ES2603617T3 - Moduladores de propiedades farmacocinéticas de la terapéutica - Google Patents

Moduladores de propiedades farmacocinéticas de la terapéutica Download PDF

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ES2603617T3
ES2603617T3 ES12167590.4T ES12167590T ES2603617T3 ES 2603617 T3 ES2603617 T3 ES 2603617T3 ES 12167590 T ES12167590 T ES 12167590T ES 2603617 T3 ES2603617 T3 ES 2603617T3
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Manoj C. Desai
Allen Y. Hong
Hon C. Hui
Hongtao Liu
Radall W. Vivian
Lianhong Xu
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Gilead Sciences Inc
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    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/08—Solutions
    • 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
    • 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
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
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    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

Abstract

Una composición farmacéutica que comprende a un compuesto de la fórmula IIB:**Fórmula** o una de sus sales, solvatos, estereoisómeros y/o ésteres farmacéuticamente aceptables donde: R10a y R10b son cada uno, independientemente, H o -C1-4 alquilo; R12 es H o -CH3; R13 es -(CH2)0-3CR17R18NR20R21, -(CH2)0-3CR17R18NR17C(O) NR20R21, -(CH2)1-3C(O)R22, -(CH2)1-3S(O)2R22 o -(CH2)1-3-R23; R14 y R15 son cada uno, independientemente, H, -C1-4 alquilo o arilalquilo; R17 y R18 son cada uno independientemente, H o -C1-3 alquilo; R19 es H, -C1-4 alquilo o arilalquilo; R20 y R21 son cada uno, independientemente, H, -C1-3 alquilo, -C(O)R17 o -S(O)2R17; o R20 y R21, tomados en conjunto con el átomo nitrógeno al cual se adhieren, forman un anillo heterociclilo de 5-6 miembros sustituido o no sustituido que contiene a 1-2 heteroátomos seleccionados un grupo que consiste de N y O; R22 es H, -C1-3alquilo, -OR19 o -NR20R21; y R23 es un anillo heterociclilo de 5-6 miembros no sustituido o sustituido que contiene a 1-2 heteroátomos seleccionados de un grupo que consiste de N y O; donde dicho anillo heterociclilo de 5-6 miembros sustituido o no sustituido formado por R20 y R21 y dicho anillo heterociclilo de 5-6 miembros sustituido o no sustituido de R23 se sustituyen o no se sustituyen, independientemente, con un C1-2 alquilo, un portador o excipiente farmacéuticamente aceptable y darunavir o una de sus sales, solvatos y/o ésteres farmacéuticamente aceptables.

Description

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puede adherirse a la porción alquenila del alquenilo de heterociclilo mediante un enlace carbono-carbono o un enlace carbono-heteroátomo, siempre y cuando, el grupo resultante sea químicamente estable. El grupo heterociclilalquenilo tiene de 3 a 20 átomos carbonos, por ejemplo, la fraccióm alquenila del grupo alquenilo de heterociclilo tiene de 2 a 6 átomos carbonos y la fracción heterociclila tiene de 1 a 14 átomos carbonos.
[0034] El término “heterociclilalquinilo” se refiere a un radical alquinilo acíclico en el cual uno de los átomos hidrógenos enlazados a un átomo carbono, comúnmente un átomo carbono terminal o sp3, pero también un átomo carbono sp, se reemplaza con un radical heterociclilo (es decir, una fracción heterociclila-alquinilena). La porción heterociclila del grupo alquinilo de heterociclilo incluye a cualquiera de los grupos heterociclilos aquí descritos, incluyendo a aquellos descritos en Principles of Modern Heterocyclic Chemistry (Principios de la Química Heterocíclica Moderna), y la porción alquinila del grupo alquinilo de heterociclilo incluye a cualquiera de los grupos alquinilos aquí descritos. Una persona con conocimiento en la industria entenderá también que el grupo heterociclilo puede adherirse a la porción alquinila del alquinilo de heterociclilo mediante un enlace carbono-carbono o un enlace carbono-heteroátomo, siempre y cuando el grupo resultante sea químicamente estable. El grupo heterociclilalquinilo tiene de 3 a 20 átomos carbonos, por ejemplo, la porción alquinila del grupo heterociclilalquinilo tiene de 2 a 6 átomos carbonos y la fracción heterociclila tiene de 1 a 14 átomos carbonos.
