HRP20100272T1 - Piridinaminosulfonil supstituirani benzamidi kao inhibitori citokroma p450 3a4 (cyp3a4) - Google Patents
Piridinaminosulfonil supstituirani benzamidi kao inhibitori citokroma p450 3a4 (cyp3a4)Info
- Publication number
- HRP20100272T1 HRP20100272T1 HR20100272T HRP20100272T HRP20100272T1 HR P20100272 T1 HRP20100272 T1 HR P20100272T1 HR 20100272 T HR20100272 T HR 20100272T HR P20100272 T HRP20100272 T HR P20100272T HR P20100272 T1 HRP20100272 T1 HR P20100272T1
- Authority
- HR
- Croatia
- Prior art keywords
- cr12ar12b
- alkyl
- heterocyclyl
- cycloalkyl
- aryl
- Prior art date
Links
- 102000004328 Cytochrome P-450 CYP3A Human genes 0.000 title 2
- 108010081668 Cytochrome P-450 CYP3A Proteins 0.000 title 2
- 229940054066 benzamide antipsychotics Drugs 0.000 title 1
- 150000003936 benzamides Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 8
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000006694 (C2-C10) heterocyclyl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 102220475869 Keratin, type I cytoskeletal 10_R12A_mutation Human genes 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 1
- 101000596772 Homo sapiens Transcription factor 7-like 1 Proteins 0.000 abstract 1
- 101000666382 Homo sapiens Transcription factor E2-alpha Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 102100035097 Transcription factor 7-like 1 Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/76—Nitrogen atoms to which a second hetero atom is attached
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious 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
-
- 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
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- 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
- C07D487/08—Bridged systems
Abstract
Spoj formule (I) naznačen time što: R1, R2, R3, R4 su nezavisno izabrani od vodika, C1-C6 alkil, -(CR12aR12b)thalo, -(CR12aR12b)tCN, -(CR12aR12b)tOR12a, -(CR12aR12b)tN(R12aR12b), -(CR12aR12b)tCF3, i -(CR12aR12b)tC6-C10 aril; R5 je vodik ili C1-C6 alkil; R6, R7, R8 i R9 su nezavisno izabrani od vodika, C1-C6 alkil, -(CR12aR12b)thalo, -(CR12aR12b)tCN, -(CR12aR12b)tCF3,-(CR12aR12b)tOR12a, -(CR12aR12b)tN(R12aR12b), -(CR12aR12b)tR12a , -(CR12aR12b)tC3-C11 cikloalkil; -(CR12aR12b)tC6-C10 aril, -(CR12aR12b)tC2-C10 heterociklil, -(CR12aR12b)theteroaril, -O(CR12aR12b)tR12a, -O(CR12aR12b)tC3-C11 cikloalkil, -O(CR12aR12b)tC6-C10 aril, -O(CR12aR12b)tC2-C10 heterociklil, -O(CR12aR12b)theteroaril, -O(CR12aR12b)tR12a i -O(CR12aR12b)tN(R12aR12b), gdje je svaka od spomenutih C1-C6 alkil, C3-C11 cikloalkil, C6-C10 aril i C2-C10 heterociklil, i heteroaril grupa po izboru supstituirana sa jednim ili više R14.R10 i R11 su nezavisno izabrani od vodika, -(CR12aR12b)tC1-C6 alkil, -(CR12aR12b)tC3-C11 cikloalkil, -(CR12aR12b)tC6-C10 aril, -(CR12aR12b)tC2-C10 heterociklil i -(CR12aR12b)theteroaril, gdje je svaka od spomenutih C1-C6 alkil, C3-C11 cikloalkil, C8-C10 aril, C2-C10 heterociklil, i heteroaril grupa po izboru supstituirana sa jednim ili više R13; iliR10 i R11 , zajedno sa atomom za koji su vezani, grade C2-C10 heterociklil grupu, po izboru supstituiranu sa jednim ili više R13;svaki R12a I R12b je nezavisno odabran od vodika i C1-C6 alkil; ili R12A i R12B , zajedno sa atomom za koji su vezani, GRADE C3-C11 cikloalkil ili C2-C10 heterociklil grupu; svaki od R13 je nezavisno odabran od C1-C6 alkil, halogen, -(CR12AR12B)TCN, -(CR12AR12B)TCF3, -(CR12AR12B)TOCF3, -(CR12AR12B)TC3-C11 cikloalkil, -(CR12AR12B)TC6-C10 aril, -(CR12AR12B)TC2-C10 heterociklil, -(CR12AR12B)Theteroaril, -O(CR12AR12B)TR12A, -O(CR12AR12B)TC6-C10 aril, -O(CR12AR12B)TC2-C10 heterociklil, -O(CR12AR12B)Theteroaril, -(CR12AR12B)TCO2(C1-C6 alkil), -(CR12AR12B)TN(R12AR12B), -(CR12AR12B)TC(O)NR12AR12B, -(CR12AR12B)TOR12A, -(CR12AR12B)TS(O)R12A i -(CR12AR12B)TS(O)2R12A, gdje je svaka od spomenutih C1-C6 alkil, C3-C11 cikloalkil, C6-C10 aril, C2-C10 heterociklil, i heteroaril grupa po izboru supstituirana s jednim ili više R14;svaki od R14 je nezavisno izabran od C1-C6 alkil, halogen, -CN, -CF3, I OR12A; Isvaki t je nezavisno izabran od 0, 1, 2, 3, 4, 5, i 6; ilinjegova farmaceutski prihvatljiva sol ili solvat. Patent sadrži još 17 patentnih zahtjeva.