JP2013541589A5 - - Google Patents
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- Publication number
- JP2013541589A5 JP2013541589A5 JP2013537814A JP2013537814A JP2013541589A5 JP 2013541589 A5 JP2013541589 A5 JP 2013541589A5 JP 2013537814 A JP2013537814 A JP 2013537814A JP 2013537814 A JP2013537814 A JP 2013537814A JP 2013541589 A5 JP2013541589 A5 JP 2013541589A5
- Authority
- JP
- Japan
- Prior art keywords
- degrees
- phenyl
- amino
- crystalline compound
- trifluoroethoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims 9
- 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 claims 9
- 238000000634 powder X-ray diffraction Methods 0.000 claims 9
- 235000019260 propionic acid Nutrition 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 8
- 125000004793 2,2,2-trifluoroethoxy group Chemical group FC(CO*)(F)F 0.000 claims 7
- 238000002844 melting Methods 0.000 claims 7
- 230000008018 melting Effects 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 208000010643 digestive system disease Diseases 0.000 claims 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- KFKIHUNFVUAOFE-ATVRCVQASA-N (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid benzenesulfonic acid Chemical compound S(=O)(=O)(O)C1=CC=CC=C1.S(=O)(=O)(O)C1=CC=CC=C1.N[C@H](C(=O)O)CC1=CC=C(C=C1)C1=NC(=NC(=C1)O[C@@H](C(F)(F)F)C1=C(C=C(C=C1)Cl)N1N=C(C=C1)C)N KFKIHUNFVUAOFE-ATVRCVQASA-N 0.000 claims 1
- SMHSRHVYJDSGFN-VNJAQMQMSA-N (2s)-2-amino-3-[4-[2-amino-6-[(1r)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid;propan-2-yl hydrogen sulfate Chemical compound CC(C)OS(O)(=O)=O.N1=C(C)C=CN1C1=CC(Cl)=CC=C1[C@H](C(F)(F)F)OC1=CC(C=2C=CC(C[C@H](N)C(O)=O)=CC=2)=NC(N)=N1 SMHSRHVYJDSGFN-VNJAQMQMSA-N 0.000 claims 1
- -1 1H-pyrazol-1-yl Chemical group 0.000 claims 1
- 206010007270 Carcinoid syndrome Diseases 0.000 claims 1
- NCLGDOBQAWBXRA-PGRDOPGGSA-N Telotristat Chemical compound N1=C(C)C=CN1C1=CC(Cl)=CC=C1[C@H](C(F)(F)F)OC1=CC(C=2C=CC(C[C@H](N)C(O)=O)=CC=2)=NC(N)=N1 NCLGDOBQAWBXRA-PGRDOPGGSA-N 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41042110P | 2010-11-05 | 2010-11-05 | |
| US61/410,421 | 2010-11-05 | ||
| PCT/US2011/059107 WO2012061576A1 (en) | 2010-11-05 | 2011-11-03 | Crystalline forms of ( s ) - 2 - amino - 3 - (4 - ( 2 - amino - 6 - ( (r) - 1 - (4 - ch loro-2- (3 -methyl- 1h- pyrazol- 1 -yl) phenyl) - 2, 2, 2 - trifluoroethoxy) pyrimidin- 4 - yl) phenyl) propanoic acid |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013541589A JP2013541589A (ja) | 2013-11-14 |
| JP2013541589A5 true JP2013541589A5 (https=) | 2014-12-04 |
Family
ID=45023872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013537814A Withdrawn JP2013541589A (ja) | 2010-11-05 | 2011-11-03 | （ｓ）−２−アミノ−３−（４−（２−アミノ−６−（（ｒ）−１−（４−クロロ−２−（３−メチル−１ｈ−ピラゾール−１−イル）フェニル）−２，２，２−トリフルオロエトキシ）ピリミジン−４−イル）フェニル）プロパン酸の結晶形態 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8772483B2 (https=) |
| EP (1) | EP2635569A1 (https=) |
| JP (1) | JP2013541589A (https=) |
| KR (1) | KR20130141572A (https=) |
