11 | Astrazeneca Ab | Therapeutic agent |
-
2003
- 2003-10-29 RU RU2005117337/04A patent/RU2350618C2/ru not_active IP Right Cessation
- 2003-10-29 BR BR0315756-3A patent/BR0315756A/pt not_active IP Right Cessation
- 2003-10-29 DE DE60319410T patent/DE60319410T2/de not_active Expired - Lifetime
- 2003-10-29 CA CA2503371A patent/CA2503371C/en not_active Expired - Fee Related
- 2003-10-29 PL PL376255A patent/PL215161B1/pl unknown
- 2003-10-29 WO PCT/GB2003/004703 patent/WO2004041829A1/en not_active Ceased
- 2003-10-29 JP JP2005502127A patent/JP4593464B2/ja not_active Expired - Fee Related
- 2003-10-29 KR KR1020057007855A patent/KR101089462B1/ko not_active Expired - Fee Related
- 2003-10-29 EP EP03769689A patent/EP1562955B1/en not_active Expired - Lifetime
- 2003-10-29 NZ NZ539408A patent/NZ539408A/en not_active IP Right Cessation
- 2003-10-29 PT PT03769689T patent/PT1562955E/pt unknown
- 2003-10-29 AT AT03769689T patent/ATE387451T1/de active
- 2003-10-29 DK DK03769689T patent/DK1562955T3/da active
- 2003-10-29 SI SI200331192T patent/SI1562955T1/sl unknown
- 2003-10-29 AU AU2003278383A patent/AU2003278383B2/en not_active Ceased
- 2003-10-29 ES ES03769689T patent/ES2300619T3/es not_active Expired - Lifetime
- 2003-10-29 US US10/533,931 patent/US7462623B2/en not_active Expired - Fee Related
- 2003-10-29 MX MXPA05004858A patent/MXPA05004858A/es active IP Right Grant
- 2003-10-30 TW TW092130284A patent/TWI320786B/zh not_active IP Right Cessation
- 2003-11-03 MY MYPI20034197A patent/MY137835A/en unknown
- 2003-11-04 AR ARP030104036A patent/AR041884A1/es not_active Application Discontinuation
-
2005
- 2005-04-13 IL IL168013A patent/IL168013A/en not_active IP Right Cessation
- 2005-04-19 NO NO20051900A patent/NO331951B1/no not_active IP Right Cessation
- 2005-04-30 EG EGNA2005000178 patent/EG24957A/xx active
- 2005-05-03 CO CO05042313A patent/CO5560578A2/es not_active Application Discontinuation
- 2005-05-19 IS IS7849A patent/IS2568B/is unknown
-
2008
- 2008-04-24 CY CY20081100460T patent/CY1108061T1/el unknown
-
2010
- 2010-07-26 JP JP2010167576A patent/JP2010270143A/ja active Pending
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5409930A (en) * | 1991-05-10 | 1995-04-25 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| RU2127263C1 (ru) * | 1992-01-20 | 1999-03-10 | Зенека Лимитед | Производные хиназолина или их фармацевтически приемлемые соли, способ их получения и фармацевтическая композиция на их основе |
| RU2111209C1 (ru) * | 1992-03-11 | 1998-05-20 | Зенека Лимитед | Производные хиназолина, способ их получения и фармацевтическая композиция на их основе |
| US5580870A (en) * | 1992-12-10 | 1996-12-03 | Zeneca Limited | Quinazoline derivatives |
| WO1995015758A1 (en) * | 1993-12-10 | 1995-06-15 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit csf-1r receptor tyrosine kinase |
| RU2153495C2 (ru) * | 1995-04-27 | 2000-07-27 | Зенека Лимитед | Производные хиназолина, способ их получения, фармацевтическая композиция и способ достижения антипролиферативного эффекта |
| WO1997030034A1 (en) * | 1996-02-14 | 1997-08-21 | Zeneca Limited | Quinazoline derivatives as antitumor agents |
| WO1998013354A1 (en) * | 1996-09-25 | 1998-04-02 | Zeneca Limited | Quinazoline derivatives and pharmaceutical compositions containing them |
| WO2000047212A1 (en) * | 1999-02-10 | 2000-08-17 | Astrazeneca Ab | Quinazoline derivatives as angiogenesis inhibitors |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2350618C2 (ru) | ПРОИЗВОДНЫЕ ХИНАЗОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Src ТИРОЗИНКИНАЗЫ | |
| Boschelli et al. | Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity | |
| CL2023001461A1 (es) | Inhibidores de prmt5 novedosos | |
| US20100173954A1 (en) | Treatment of cancers having resistance to chemotherapeutic agents | |
| DE60237145D1 (de) | Chinazolinderivate | |
| BRPI0407834A (pt) | composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase | |
| CO5700751A2 (es) | Derivados de 4-(6-cloro-2,3-metilendioxianilino)-7 (alcoxi sustituiidos)-5-tetrahidropiran-4-iloxiquinazolina como inhibidores de la enzima tirosina quinasa no receptora y composiciones que los contienen | |
| DE60206911D1 (de) | Imidazol-2-carbonsäureamid derivate als raf-kinase-inhibitoren | |
| EA200900152A1 (ru) | Ингибиторы пирролотриазинкиназы | |
| BRPI0408005A (pt) | composto, composição farmacêutica, métodos para inibir angiogênese, atividade de pde4 em uma célula e proliferação de célula de cáncer, para inibir ou reduzir polimerização de tubulina ou estabilidade de tubulina em uma célula, para tratar ou melhorar um distúrbio inflamatório, um cáncer e um distúrbio do sistema nervoso central e para visar, bloquear ou destruir a função de vasculatura de tumor e o endotélio de vasos de tumor | |
| RU2003107683A (ru) | Производные хиназолина | |
| DE60214198D1 (de) | Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen | |
| NO20060415L (no) | Piperidyl-Kinazolinderivater som Tyrosin-Kinase-Inhibitorer | |
| JP2018531983A (ja) | タンパク質分解誘導キメラ化合物ならびにその調製方法および使用方法 | |
| UY27742A1 (es) | Derivados de quinazolina | |
| CY1107433T1 (el) | Παραγωγα 1-(2η-πυραζολ-3-υλο)-3-(4-[1-(βενζοϋλο)-πιπepιδιν-4-υλομεθυλο]-φαινυλο)-ουριας και συναφεις ενωσεις ως αναστολεις της ρ38 κινασης και/ή tnf-αναστολεις για την αντιμετωπιση φλεγμονων | |
| UY28059A1 (es) | Nuevos derivados de dihidropirimido (4,5-d) pirimidona sustituida por amino. fabricacion y uso de los mismos como agentes farmaceuticos. | |
| NO20061746L (no) | Kinazolinderivater som antiproliferative midler | |
| DE60316013D1 (de) | Heteroaryl-pyrimidinderivate als jak-inhibitoren | |
| GEP20115147B (en) | Pyrimidine derivatives used as pi-3 kinase inhibitors | |
| EA200400466A1 (ru) | Производные пиперазина с антагонистической активностью к рецептору ccr1 | |
| ATE353888T1 (de) | Chinazolinderivate | |
| DE60215178D1 (de) | Quinolin-derivate und ihre verwendung als inhibitoren der tyrosine kinase | |
| SE0402735D0 (sv) | Novel compounds | |
| JP2003528917A5 (https=) |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20161030 |