CO6270323A2 - Formas solidas de acido (s)-2-amino-3-(4-(2-amino-6-((r)-2,2,2-trifluoro- 1-(3'-metoxibifenil-4-il)etoxi)pirimidin-4-il)fenil)propanoico y metodos para su uso - Google Patents
Formas solidas de acido (s)-2-amino-3-(4-(2-amino-6-((r)-2,2,2-trifluoro- 1-(3'-metoxibifenil-4-il)etoxi)pirimidin-4-il)fenil)propanoico y metodos para su usoInfo
- Publication number
- CO6270323A2 CO6270323A2 CO10054926A CO10054926A CO6270323A2 CO 6270323 A2 CO6270323 A2 CO 6270323A2 CO 10054926 A CO10054926 A CO 10054926A CO 10054926 A CO10054926 A CO 10054926A CO 6270323 A2 CO6270323 A2 CO 6270323A2
- Authority
- CO
- Colombia
- Prior art keywords
- amino
- trifluoro
- phenyl
- crystalline compound
- acid
- Prior art date
Links
- 239000002253 acid Substances 0.000 title abstract 2
- 239000007787 solid Substances 0.000 title abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 8
- -1 3'-methoxybiphenyl-4-yl Chemical group 0.000 abstract 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- XNMUICFMGGQSMZ-WIOPSUGQSA-N (2s)-2-amino-3-[4-[2-amino-6-[(1r)-2,2,2-trifluoro-1-[4-(3-methoxyphenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid Chemical compound COC1=CC=CC(C=2C=CC(=CC=2)[C@@H](OC=2N=C(N)N=C(C=2)C=2C=CC(C[C@H](N)C(O)=O)=CC=2)C(F)(F)F)=C1 XNMUICFMGGQSMZ-WIOPSUGQSA-N 0.000 abstract 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 abstract 1
- 230000008018 melting Effects 0.000 abstract 1
- 238000002844 melting Methods 0.000 abstract 1
- 150000004682 monohydrates Chemical class 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
- 235000019260 propionic acid Nutrition 0.000 abstract 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/34—Phthalazines with nitrogen atoms directly attached to carbon atoms of the nitrogen-containing ring, e.g. hydrazine radicals
-
- 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
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Se describen formas solidas de acido (S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-metoxibifenil-4-il)etoxi)pirimidin-4-iI)fenil)propanoico y sales del mismo.1.- Un compuesto cristalino, que es acido (S)2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-metoxibifenil-4-il) etoxi)pirimidin-4-il)fenil)propanoico o una sal del mismo.2.- Un compuesto cristalino, que es tosilato de (S)-2- amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3'-metoxibifenil-4-il)etoxi)pirimidin-4-il)fenil)propanoato.3.- El compuesto cristalino de la reivindicacion 2, que es anhidro.4.- El compuesto cristalino de la reivindicacion 3, que tiene un punto de fusion de aproximadamente 241°C.5.- El compuesto cristalino de la reivindicacion 3, que tiene un patron de difraccion de polvo de rayos x que comprende un pico en uno o mas de aproximadamente 3.5, 7.0, 8.6, 10.9, 13.5, 14.0, 15.1, 17.3 y/o 20.5 2? grados.6.- El compuesto de la reivindicacion 3, que tiene un patron de difraccion de polvo de rayos x sustancialmente el mismo como el que se muestra en la Figura 1.7.- El compuesto cristalino de la reivindicacion 2, que es un hidrato.8.- El compuesto cristalino de la reivindicacion 7, que es un monohidrato.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97830307P | 2007-10-08 | 2007-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6270323A2 true CO6270323A2 (es) | 2011-04-20 |
Family
ID=40344344
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO10054926A CO6270323A2 (es) | 2007-10-08 | 2010-05-07 | Formas solidas de acido (s)-2-amino-3-(4-(2-amino-6-((r)-2,2,2-trifluoro- 1-(3'-metoxibifenil-4-il)etoxi)pirimidin-4-il)fenil)propanoico y metodos para su uso |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20090099206A1 (es) |
| EP (1) | EP2231618A1 (es) |
| JP (1) | JP2010540665A (es) |
| KR (1) | KR20100066548A (es) |
| CN (1) | CN101932563A (es) |
| AR (1) | AR068837A1 (es) |
| AU (1) | AU2008310979A1 (es) |
| BR (1) | BRPI0818350A2 (es) |
| CA (1) | CA2701904A1 (es) |
| CL (1) | CL2008002980A1 (es) |
| CO (1) | CO6270323A2 (es) |
| EA (1) | EA201070455A1 (es) |
| EC (1) | ECSP10010162A (es) |
| IL (1) | IL204582A0 (es) |
| MX (1) | MX2010003803A (es) |
| PE (1) | PE20091213A1 (es) |
| TW (1) | TW200932729A (es) |
| UY (1) | UY31381A1 (es) |
| WO (1) | WO2009048864A1 (es) |
| ZA (1) | ZA201001870B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0620756B1 (pt) | 2005-12-29 | 2021-06-01 | Tersera Therapeutics Llc | Derivados de aminoácido multicíclicos, formulação farmacêutica compreendendo os mesmos e seus usos para inibir a atividade de triptofano hidroxilase 1 (tph1) |
