RU2325159C2 - Применение производных изохинолина для лечения рака и заболеваний, связанных с киназой мар - Google Patents
Применение производных изохинолина для лечения рака и заболеваний, связанных с киназой мар Download PDFInfo
- Publication number
- RU2325159C2 RU2325159C2 RU2005131168/04A RU2005131168A RU2325159C2 RU 2325159 C2 RU2325159 C2 RU 2325159C2 RU 2005131168/04 A RU2005131168/04 A RU 2005131168/04A RU 2005131168 A RU2005131168 A RU 2005131168A RU 2325159 C2 RU2325159 C2 RU 2325159C2
- Authority
- RU
- Russia
- Prior art keywords
- ness
- phenyl
- alkyl
- substituted
- halogen
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title claims abstract 5
- 201000011510 cancer Diseases 0.000 title claims abstract 5
- 201000010099 disease Diseases 0.000 title claims abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract 5
- 108091000080 Phosphotransferase Proteins 0.000 title claims 2
- 102000020233 phosphotransferase Human genes 0.000 title claims 2
- 238000000034 method Methods 0.000 claims abstract 23
- 201000001441 melanoma Diseases 0.000 claims abstract 14
- 102000009929 raf Kinases Human genes 0.000 claims abstract 13
- 108010077182 raf Kinases Proteins 0.000 claims abstract 13
- 150000001875 compounds Chemical class 0.000 claims abstract 7
- 102000043136 MAP kinase family Human genes 0.000 claims abstract 4
- 108091054455 MAP kinase family Proteins 0.000 claims abstract 4
- 230000035772 mutation Effects 0.000 claims abstract 4
- 239000003814 drug Substances 0.000 claims abstract 3
- -1 hydroxy, hydroxy Chemical group 0.000 claims 40
- 125000000217 alkyl group Chemical group 0.000 claims 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 24
- 150000002367 halogens Chemical group 0.000 claims 18
- 125000003282 alkyl amino group Chemical group 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 14
- 125000002947 alkylene group Chemical group 0.000 claims 13
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 8
- 125000004414 alkyl thio group Chemical group 0.000 claims 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 8
- 125000001589 carboacyl group Chemical group 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 6
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 6
- 241000534944 Thia Species 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 125000004423 acyloxy group Chemical group 0.000 claims 4
- 125000005236 alkanoylamino group Chemical group 0.000 claims 4
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 4
- 125000003277 amino group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 230000014509 gene expression Effects 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims 4
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 4
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 4
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 230000002018 overexpression Effects 0.000 claims 3
- 230000019491 signal transduction Effects 0.000 claims 3
- 230000011664 signaling Effects 0.000 claims 3
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims 2
- 230000003213 activating effect Effects 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 2
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 2
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000043 benzamido group Chemical group [H]N([*])C(=O)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 102100025093 Zinc fingers and homeoboxes protein 2 Human genes 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 125000005156 substituted alkylene group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 239000007924 injection Substances 0.000 abstract 1
- 238000002347 injection Methods 0.000 abstract 1
