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
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 102000051367 mu Opioid Receptors Human genes 0.000 title abstract 2
- 108020001612 μ-opioid receptors Proteins 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 239000007787 solid Substances 0.000 abstract 11
- -1 (2S, 3S) -7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino Chemical group 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 2
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 2
- 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 abstract 1
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000000126 substance Substances 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
-
- 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
-
- 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 |
|---|---|---|---|---|
| ES2402748T3 (es) | 2007-12-11 | 2013-05-08 | Theravance, Inc. | Compuestos de aminotetralina como antagonistas del receptor de opioide mu |
| MY149973A (en) * | 2007-12-11 | 2013-11-15 | Theravance Inc | 3-carboxypropyl-aminotetralin derivatives as mu opioid receptor antagonists |
| JP5797655B2 (ja) * | 2009-09-18 | 2015-10-21 | アドラー・コーポレーション | 消化管障害のためのオピオイド受容体アンタゴニストの使用 |
| CN103814010A (zh) * | 2011-09-30 | 2014-05-21 | 施万制药 | 3-[2-甲磺酰基-1-(4-三氟甲基苯氧基)乙基]吡咯烷化合物的结晶形式 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6498196B1 (en) * | 1998-12-22 | 2002-12-24 | Edward Roberts | Compounds useful in pain management |
| US6844368B1 (en) * | 1998-12-22 | 2005-01-18 | 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 |
| JP2006522819A (ja) * | 2003-04-08 | 2006-10-05 | プロジェニックス ファーマシューティカルズ，インコーポレーテッド | 緩下薬および末梢オピオイドアンタゴニストを組み合わせた便秘の組み合わせ療法 |
| SE0301794D0 (sv) * | 2003-06-19 | 2003-06-19 | Astrazeneca Ab | New use III |
| BRPI0718554A2 (pt) | 2006-11-07 | 2013-11-19 | Nektar Therapeutics Al Corp | Formas de dosagem e co-admimstração de um agonista opióide e um antagonista opióide |
| 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 |
| ES2402748T3 (es) | 2007-12-11 | 2013-05-08 | Theravance, Inc. | Compuestos de aminotetralina como antagonistas del receptor de opioide mu |
| MY149973A (en) * | 2007-12-11 | 2013-11-15 | Theravance Inc | 3-carboxypropyl-aminotetralin derivatives 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 MX MX2011006209A patent/MX2011006209A/es active IP Right Grant
- 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 KR KR1020117015637A patent/KR101685187B1/ko not_active Expired - Fee Related
- 2009-12-09 WO PCT/US2009/067271 patent/WO2010068649A1/en not_active Ceased
- 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 AU AU2009324709A patent/AU2009324709B2/en not_active Ceased
- 2009-12-09 EP EP09793383.2A patent/EP2376427B1/en not_active Not-in-force
- 2009-12-09 ES ES09793383.2T patent/ES2645087T3/es active Active
- 2009-12-09 MY MYPI2011002349A patent/MY179041A/en unknown
- 2009-12-09 RU RU2011128393/04A patent/RU2512390C2/ru active
- 2009-12-09 CA CA2745441A patent/CA2745441C/en active Active
- 2009-12-09 BR BRPI0922920A patent/BRPI0922920A2/pt not_active IP Right Cessation
- 2009-12-09 CN CN200980149818.7A patent/CN102245564B/zh 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 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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