| US7855291B2 (en) * | 2005-12-29 | 2010-12-21 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| US7897763B2 (en) | 2005-12-29 | 2011-03-01 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| MX2009013982A (es) * | 2007-06-26 | 2010-04-09 | Lexicon Pharmaceuticals Inc | Composiciones que comprenden inhibidores de triptofano hidroxilasa. |
| TWI439457B (zh) | 2007-09-28 | 2014-06-01 | Lexicon Pharmaceuticals Inc | （ｓ）－２－胺基－３－（４－（２－胺基－６－（（ｒ）－１－（４－氯－２－（３－甲基－１ｈ－吡唑－１－基）苯基）－２，２，２－三氟乙氧）－嘧啶－４－基）苯基）丙酸乙酯之固體形式與其使用方法 |
| US8759364B2 (en) * | 2008-03-31 | 2014-06-24 | The Trustees Of Columbia University In The City Of New York | Methods of treating bone mass diseases |
| CN102711757A (zh) * | 2009-11-23 | 2012-10-03 | 莱西肯医药有限公司 | 用于治疗肠易激综合征的方法和分析法 |
| US20130303763A1 (en) * | 2012-03-30 | 2013-11-14 | Michael D. Gershon | Methods and compositions for the treatment of necrotizing enterocolitis |
| CA3119912A1 (en) * | 2018-11-14 | 2020-05-22 | Altavant Sciences Gmbh | A crystalline spirocyclic compound inhibitor of tryptophan hydroxylase 1 (tph1) for treating diseases or disorders associated with peripheral serotonin |
| TW202210462A (zh) * | 2020-05-28 | 2022-03-16 | 中國大陸商杭州中美華東製藥有限公司 | （ｓ）－２－胺基－３－（４－（２，３－二甲基吡啶－４－基）苯基丙酸甲酯及其鹽的製備方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7382793B1 (en) * | 2002-01-17 | 2008-06-03 | Juniper Networks, Inc. | Systems and methods for determining the bandwidth used by a queue |
| BRPI0620756B1 (pt) * | 2005-12-29 | 2021-06-01 | Tersera Therapeutics Llc | Derivados de aminoácido multicíclicos, formulação farmacêutica compreendendo os mesmos e seus usos para inibir a atividade de triptofano hidroxilase 1 (tph1) |
| US7855291B2 (en) * | 2005-12-29 | 2010-12-21 | Lexicon Pharmaceuticals, Inc. | Process for the preparation of substituted phenylalanines |
| 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 |
| CN101784269A (zh) * | 2007-06-26 | 2010-07-21 | 莱西肯医药有限公司 | 治疗由5-羟色胺介导的疾病和病症的方法 |
| MX2009013982A (es) * | 2007-06-26 | 2010-04-09 | Lexicon Pharmaceuticals Inc | Composiciones que comprenden inhibidores de triptofano hidroxilasa. |
| CA2693400A1 (en) * | 2007-07-11 | 2009-01-15 | Lexicon Pharmaceuticals, Inc. | Methods and compositions for treating pulmonary hypertension and related diseases and disorders |
| AU2008279426A1 (en) * | 2007-07-26 | 2009-01-29 | Lexicon Pharmaceuticals, Inc. | Methods of affecting gastrointestinal transit and gastric emptying, and compounds useful therein |
-
2008
- 2008-10-02 TW TW097137954A patent/TW200932729A/zh unknown
- 2008-10-07 EP EP08837474A patent/EP2231618A1/en not_active Withdrawn
- 2008-10-07 JP JP2010528220A patent/JP2010540665A/ja not_active Withdrawn
- 2008-10-07 EA EA201070455A patent/EA201070455A1/ru unknown
- 2008-10-07 MX MX2010003803A patent/MX2010003803A/es not_active Application Discontinuation
- 2008-10-07 AU AU2008310979A patent/AU2008310979A1/en not_active Abandoned
- 2008-10-07 PE PE2008001736A patent/PE20091213A1/es not_active Application Discontinuation
- 2008-10-07 CL CL2008002980A patent/CL2008002980A1/es unknown
- 2008-10-07 BR BRPI0818350A patent/BRPI0818350A2/pt not_active IP Right Cessation
- 2008-10-07 CN CN200880110755XA patent/CN101932563A/zh active Pending
- 2008-10-07 WO PCT/US2008/079042 patent/WO2009048864A1/en active Application Filing
- 2008-10-07 CA CA2701904A patent/CA2701904A1/en not_active Abandoned
- 2008-10-07 US US12/246,735 patent/US20090099206A1/en not_active Abandoned
- 2008-10-07 UY UY31381A patent/UY31381A1/es not_active Application Discontinuation
- 2008-10-07 KR KR1020107007548A patent/KR20100066548A/ko not_active Application Discontinuation
- 2008-10-08 AR ARP080104405A patent/AR068837A1/es unknown
-
2010
- 2010-03-16 ZA ZA2010/01870A patent/ZA201001870B/en unknown
- 2010-03-18 IL IL204582A patent/IL204582A0/en unknown
- 2010-05-06 EC EC2010010162A patent/ECSP10010162A/es unknown
- 2010-05-07 CO CO10054926A patent/CO6270323A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PE20091213A1 (es) | 2009-08-26 |
| BRPI0818350A2 (pt) | 2017-10-10 |
| TW200932729A (en) | 2009-08-01 |
| EA201070455A1 (ru) | 2010-08-30 |
| EP2231618A1 (en) | 2010-09-29 |
| CL2008002980A1 (es) | 2009-03-20 |
| IL204582A0 (en) | 2010-11-30 |
| MX2010003803A (es) | 2010-04-21 |
| KR20100066548A (ko) | 2010-06-17 |
| WO2009048864A1 (en) | 2009-04-16 |
| ECSP10010162A (es) | 2010-06-29 |
| ZA201001870B (en) | 2011-06-29 |
| UY31381A1 (es) | 2009-04-30 |
| US20090099206A1 (en) | 2009-04-16 |
| JP2010540665A (ja) | 2010-12-24 |
| CN101932563A (zh) | 2010-12-29 |
| AR068837A1 (es) | 2009-12-09 |
| CA2701904A1 (en) | 2009-04-16 |
| AU2008310979A1 (en) | 2009-04-16 |
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