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72015105P | 2005-09-23 | 2005-09-23 | |
| US72311505P | 2005-10-03 | 2005-10-03 | |
| US72546905P | 2005-10-11 | 2005-10-11 | |
| US76225606P | 2006-01-25 | 2006-01-25 | |
| US82166406P | 2006-08-07 | 2006-08-07 | |
| PCT/IB2006/002639 WO2007034312A2 (en) | 2005-09-23 | 2006-09-11 | Pyridinaminosulfonyl substituted benzamides as inhibitors of cytochrome p450 3a4 (cyp3a4) |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20100272T1 true HRP20100272T1 (hr) | 2010-06-30 |
| HRP20100272T2 HRP20100272T2 (hr) | 2010-07-31 |
Family
ID=37889174
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20100272T HRP20100272T2 (hr) | 2005-09-23 | 2010-05-14 | Piridinaminosulfonil supstituirani benzamidi kao inhibitori citokroma p450 3a4 (cyp3a4) |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US7868026B2 (hr) |
| EP (1) | EP1937639B1 (hr) |
| JP (1) | JP4336738B2 (hr) |
| KR (1) | KR100975448B1 (hr) |
| CN (1) | CN101287708B (hr) |
| AT (1) | ATE459603T1 (hr) |
| AU (1) | AU2006293605B2 (hr) |
| BR (1) | BRPI0616156A2 (hr) |
| CA (1) | CA2621805C (hr) |
| CY (1) | CY1110010T1 (hr) |
| DE (1) | DE602006012713D1 (hr) |
| DK (1) | DK1937639T3 (hr) |
| EA (1) | EA014329B1 (hr) |
| EC (1) | ECSP088296A (hr) |
| ES (1) | ES2340200T3 (hr) |
| GE (1) | GEP20115230B (hr) |
| HK (1) | HK1120506A1 (hr) |
| HR (1) | HRP20100272T2 (hr) |
| IL (1) | IL189666A (hr) |
| MA (1) | MA29791B1 (hr) |
| MY (1) | MY143391A (hr) |
| NO (1) | NO20081844L (hr) |
| NZ (1) | NZ566136A (hr) |
| PL (1) | PL1937639T3 (hr) |
| PT (1) | PT1937639E (hr) |
| RS (2) | RS51349B (hr) |
| SI (1) | SI1937639T1 (hr) |
| TN (1) | TNSN08139A1 (hr) |
| WO (1) | WO2007034312A2 (hr) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ574207A (en) * | 2006-07-05 | 2010-10-29 | Pfizer Prod Inc | Pyrazole derivatives as cytochrome p450 inhibitors |
| CA2673586A1 (en) * | 2006-12-26 | 2008-07-24 | Amgen Inc. | N-cyclohexyl benzamides and benzeneacetamides as inhibitors of 11-beta-hydroxysteroid dehydrogenases |
| CA2679882C (en) | 2007-03-08 | 2015-12-29 | The Board Of Trustees Of The Leland Stanford Junior University | Mitochondrial aldehyde dehydrogenase-2 modulators and methods of use thereof |
| MX2010003155A (es) * | 2007-10-04 | 2010-04-01 | Hoffmann La Roche | Derivados de ciclopropil aril amida y uso de los mismos. |
| ES2477552T3 (es) | 2008-09-08 | 2014-07-17 | The Board Of Trustees Of The Leland Stanford Junior University | Moduladores de la actividad de la aldehidodeshidrogenasa y métodos de uso de los mismos |
| EP2349279A4 (en) * | 2008-10-28 | 2013-12-25 | Univ Leland Stanford Junior | ALDEHYDE DEHYDROGENASE MODULATORS AND METHOD OF USE THEREOF |
| DK2385938T3 (en) | 2009-01-12 | 2015-04-27 | Pfizer Ltd | Sulfonamidderivater |
| EP2424517A4 (en) * | 2009-05-01 | 2013-01-23 | Raqualia Pharma Inc | SULFAMOYLBENZOIC ACID DERIVATIVES AS TRPM8 ANTAGONISTS |
| EP2590972B1 (en) | 2010-07-09 | 2015-01-21 | Pfizer Limited | N-sulfonylbenzamides as inhibitors of voltage-gated sodium channels |
| US10457659B2 (en) | 2011-04-29 | 2019-10-29 | The Board Of Trustees Of The Leland Stanford Junior University | Compositions and methods for increasing proliferation of adult salivary stem cells |
