CO5261510A1 - Inhibidores de aspartil proteasa - Google Patents
Inhibidores de aspartil proteasaInfo
- Publication number
- CO5261510A1 CO5261510A1 CO00008433A CO00008433A CO5261510A1 CO 5261510 A1 CO5261510 A1 CO 5261510A1 CO 00008433 A CO00008433 A CO 00008433A CO 00008433 A CO00008433 A CO 00008433A CO 5261510 A1 CO5261510 A1 CO 5261510A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- optionally substituted
- alkenyl
- carbon atoms
- independently selected
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
- C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/19—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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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
- A61P31/18—Antivirals for RNA viruses for HIV
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
- C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/37—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07C311/38—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
- C07C311/39—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
- C07C311/42—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
- C07C311/46—Y being a hydrogen or a carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/16—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C317/18—Sulfones; Sulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
- C07D307/20—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D319/04—1,3-Dioxanes; Hydrogenated 1,3-dioxanes
- C07D319/06—1,3-Dioxanes; Hydrogenated 1,3-dioxanes not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Abstract
Un compuesto de fórmula I:<EMI FILE="00008433_1" ID="1" IMF=JPEG >o una sal farmacéuticamente aceptable del mismo, en donde:E' es -CO- o -SO2-;A se selecciona a partir de H; Ht; R1-Ht; -R1-C1-C6 alquilo, el cual esta sustituido opcionalmente con 1 o más grupos independientemente seleccionados de hidroxi , alcoxi con 1 a 4 átomos de carbono, Ht, -O-Ht, -NR2-CO-N(R2)2, -SO2-R2 o -CO-N(R2)2, -R1 alquenilo con 2 a 6 átomos de carbono, el cual es sustituido opcionalmente con 1 o mas grupos independientemente seleccionados de hidroxi, alcoxi con 1 a 4 átomos de carbono, Ht, -O-Ht, -NR2-CO-N(R2)2 o -CO-N(R2)2; o R7; en donde:Cada R1 es independientemente seleccionado a partir de -C(O)-, -S(O)2-, -C(O)-C(O)-, -O-C(O)-, -O-S(O)2, -NR2-S(O)2-, -NR2-C(O)- o -NR2-C(O)-C(O)-;Cada Ht seleccionado independientemente de cicloalquilo con 3 a 7 átomos de carbono, cicloalquenilo con 5 a 7 átomos de carbono; arilo con 6 a 14 átomos de carbono; o un heterociclo no saturado o saturado con 5 a 7 miembros, que contiene 1 o mas heteroátomos seleccionados entre N, O, o S; en donde dicho arilo o dicho heterociclo esta opcionalmente fundido a Q; y en donde cualquier miembro de dicho Ht es opcionalmente sustituido con 1 o mas sustituyentes independientemente seleccionados de oxo, -OR2, SR2, -R2, -N(R2)(R2), -R2-OH, -CN, -CO2R2, -C(O)-N(R2)2, -S(O)2-N(R2)2, -N(R2)-C(O)-R2, -N(R2)-C(O)O-R2, -C(O)-R2, -S(O)n-R2, -OCF3, -S(O)n-Q, metilenedioxi, -N(R2)-S(O)2(R2), halo, -CF3, -NO2, Q, OQ, -OR7, -SR7, -R7, -N(R2)(R7) o -N(R7)2;Cada Q se selecciona independientemente a partir de un sistema de anillo carboxílico parcialmente saturado