CL2011001391A1 - Formas solidas cristalinas del acido (s)-4-((2s,3s)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-ciclohexilmetil-butirico y de la sal clorhidrato; procesos de preparacion; compuestos intermediarios; composicion farmaceutica; y uso para mejorar la movilidad del tracto gastrointestinal. - Google Patents
Formas solidas cristalinas del acido (s)-4-((2s,3s)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-ciclohexilmetil-butirico y de la sal clorhidrato; procesos de preparacion; compuestos intermediarios; composicion farmaceutica; y uso para mejorar la movilidad del tracto gastrointestinal.Info
- Publication number
- CL2011001391A1 CL2011001391A1 CL2011001391A CL2011001391A CL2011001391A1 CL 2011001391 A1 CL2011001391 A1 CL 2011001391A1 CL 2011001391 A CL2011001391 A CL 2011001391A CL 2011001391 A CL2011001391 A CL 2011001391A CL 2011001391 A1 CL2011001391 A1 CL 2011001391A1
- Authority
- CL
- Chile
- Prior art keywords
- formula
- acid
- crystalline forms
- tetrahydronaphthalen
- cyclohexylmethyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 239000002253 acid Substances 0.000 title abstract 3
- 239000007787 solid Substances 0.000 title abstract 3
- 210000001035 gastrointestinal tract Anatomy 0.000 title abstract 2
- -1 (s) -4 - ((2s, 3s) -7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino) -2-cyclohexylmethyl Chemical group 0.000 title 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 238000002360 preparation method Methods 0.000 title 1
- 238000001228 spectrum Methods 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 238000002441 X-ray diffraction Methods 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000004064 dysfunction Effects 0.000 abstract 1
- 230000000968 intestinal effect Effects 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/38—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
-
- 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
- A61P1/14—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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/22—Separation; Purification; Stabilisation; Use of additives
- C07C231/24—Separation; Purification
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
- C07C237/48—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system of the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nutrition Science (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
FORMAS CRISTALINAS I Y 11 DEL ÁCIDO (S: -4-":25, 35)- 7 -CARBAMOLL-1 .1-( -ETIL-3-METOXI-1 ,2,3.4 -TETRAHIDRONAFTALEN-2 ILAMINO)-2 CICLOHEXILMETIL BUTIRICO. DE FORMULA I. CARACTERIZADAS POR VALORES 2E DEL ESPECTRO DE DIFRACCIÓN DE RAYOS X CADA UNA, ADEMÁS DE LA FORMA SÓLIDA CRISTALINA DE LA SAL CLORTL DRATO DEL MISMO CON SUS RESPECTIVOS VALORES 2E DEL ESPECTRO DE DIFRACCIÓN DE RAYOS X. PROCESO DE SÍNTESIS DEL COMPUESTO DE FORMULA IA PARTIR DEL COMPUESTO INTERMEDIARIO DE FÓRMULA 4, EL CUAL PRESENTA UN PRECURSOR DE FÓRMULA 5. EN COMBINACIÓN CON UN COMPUESTO DE FÓRMULA 3 PARA FORMAR Y REIVINDICAR UN COMPUESTO DE FÓRMULA 2 O SU SAL CLORHIDRATO. CAMPOSICION FARMACÉUTICA QUE COMPRENDE LAS FORMAS SÓLIDAS CRISTALINAS DEL ÁCIDO ($)-4(( 28.38)-7-CA RBAMOIL- 1,1•DIETIL-3-METOXI•1.2. 3, 4-TETRAHIDROBAFTALER-ILAMI)-22•CICLOHEXILMETIL-BULIRICO. Y USO DE LA FORMA SÓLIDA CRISTALINA DEL MISMO PARA EL TRATAMIENTO DE LA DISFUNCLÓN INTESTINAL INDUCIDA POR AGENTES OPIOLDES O ILEO POSOPERATORIO. DEL TRASTORNO DE MOVILIDAD REDUCIDA DEL TRACTO INTESTINAL Y PARA ANTAGONIZAR UN RECEPTOR OPIOLDE U EN UN MAMÍFERO.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12125408P | 2008-12-10 | 2008-12-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2011001391A1 true CL2011001391A1 (es) | 2011-11-11 |
Family
ID=42122774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2011001391A CL2011001391A1 (es) | 2008-12-10 | 2011-06-08 | Formas solidas cristalinas del acido (s)-4-((2s,3s)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-ciclohexilmetil-butirico y de la sal clorhidrato; procesos de preparacion; compuestos intermediarios; composicion farmaceutica; y uso para mejorar la movilidad del tracto gastrointestinal. |
Country Status (21)
| Country | Link |
|---|---|
| US (4) | US8101794B2 (es) |
| EP (1) | EP2376427B1 (es) |
| JP (1) | JP5650657B2 (es) |
| KR (1) | KR101685187B1 (es) |
| CN (1) | CN102245564B (es) |
| AR (1) | AR074592A1 (es) |
| AU (1) | AU2009324709B2 (es) |
