PE20181038A1 - Inhibidor de la isocitrato deshidrogenasa mutada idh1 r132h - Google Patents
Inhibidor de la isocitrato deshidrogenasa mutada idh1 r132hInfo
- Publication number
- PE20181038A1 PE20181038A1 PE2018000133A PE2018000133A PE20181038A1 PE 20181038 A1 PE20181038 A1 PE 20181038A1 PE 2018000133 A PE2018000133 A PE 2018000133A PE 2018000133 A PE2018000133 A PE 2018000133A PE 20181038 A1 PE20181038 A1 PE 20181038A1
- Authority
- PE
- Peru
- Prior art keywords
- inhibitor
- isocitrate dehydrogenase
- acid
- idh1
- mutated isocitrate
- Prior art date
Links
- 108010075869 Isocitrate Dehydrogenase Proteins 0.000 title 1
- 102000012011 Isocitrate Dehydrogenase Human genes 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102200069690 rs121913500 Human genes 0.000 title 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 3
- 235000011087 fumaric acid Nutrition 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 abstract 1
- 239000001530 fumaric acid Substances 0.000 abstract 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 235000019260 propionic acid Nutrition 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se refiere a un aducto formado por el acido (2E)-but-2-enedioico y un acido 3-(2-{[4-4-trifluorometoxi)fenil]amino}-1-[(1R,5R)-3,3,5-trimetilciclohexil]-1H-benzimidazol-5-il)propanoico que comprende una molecula de acido fumarico a cuatro moleculas de acido 3-(2-{[4-4-trifluorometoxi)fenil]amino}-1-[(1R,5R)-3,3,5-trimetilciclohexil]-1H-benzimidazol-5-il)propanoico. Dicho aducto en su forma cristalina posee picos maximos en un difractograma de rayos X (2 theta) tales como 5,4; 6,8; 10,2; 10,3; 10,8; 11,1; 16,8 y 21,6. La presente invencion es util para el tratamiento y profilaxis de tumores
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15178419 | 2015-07-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181038A1 true PE20181038A1 (es) | 2018-07-03 |
Family
ID=53758092
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018000133A PE20181038A1 (es) | 2015-07-27 | 2016-07-22 | Inhibidor de la isocitrato deshidrogenasa mutada idh1 r132h |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US10344004B2 (es) |
| EP (1) | EP3328837B1 (es) |
| JP (1) | JP6804516B2 (es) |
| KR (1) | KR20180030789A (es) |
| CN (1) | CN107810181B (es) |
| AR (1) | AR105493A1 (es) |
| AU (1) | AU2016300980B2 (es) |
| BR (1) | BR112018001534A2 (es) |
| CA (1) | CA2993473A1 (es) |
| CL (1) | CL2018000249A1 (es) |
| CO (1) | CO2018000793A2 (es) |
| CR (1) | CR20180053A (es) |
| CU (1) | CU20180014A7 (es) |
| DO (1) | DOP2018000027A (es) |
| EA (1) | EA201890386A1 (es) |
| EC (1) | ECSP18006465A (es) |
| ES (1) | ES2860693T3 (es) |
| HK (1) | HK1252449A1 (es) |
| IL (1) | IL256024A (es) |
| MX (1) | MX2018001205A (es) |
| NI (1) | NI201800014A (es) |
| PE (1) | PE20181038A1 (es) |
| SV (1) | SV2018005621A (es) |
| TN (1) | TN2018000038A1 (es) |
| TW (1) | TW201708193A (es) |