[0035] El término “heteroarilo” se refiere a un heterociclilo aromático que tiene por lo menos un heteroátomo en el anillo. Ejemplos no limitantes de heteroátomos adecuados que pueden incluirse en el anillo aromático incluyen al oxígeno, al azufre y al nitrógeno. Ejemplos no limitantes de anillos heteroarilos incluyen a todos aquellos listados en la definición de “heterociclilos” incluyendo el piridinilo, pirrolilo, oxazolilo, indolilo, isoindolilo, purinilo, furanilo, thienilo, benzofuranilo, benzotiofenilo, carbazolilo, imidazolilo, tiazolilo, isoxazolilo, pirazolilo, isotiazolilo, quinolilo, isoquinolilo, piridazilo, pirimidilo, pirazilo, etc. Radicales alquinilenos comunes incluyen, pero no se limitan a, acetileno (-C≡C-), propargilo (-CH2C≡C-), y 4-pentinilo (-CH2CH2CH2C≡CH-).
[0036] El término “carbociclo” o “carbociclilo” se refiere a un anillo saturado (es decir, el cicloalquilo), parcialmente insaturado (por ejemplo, el cicloalquenilo, el cicloalcadienilo, etc.) o aromático que tiene de 3 a 7 átomos carbonos tal como un monociclo, de 7 a 12 átomos carbonos tal como un biciclo, y hasta alrededor de 20 átomos carbonos tal como un policiclo. Los carbociclos monocíclicos tienen de 3 a 6 átomos anulares, aún más comúnmente 5 o 6 átomos anulares. Los carbociclos bicíclicos tienen de 7 a 12 átomos anulares, por ejemplo, configurados como un sistema biciclo [4,5], [5,5], [5,6] o [6,6], o 9 o 10 átomos anulares configurados como un sistema biciclo [5,6] o [6,6], o anillos fusionados espiro. Ejemplos no limitantes de carbociclos monocíclicos incluyen a ciclopropilos, ciclobutilos, ciclopentilos, 1-ciclopent-1-enilos, 1-ciclopent-2-enilos, 1-ciclopent-3-enilos, ciclohexilos, 1-ciclohex-1-enilos, 1ciclohex-2-enilos, 1-ciclohex-3-enilos, y fenilos. Ejemplos no limitantes de carbociclos biciclos incluyen al naftilo.
[0037] El término “arilheteroalquilo” se refiere a un heteroalquilo tal como se define en este documento, en el cual un átomo hidrógeno (que podría adherirse ya sea al átomo carbono o al heteroátomo) se reemplaza con un grupo arilo tal como se define en este documento. Los grupos arilos podrían enlazarse a un átomo carbono del grupo heteroalquilo, o a un heteroátomo del grupo heteroalquilo, siempre y cuando el grupo arilheteroalquilo resultante facilite una fracción químicamente estable. Por ejemplo, un grupo arilheteroalquilo puede tener las fórmulas generales -alquileno-O-arilo, -alquileno-O-alquileno-arilo, -alquileno-NH-arilo, -alquileno-NH-alquileno-arilo, alquileno-S-arilo, -alquileno-S-alquileno-arilo, etc. adicionalmente, cualquiera de las fracciones alquilenas en las fórmulas generales que se acaban de mencionar pueden sustituirse además con cualquiera de los sustituyentes definidos o usados como ejemplos en este documento.
[0038] El término “heteroarilalquilo” se refiere a un grupo alquilo, tal como se define en este documento, en el cual un átomo hidrógeno se reemplaza con un grupo heteroarilo tal como se define en este documento. Ejemplos no limitantes de alquilos de heteroarilos incluyen a -CH2-piridinilo, -CH2-pirrolilo, -CH2-oxazolilo, -CH2-indolilo, -CH2isoindolilo, -CH2-purinilo, -CH2-furanilo, -CH2-tienilo, -CH2-benzofuranilo, -CH2-benzotiofenilo, -CH2-carbazolilo, -CH2imidazolilo, -CH2-tiazolilo, -CH2-isoxazolilo, -CH2-p irazolilo, -CH2-isotiazolilo, -CH2-quinolilo, -CH2-isoquinolilo, -CH2piridazilo, -CH2-pirimidilo, -CH2-pirazilo, -CH(CH3)-piridinilo, -CH(CH3)-pirrolilo, -CH(CH3)-oxazolilo, -CH(CH3)-indolilo, -CH(CH3)-isoindolilo, -CH(CH3)-purinilo, -CH(CH3)-furanilo, -CH(CH3)-tienilo, -CH(CH3)-benzofuranilo, -CH(CH3)benzotiofenilo, -CH(CH3)-carbazolilo, -CH(CH3)-imidazolilo, -CH(CH3)-tiazolilo, -CH(CH3)-isoxazolilo, -CH(CH3)pirazolilo, -CH(CH3)-isotiazolilo, -CH(CH3)-quinolilo, -CH(CH3)-isoquinolilo, -CH(CH3)-piridazilo, -CH(CH3)-pirimidilo, CH(CH3)-pirazilo, etc.