o no saturado con 3 a 7 miembros saturados; o un anillo heterocíclico parcialmente saturado o no saturado con 5 a - 2 -7 miembros saturados que contiene uno o más heteroátomos seleccionados a partir de O, N, o S, en donde Q es sustituido opcionalmente con 1 o más grupos que seleccionan de oxo, -OR2, -R2, -SO2R2, -SO2-N(R2)2, -N(R2)2, -N(R2)-C(O)-R2, -R2-OH, -CN, -CO2R2, -C(O)-N(R2)2, halo o CF3;Cada R2 se selecciona independientemente de H, o alquilo con 1 a 4 átomos de carbono en donde dicho alquilo, cuando no es un sustituyente de Q, es sustituido opcionalmente con Q o -OR3; en donde cuando dicho R2 es una porción substituida -OR3, dicho R3 en -OR3 puede no ser -OR2 substituido;B, cuando está presente, es -N(R2)-C(R3)2-C(O)-;Cada x es independientemente 0 o 1;Cada R3 es seleccionado independientemente de H, Ht, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 o cicloalquenilo C5-6; en donde cualquier miembro de dicho R3, excepto H, es sustituido opcionalmente con uno o más sustituyentes seleccionados a partir de -OR2, -C(O)-NH-R2, -S(O)n-N(R2)(R2), -N(R2)2, -N(R2)-C(O)-O(R2), -N(R2)-C(O)-N(R2), -N(R2)-C(O)-(R2), Ht, -CN, -SR2, -CO2R2, o NR2-C(O)-R2;Cada n es independientemente 1 o 2;G, cuando está presente, se selecciona a partir de H, R7 o alquilo C1-4, o, cuando G es alquilo con 1 a 4 átomos de carbono, G y R7 están opcionalmente ligados uno al otro sea directamente o a través de un ligador con 1 a 3 átomos de carbono para formar un anillo heterocíclico; oCuando G no está presente, el nitrógeno al cual G está ligado se liga directamente al grupo R7 en -OR7 con el desplazamiento concomitante de un grupo -ZM desde R7;D es seleccionado a partir de Q, alquilo C1-6 opcionalmente sustituido con 1 o más grupos seleccionados a partir de cicloalquilo C3-6, -OR2, -S-Ht, -R3, -O-Q o Q; alquenilo con 2 a 4 átomos de carbono sustituido opcionalmente con 1 o más grupos seleccionados a partir de -OR2, -S-Ht, -R3, -O-Q o Q; cicloalquilo C3-6 opcionalmente sustituido con o fundido con Q; o cicloalquenilo C5-6 opcionalmente sustituido con o fundido a Q;D' es seleccionado de alquilo C1-C15, alquenilo C2-C15 o alquinilo C2-C15, cada uno de los cuales contiene uno o más sustituyentes seleccionados de oxo, halo, -CF3, -OCF3, -NO2, azido, -SH, -SR3, - N(R3)-N(R3)2, -O-N(R3)2, -(R3)N-O-(R3), -N(R3)2, -CN, -CO2R, -C(O)-N(R3)2 -S(O)n-N(R3)2, -N(R3)-C(O)-R3, -N(R3)-C(O)-N(R3)2, -N(R3)-C(O)-S(R3)2, -C(O)-R3, -S(O)n-R3, -N(R3)-S(O)n(R3), -N(R3)-S(O)n-N(R3)2, -S-NR3-C(O)R3, -C(S)N(R3)2, - C(S)R3, -NR3-C(O)OR3, -O-C(O)OR3, -O-C(O)N(R3)2, -NR3 C(S)R3, =N-OH, =N-OR3, =N-N(R3)2, =NR3, =NNR3C(O)N(R3)2, =NNR3C(O)OR3, =NNR3S(O)n-N(R3)2, -NR3-C(S)OR3, -NR3-C(S)N(R3)2, -NR3-C[=N(R3)]-N(R3)2, -N(R3)-C[=N-NO2]-N(R3)2, -N(R3)-C[=N-NO2]-OR3, -N(R3)-C[=N-CN]-OR3, N(R3)-C[=N-CN]-(R3)2, -OC(O)R3, -OC(S)R3, -OC(O)N(R3)2, -C(O)N(R3)-N(R3)2, -O-C(O)N(R3)-N(R3)2, O-C(O)N(OR3)(R3), N(R3)-N(R3)C(O)R3, N(R3)-OC(O)R3, N(R3)-OC(O)R3, N(R3)-OC(O)R3, -OC(S)N(R3)2, -OC(S)N(R3)(R3), o PO3-R3; con la condición de que cuando R7 es H, E´ es -SO2, G es H o alquilo, y cuando B esta presente o cuando B no está presente y R1 es -C(O)-, D´ puede no ser alquilo sustituido de 1 a 15 carbonos con un sustituyente seleccionado de -N(R3)2, -SR3 o -S(O)n-R3, o sustituido con dos -N(R3)2 sustituyentes; E se selecciona a partir de Ht; O-Ht; Ht-Ht; Ht fundido con Ht; -O-R3; -N(R2)(R3); alquilo C1-C6 opcionalmente sustituido con uno o más grupos seleccionados a partir de R4 o Ht; alquenilo C2-C6 opcionalmente substituido con 1 o más grupos seleccionados a partir de R4 o Ht; carbociclo saturado con C3-C6 opcionalmente sustituido con o más grupos seleccionados a partir de R4 o Ht; o carbociclo insaturado con C5-C6 opcionalmente sustituido con uno o más grupos seleccionados de R4 o Ht; Cada R4 es seleccionado independientemente a partir de -OR2, -OR3, -SR2, -SOR2, -SO2R2, CO2R2, -C(O)-NHR2, -C(O)-N(R2)2, -C(O)-NR2(OR2), -S(O)2-NHR2, halo, -NR2-C(O)-R2, -N(R2)2 O -CN;Cada R7 es seleccionado independientemente a partir de hidrógeno, <EMI FILE="00008433_2" ID="2" IMF=JPEG > En donde cada M es seleccionado independientemente a partir de H, Li, Na, K, Mg, Ca, Ba, -N(R2)4, alquilo C1-C12, - 3 - alquenilo C2-C12, o -R6; en donde 1 a 4 de los radicales -CH2 del grupo alquilo o alquenilo, diferentes del -CH2 que esta ligado al Z, es reemplazado opcionalmente por un grupo heteroátomo seleccionado a partir de O, S(O), S(O)2, o N(R2); y en donde cualquier hidrógeno en dicho alquilo, alquenilo o R6 es reemplazado opcionalmente con un sustituyente seleccionado a partir de oxo, -OR2, -R2, N(R2)2, N(R2)3, R2OH, -CN, -CO2R2, -C(O)-N(R2)2, S(O)2-N(R2)2, N(R2)-C(O)-R2, C(O)R2, -S(O)n-R2, OCF3, -S(O)n-R6, -N(R2)-S(O)2-(R2), halo, -CF3, o -NO2;M' es H, alquilo C1-C12, alquenilo C2-C12, o R6; en donde los radicales 1 a 4 de -CH2 del grupo alquilo o alquenilo se reemplazan opcionalmente por un grupo de heteroátomos seleccionados a partir de O, S, S(O), S(O)2, o N(R2); y en donde cualquier hidrógeno en dicho alquilo, alquenilo, o R6 es reemplazado opcionalmente con un sustituyente seleccionado a partir de oxo, -OR2, -R2, -N(R2)2, N(R2)3, -R2OH, -CN, -CO2R2, -C(O)-N(R2)2, -S(O)2-N(R2)2, -N(R2)-C(O)-R2, C(O)R2, -S(O)n-R2, OCF3, -S(O)n-R6, -N(R2)-S(O)2-(R2), halo, -CF3, o -NO2;Z es O, S, N(R2)2, o, cuando M no esta presente, H.Y es P o S;X es O o S;R9 es C(R2)2, O o N(R2); en donde cuando Y es S, Z no es S;R6 es un sistema de anillo heterocíclico o carbocíclico saturado o no saturado parcialmente con 5 a 6 miembros saturados, o un sistema de anillo bicíclico parcialmente saturado o no saturado con 8 a 10 miembros saturados; en donde cada uno de dichos sistemas de anillos heterocíclicos contiene uno o más heteroátomos seleccionados a partir de O, N, S, S(O)n o N(R2); y en donde cualquiera de los sistemas de dichos anillos contiene opcionalmente 1 a 4 sustituyentes independientemente seleccionados a partir de OH, alquilo C1-C4, alquilo -O-C1-C4- o alquilo -O-C(O)-C1-C4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12004799P | 1999-02-12 | 1999-02-12 |
Publications (1)
Publication Number | Publication Date |
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CO5261510A1 true CO5261510A1 (es) | 2003-03-31 |
Family
ID=37874715
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CO00008433A CO5261510A1 (es) | 1999-02-12 | 2000-02-09 | Inhibidores de aspartil proteasa |
Country Status (4)
Country | Link |
---|---|
US (4) | US6319946B1 (es) |