- 230000008054 signal transmission Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
Classifications
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Quinoline Compounds (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45362403P | 2003-03-11 | 2003-03-11 | |
| US60/453,624 | 2003-03-11 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2005131168A RU2005131168A (ru) | 2006-05-27 |
| RU2325159C2 true RU2325159C2 (ru) | 2008-05-27 |
Family
ID=32990797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005131168/04A RU2325159C2 (ru) | 2003-03-11 | 2004-03-10 | Применение производных изохинолина для лечения рака и заболеваний, связанных с киназой мар |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1603566B1 (enExample) |
| JP (1) | JP2006519807A (enExample) |
| KR (1) | KR20050108383A (enExample) |
| CN (1) | CN1758910A (enExample) |
| AT (1) | ATE421324T1 (enExample) |
| AU (1) | AU2004218914A1 (enExample) |
| BR (1) | BRPI0408257A (enExample) |
| CA (1) | CA2518530A1 (enExample) |
| DE (1) | DE602004019193D1 (enExample) |
| ES (1) | ES2318276T3 (enExample) |
| HR (1) | HRP20050788A2 (enExample) |
| IS (1) | IS8064A (enExample) |
| MA (1) | MA27724A1 (enExample) |
| MX (1) | MXPA05009687A (enExample) |
| NO (1) | NO20054647L (enExample) |
| PL (1) | PL1603566T3 (enExample) |
| PT (1) | PT1603566E (enExample) |
| RU (1) | RU2325159C2 (enExample) |
| TN (1) | TNSN05223A1 (enExample) |
| TW (1) | TW200501955A (enExample) |
| WO (1) | WO2004080464A1 (enExample) |
| ZA (1) | ZA200506571B (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004247626B8 (en) | 2003-05-15 | 2011-05-19 | Arqule, Inc. | Imidazothiazoles and imidazoxazole derivatives as inhibitors of p38 |
| PE20050952A1 (es) * | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
| WO2006010082A1 (en) | 2004-07-08 | 2006-01-26 | Arqule, Inc. | 1,4-disubstituted naphtalenes as inhibitors of p38 map kinase |
| US8178672B2 (en) | 2004-10-19 | 2012-05-15 | Arqule, Inc. | Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase |
| CN101160131A (zh) * | 2005-02-25 | 2008-04-09 | 诺瓦提斯公司 | Bcr-abl和raf抑制剂的药物组合产品 |
| JP5049970B2 (ja) * | 2005-07-26 | 2012-10-17 | サノフイ | Ｒｈｏ−キナーゼ阻害剤としてのシクロヘキシルアミンイソキノロン誘導体 |
| US8318941B2 (en) | 2006-07-06 | 2012-11-27 | Bristol-Myers Squibb Company | Pyridone/hydroxypyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| JP2009077712A (ja) * | 2007-09-11 | 2009-04-16 | F Hoffmann La Roche Ag | Ｂ−Ｒａｆキナーゼ阻害剤に対する感受性についての診断試験 |
| US20110152770A1 (en) | 2009-07-30 | 2011-06-23 | Tandem Diabetes Care, Inc. | Infusion pump system with disposable cartridge having pressure venting and pressure feedback |
| BR112012022801B8 (pt) * | 2010-03-09 | 2019-10-29 | Dana Farber Cancer Inst Inc | método de identificar um indivíduo que tem câncer que é provável beneficiar-se do tratamento com uma terapia de combinação com um inibidor de raf e um segundo inibidor e uso de um inibidor de raf e um segundo inibidor para a fabricação de um medicamento para tratar câncer |
| US9056855B2 (en) * | 2010-10-28 | 2015-06-16 | Viamet Pharmaceuticals, Inc. | Metalloenzyme inhibitor compounds |
| CN103435430B (zh) * | 2013-08-08 | 2015-02-18 | 四川大学 | 一种还原酰胺类化合物的方法 |
| KR102119943B1 (ko) | 2018-05-23 | 2020-06-05 | 주식회사 포스코 | 시편배치유닛 및 이를 포함하는 도장밀착성 실험장치 |
| US20210275516A1 (en) * | 2018-07-02 | 2021-09-09 | Ecole Polytechnique Federale De Lausanne (Epfl) | Lactate enhancing compounds and uses thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2000102667A (ru) * | 1997-07-11 | 2001-10-20 | Новартис Аг | Производные пиридина |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW544448B (en) * | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| BR9912938B1 (pt) * | 1998-08-11 | 2011-06-28 | derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos. | |