[0039] El término “opcionalmente sustituido” en referencia a una fracción particular del compuesto de la fórmula IIB (por ejemplo, un grupo arilo opcionalmente sustituido) se refiere a una fracción que tiene 0, 1, 2 o más sustituyentes.
[0040] El término “Ac” se refiere a acetilo (-C(O)CH3).
[0041] El término "AC2O" se refiere a anhídrido acético.
[0042] El término “DCM” se refiere a diclorometano (CH2Cl2).
[0043] El término “DIBAL” se refiere a hidruro de diisobutilalumino
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Claims (1)

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ES12167590.4T 2007-02-23 2008-02-22 Moduladores de propiedades farmacocinéticas de la terapéutica Active ES2603617T3 (es)

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US90322807P 2007-02-23 2007-02-23
US903228P 2007-02-23
US95871607P 2007-07-06 2007-07-06
US958716P 2007-07-06

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ES12167589.6T Active ES2601820T3 (es) 2007-02-23 2008-02-22 Moduladores de propiedades terapéutica de las farmacocinéticas
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Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL1628685T3 (pl) 2003-04-25 2011-05-31 Gilead Sciences Inc Przeciwwirusowe analogi fosfonianowe
DK1778251T3 (da) 2004-07-27 2011-07-18 Gilead Sciences Inc Nukleosidphosphatkonjugater som anti-HIV-midler
RS54237B9 (sr) * 2006-07-07 2019-07-31 Gilead Sciences Inc Modulatori farmakokinetičkih svojstava terapeutika
EP2465856A3 (en) * 2006-08-31 2012-12-12 Abbott Laboratories Cytochrome P450 oxidase inhibitors and uses thereof
SI2487161T1 (sl) 2007-02-23 2016-12-30 Gilead Sciences, Inc. Modulatorji farmakokinetičnih lastnosti terapevtikov
PL3150586T3 (pl) 2007-02-23 2020-06-01 Gilead Sciences, Inc. Modulatory farmakokinetycznych właściwości środków terapeutycznych
WO2009067225A2 (en) * 2007-11-20 2009-05-28 Concert Pharmaceuticals, Inc. Boceprevir derivatives for the treatment of hcv infections
JP5629585B2 (ja) * 2008-01-04 2014-11-19 ギリアード サイエンシーズ， インコーポレイテッド シトクロムｐ４５０のインヒビター
EA201591353A1 (ru) * 2008-05-02 2016-01-29 Джилид Сайэнс, Инк. Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента
CN102089318B (zh) 2008-07-08 2014-05-21 吉里德科学公司 Hiv抑制剂化合物的盐
PL2364314T3 (pl) 2008-12-09 2014-08-29 Gilead Sciences Inc Modulatory receptorów Toll-podobnych
BRPI1008664A2 (pt) 2009-02-06 2016-03-08 Gilead Sciences Inc comprimidos para a terapia de combinação
AU2015200637C1 (en) * 2009-02-06 2017-08-03 Gilead Sciences, Inc. Tablets for combination therapy
UA108738C2 (uk) * 2009-04-03 2015-06-10 Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки
WO2010151672A2 (en) * 2009-06-26 2010-12-29 Georgetown University Amino acid derived ureas
EP3351249A1 (en) 2010-01-27 2018-07-25 VIIV Healthcare Company Antiviral therapy
NL2005306C2 (nl) * 2010-09-02 2012-03-05 Tersia Nederland B V Koppelstuk voor meerlaagse leidingen, lasapparaaat voor het verbinden van het koppelstuk met meerlaagse leidingen, werkwijze van koppelen en een samenstel verkregen via de werkwijze.
