AR074592A1 - Formas cristalinas de un compuesto 3-carboxipropil-aminotetralina, procesos e intermediario para su sintesis y su uso en el tratamiento de una enfermedad mediada por un antagonista de los receptores mu opioides. - Google Patents
Formas cristalinas de un compuesto 3-carboxipropil-aminotetralina, procesos e intermediario para su sintesis y su uso en el tratamiento de una enfermedad mediada por un antagonista de los receptores mu opioides.Info
- Publication number
- AR074592A1 AR074592A1 ARP090104803A ARP090104803A AR074592A1 AR 074592 A1 AR074592 A1 AR 074592A1 AR P090104803 A ARP090104803 A AR P090104803A AR P090104803 A ARP090104803 A AR P090104803A AR 074592 A1 AR074592 A1 AR 074592A1
- Authority
- AR
- Argentina
- Prior art keywords
- solid form
- crystalline
- crystalline solid
- tetrahydronaphthalen
- cyclohexylmethyl
- Prior art date
Links
Classifications
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- 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
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- 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
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- 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
- 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)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (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 sólidas cristalinas de ácido (S)-4-((2S,3S)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-(cicIohexilmetil)butírico. Uso de dichas formas sólidas cristalinas para tratar enfermedades asociadas con la actividad de los receptores mu de opioides, y procesos útiles para preparar dichas formas cristalinas sólidas. Reivindicación 2: La forma sólida cristalina de la reivindicación 1, caracterizada porque la forma sólida cristalina es del ácido (S)-4-((2S,3S)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-(ciclohexilmetil)butírico cristalino. Reivindicación 3: La forma sólida cristalina de la reivindicación 2, caracterizada porque la forma sólida cristalina se caracteriza por un patrón de difracción de rayos X en polvo con picos de difracción, en valores 2theta de 6,92ñ0,20 y 15,34ñ0,20, y con dos o más picos de difracción, en valores 2theta que se seleccionan entre 10,24ñ0,20, 11,48ñ0,20, 12,32ñ0,20, 13,46ñ0,20, 14,04ñ0,20, 17,30ñ0,20, 18,06ñ0,20, 20,30ñ0,20, 21,42ñ0,20, 23,48ñ0,20, 25,54ñ0,20, 26,96ñ0,20, 29,30ñ0,20, y 30,72ñ0,20. Reivindicación 10: La forma sólida cristalina de la reivindicación 1, caracterizada porque la forma sólida cristalina es la sal cristalina clorhidrato del ácido (S)-4-((2S,3S)-7-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-(ciclohexilmetil)butírico. Reivindicación 11: La forma sólida cristalina de la reivindicación 10, caracterizada porque la forma sólida cristalina se caracteriza por un patrón de difracción de rayos X en polvo con dos o más picos de difracción, en valores 2theta que se seleccionan entre 6,80ñ0,20, 9,80ñ020, 12,71ñ0,20, 13,31ñ0,20, 15,14ñ0,20, 19,97ñ0,20, 21,44ñ0,20, 22,64ñ0,20, 23,27ñ0,20, 24,44ñ0,20, y 25,37ñ0,20. Reivindicación 17: Un compuesto caracterizado porque tiene la fórmula 2 denotado por el nombre químico éster bencílico del ácido (S)-4-((2S,3S)-carbamoil-1,1-dietil-3-metoxi-1,2,3,4-tetrahidronaftalen-2-ilamino)-2-ciclohexilmetil-butírico o una sal clorhidrato del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12125408P | 2008-12-10 | 2008-12-10 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR074592A1 true AR074592A1 (es) | 2011-01-26 |
