AR087344A1 - Formas polimorficas del acido 5-(3,3-dimetil-but-1-inil)-3-[(trans-4-hidroxi-ciclohexil)-(trans-4-metil-ciclohexancarbonil)-amino]-tiofen-2-carboxilico y su uso en el tratamiento de la hepatitis c - Google Patents
Formas polimorficas del acido 5-(3,3-dimetil-but-1-inil)-3-[(trans-4-hidroxi-ciclohexil)-(trans-4-metil-ciclohexancarbonil)-amino]-tiofen-2-carboxilico y su uso en el tratamiento de la hepatitis cInfo
- Publication number
- AR087344A1 AR087344A1 ARP120102726A ARP120102726A AR087344A1 AR 087344 A1 AR087344 A1 AR 087344A1 AR P120102726 A ARP120102726 A AR P120102726A AR P120102726 A ARP120102726 A AR P120102726A AR 087344 A1 AR087344 A1 AR 087344A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- polymorphic form
- formula
- diffraction pattern
- ray powder
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D333/40—Thiophene-2-carboxylic acid
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- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Abstract
Un método para preparar la Forma polimórfica M del compuesto de fórmula (1) incluye agitar una mezcla del compuesto de fórmula (1) y un sistema de solvente que incluye isopropanol, etil acetato, n-butil acetato, metil acetato, acetona, 2-butanona (metiletilcetona (MEK)), o heptano, o una combinación de los mismos a una temperatura comprendida entre 10ºC y 47ºC para formar la Forma M del compuesto de fórmula (1). Un método para preparar la Forma polimórfica H del compuesto de fórmula (1) incluye agitar una solución del compuesto de fórmula (1) a una temperatura comprendida entre 48ºC y 70ºC para formar la Forma H del compuesto de fórmula (1). Un método para preparar la Forma P del compuesto de fórmula (1) incluye agitar una mezcla del compuesto de fórmula (1) y un sistema de solvente que incluye un solvente seleccionado entre el grupo formado por diclorometano y tetrahidrofurano (THF), y una mezcla de los mismos a temperatura ambiente para formar la Forma P del compuesto de fórmula (1). Un método para preparar la Forma X del compuesto de fórmula (1) incluye remover el solvato G de etil acetato del compuesto de fórmula (1). Un método para preparar la Forma ZA del compuesto de fórmula (1) incluye remover el n-butil acetato del solvato A de n-butil acetato del compuesto de fórmula (1).Reivindicación 1: Una forma polimórfica del compuesto (1) representado por la fórmula estructural (1), en donde la forma polimórfica es la forma polimórfica M, forma polimórfica H, forma polimórfica P, forma polimórfica X o forma polimórfica ZA. Reivindicación 4: La forma polimórfica de acuerdo con la reivindicación 2, en donde la forma polimórfica M se caracteriza por tener un patrón de difracción de polvos por rayos X con picos característicos expresados en 2-q ± 0,2 en las siguientes posiciones: 19,6, 16,6, 18,1, 9,0, 22,2 y 11,4, en donde el patrón de difracción de polvos por rayos X se obtiene a temperatura ambiente usando radiación CuKa. Reivindicación 11: La forma polimórfica de acuerdo con la reivindicación 9, en donde la forma polimórfica H se caracteriza por tener un patrón de difracción de polvos por rayos X con picos característicos expresados en 2-q ± 0,2 en las siguientes posiciones: 6,6, 18,7, 8,5, 17,3, 15,8 y 19,4, en donde el patrón de difracción de polvos por rayos X se obtiene a temperatura ambiente usando radiación CuKa. Reivindicación 18: La forma polimórfica de acuerdo con la reivindicación 16, en donde la forma polimórfica P se caracteriza por tener un patrón de difracción de polvos por rayos X con picos característicos expresados en 2-q ± 0,2 en las siguientes posiciones: 7,0, 15,8, 9,8, 19,3, 8,5 y 21,9, en donde el patrón de difracción de polvos por rayos X se obtiene a temperatura ambiente usando radiación CuKa. Reivindicación 25: La forma polimórfica de acuerdo con la reivindicación 23, en donde la forma polimórfica X se caracteriza por tener un patrón de difracción de polvos por rayos X con picos característicos expresados en 2-q ± 0,2 en las siguientes posiciones: 7,5, 12,1, 13,0, 13,8, 16,2 y 19,7 en donde el patrón de difracción de polvos por rayos X se obtiene a temperatura ambiente usando radiación CuKa. Reivindicación 29: La forma polimórfica de acuerdo con la reivindicación 27, en donde la forma polimórfica ZA se caracteriza por tener un patrón de difracción de polvos por rayos X con picos característicos expresados en 2-q ± 0,2 en las siguientes posiciones: 5,2, 10,2, 16,5, 18,6, 19,8 y 20,3, en donde el patrón de difracción de polvos por rayos X se obtiene a temperatura ambiente usando radiación CuKa. Reivindicación 31: Una forma amorfa del compuesto (1) representado por la fórmula estructural (1).