WO2012045007A1 (en) 2010-10-01 2012-04-05 Gilead Sciences, Inc. Method of preparation of (4 - {4 -acetylamino- 2 - [3- ( 2 - isopropyl - thiazol - 4 - ylmethyl) - 3 -methyl - ureido] - butyryl amino} -1 -benzyl- 5 -phenyl- pentyl) -carbamic acid thiazol - 5 - ylmethyl ester
EP2826466A1 (en) * 2010-11-19 2015-01-21 Gilead Sciences, Inc. Therapeutic compositions comprising rilpivirin hcl and tenofovir disoproxil fumarate
WO2012088156A1 (en) 2010-12-21 2012-06-28 Gilead Sciences, Inc. Inhibitors of cytochrome p450
WO2012088153A1 (en) * 2010-12-21 2012-06-28 Gilead Sciences, Inc. Inhibitors of cytochrome p450
WO2012088178A1 (en) 2010-12-21 2012-06-28 Gilead Sciences, Inc. Inhibitors of cytochrome p450 (cyp3a4)
EP2472320A2 (en) 2010-12-30 2012-07-04 Rohm and Haas Electronic Materials LLC Compositions comprising base-reactive component and processes for photolithography
EP2705027B1 (en) * 2011-05-02 2015-06-03 Gilead Sciences, Inc. Amorphous solid salts of Cobicistat (GS-9350)
JP6122427B2 (ja) 2011-07-07 2017-04-26 ヤンセン・サイエンシズ・アイルランド・ユーシー ダルナビル複合製剤
HRP20161696T4 (hr) 2011-08-16 2023-10-13 Gilead Sciences, Inc. Tenofovir alafenamid hemifumarat
CA2863662A1 (en) * 2012-02-03 2013-08-08 Gilead Sciences, Inc. Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections
AU2012327170A1 (en) * 2012-02-03 2013-08-22 Gilead Sciences, Inc. Therapeutic compounds
MX2014009344A (es) 2012-02-03 2015-05-11 Gilead Sciences Inc Metodos e intermediarios para preparar agentes farmaceuticos.
CN103694196A (zh) * 2012-09-27 2014-04-02 上海迪赛诺化学制药有限公司 细胞色素p450单加氧酶抑制剂中间体及其制法和用途
WO2014057498A2 (en) 2012-10-08 2014-04-17 Mylan Laboratories Ltd. Process for the preparation of cobicistat intermediates
CN104884063A (zh) * 2012-10-23 2015-09-02 西普拉有限公司 抗逆转录病毒药物组合物
SI3608325T1 (sl) 2012-12-21 2022-09-30 Gilead Sciences, Inc. Policiklične-karbamoilpiridonske spojine in njihova farmacevtska uporaba
JP2016504364A (ja) 2012-12-26 2016-02-12 アッシア・ケミカル・インダストリーズ・リミテッド コビシスタット塩
WO2015006731A1 (en) 2013-07-12 2015-01-15 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their use for the treatment of hiv infections
NO2865735T3 (es) 2013-07-12 2018-07-21
EP3421033B1 (en) 2013-10-07 2022-07-27 Bristol-Myers Squibb Holdings Ireland Unlimited Company Hiv treatment formulation of atazanavir and cobicistat
WO2015083066A1 (en) 2013-12-03 2015-06-11 Mylan Laboratories Ltd. Preparation of cobicistat intermediates
WO2015145324A1 (en) 2014-03-25 2015-10-01 Mylan Laboratories Ltd Process for the preparation of cobicistat
NO2717902T3 (es) 2014-06-20 2018-06-23
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
AU2015287773B2 (en) 2014-07-11 2018-03-29 Gilead Sciences, Inc. Modulators of toll-like receptors for the treatment of HIV
CR20170061A (es) * 2014-07-17 2017-07-17 Chdi Foundation Inc Métodos y composiciones para el tratamiento de trastornos relacionados con vih
EP3194401B1 (en) 2014-09-16 2020-10-21 Gilead Sciences, Inc. Solid forms of a toll-like receptor modulator
TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
US20190022116A1 (en) 2014-12-26 2019-01-24 Emory University N4-Hydroxycytidine and Derivatives and Anti-Viral Uses Related Thereto
ES2837383T3 (es) 2015-04-02 2021-06-30 Gilead Sciences Inc Compuestos de carbamoilpiridonas policíclicos y su utilización farmacéutica
CN105198829B (zh) * 2015-08-15 2017-10-31 浙江永宁药业股份有限公司 一种可比司他中间体的制备方法及其中间体和用途
CN107513046B (zh) * 2016-06-15 2019-12-13 江苏欧信制药有限公司 一种可比司他的合成方法
JP6764017B2 (ja) * 2016-08-04 2020-09-30 ギリアード サイエンシーズ， インコーポレイテッド がんの処置での使用のためのコビシスタット
BR112019002132A2 (pt) 2016-08-08 2019-05-14 Hetero Labs Limited composições anti-retrovirais
EP3496719B1 (en) 2016-08-08 2023-06-14 Hetero Labs Limited A multi-class anti-retroviral composition
KR101908853B1 (ko) * 2017-05-17 2018-10-16 경북대학교 산학협력단 아세틸시코닌을 유효성분으로 함유하는 시토크롬 p450 동효소 억제용 조성물
