RU2440991C2 - Хиназолины, полезные в качестве модуляторов ионных каналов - Google Patents
Хиназолины, полезные в качестве модуляторов ионных каналов Download PDFInfo
- Publication number
- RU2440991C2 RU2440991C2 RU2007111897/04A RU2007111897A RU2440991C2 RU 2440991 C2 RU2440991 C2 RU 2440991C2 RU 2007111897/04 A RU2007111897/04 A RU 2007111897/04A RU 2007111897 A RU2007111897 A RU 2007111897A RU 2440991 C2 RU2440991 C2 RU 2440991C2
- Authority
- RU
- Russia
- Prior art keywords
- compound
- independently
- ring
- halogen
- membered saturated
- Prior art date
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- 102000004310 Ion Channels Human genes 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 85
- 125000005842 heteroatom Chemical group 0.000 claims abstract 38
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 38
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 36
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 25
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 24
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 10
- 125000003118 aryl group Chemical group 0.000 claims abstract 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims abstract 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000004429 atom Chemical group 0.000 claims abstract 4
- 229910052799 carbon Inorganic materials 0.000 claims abstract 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 44
- 239000001257 hydrogen Substances 0.000 claims 44
- 229910052736 halogen Inorganic materials 0.000 claims 33
- 150000002367 halogens Chemical class 0.000 claims 32
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 28
- 125000001931 aliphatic group Chemical group 0.000 claims 28
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 28
- 239000001301 oxygen Chemical group 0.000 claims 28
- 125000001424 substituent group Chemical group 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 150000002431 hydrogen Chemical group 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 229910052717 sulfur Chemical group 0.000 claims 5
- 239000011593 sulfur Chemical group 0.000 claims 5
- -1 tetrahydro [2H] pyranyl Chemical group 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 3
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 229940126121 sodium channel inhibitor Drugs 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 108010052164 Sodium Channels Proteins 0.000 abstract 2
- 102000018674 Sodium Channels Human genes 0.000 abstract 2
- 230000001419 dependent effect Effects 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000005647 linker group Chemical group 0.000 abstract 2
- 208000000094 Chronic Pain Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 230000036982 action potential Effects 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 230000001747 exhibiting effect Effects 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 210000000107 myocyte Anatomy 0.000 abstract 1
- 210000002569 neuron Anatomy 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 0 CN(*)c1nc(C2C=C=C*(*)C=C2)n*(C=C2)c1C=C*2N Chemical compound CN(*)c1nc(C2C=C=C*(*)C=C2)n*(C=C2)c1C=C*2N 0.000 description 3
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Heart & Thoracic Surgery (AREA)
- Anesthesiology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Reproductive Health (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Compounds Of Unknown Constitution (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US60703604P | 2004-09-02 | 2004-09-02 | |
| US60703704P | 2004-09-02 | 2004-09-02 | |
| US60715004P | 2004-09-02 | 2004-09-02 | |
| US60703304P | 2004-09-02 | 2004-09-02 | |
| US60724504P | 2004-09-02 | 2004-09-02 | |
| US60/607,245 | 2004-09-02 | ||
| US60/607,036 | 2004-09-02 | ||
| US60/607,033 | 2004-09-02 | ||
| US60/607,037 | 2004-09-02 | ||
| US60/607,150 | 2004-09-02 | ||
| PCT/US2005/031146 WO2006028904A1 (en) | 2004-09-02 | 2005-08-31 | Quinazolines useful as modulators of ion channels |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2007111897A RU2007111897A (ru) | 2008-10-10 |
| RU2440991C2 true RU2440991C2 (ru) | 2012-01-27 |
Family
ID=35517001
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007111897/04A RU2440991C2 (ru) | 2004-09-02 | 2005-08-31 | Хиназолины, полезные в качестве модуляторов ионных каналов |
Country Status (18)
| Country | Link |
|---|---|
| EP (1) | EP1784393B1 (https=) |
| JP (1) | JP5014994B2 (https=) |
| KR (1) | KR20070057914A (https=) |
| CN (1) | CN101068794B (https=) |
| AT (1) | ATE435214T1 (https=) |
| AU (1) | AU2005282761B2 (https=) |
| BR (1) | BRPI0514893A (https=) |
| CA (1) | CA2578739A1 (https=) |