| WO2014000178A1 (en) * | 2012-06-27 | 2014-01-03 | Merck Sharp & Dohme Corp. | Sulfonamide derivatives and methods of use thereof for improving the pharmacokinetics of a drug |
| CN104540813A (zh) * | 2012-06-27 | 2015-04-22 | 默沙东公司 | 磺酰胺衍生物以及使用它们用于改善药物的药物动力学的方法 |
| CN105358531B (zh) | 2013-03-14 | 2017-11-14 | 利兰-斯坦福大学初级学院的董事会 | 线粒体醛脱氢酶‑2调节剂和其使用方法 |
| TW201512171A (zh) | 2013-04-19 | 2015-04-01 | Pfizer Ltd | 化學化合物 |
| WO2014194519A1 (en) | 2013-06-07 | 2014-12-11 | Merck Sharp & Dohme Corp. | Imidazole derivatives and methods of use thereof for improving pharmacokinetics of drug |
| WO2015070367A1 (en) | 2013-11-12 | 2015-05-21 | Merck Sharp & Dohme Corp. | Piperidine or piperazine linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug |
| WO2015070366A1 (en) | 2013-11-12 | 2015-05-21 | Merck Sharp & Dohme Corp. | Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug |
| CN106103446B (zh) | 2014-03-26 | 2019-07-30 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物 |
| WO2016101118A1 (en) * | 2014-12-23 | 2016-06-30 | Merck Sharp & Dohme Corp. | Amidoethyl azole orexin receptor antagonists |
| CN108026077B (zh) | 2015-09-04 | 2021-11-05 | 豪夫迈·罗氏有限公司 | 苯氧基甲基衍生物 |
| CN110382484B (zh) | 2017-03-16 | 2022-12-06 | 豪夫迈·罗氏有限公司 | 新的作为atx抑制剂的二环化合物 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7169763B2 (en) * | 2002-02-22 | 2007-01-30 | Oliver Yoa-Pu Hu | Cytochrome P450 3A inhibitors and enhancers |
-
2006
- 2006-09-11 EA EA200800542A patent/EA014329B1/ru not_active IP Right Cessation
- 2006-09-11 KR KR1020087006967A patent/KR100975448B1/ko not_active IP Right Cessation
- 2006-09-11 CN CN2006800348278A patent/CN101287708B/zh not_active Expired - Fee Related
- 2006-09-11 PT PT06795544T patent/PT1937639E/pt unknown
- 2006-09-11 EP EP06795544A patent/EP1937639B1/en active Active
- 2006-09-11 CA CA2621805A patent/CA2621805C/en not_active Expired - Fee Related
- 2006-09-11 BR BRPI0616156-1A patent/BRPI0616156A2/pt not_active IP Right Cessation
- 2006-09-11 AU AU2006293605A patent/AU2006293605B2/en not_active Ceased
- 2006-09-11 AT AT06795544T patent/ATE459603T1/de active
- 2006-09-11 DK DK06795544.3T patent/DK1937639T3/da active
- 2006-09-11 SI SI200630666T patent/SI1937639T1/sl unknown
- 2006-09-11 WO PCT/IB2006/002639 patent/WO2007034312A2/en active Application Filing
- 2006-09-11 JP JP2008531812A patent/JP4336738B2/ja not_active Expired - Fee Related
- 2006-09-11 RS RSP-2010/0237A patent/RS51349B/en unknown
- 2006-09-11 NZ NZ566136A patent/NZ566136A/en not_active IP Right Cessation
- 2006-09-11 DE DE602006012713T patent/DE602006012713D1/de active Active
- 2006-09-11 PL PL06795544T patent/PL1937639T3/pl unknown
- 2006-09-11 RS RSP-2008/0118A patent/RS20080118A/sr unknown
- 2006-09-11 ES ES06795544T patent/ES2340200T3/es active Active
- 2006-09-11 GE GEAP200610575A patent/GEP20115230B/en unknown
-
2007
- 2007-01-09 US US11/621,410 patent/US7868026B2/en not_active Expired - Fee Related
-
2008
- 2008-02-21 IL IL189666A patent/IL189666A/en not_active IP Right Cessation
- 2008-03-19 EC EC2008008296A patent/ECSP088296A/es unknown
- 2008-03-19 MA MA30764A patent/MA29791B1/fr unknown
- 2008-03-19 TN TNP2008000139A patent/TNSN08139A1/fr unknown
- 2008-03-21 MY MYPI20080779A patent/MY143391A/en unknown
- 2008-04-16 NO NO20081844A patent/NO20081844L/no not_active Application Discontinuation
- 2008-12-15 HK HK08113572.1A patent/HK1120506A1/xx not_active IP Right Cessation
-
2010
- 2010-04-20 CY CY20101100359T patent/CY1110010T1/el unknown
- 2010-05-14 HR HR20100272T patent/HRP20100272T2/hr unknown
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