PT3661937T (pt) 2017-08-01 2021-09-24 Gilead Sciences Inc Formas cristalinas de ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-il)-4-fluoro-2,5-dihidrofurano-2-il)oxi)metil)(fenoxi)fosforil)-l-alaninato de etil (gs-9131) para tratamento de infeções virais
CA3082191C (en) 2017-12-07 2021-09-21 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
CN109912530A (zh) * 2017-12-13 2019-06-21 上海奥博生物医药技术有限公司 一种可比司他原料杂质的制备方法
CN111989316B (zh) * 2018-01-30 2023-09-08 潘贝拉治疗股份有限公司 用于生产(6s,15s)-3,8,13,18-四氮杂二十烷-6,15-二醇的方法
WO2021209563A1 (en) 2020-04-16 2021-10-21 Som Innovation Biotech, S.A. Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus
CN117105928B (zh) * 2023-08-22 2024-03-26 上海蓝木化工有限公司 一种蛋白酶抑制剂及其制备方法

Family Cites Families (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US77295A (en) * 1868-04-28 theqdoee krausch
US115665A (en) * 1871-06-06 Improvement in folding-steps for carriages
US199851A (en) * 1878-01-29 Improvement in circular saws
US191319A (en) * 1877-05-29 Improvement in stoves
US108617A (en) * 1870-10-25 Improvement in ore-pulverizers
US127689A (en) * 1872-06-11 Improvement in differential pulley-blocks
US143314A (en) * 1873-09-30 Improvement in condenser-tube fastenings
US181902A (en) * 1876-09-05 Improvement in bell toys
US99902A (en) * 1870-02-15 1870-02-15 Improvement in adjustable dials for travelers watches
US3400197A (en) 1965-01-26 1968-09-03 Robins Co Inc A H Compressible sustained release pharmaceutical tablet lipid-colloidal silica gel matrix fragment granules
US3882114A (en) 1967-10-26 1975-05-06 Oreal N-(morpholinomethyl carbamyl) cysteamine and glycine
GB1241024A (en) 1968-10-29 1971-07-28 Boehringer Sohn Ingelheim Pharmaceutical tablet base and a process for its manufacture
CA926708A (en) 1970-06-15 1973-05-22 Oushima Yoshitaka Process for producing spherical pellets
GB1339764A (en) 1971-03-29 1973-12-05 Ici Ltd Pyridine derivatives
CH586568A5 (es) 1972-04-10 1977-04-15 Hoffmann La Roche
US3957774A (en) 1972-04-17 1976-05-18 L'oreal N-morpholinomethyl-n-'-substituted ethyl and propylureas
DE2845326C2 (de) 1978-10-18 1985-05-23 Beiersdorf Ag, 2000 Hamburg Verwendung einer spezifischen mikrodispersen, amorphen, porösen Kieselsäure zur Herstellung von Digoxin enthaltenden Tabletten mit stark beschleunigter Wirkstoff-Freisetzung
US5142056A (en) * 1989-05-23 1992-08-25 Abbott Laboratories Retroviral protease inhibiting compounds
HU186777B (en) 1981-07-09 1985-09-30 Magyar Tudomanyos Akademia Process for producing complex-forming agents of crown-ether base and ionoselective membranelektrodes containing them
US4603143A (en) 1983-05-02 1986-07-29 Basf Corporation Free-flowing, high density, fat soluble vitamin powders with improved stability
GB8413191D0 (en) 1984-05-23 1984-06-27 Beecham Group Plc Pharmaceutical composition
FR2631620B1 (fr) 1988-05-19 1990-07-27 Rhone Poulenc Chimie Nouvelle silice precipitee absorbante et composition a base de cette s ilice
US5362912A (en) 1989-05-23 1994-11-08 Abbott Laboratories Process for the preparation of a substituted diaminodiol
US5354866A (en) * 1989-05-23 1994-10-11 Abbott Laboratories Retroviral protease inhibiting compounds
US5539122A (en) * 1989-05-23 1996-07-23 Abbott Laboratories Retroviral protease inhibiting compounds
EP0428849A3 (en) 1989-09-28 1991-07-31 Hoechst Aktiengesellschaft Retroviral protease inhibitors
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
US5914331A (en) 1990-02-01 1999-06-22 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US5204466A (en) 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
IE913840A1 (en) * 1990-11-20 1992-05-20 Abbott Lab Retroviral protease inhibiting compounds
GB9109862D0 (en) 1991-05-08 1991-07-03 Beecham Lab Sa Pharmaceutical formulations
JPH06127981A (ja) 1992-03-03 1994-05-10 Fuainiteii Kk 複合複層ガラス及びそれを使用した窓
US5968942A (en) * 1992-08-25 1999-10-19 G. D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
ES2317977T3 (es) 1992-12-29 2009-05-01 Abbott Laboratories Procedimientos e intermediarios para la preparacion de inhibidores de proteasa retrovirales.