CO (1) | CO5261510A1 (es) |
TN (1) | TNSN00027A1 (es) |
TW (1) | TWI260322B (es) |
Families Citing this family (68)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20040122000A1 (en) * | 1981-01-07 | 2004-06-24 | Vertex Pharmaceuticals Incorporated. | Inhibitors of aspartyl protease |
US6436989B1 (en) * | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
TWI260322B (en) * | 1999-02-12 | 2006-08-21 | Vertex Pharma | Inhibitors of aspartyl protease |
TWI286476B (en) * | 2001-12-12 | 2007-09-11 | Tibotec Pharm Ltd | Combination of cytochrome P450 dependent protease inhibitors |
EP1483254A4 (en) * | 2002-01-07 | 2005-06-08 | Sequoia Pharmaceuticals | INHIBITORS OF ANTI-RESISTANCE RETROVIRAL PROTEASE |
US7157489B2 (en) * | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
JP2005523922A (ja) * | 2002-04-26 | 2005-08-11 | ギリアード サイエンシーズ, インコーポレイテッド | 非ヌクレオシド逆転写酵素阻害剤 |
US7470724B2 (en) * | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
WO2005002626A2 (en) * | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
US7300924B2 (en) * | 2003-04-25 | 2007-11-27 | Gilead Sciences, Inc. | Anti-infective phosphonate analogs |
US20050261237A1 (en) * | 2003-04-25 | 2005-11-24 | Boojamra Constantine G | Nucleoside phosphonate analogs |
WO2004096287A2 (en) * | 2003-04-25 | 2004-11-11 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
US7452901B2 (en) | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
SG182849A1 (en) * | 2003-04-25 | 2012-08-30 | Gilead Sciences Inc | Antiviral phosphonate analogs |
US7407965B2 (en) * | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
EP1620109A2 (en) * | 2003-04-25 | 2006-02-01 | Gilead Sciences, Inc. | Kinase inhibitor phosphonate conjugates |
US20090247488A1 (en) * | 2003-04-25 | 2009-10-01 | Carina Cannizzaro | Anti-inflammatory phosphonate compounds |
CN101410120A (zh) * | 2003-04-25 | 2009-04-15 | 吉里德科学公司 | 抗炎的膦酸酯化合物 |
US7432261B2 (en) * | 2003-04-25 | 2008-10-07 | Gilead Sciences, Inc. | Anti-inflammatory phosphonate compounds |
US20060148865A1 (en) * | 2003-06-27 | 2006-07-06 | Martin Michael T | Preparation of chemical compounds |
US7427624B2 (en) * | 2003-10-24 | 2008-09-23 | Gilead Sciences, Inc. | Purine nucleoside phosphorylase inhibitory phosphonate compounds |
CA2543294A1 (en) * | 2003-10-24 | 2005-05-26 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
WO2005044308A1 (en) * | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
US20070281907A1 (en) * | 2003-12-22 | 2007-12-06 | Watkins William J | Kinase Inhibitor Phosphonate Conjugates |
CN1906196A (zh) * | 2003-12-22 | 2007-01-31 | 吉里德科学公司 | 具有hiv和hcv抗病毒活性的4'-取代的卡波韦-和阿巴卡韦-衍生物以及相关化合物 |
US20050153990A1 (en) * | 2003-12-22 | 2005-07-14 | Watkins William J. | Phosphonate substituted kinase inhibitors |
AU2005222435B2 (en) * | 2004-03-11 | 2012-03-15 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
WO2005110428A2 (en) | 2004-05-07 | 2005-11-24 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
US7871991B2 (en) | 2004-07-27 | 2011-01-18 | Gilead Sciences, Inc. | Phosphonate analogs of HIV inhibitor compounds |
WO2009070744A1 (en) | 2007-11-28 | 2009-06-04 | Sequoia Pharmaceuticals, Inc. | Compositions and methods for inhibiting cytochrome p450 2d6 |