| WO (1) | WO2017016992A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3105210B1 (en) | 2014-02-11 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| KR20160115991A (ko) | 2014-02-11 | 2016-10-06 | 바이엘 파마 악티엔게젤샤프트 | Midh1 억제제로서의 벤즈이미다졸-2-아민 |
| US10137110B2 (en) | 2014-10-23 | 2018-11-27 | Bayer Pharma Aktiengesellschaft | 1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors |
| US10370339B2 (en) | 2015-06-08 | 2019-08-06 | Bayer Pharma Aktiengesellschaft | N-Methylbenzimidazoles as mIDH1 inhibitors |
| CA2991360A1 (en) | 2015-07-07 | 2017-01-12 | Bayer Pharma Aktiengesellschaft | 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors |
| EP3322694B1 (en) | 2015-07-16 | 2020-02-19 | Bayer Pharma Aktiengesellschaft | 5-hydroxyalkylbenzimidazoles as midh1 inhibitors |
| EP3121166A1 (en) | 2015-07-21 | 2017-01-25 | Bayer Pharma Aktiengesellschaft | Fused imidazoles as midh1 inhibitors |
| TW201718513A (zh) | 2015-07-27 | 2017-06-01 | 拜耳製藥公司 | 製備經取代之３－（２－苯胺－１－環己基－１ｈ－苯并咪唑－５－基）丙酸衍生物之方法 |
| WO2019015672A1 (zh) * | 2017-07-21 | 2019-01-24 | 南京明德新药研发股份有限公司 | 吡啶并咪唑类化合物及其应用 |
| EP3661559A1 (en) | 2017-08-01 | 2020-06-10 | Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts | Combination of midh1 inhibitors and dna hypomethylating agents (hma) |
| CN108948205B (zh) * | 2018-07-13 | 2021-09-28 | 北京金岱生物科技有限公司 | 抗idh1r132h单克隆抗体及其应用 |
| TWI760017B (zh) | 2019-12-23 | 2022-04-01 | 大陸商昆藥集團股份有限公司 | 一種ｉｄｈ１突變體抑制劑的鹽型、晶型及其製備方法 |
| CN116348145A (zh) | 2020-07-21 | 2023-06-27 | 第一三共株式会社 | 替莫唑胺和突变型idh1酶抑制剂的组合药物 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2766550C (en) * | 2009-06-23 | 2017-04-11 | The Translational Genomics Research Intstitute | Benzamide derivatives |
| US9012464B2 (en) * | 2010-11-25 | 2015-04-21 | Ratiopharm Gmbh | Salts and polymorphic forms of Afatinib |
| CN103958506B (zh) | 2011-09-27 | 2017-02-22 | 诺华股份有限公司 | 用作突变idh抑制剂的3‑嘧啶‑4‑基‑噁唑烷‑2‑酮化合物 |
| KR20160115991A (ko) | 2014-02-11 | 2016-10-06 | 바이엘 파마 악티엔게젤샤프트 | Midh1 억제제로서의 벤즈이미다졸-2-아민 |
| EP3105210B1 (en) | 2014-02-11 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| US10137110B2 (en) * | 2014-10-23 | 2018-11-27 | Bayer Pharma Aktiengesellschaft | 1-cyclohexyl-2-phenylaminobenzimidazoles as mIDH1 inhibitors for the treatment of tumors |
| WO2016062677A1 (en) | 2014-10-23 | 2016-04-28 | Bayer Pharma Aktiengesellschaft | Benzimidazol-2-amines as midh1 inhibitors |
| US10370339B2 (en) * | 2015-06-08 | 2019-08-06 | Bayer Pharma Aktiengesellschaft | N-Methylbenzimidazoles as mIDH1 inhibitors |
| CA2991360A1 (en) | 2015-07-07 | 2017-01-12 | Bayer Pharma Aktiengesellschaft | 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors |
| EP3322694B1 (en) | 2015-07-16 | 2020-02-19 | Bayer Pharma Aktiengesellschaft | 5-hydroxyalkylbenzimidazoles as midh1 inhibitors |
| EP3121166A1 (en) * | 2015-07-21 | 2017-01-25 | Bayer Pharma Aktiengesellschaft | Fused imidazoles as midh1 inhibitors |
| TW201718513A (zh) | 2015-07-27 | 2017-06-01 | 拜耳製藥公司 | 製備經取代之３－（２－苯胺－１－環己基－１ｈ－苯并咪唑－５－基）丙酸衍生物之方法 |
