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)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Psychiatry (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 (enExample) |
| EP (1) | EP2635569A1 (enExample) |
| JP (1) | JP2013541589A (enExample) |
| KR (1) | KR20130141572A (enExample) |
| CN (1) | CN103228648A (enExample) |
| AR (1) | AR083755A1 (enExample) |
| AU (1) | AU2011323302A1 (enExample) |
| BR (1) | BR112013011015A2 (enExample) |
| CA (1) | CA2816963A1 (enExample) |
| MX (1) | MX2013004921A (enExample) |
| RU (1) | RU2013125756A (enExample) |
| SG (1) | SG189535A1 (enExample) |
| TW (1) | TW201245183A (enExample) |
| WO (1) | WO2012061576A1 (enExample) |
| ZA (1) | ZA201303049B (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120077831A1 (en) * | 2009-11-23 | 2012-03-29 | Philip Manton Brown | Methods and assays for the treatment of irritable bowel syndrome |
| WO2011063181A1 (en) * | 2009-11-23 | 2011-05-26 | Lexicon Pharmaceuticals, Inc. | 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 |
| AU2019382168A1 (en) * | 2018-11-16 | 2021-06-03 | Altavant Sciences Gmbh | A method for treating pulmonary arterial hypertension and associated pulmonary arterial hypertension |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7855291B2 (en) | 2005-12-29 | 2010-12-21 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| AU2006337137B2 (en) * | 2005-12-29 | 2012-06-14 | Tersera Therapeutics Llc | Multicyclic amino acid derivatives and methods of their use |
| US7897763B2 (en) | 2005-12-29 | 2011-03-01 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| 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 |
| ES2848152T3 (es) | 2007-08-24 | 2021-08-05 | Tersera Therapeutics Llc | Métodos de preparación de compuestos a base de 4-fenil-6-(2,2,2-trifluoro-1-feniletoxi)pirimidina |
-
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 KR KR1020137014387A patent/KR20130141572A/ko not_active Withdrawn
- 2011-11-03 EP EP11787757.1A patent/EP2635569A1/en not_active Withdrawn
- 2011-11-03 SG SG2013032156A patent/SG189535A1/en unknown
- 2011-11-03 CN CN2011800534249A patent/CN103228648A/zh active Pending
- 2011-11-03 US US13/288,366 patent/US8772483B2/en active Active
- 2011-11-03 RU RU2013125756/04A patent/RU2013125756A/ru not_active Application Discontinuation
- 2011-11-03 WO PCT/US2011/059107 patent/WO2012061576A1/en not_active Ceased
- 2011-11-03 CA CA2816963A patent/CA2816963A1/en not_active Abandoned
- 2011-11-03 JP JP2013537814A patent/JP2013541589A/ja not_active Withdrawn
- 2011-11-03 BR BR112013011015A patent/BR112013011015A2/pt not_active IP Right Cessation
- 2011-11-03 AU AU2011323302A patent/AU2011323302A1/en not_active Abandoned
- 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 |
|---|---|
| SG189535A1 (en) | 2013-06-28 |
| AR083755A1 (es) | 2013-03-20 |
| KR20130141572A (ko) | 2013-12-26 |
| AU2011323302A1 (en) | 2013-05-30 |
| JP2013541589A (ja) | 2013-11-14 |
| US8772483B2 (en) | 2014-07-08 |
| US20120122904A1 (en) | 2012-05-17 |
| EP2635569A1 (en) | 2013-09-11 |
| MX2013004921A (es) | 2013-06-28 |
| CA2816963A1 (en) | 2012-05-10 |
| ZA201303049B (en) | 2014-07-30 |
| TW201245183A (en) | 2012-11-16 |
| CN103228648A (zh) | 2013-07-31 |
| WO2012061576A1 (en) | 2012-05-10 |
| BR112013011015A2 (pt) | 2016-08-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20160314 |