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161511643P | 2011-07-26 | 2011-07-26 | |
US201161511644P | 2011-07-26 | 2011-07-26 | |
US201161511647P | 2011-07-26 | 2011-07-26 | |
US201161511648P | 2011-07-26 | 2011-07-26 | |
US201161512079P | 2011-07-27 | 2011-07-27 | |
US201161545751P | 2011-10-11 | 2011-10-11 | |
US201261623144P | 2012-04-12 | 2012-04-12 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR087344A1 true AR087344A1 (es) | 2014-03-19 |
Family
ID=46604098
Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120102727A AR087345A1 (es) | 2011-07-26 | 2012-07-26 | Metodos para la preparacion de compuestos de tiofeno |
ARP120102728A AR087346A1 (es) | 2011-07-26 | 2012-07-26 | Formulaciones de compuestos de tiofeno |
ARP120102726A AR087344A1 (es) | 2011-07-26 | 2012-07-26 | Formas polimorficas del acido 5-(3,3-dimetil-but-1-inil)-3-[(trans-4-hidroxi-ciclohexil)-(trans-4-metil-ciclohexancarbonil)-amino]-tiofen-2-carboxilico y su uso en el tratamiento de la hepatitis c |
Family Applications Before (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120102727A AR087345A1 (es) | 2011-07-26 | 2012-07-26 | Metodos para la preparacion de compuestos de tiofeno |
ARP120102728A AR087346A1 (es) | 2011-07-26 | 2012-07-26 | Formulaciones de compuestos de tiofeno |
Country Status (6)
Country | Link |
---|---|
US (3) | US20140235705A1 (es) |
EP (1) | EP2736893A1 (es) |
AR (3) | AR087345A1 (es) |
AU (1) | AU2012286853A1 (es) |
TW (2) | TW201317223A (es) |
WO (4) | WO2013016492A1 (es) |
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EP2762124A1 (en) | 2013-01-31 | 2014-08-06 | IP Gesellschaft für Management mbH | Packaging comprising administration units of polymorphs, amorphous forms or solvates |
WO2014134251A1 (en) * | 2013-02-28 | 2014-09-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions |
WO2017003951A1 (en) * | 2015-06-29 | 2017-01-05 | Phloronol, Inc. | Solid pharmaceutical compositions of brown algae |
TW202208281A (zh) * | 2020-07-10 | 2022-03-01 | 紐西蘭商艾克福特士技術有限公司 | 鹽回收溶液及其使用方法 |
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EP2421855A1 (en) | 2009-04-24 | 2012-02-29 | Tibotec Pharmaceuticals | Diaryl ethers |
MX2011011290A (es) | 2009-04-28 | 2012-02-13 | Boehringer Ingelheim Int | Tratamiento ex-vivo de trastornos inmunologicos con inhibidores de pkc-teta. |
EP2430015B1 (en) | 2009-05-12 | 2015-06-17 | Merck Sharp & Dohme Corp. | Fused tricyclic compounds useful for the treatment of viral diseases |
-
2012
- 2012-07-26 WO PCT/US2012/048261 patent/WO2013016492A1/en active Application Filing
- 2012-07-26 AR ARP120102727A patent/AR087345A1/es not_active Application Discontinuation
- 2012-07-26 WO PCT/US2012/048258 patent/WO2013016490A1/en unknown
- 2012-07-26 AR ARP120102728A patent/AR087346A1/es unknown
- 2012-07-26 EP EP12743039.5A patent/EP2736893A1/en not_active Withdrawn
- 2012-07-26 WO PCT/US2012/048272 patent/WO2013016501A1/en active Application Filing
- 2012-07-26 WO PCT/US2012/048260 patent/WO2013016491A1/en active Application Filing
- 2012-07-26 AR ARP120102726A patent/AR087344A1/es not_active Application Discontinuation
- 2012-07-26 TW TW101127011A patent/TW201317223A/zh unknown
- 2012-07-26 TW TW101127020A patent/TW201313697A/zh unknown
- 2012-07-26 AU AU2012286853A patent/AU2012286853A1/en not_active Abandoned
-
2014
- 2014-01-24 US US14/163,064 patent/US20140235705A1/en not_active Abandoned
- 2014-01-24 US US14/162,997 patent/US20140235703A1/en not_active Abandoned
- 2014-01-24 US US14/163,014 patent/US20140235704A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US20140235703A1 (en) | 2014-08-21 |
US20140235704A1 (en) | 2014-08-21 |
US20140235705A1 (en) | 2014-08-21 |
AU2012286853A1 (en) | 2013-05-02 |
TW201313697A (zh) | 2013-04-01 |
WO2013016491A1 (en) | 2013-01-31 |
WO2013016501A1 (en) | 2013-01-31 |
TW201317223A (zh) | 2013-05-01 |
AR087346A1 (es) | 2014-03-19 |
EP2736893A1 (en) | 2014-06-04 |
WO2013016492A1 (en) | 2013-01-31 |
WO2013016490A1 (en) | 2013-01-31 |
AR087345A1 (es) | 2014-03-19 |
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