| DE (1) | DE602005015231D1 (https=) |
| ES (1) | ES2327945T4 (https=) |
| IL (1) | IL181700A0 (https=) |
| MA (1) | MA28909B1 (https=) |
| MX (1) | MX2007002582A (https=) |
| NO (1) | NO20071742L (https=) |
| NZ (1) | NZ589252A (https=) |
| RU (1) | RU2440991C2 (https=) |
| WO (1) | WO2006028904A1 (https=) |
| ZA (1) | ZA200702375B (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2836663C1 (ru) * | 2020-08-12 | 2025-03-18 | Дженентек, Инк. | Синтез соединений хиназолина |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI351284B (en) | 2004-04-09 | 2011-11-01 | Chugai Pharmaceutical Co Ltd | Novel water-soluble prodrugs |
| US7928107B2 (en) | 2004-09-02 | 2011-04-19 | Vertex Pharmaceuticals Incorporated | Quinazolines useful as modulators of ion channels |
| TW200744603A (en) | 2005-08-22 | 2007-12-16 | Chugai Pharmaceutical Co Ltd | Novel anticancer concomitant drug |
| US20090118271A1 (en) * | 2005-10-19 | 2009-05-07 | Chugai Seiyaku Kabushiki Kaisha | Preventive or Therapeutic Agents for Pancreatic Cancer, Ovarian Cancer, or Liver Cancer Comprising a Novel Water-Soluble Prodrug |
| ES2377988T3 (es) * | 2005-11-14 | 2012-04-03 | Vertex Pharmaceuticals, Inc. | Quinazolinas útiles como moduladores de canales iónicos controlados por voltaje |
| KR20080089416A (ko) * | 2005-12-21 | 2008-10-06 | 페인셉터 파마 코포레이션 | 개폐 이온 통로를 조절하기 위한 조성물 및 방법 |
| WO2007146284A2 (en) | 2006-06-12 | 2007-12-21 | Vertex Pharmaceuticals Incorporated | Thienopyrimidines useful as modulators of ion channels |
| WO2008069976A2 (en) | 2006-12-01 | 2008-06-12 | President And Fellows Of Harvard College | Compounds and methods for enzyme-mediated tumor imaging and therapy |
| WO2008147864A2 (en) * | 2007-05-22 | 2008-12-04 | Xenon Pharmaceuticals Inc. | Methods of using piperazine compounds in treating sodium channel-mediated diseases or conditions |
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2005
- 2005-08-31 KR KR1020077007601A patent/KR20070057914A/ko not_active Ceased
- 2005-08-31 RU RU2007111897/04A patent/RU2440991C2/ru not_active IP Right Cessation
- 2005-08-31 ES ES05807734T patent/ES2327945T4/es not_active Expired - Lifetime
- 2005-08-31 AU AU2005282761A patent/AU2005282761B2/en not_active Ceased
- 2005-08-31 AT AT05807734T patent/ATE435214T1/de active
- 2005-08-31 MX MX2007002582A patent/MX2007002582A/es unknown
- 2005-08-31 WO PCT/US2005/031146 patent/WO2006028904A1/en not_active Ceased
- 2005-08-31 NZ NZ589252A patent/NZ589252A/en not_active IP Right Cessation
- 2005-08-31 JP JP2007530356A patent/JP5014994B2/ja not_active Expired - Fee Related
- 2005-08-31 CN CN2005800374969A patent/CN101068794B/zh not_active Expired - Fee Related
- 2005-08-31 ZA ZA200702375A patent/ZA200702375B/xx unknown
- 2005-08-31 EP EP05807734A patent/EP1784393B1/en not_active Expired - Lifetime
- 2005-08-31 DE DE602005015231T patent/DE602005015231D1/de not_active Expired - Lifetime
- 2005-08-31 CA CA002578739A patent/CA2578739A1/en not_active Abandoned
- 2005-08-31 BR BRPI0514893-6A patent/BRPI0514893A/pt not_active IP Right Cessation
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2007
- 2007-03-02 MA MA29735A patent/MA28909B1/fr unknown
- 2007-03-04 IL IL181700A patent/IL181700A0/en unknown
- 2007-04-02 NO NO20071742A patent/NO20071742L/no not_active Application Discontinuation
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| WO2003049739A1 (en) * | 2001-12-07 | 2003-06-19 | Vertex Pharmaceuticals, Inc. | Pyrimidine-based compounds useful as gsk-3 inhibitors |
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| RU2836663C1 (ru) * | 2020-08-12 | 2025-03-18 | Дженентек, Инк. | Синтез соединений хиназолина |
Also Published As
| Publication number | Publication date |
|---|---|
| DE602005015231D1 (de) | 2009-08-13 |
| KR20070057914A (ko) | 2007-06-07 |
| IL181700A0 (en) | 2007-07-04 |
| JP2008511670A (ja) | 2008-04-17 |
| EP1784393B1 (en) | 2009-07-01 |
| WO2006028904A9 (en) | 2006-06-22 |
| EP1784393A1 (en) | 2007-05-16 |
| NO20071742L (no) | 2007-04-02 |
| RU2007111897A (ru) | 2008-10-10 |
| MA28909B1 (fr) | 2007-10-01 |
| CN101068794B (zh) | 2012-12-19 |
| ZA200702375B (en) | 2009-03-25 |
| AU2005282761A1 (en) | 2006-03-16 |
| ATE435214T1 (de) | 2009-07-15 |
| AU2005282761B2 (en) | 2012-02-02 |
| CA2578739A1 (en) | 2006-03-16 |
| ES2327945T3 (es) | 2009-11-05 |
| JP5014994B2 (ja) | 2012-08-29 |
| WO2006028904A1 (en) | 2006-03-16 |
| ES2327945T4 (es) | 2010-07-02 |
| HK1104544A1 (en) | 2008-01-18 |
| NZ589252A (en) | 2012-06-29 |
| MX2007002582A (es) | 2008-01-14 |
| CN101068794A (zh) | 2007-11-07 |
| BRPI0514893A (pt) | 2007-11-27 |
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