WO1995005808A1 (en) 1993-08-24 1995-03-02 Abbott Laboratories Oil-based tableting method
US5567592A (en) 1994-02-02 1996-10-22 Regents Of The University Of California Screening method for the identification of bioenhancers through the inhibition of P-glycoprotein transport in the gut of a mammal
US5585115A (en) 1995-01-09 1996-12-17 Edward H. Mendell Co., Inc. Pharmaceutical excipient having improved compressability
US5567823A (en) 1995-06-06 1996-10-22 Abbott Laboratories Process for the preparation of an HIV protease inhibiting compound
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US5763464A (en) 1995-11-22 1998-06-09 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Retroviral agents containing anthranilamide, substituted benzamide and other subunits, and methods of using same
JP4064476B2 (ja) 1996-03-29 2008-03-19 エラワン ファーマスーティカル リサーチ アンドラボラトリー カンパニー リミテッド 二酸化珪素を有する球状凝集した澱粉
US6348216B1 (en) 1996-06-10 2002-02-19 Knoll Pharmaceutical Company Ibuprofen and narcotic analgesic compositions
US6361794B1 (en) 1996-06-12 2002-03-26 Basf Corporation Method of making ibuprofen and narcotic analgesic composition
US5922695A (en) 1996-07-26 1999-07-13 Gilead Sciences, Inc. Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability
US5939090A (en) 1996-12-03 1999-08-17 3M Innovative Properties Company Gel formulations for topical drug delivery
JP4494539B2 (ja) 1997-02-28 2010-06-30 ディーエスエム アイピー アセッツ ビー．ブイ． 流動自由な乾燥粒子
US5935946A (en) 1997-07-25 1999-08-10 Gilead Sciences, Inc. Nucleotide analog composition and synthesis method
FR2767071B1 (fr) 1997-08-06 1999-09-10 Rhodia Chimie Sa Composition comprenant un liquide absorbe sur un support a base de silice precipitee
AU2010299A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs os aspartyl protease inhibitors
FR2773994B1 (fr) 1998-01-23 2002-10-11 Univ Nice Sophia Antipolis Prodrogues issues d'anti-proteases inhibitrices du virus de l'immunodeficience humaine (vih) pour l'amelioration de leur biodisponibilite, de leur tropisme vers et/ou de leur delivrance dans le systeme nerveux central
JP4027535B2 (ja) 1998-05-26 2007-12-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 脂溶性薬物を含有した粉末
US6342249B1 (en) 1998-12-23 2002-01-29 Alza Corporation Controlled release liquid active agent formulation dosage forms
CA2371109C (en) * 1999-06-04 2011-04-26 Laman A. Alani Improved pharmaceutical formulations
WO2001025240A1 (en) 1999-10-06 2001-04-12 Tibotec Pharmaceuticals Ltd. HEXAHYDROFURO'2,3-B!FURAN-3-YL-N- {3'(1,3-BENZODIOXOL -5- YLSULFONYL) (ISOBUTYL) AMINO! -1-BENZYL-2-HYDROXYPROPYL} CARBAMATE AS RETROVIRAL PROTEASE INHIBITOR
CA2311734C (en) 2000-04-12 2011-03-08 Bristol-Myers Squibb Company Flash-melt oral dosage formulation
US6448245B1 (en) 2000-05-04 2002-09-10 The United States Of America As Represented By The Department Of Health And Human Services Methods of and compounds for inhibiting calpains
US20030035834A1 (en) 2000-05-26 2003-02-20 Pawan Seth Sustained release verapamil pharmaceutical composition free of food effect and a method for alleviating food effect in drug release
JPWO2002024167A1 (ja) 2000-09-19 2004-01-29 第一製薬株式会社 医薬組成物
US7056951B2 (en) 2000-09-26 2006-06-06 Mutual Pharmaceutical Co., Inc. Stable solid dosage forms of amino acids and processes for producing same
US6524615B2 (en) 2001-02-21 2003-02-25 Kos Pharmaceuticals, Incorporated Controlled release pharmaceutical composition
DE10112651A1 (de) 2001-03-16 2002-09-19 Degussa Inhomogene Kieselsäuren als Trägermaterial
AP2003002900A0 (en) 2001-05-01 2003-12-31 Pfizer Prod Inc Method for manufacturing a low dose pharmaceutical composition
DE10126163A1 (de) 2001-05-30 2002-12-05 Degussa Pharmazeutische Zubereitungen
ES2739852T3 (es) 2001-07-06 2020-02-04 Veloxis Pharmaceuticals As Aglomeración controlada
US7193065B2 (en) * 2001-07-13 2007-03-20 Roche Diagnostics Operations, Inc. Protease inhibitor conjugates and antibodies useful in immunoassay
US6946449B2 (en) 2001-07-13 2005-09-20 Cv Therapeutics, Inc. Partial and full agonists of A1 adenosine receptors
GB0123400D0 (en) 2001-09-28 2001-11-21 Novartis Ag Organic compounds
US7815936B2 (en) 2001-10-30 2010-10-19 Evonik Degussa Gmbh Use of granular materials based on pyrogenically produced silicon dioxide in pharmaceutical compositions