| GT200000158A (es) * | 1999-09-28 | 2002-03-16 | Piridinas y piridacinas sustituidas con actividad de inhibicion de angiogenesis. | |
| WO2001058899A1 (en) * | 2000-02-09 | 2001-08-16 | Novartis Ag | Pyridine derivatives inhibiting angiogenesis and/or vegf receptor tyrosine kinase |
| WO2002060392A2 (en) * | 2001-01-31 | 2002-08-08 | Synaptic Pharmaceutical Corporation | Use of gal3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods |
| EP1364212B1 (en) * | 2001-03-02 | 2011-02-02 | GPC Biotech AG | Three hybrid assay system |
| MXPA04005561A (es) * | 2001-12-21 | 2004-12-06 | Bayer Pharmaceuticals Corp | Terapias de combinacion anti-angiogenesis que comprenden derivados de piridazina o piridina. |
| US7220775B2 (en) * | 2002-08-07 | 2007-05-22 | H. Lundbeck A/S | Compound useful for the treatment of neuropathic pain |
-
2004
- 2004-03-10 AU AU2004218914A patent/AU2004218914A1/en not_active Abandoned
- 2004-03-10 PL PL04718960T patent/PL1603566T3/pl unknown
- 2004-03-10 JP JP2006504625A patent/JP2006519807A/ja active Pending
- 2004-03-10 PT PT04718960T patent/PT1603566E/pt unknown
- 2004-03-10 TW TW093106341A patent/TW200501955A/zh unknown
- 2004-03-10 MX MXPA05009687A patent/MXPA05009687A/es active IP Right Grant
- 2004-03-10 DE DE602004019193T patent/DE602004019193D1/de not_active Expired - Lifetime
- 2004-03-10 ES ES04718960T patent/ES2318276T3/es not_active Expired - Lifetime
- 2004-03-10 CA CA002518530A patent/CA2518530A1/en not_active Abandoned
- 2004-03-10 HR HR20050788A patent/HRP20050788A2/xx not_active Application Discontinuation
- 2004-03-10 RU RU2005131168/04A patent/RU2325159C2/ru not_active IP Right Cessation
- 2004-03-10 BR BRPI0408257-5A patent/BRPI0408257A/pt not_active IP Right Cessation
- 2004-03-10 EP EP04718960A patent/EP1603566B1/en not_active Expired - Lifetime
- 2004-03-10 CN CNA2004800065706A patent/CN1758910A/zh active Pending
- 2004-03-10 AT AT04718960T patent/ATE421324T1/de active
- 2004-03-10 WO PCT/EP2004/002460 patent/WO2004080464A1/en not_active Ceased
- 2004-03-10 KR KR1020057016936A patent/KR20050108383A/ko not_active Ceased
-
2005
- 2005-08-17 ZA ZA200506571A patent/ZA200506571B/en unknown
- 2005-09-09 TN TNP2005000223A patent/TNSN05223A1/en unknown
- 2005-09-23 MA MA28511A patent/MA27724A1/fr unknown
- 2005-10-10 IS IS8064A patent/IS8064A/is unknown
- 2005-10-10 NO NO20054647A patent/NO20054647L/no not_active Application Discontinuation
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2000102667A (ru) * | 1997-07-11 | 2001-10-20 | Новартис Аг | Производные пиридина |
Also Published As
| Publication number | Publication date |
|---|---|
| HRP20050788A2 (en) | 2006-12-31 |
| EP1603566A1 (en) | 2005-12-14 |
| TW200501955A (en) | 2005-01-16 |
| CA2518530A1 (en) | 2004-09-23 |
| PT1603566E (pt) | 2009-04-27 |
| ES2318276T3 (es) | 2009-05-01 |
| DE602004019193D1 (de) | 2009-03-12 |
| ATE421324T1 (de) | 2009-02-15 |
| AU2004218914A1 (en) | 2004-09-23 |
| MXPA05009687A (es) | 2005-10-20 |
| JP2006519807A (ja) | 2006-08-31 |
| TNSN05223A1 (en) | 2007-06-11 |
| IS8064A (is) | 2005-10-10 |
| MA27724A1 (fr) | 2006-01-02 |
| CN1758910A (zh) | 2006-04-12 |
| BRPI0408257A (pt) | 2006-03-07 |
| NO20054647D0 (no) | 2005-10-10 |
| WO2004080464A1 (en) | 2004-09-23 |
| RU2005131168A (ru) | 2006-05-27 |
| NO20054647L (no) | 2005-12-09 |
| EP1603566B1 (en) | 2009-01-21 |
| ZA200506571B (en) | 2006-07-26 |
| PL1603566T3 (pl) | 2009-07-31 |
| KR20050108383A (ko) | 2005-11-16 |
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