CN101702908A (zh) * | 2007-03-23 | 2010-05-05 | 麻萨诸塞州大学 | Hiv-1蛋白酶抑制剂 |
US8906647B2 (en) | 2008-02-21 | 2014-12-09 | Sequoia Pharmaceuticals, Inc. | Diamide inhibitors of cytochrome P450 |
BRPI0915878A2 (pt) | 2008-07-08 | 2015-11-03 | Gilead Sciences Inc | sais ou hidratos de compostos inibidores de hiv, seu uso e composição farmacêutica que os compreende |
BR122019026068B8 (pt) | 2011-06-21 | 2022-10-18 | Alnylam Pharmaceuticals | Ácido ribonucleico de fita dupla (dsrna) para inibir a expressão de angptl3 e seu uso, composição farmacêutica e método in vitro para inibir a expressão de angptl3 em uma célula |
EP4134433A1 (en) | 2011-06-23 | 2023-02-15 | Alnylam Pharmaceuticals, Inc. | Serpina1 sirnas: compositions of matter and methods of treatment |
EP2726108B1 (en) | 2011-06-29 | 2018-01-10 | The Trustees of Columbia University in the City of New York | Inhibitor of neuronal connectivity linked to schizophrenia susceptibility and cognitive dysfunction |
US9127274B2 (en) | 2012-04-26 | 2015-09-08 | Alnylam Pharmaceuticals, Inc. | Serpinc1 iRNA compositions and methods of use thereof |
WO2014075096A1 (en) * | 2012-11-09 | 2014-05-15 | The Trustees Of Columbia University In The City Of New York | Inhibitors of central nervous system vasoactive inhibitory peptide receptor 2 |
MX367076B (es) | 2012-12-05 | 2019-08-05 | Alnylam Pharmaceuticals Inc | Composiciones de arni de proteina convertasa subtilisina kexina 9 (pcsk9) y metodos de uso de las mismas. |
EP3312281A3 (en) | 2013-03-14 | 2018-06-27 | Alnylam Pharmaceuticals, Inc. | Complement component c5 irna compositions and methods of use thereof |
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UY35582A (es) | 2013-05-22 | 2014-10-31 | Alnylam Pharmaceuticals Inc | COMPOSICIONES DE ARNi DE SERPINA1 Y SUS MÉTODOS DE USO |
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TW201607559A (zh) | 2014-05-12 | 2016-03-01 | 阿尼拉製藥公司 | 治療serpinc1相關疾患之方法和組成物 |
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EP3192794A4 (en) * | 2014-09-11 | 2018-06-27 | Shionogi & Co., Ltd. | Sustained hiv protease inhibitor |
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JP2017535552A (ja) | 2014-11-17 | 2017-11-30 | アルナイラム ファーマシューティカルズ, インコーポレイテッドAlnylam Pharmaceuticals, Inc. | アポリポタンパク質C3(APOC3)iRNA組成物およびその使用方法 |
WO2016130806A2 (en) | 2015-02-13 | 2016-08-18 | Alnylam Pharmaceuticals, Inc. | Patatin-like phospholipase domain containing 3 (pnpla3) irna compositions and methods of use thereof |
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EA201792444A1 (ru) | 2015-05-06 | 2018-06-29 | Элнилэм Фармасьютикалз, Инк. | КОМПОЗИЦИИ НА ОСНОВЕ iRNA ДЛЯ ФАКТОРА XII (ФАКТОРА ХАГЕМАНА) (F12), ПЛАЗМЕННОГО КАЛЛИКРЕИНА B (ФАКТОРА ФЛЕТЧЕРА) 1 (KLKB1) И КИНИНОГЕНА 1 (KNG1) И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
WO2016201301A1 (en) | 2015-06-12 | 2016-12-15 | Alnylam Pharmaceuticals, Inc. | Complement component c5 irna compositions and methods of use thereof |
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KR20180095843A (ko) | 2015-12-07 | 2018-08-28 | 젠자임 코포레이션 | Serpinc1-연관 장애의 치료를 위한 방법 및 조성물 |
JP2018536689A (ja) | 2015-12-10 | 2018-12-13 | アルナイラム ファーマシューティカルズ, インコーポレイテッドAlnylam Pharmaceuticals, Inc. | ステロール調節エレメント結合タンパク質(SREBP)シャペロン(SCAP)iRNA組成物およびその使用方法 |