AU2002219964A1 (en) 2001-11-29 2003-06-17 Penwest Pharmaceutical Company Agglomerated particles including an active agent coprocessed with silicified microcrystalline cellulose
US20030206978A1 (en) 2001-11-29 2003-11-06 Bob Sherwood Agglomerated particles including an active agent coprocessed with silicified microcrystalline cellulose
US7285566B2 (en) 2002-01-07 2007-10-23 Erickson John W Resistance-repellent retroviral protease inhibitors
EP1467970B1 (en) 2002-01-17 2007-08-22 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
US6926906B2 (en) 2002-02-20 2005-08-09 M./S. Strides, Inc. Orally administrable pharmaceutical formulation
US6726448B2 (en) 2002-05-15 2004-04-27 General Electric Company Ceramic turbine shroud
PA8576201A1 (es) 2002-07-10 2004-05-26 Pfizer Prod Inc Composicion farmaceutica que tiene una distribucion y potencia uniforme de farmaco
DE10250711A1 (de) 2002-10-31 2004-05-19 Degussa Ag Pharmazeutische und kosmetische Zubereitungen
PE20040840A1 (es) 2002-11-20 2004-12-30 Japan Tobacco Inc Derivados de 4-oxoquinolina como inhibidores de la integrasa del vih
US7189416B2 (en) 2002-11-23 2007-03-13 Glykon Technologies Group, Llc Method for stable and controlled delivery of (-)-hydroxycitric acid
JP2004184681A (ja) 2002-12-03 2004-07-02 Konica Minolta Holdings Inc 熱現像感光材料
CA2512319A1 (en) 2003-01-14 2004-08-05 Gilead Sciences, Inc. Compositions and methods for combination antiviral therapy
EP1596835A1 (en) 2003-02-19 2005-11-23 H. Lundbeck A/S Method for preparation of an agglomerate using melt agglomeration
FR2851918B1 (fr) 2003-03-06 2006-06-16 Poudre impregnee ameliorant la biodisponibilite et/ou la solubilite et procede de fabrication
TW200505441A (en) 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
JP4018664B2 (ja) 2003-04-30 2007-12-05 第一三共株式会社 安定化固形製剤
DE10337198A1 (de) 2003-08-13 2005-03-17 Degussa Ag Träger auf Basis von Granulaten, die aus pyrogen hergestelltem Siliciumdioxiden hergestellt sind
US20050048112A1 (en) 2003-08-28 2005-03-03 Jorg Breitenbach Solid pharmaceutical dosage form
US8025899B2 (en) 2003-08-28 2011-09-27 Abbott Laboratories Solid pharmaceutical dosage form
JP2005075826A (ja) 2003-08-29 2005-03-24 Boehringer Ingelheim Internatl Gmbh 多孔質シリカ担体を含有する徐放性製剤
JP2005091988A (ja) 2003-09-19 2005-04-07 Konica Minolta Medical & Graphic Inc 熱現像感光材料及び画像形成方法
EP1675576A1 (en) 2003-10-03 2006-07-05 LifeCycle Pharma A/S A method for preparing modified release pharmaceutical compositions
US20050096390A1 (en) 2003-10-10 2005-05-05 Per Holm Compositions comprising fenofibrate and pravastatin
US20050095287A1 (en) 2003-10-29 2005-05-05 Matharu Amol S. Fosinopril composition
US7834043B2 (en) 2003-12-11 2010-11-16 Abbott Laboratories HIV protease inhibiting compounds
WO2005084670A1 (en) 2004-03-01 2005-09-15 Lek Pharmaceuticals D.D. Pharmaceutical formulation
MY142989A (en) 2004-03-10 2011-02-14 Bayer Schering Pharma Ag Stabilised supersaturated solids of lipophilic drugs
WO2005105040A2 (en) 2004-04-26 2005-11-10 Micelle Products, Inc. Water-soluble formulations of fat soluble vitamins and pharmaceutical agents and their applications
BRPI0401742B8 (pt) 2004-05-13 2021-05-25 Cristalia Produtos Quim Farmaceuticos Ltda composto análogo do ritonavir útil como inibidor de protease retroviral, preparação do composto análogo do ritonavir e composição farmacêutica do composto análogo do ritonavir
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
EP1758581A1 (en) 2004-05-21 2007-03-07 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-hiv agents
JP2006003701A (ja) 2004-06-18 2006-01-05 Konica Minolta Medical & Graphic Inc 熱現像感光材料および画像形成方法
EA013632B1 (ru) 2004-06-28 2010-06-30 Лайфсайкл Фарма А/С Пористые таблетки в качестве носителей для жидких композиций
US7718633B2 (en) * 2004-07-06 2010-05-18 Abbott Laboratories Prodrugs of HIV protease inhibitors
AR045841A1 (es) 2004-09-28 2005-11-16 Richmond Sa Com Ind Y Financie Una composicion farmaceutica solida que comprende al tiazolil metil ester del acido [5s-(5r*, 8r*, 10r*,11r*)] -10- hidroxi-2- metil-5-(1-metiletil)-1-[2-(1-metiletil)-4-tiazolil]-3,6-dioxo-8,11-bis(fenilmetil)-2,4,7,12- tetraazatridecan-13-oico y un procedimiento para prepararla.