| BR (1) | BRPI0922920A2 (es) |
| CA (1) | CA2745441C (es) |
| CL (1) | CL2011001391A1 (es) |
| CO (1) | CO6390054A2 (es) |
| ES (1) | ES2645087T3 (es) |
| IL (1) | IL213093A0 (es) |
| MX (1) | MX2011006209A (es) |
| MY (1) | MY179041A (es) |
| NZ (1) | NZ593377A (es) |
| RU (1) | RU2512390C2 (es) |
| SG (1) | SG172016A1 (es) |
| TW (1) | TWI449685B (es) |
| WO (1) | WO2010068649A1 (es) |
| ZA (1) | ZA201104319B (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2482107C2 (ru) | 2007-12-11 | 2013-05-20 | Тереванс, Инк. | Производные 3-карбоксипропил-аминотетралина и родственные соединения в качестве антагонистов mu-опиоидного рецептора |
| WO2009076399A2 (en) | 2007-12-11 | 2009-06-18 | Theravance, Inc. | Aminotetralin compounds as mu opioid receptor antagonists |
| AU2010295464B2 (en) * | 2009-09-18 | 2015-11-26 | Merck Sharp & Dohme Corp. | Use of opioid receptor antagonist for gastrointestinal tract disorders |
| US8658691B2 (en) * | 2011-09-30 | 2014-02-25 | Theravance, Inc. | Crystalline forms of a 3-[2-methanesulfonyl-1-(4-trifluoromethyl-phenoxy)ethyl]pyrrolidine compound |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6844368B1 (en) * | 1998-12-22 | 2005-01-18 | Edward Roberts | Compounds useful in pain management |
| US6498196B1 (en) * | 1998-12-22 | 2002-12-24 | Edward Roberts | Compounds useful in pain management |
| US6231594B1 (en) | 1999-08-11 | 2001-05-15 | Radiant Medical, Inc. | Method of controlling body temperature while reducing shivering |
| WO2003097586A1 (en) * | 2002-05-17 | 2003-11-27 | Janssen Pharmaceutica N.V. | Aminotetralin-derived urea modulators of vanilloid vr1 receptor |
| RU2005134364A (ru) * | 2003-04-08 | 2006-06-10 | Проджиникс Фармасьютикалз, Инк. (Us) | Комбинированное лечение запора |
| SE0301794D0 (sv) * | 2003-06-19 | 2003-06-19 | Astrazeneca Ab | New use III |
| JP2010509227A (ja) | 2006-11-07 | 2010-03-25 | ネクター セラピューティックス エイエル,コーポレイション | オピオイド作動薬およびオピオイド拮抗薬の用量形態および同時投与 |
| EP1997493A1 (en) * | 2007-05-28 | 2008-12-03 | Laboratorios del Dr. Esteve S.A. | Combination of a 5-HT7 receptor ligand and an opioid receptor ligand |
| RU2482107C2 (ru) * | 2007-12-11 | 2013-05-20 | Тереванс, Инк. | Производные 3-карбоксипропил-аминотетралина и родственные соединения в качестве антагонистов mu-опиоидного рецептора |
| WO2009076399A2 (en) | 2007-12-11 | 2009-06-18 | Theravance, Inc. | Aminotetralin compounds as mu opioid receptor antagonists |
| US8153686B2 (en) | 2008-04-01 | 2012-04-10 | Theravance, Inc. | Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists |
-
2009
- 2009-12-09 JP JP2011540855A patent/JP5650657B2/ja not_active Expired - Fee Related
- 2009-12-09 SG SG2011041605A patent/SG172016A1/en unknown
- 2009-12-09 NZ NZ593377A patent/NZ593377A/xx not_active IP Right Cessation
- 2009-12-09 TW TW098142108A patent/TWI449685B/zh not_active IP Right Cessation
- 2009-12-09 WO PCT/US2009/067271 patent/WO2010068649A1/en not_active Ceased
- 2009-12-09 MX MX2011006209A patent/MX2011006209A/es active IP Right Grant
- 2009-12-09 KR KR1020117015637A patent/KR101685187B1/ko not_active Expired - Fee Related
- 2009-12-09 AU AU2009324709A patent/AU2009324709B2/en not_active Ceased
- 2009-12-09 BR BRPI0922920A patent/BRPI0922920A2/pt not_active IP Right Cessation
- 2009-12-09 MY MYPI2011002349A patent/MY179041A/en unknown
- 2009-12-09 EP EP09793383.2A patent/EP2376427B1/en not_active Not-in-force
- 2009-12-09 US US12/633,944 patent/US8101794B2/en not_active Expired - Fee Related
- 2009-12-09 RU RU2011128393/04A patent/RU2512390C2/ru active
- 2009-12-09 CA CA2745441A patent/CA2745441C/en active Active
- 2009-12-09 ES ES09793383.2T patent/ES2645087T3/es active Active
- 2009-12-09 CN CN200980149818.7A patent/CN102245564B/zh not_active Expired - Fee Related
- 2009-12-10 AR ARP090104803A patent/AR074592A1/es unknown
-
2011
- 2011-05-24 IL IL213093A patent/IL213093A0/en active IP Right Grant
- 2011-06-08 CO CO11070977A patent/CO6390054A2/es active IP Right Grant
- 2011-06-08 CL CL2011001391A patent/CL2011001391A1/es unknown
- 2011-06-09 ZA ZA2011/04319A patent/ZA201104319B/en unknown
- 2011-12-19 US US13/330,358 patent/US8324236B2/en not_active Expired - Fee Related
-
2012
- 2012-10-29 US US13/663,083 patent/US8486958B2/en not_active Expired - Fee Related
-
2013
- 2013-06-17 US US13/919,260 patent/US8969367B2/en not_active Expired - Fee Related
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