RU2013125756A - Твердые формы (s)-2-амино-3-(4-(2-амино-6-((r)-1-(4-хлор-2-(3-метил-1н-пиразол-1-ил)фенил)-2,2,2-трифторэтокси)пиримидин-4-ил)фенил)пропановой кислоты - Google Patents
Твердые формы (s)-2-амино-3-(4-(2-амино-6-((r)-1-(4-хлор-2-(3-метил-1н-пиразол-1-ил)фенил)-2,2,2-трифторэтокси)пиримидин-4-ил)фенил)пропановой кислоты Download PDFInfo
- Publication number
- RU2013125756A RU2013125756A RU2013125756/04A RU2013125756A RU2013125756A RU 2013125756 A RU2013125756 A RU 2013125756A RU 2013125756/04 A RU2013125756/04 A RU 2013125756/04A RU 2013125756 A RU2013125756 A RU 2013125756A RU 2013125756 A RU2013125756 A RU 2013125756A
- Authority
- RU
- Russia
- Prior art keywords
- phenyl
- amino
- crystalline compound
- compound according
- pyrimidin
- Prior art date
Links
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title claims 11
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical compound CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 title claims 6
- 239000007787 solid Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 35
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims abstract 12
- 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 abstract 10
- 238000002844 melting Methods 0.000 claims abstract 10
- 230000008018 melting Effects 0.000 claims abstract 10
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- 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 5
- 235000019260 propionic acid Nutrition 0.000 claims 5
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 5
- 238000002441 X-ray diffraction Methods 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000000843 powder Substances 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- 125000004353 pyrazol-1-yl group Chemical group [H]C1=NN(*)C([H])=C1[H] 0.000 claims 3
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 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
- 206010007270 Carcinoid syndrome Diseases 0.000 claims 1
- 229940092714 benzenesulfonic acid Drugs 0.000 claims 1
- 229950004221 besilate Drugs 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 229950008913 edisilate Drugs 0.000 claims 1
- 229950007655 esilate Drugs 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
Classifications
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Nutrition Science (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| RU2013125756A true RU2013125756A (ru) | 2014-12-10 |
Family
ID=45023872
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013125756/04A RU2013125756A (ru) | 2010-11-05 | 2011-11-03 | Твердые формы (s)-2-амино-3-(4-(2-амино-6-((r)-1-(4-хлор-2-(3-метил-1н-пиразол-1-ил)фенил)-2,2,2-трифторэтокси)пиримидин-4-ил)фенил)пропановой кислоты |
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
Also Published As
| Publication number | Publication date |
|---|---|
| EP2635569A1 (en) | 2013-09-11 |
| US8772483B2 (en) | 2014-07-08 |
| JP2013541589A (ja) | 2013-11-14 |
| ZA201303049B (en) | 2014-07-30 |
| US20120122904A1 (en) | 2012-05-17 |
| WO2012061576A1 (en) | 2012-05-10 |
| AR083755A1 (es) | 2013-03-20 |
| BR112013011015A2 (pt) | 2016-08-23 |
| KR20130141572A (ko) | 2013-12-26 |
| TW201245183A (en) | 2012-11-16 |
| MX2013004921A (es) | 2013-06-28 |
| SG189535A1 (en) | 2013-06-28 |
| CA2816963A1 (en) | 2012-05-10 |
| AU2011323302A1 (en) | 2013-05-30 |
| CN103228648A (zh) | 2013-07-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20160314 |