CA2584670A1 (en) 2004-10-19 2006-04-27 Achillion Pharmaceuticals, Inc. Combination therapy for treating viral infections
US7786153B2 (en) 2005-03-02 2010-08-31 Abbott Laboratories Inc. Compounds that are useful for improving pharmacokinetics
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
US20070014854A1 (en) 2005-07-15 2007-01-18 Ilan Zalit Novel granulation process
EP1978939A2 (en) 2005-12-27 2008-10-15 Jubilant Organosys Limited Mouth dissolving pharmaceutical composition and process for preparing the same using a high amount of silicon dioxine
SG170795A1 (en) 2005-12-30 2011-05-30 Gilead Sciences Inc Methods for improving the pharmacokinetics of hiv integrase inhibitors
US20090233964A1 (en) 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
US20090186081A1 (en) 2006-01-05 2009-07-23 Lifecycle Pharma A/S Disintegrating Loadable Tablets
US20100285157A1 (en) 2006-02-20 2010-11-11 Asahi Breweries, Ltd Granules, tablets and method of producing the same
US20070287664A1 (en) 2006-03-23 2007-12-13 Schering Corporation Combinations of HCV protease inhibitor(s) and CYP3A4 inhibitor(s), and methods of treatment related thereto
RS54237B9 (sr) 2006-07-07 2019-07-31 Gilead Sciences Inc Modulatori farmakokinetičkih svojstava terapeutika
CL2007002331A1 (es) 2006-08-10 2008-04-18 Cipla Ltd Composicion oral solida que comprede uno o mas farmacos antirretrovirales y al menos un polimero insoluble en agua, en relacion aproximadamente 1:1 hasta 1:6; proceso de elaboracion; y uso para el tratamiento del vih.
EP2465856A3 (en) 2006-08-31 2012-12-12 Abbott Laboratories Cytochrome P450 oxidase inhibitors and uses thereof
US20090281132A1 (en) 2006-09-04 2009-11-12 Kiran Kumar Narsaiah Velaveni Pharmaceutical formulation for use in hiv therapy
US7749537B2 (en) 2006-12-04 2010-07-06 Scolr Pharma, Inc. Method of forming a tablet
PL3150586T3 (pl) 2007-02-23 2020-06-01 Gilead Sciences, Inc. Modulatory farmakokinetycznych właściwości środków terapeutycznych
WO2009006203A1 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
SG182229A1 (en) 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
AU2008275744A1 (en) * 2007-07-06 2009-01-15 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
BRPI0821700A2 (pt) 2007-12-27 2015-06-16 Baxter Int Métodos para determinar o número de moléculas de polímero fisiologicamente aceitáveis ligadas a uma proteína ou a um complexo de proteína em um conjugado polímero-proteína e para determinar o número de moléculas de polímero fisiologicamente aceitáveis ligadas a uma proteína ou a um complexo de proteína ou livre em solução
EA201591353A1 (ru) * 2008-05-02 2016-01-29 Джилид Сайэнс, Инк. Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента
BRPI1008664A2 (pt) 2009-02-06 2016-03-08 Gilead Sciences Inc comprimidos para a terapia de combinação
EP2238979A1 (en) 2009-04-06 2010-10-13 LEK Pharmaceuticals d.d. Active pharmaceutical ingredient adsorbed on solid support
WO2013105474A1 (ja) 2012-01-10 2013-07-18 Jnc株式会社 発光層用材料およびこれを用いた有機電界発光素子
CA2863662A1 (en) 2012-02-03 2013-08-08 Gilead Sciences, Inc. Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections

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