-
2016
- 2016-07-14 TW TW105122262A patent/TW201708193A/zh unknown
- 2016-07-22 PE PE2018000133A patent/PE20181038A1/es unknown
- 2016-07-22 EA EA201890386A patent/EA201890386A1/ru unknown
- 2016-07-22 ES ES16741332T patent/ES2860693T3/es active Active
- 2016-07-22 US US15/748,014 patent/US10344004B2/en not_active Expired - Fee Related
- 2016-07-22 KR KR1020177036977A patent/KR20180030789A/ko not_active Withdrawn
- 2016-07-22 CA CA2993473A patent/CA2993473A1/en not_active Abandoned
- 2016-07-22 TN TNP/2018/000038A patent/TN2018000038A1/en unknown
- 2016-07-22 EP EP16741332.7A patent/EP3328837B1/en active Active
- 2016-07-22 CR CR20180053A patent/CR20180053A/es unknown
- 2016-07-22 AU AU2016300980A patent/AU2016300980B2/en not_active Ceased
- 2016-07-22 BR BR112018001534A patent/BR112018001534A2/pt not_active Application Discontinuation
- 2016-07-22 MX MX2018001205A patent/MX2018001205A/es unknown
- 2016-07-22 JP JP2018504187A patent/JP6804516B2/ja not_active Expired - Fee Related
- 2016-07-22 HK HK18111750.7A patent/HK1252449A1/zh unknown
- 2016-07-22 CN CN201680038633.9A patent/CN107810181B/zh not_active Expired - Fee Related
- 2016-07-22 CU CUP2018000014A patent/CU20180014A7/es unknown
- 2016-07-22 WO PCT/EP2016/067477 patent/WO2017016992A1/en not_active Ceased
- 2016-07-27 AR ARP160102274A patent/AR105493A1/es unknown
-
2017
- 2017-11-30 IL IL256024A patent/IL256024A/en unknown
-
2018
- 2018-01-26 DO DO2018000027A patent/DOP2018000027A/es unknown
- 2018-01-26 EC ECIEPI20186465A patent/ECSP18006465A/es unknown
- 2018-01-26 SV SV2018005621A patent/SV2018005621A/es unknown
- 2018-01-26 NI NI201800014A patent/NI201800014A/es unknown
- 2018-01-26 CL CL2018000249A patent/CL2018000249A1/es unknown
- 2018-01-26 CO CONC2018/0000793A patent/CO2018000793A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP6804516B2 (ja) | 2020-12-23 |
| US20180222870A1 (en) | 2018-08-09 |
| EP3328837A1 (en) | 2018-06-06 |
| US10344004B2 (en) | 2019-07-09 |
| CN107810181A (zh) | 2018-03-16 |
| TW201708193A (zh) | 2017-03-01 |
| KR20180030789A (ko) | 2018-03-26 |
| WO2017016992A1 (en) | 2017-02-02 |
| NI201800014A (es) | 2018-09-06 |
| EA201890386A1 (ru) | 2018-08-31 |
| CL2018000249A1 (es) | 2018-07-06 |
| IL256024A (en) | 2018-01-31 |
| AR105493A1 (es) | 2017-10-11 |
| BR112018001534A2 (pt) | 2018-09-11 |
| AU2016300980A1 (en) | 2017-12-21 |
| TN2018000038A1 (en) | 2019-07-08 |
| SV2018005621A (es) | 2018-12-05 |
| MX2018001205A (es) | 2018-04-24 |
| CN107810181B (zh) | 2021-06-22 |
| CR20180053A (es) | 2018-03-20 |
| HK1252449A1 (zh) | 2019-05-24 |
| CO2018000793A2 (es) | 2018-05-10 |
| DOP2018000027A (es) | 2018-02-28 |
| EP3328837B1 (en) | 2021-01-06 |
| ES2860693T3 (es) | 2021-10-05 |
| CU20180014A7 (es) | 2018-06-05 |
| AU2016300980B2 (en) | 2020-12-24 |
| JP2018521095A (ja) | 2018-08-02 |
| CA2993473A1 (en) | 2017-02-02 |
| ECSP18006465A (es) | 2018-04-30 |
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