JP2019518028A (ja) | 2016-06-10 | 2019-06-27 | アルナイラム ファーマシューティカルズ, インコーポレイテッドAlnylam Pharmaceuticals, Inc. | 補体成分C5iRNA組成物及び発作性夜間血色素尿症(PNH)を処置するためのその使用方法 |
TWI788312B (zh) | 2016-11-23 | 2023-01-01 | 美商阿尼拉製藥公司 | 絲胺酸蛋白酶抑制因子A1 iRNA組成物及其使用方法 |
JP7058656B2 (ja) | 2016-12-16 | 2022-04-22 | アルナイラム ファーマシューティカルズ, インコーポレイテッド | トランスサイレチン(TTR)iRNA組成物を用いてTTR関連疾患を治療または予防するための方法 |
MX2020000790A (es) | 2017-07-21 | 2020-11-11 | Viiv Healthcare Co | Pautas para el tratamiento de infecciones por el vih y sida. |
EP3661937B1 (en) | 2017-08-01 | 2021-07-28 | Gilead Sciences, Inc. | Crystalline forms of ethyl ((s)-((((2r,5r)-5-(6-amino-9h-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-l-alaninate (gs-9131) for treating viral infections |
WO2019089922A1 (en) | 2017-11-01 | 2019-05-09 | Alnylam Pharmaceuticals, Inc. | Complement component c3 irna compositions and methods of use thereof |
CN112673103A (zh) | 2018-08-13 | 2021-04-16 | 阿尔尼拉姆医药品有限公司 | 乙型肝炎病毒(HBV)dsRNA剂组合物及其使用方法 |
MX2021008628A (es) | 2019-01-16 | 2021-11-17 | Genzyme Corp | Composiciones de arni para serpinc1 y metodos de uso de las mismas. |
WO2021154941A1 (en) | 2020-01-31 | 2021-08-05 | Alnylam Pharmaceuticals, Inc. | Complement component c5 irna compositions for use in the treatment of amyotrophic lateral sclerosis (als) |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4604402A (en) | 1984-03-30 | 1986-08-05 | E. R. Squibb & Sons, Inc. | Hydroxy substituted ureido amino and imino acids |
US4629724A (en) | 1984-12-03 | 1986-12-16 | E. R. Squibb & Sons, Inc. | Amino acid ester and amide renin inhibitors |
DE69321845T2 (de) | 1992-08-25 | 1999-04-29 | Searle & Co | Hydroxyethylaminosulfonamide verwendbar als inhibitoren retroviraler proteasen |
US5723490A (en) | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
TW372972B (en) | 1992-10-23 | 1999-11-01 | Novartis Ag | Antiretroviral acyl compounds |
ES2134924T3 (es) | 1992-10-30 | 1999-10-16 | Searle & Co | Acidos sulfonilalcanoilamino-hidroxietilamino-sulfamicos utiles como inhibidores de proteasas retrovirales. |
US5484926A (en) | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
ES2127938T3 (es) | 1993-08-24 | 1999-05-01 | Searle & Co | Hidroxietilamino sulfonamidas utiles como inhibidores de proteasas retroviricas. |
IL110898A0 (en) | 1993-09-10 | 1994-11-28 | Narhex Australia Pty Ltd | Polar-substituted hydrocarbons |
IL111584A0 (en) | 1993-11-18 | 1995-01-24 | Merck & Co Inc | Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them |
US5527829A (en) | 1994-05-23 | 1996-06-18 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
US6143747A (en) * | 1995-01-20 | 2000-11-07 | G. D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
US5691372A (en) * | 1995-04-19 | 1997-11-25 | Vertex Pharmaceuticals Incorporated | Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease |
TWI260322B (en) * | 1999-02-12 | 2006-08-21 | Vertex Pharma | Inhibitors of aspartyl protease |
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US7919523B2 (en) | 2011-04-05 |
US20040127488A1 (en) | 2004-07-01 |
US6617350B2 (en) | 2003-09-09 |
US6319946B1 (en) | 2001-11-20 |
TNSN00027A1 (fr) | 2005-11-10 |
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