Family
ID=42122774
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090104803A AR074592A1 (es) | 2008-12-10 | 2009-12-10 | Formas cristalinas de un compuesto 3-carboxipropil-aminotetralina, procesos e intermediario para su sintesis y su uso en el tratamiento de una enfermedad mediada por un antagonista de los receptores mu opioides. |
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 |
---|---|---|---|---|
EP2231589B1 (en) | 2007-12-11 | 2013-02-13 | Theravance, Inc. | Aminotetralin compounds as mu opioid receptor antagonists |
JP5403762B2 (ja) | 2007-12-11 | 2014-01-29 | セラヴァンス, インコーポレーテッド | μオピオイド受容体アンタゴニストとしての3−カルボキシプロピル−アミノテトラリン誘導体 |
CA2774021A1 (en) * | 2009-09-18 | 2011-03-24 | Adolor Corporation | Use of opioid receptor antagonist for gastrointestinal tract disorders |
EP2760826A1 (en) * | 2011-09-30 | 2014-08-06 | 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 |
EP1506166B1 (en) * | 2002-05-17 | 2011-11-16 | Janssen Pharmaceutica NV | Aminotetralin-derived urea modulators of vanilloid vr1 receptor |
CA2521420A1 (en) * | 2003-04-08 | 2004-10-28 | Progenics Pharmaceuticals, Inc. | Combination therapy for constipation comprising a laxative and a peripheral opioid antagonist |
SE0301794D0 (sv) * | 2003-06-19 | 2003-06-19 | Astrazeneca Ab | New use III |
MX2009004965A (es) | 2006-11-07 | 2009-06-05 | Nektar Therapeutics Al Corp | Formas de dosificacion y co-administracion de un agonista de opioides y un antagonista de opioides. |
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 |
EP2231589B1 (en) | 2007-12-11 | 2013-02-13 | Theravance, Inc. | Aminotetralin compounds as mu opioid receptor antagonists |
JP5403762B2 (ja) | 2007-12-11 | 2014-01-29 | セラヴァンス, インコーポレーテッド | μオピオイド受容体アンタゴニストとしての3−カルボキシプロピル−アミノテトラリン誘導体 |
EP2280933B1 (en) | 2008-04-01 | 2013-07-24 | Theravance, Inc. | 2 -aminotetralin derivatives as mu opioid receptor antagonists |
-
2009
- 2009-12-09 SG SG2011041605A patent/SG172016A1/en unknown
- 2009-12-09 EP EP09793383.2A patent/EP2376427B1/en not_active Not-in-force
- 2009-12-09 WO PCT/US2009/067271 patent/WO2010068649A1/en active Application Filing
- 2009-12-09 MY MYPI2011002349A patent/MY179041A/en unknown
- 2009-12-09 AU AU2009324709A patent/AU2009324709B2/en not_active Ceased
- 2009-12-09 MX MX2011006209A patent/MX2011006209A/es active IP Right Grant
- 2009-12-09 CA CA2745441A patent/CA2745441C/en active Active
- 2009-12-09 RU RU2011128393/04A patent/RU2512390C2/ru active
- 2009-12-09 KR KR1020117015637A patent/KR101685187B1/ko active IP Right Grant
- 2009-12-09 NZ NZ593377A patent/NZ593377A/xx not_active IP Right Cessation
- 2009-12-09 BR BRPI0922920A patent/BRPI0922920A2/pt not_active IP Right Cessation
- 2009-12-09 TW TW098142108A patent/TWI449685B/zh not_active IP Right Cessation
- 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
- 2009-12-09 JP JP2011540855A patent/JP5650657B2/ja not_active Expired - Fee Related
- 2009-12-09 US US12/633,944 patent/US8101794B2/en 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 CL CL2011001391A patent/CL2011001391A1/es unknown
- 2011-06-08 CO CO11070977A patent/CO6390054A2/es active IP Right Grant
- 2011-06-09 ZA ZA2011/04319A patent/ZA201104319B/en unknown
- 2011-12-19 US US13/330,358 patent/US8324236B2/en active Active
-
2012
- 2012-10-29 US US13/663,083 patent/US8486958B2/en active Active
-
2013
- 2013-06-17 US US13/919,260 patent/US8969367B2/en not_active Expired - Fee Related
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