| CN (1) | CN103228648A (https=) |
| AR (1) | AR083755A1 (https=) |
| AU (1) | AU2011323302A1 (https=) |
| BR (1) | BR112013011015A2 (https=) |
| CA (1) | CA2816963A1 (https=) |
| MX (1) | MX2013004921A (https=) |
| RU (1) | RU2013125756A (https=) |
| SG (1) | SG189535A1 (https=) |
| TW (1) | TW201245183A (https=) |
| WO (1) | WO2012061576A1 (https=) |
| ZA (1) | ZA201303049B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011063181A1 (en) * | 2009-11-23 | 2011-05-26 | Lexicon Pharmaceuticals, Inc. | Methods and assays for the treatment of irritable bowel syndrome |
| US20120077831A1 (en) * | 2009-11-23 | 2012-03-29 | Philip Manton Brown | Methods and assays for the treatment of irritable bowel syndrome |
| UA119247C2 (uk) | 2013-09-06 | 2019-05-27 | РОЙВЕНТ САЙЕНСИЗ ҐмбГ | Спіроциклічні сполуки як інгібітори триптофангідроксилази |
| US9611201B2 (en) | 2015-03-05 | 2017-04-04 | Karos Pharmaceuticals, Inc. | Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone |
| CN109180650A (zh) * | 2018-08-28 | 2019-01-11 | 湖南华腾制药有限公司 | 一种氘代色氨酸羟化酶抑制剂的晶型 |
| JP2022507533A (ja) * | 2018-11-16 | 2022-01-18 | アルタバント・サイエンシズ・ゲーエムベーハー | 肺動脈性高血圧症および他疾患に関連する肺動脈性肺高血圧症の治療法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7897763B2 (en) | 2005-12-29 | 2011-03-01 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| US7855291B2 (en) | 2005-12-29 | 2010-12-21 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| DK1984344T3 (da) * | 2005-12-29 | 2013-01-14 | Lexicon Pharmaceuticals Inc | Multicykliske aminosyrederivater og fremgangsmåder til anvendelse heraf |
| UA99270C2 (en) | 2006-12-12 | 2012-08-10 | Лексикон Фармасьютикалз, Инк. | 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use |
| KR101582697B1 (ko) | 2007-08-24 | 2016-01-05 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 4-페닐-6-(2,2,2-트리플루오로-1-페닐에톡시)피리미딘-기재화합물의 제조 방법 |
-
2011
- 2011-10-20 TW TW100138117A patent/TW201245183A/zh unknown
- 2011-11-03 MX MX2013004921A patent/MX2013004921A/es not_active Application Discontinuation
- 2011-11-03 RU RU2013125756/04A patent/RU2013125756A/ru not_active Application Discontinuation
- 2011-11-03 JP JP2013537814A patent/JP2013541589A/ja not_active Withdrawn
- 2011-11-03 CN CN2011800534249A patent/CN103228648A/zh active Pending
- 2011-11-03 EP EP11787757.1A patent/EP2635569A1/en not_active Withdrawn
- 2011-11-03 SG SG2013032156A patent/SG189535A1/en unknown
- 2011-11-03 BR BR112013011015A patent/BR112013011015A2/pt not_active IP Right Cessation
- 2011-11-03 CA CA2816963A patent/CA2816963A1/en not_active Abandoned
- 2011-11-03 AU AU2011323302A patent/AU2011323302A1/en not_active Abandoned
- 2011-11-03 WO PCT/US2011/059107 patent/WO2012061576A1/en not_active Ceased
- 2011-11-03 US US13/288,366 patent/US8772483B2/en active Active
- 2011-11-03 KR KR1020137014387A patent/KR20130141572A/ko not_active Withdrawn
- 2011-11-04 AR ARP110104110A patent/AR083755A1/es unknown
-
2013
- 2013-04-25 ZA ZA2013/03049A patent/ZA201303049B/en unknown
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