AR076268A1 - Combinaciones de inhibidor de vhc y agentes terapeuticos. metodo. uso. - Google Patents
Combinaciones de inhibidor de vhc y agentes terapeuticos. metodo. uso.Info
- Publication number
- AR076268A1 AR076268A1 ARP100101149A ARP100101149A AR076268A1 AR 076268 A1 AR076268 A1 AR 076268A1 AR P100101149 A ARP100101149 A AR P100101149A AR P100101149 A ARP100101149 A AR P100101149A AR 076268 A1 AR076268 A1 AR 076268A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- alkoxy
- aryl
- heterocyclyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 5
- 239000003814 drug Substances 0.000 title abstract 3
- 229940124597 therapeutic agent Drugs 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 38
- 125000003545 alkoxy group Chemical group 0.000 abstract 24
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 17
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 11
- 125000001072 heteroaryl group Chemical group 0.000 abstract 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 10
- 150000002367 halogens Chemical group 0.000 abstract 10
- 125000000623 heterocyclic group Chemical group 0.000 abstract 10
- 125000001424 substituent group Chemical group 0.000 abstract 9
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- -1 nitro, carboxyl Chemical group 0.000 abstract 5
- 241000711549 Hepacivirus C Species 0.000 abstract 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- 125000003282 alkyl amino group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 229940122604 HCV protease inhibitor Drugs 0.000 abstract 2
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 abstract 2
- 101800001838 Serine protease/helicase NS3 Proteins 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 108010016626 Dipeptides Proteins 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000004949 alkyl amino carbonyl amino group Chemical group 0.000 abstract 1
- 125000005093 alkyl carbonyl alkyl group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000004658 aryl carbonyl amino group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical group 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Producto combinado para tratar o mitigar la infeccion por virus de hepatitis C (VHC) o los trastornos o síntomas asociados con la misma en un sujeto que lo necesita que comprende, un inhibidor del VHC y uno o más agentes terapéuticos seleccionados entre cualquiera de los dos o ambos de los siguientes: un inhibidor de la proteasa del VHC y uno o más agentes terapéuticos diferentes administrados en combinacion en una cantidad eficaz al sujeto. Reivindicacion 2: El producto de acuerdo con la reivindicacion 1, donde el inhibidor del VHC de la reivindicacion 1 o un enantiomero, estereoisomero, diastereomero, racemato, tautomero, éster, prodroga, solvato, hidrato, isotopologo o forma de sal del mismo es un compuesto de Formula (1): donde X es hidrogeno, halogeno, ciano, nitro, carboxilo, alquil C1-8-carboniIo, alcoxi C1-8-carbonilo, formilo, amino, alquil C1-8-amino, amino-carbonilo, alquil C1-8-amino-carboniIo o alquil C1-8-sulfonilo; Ar es heteroarilo o heterociclilo, cada uno opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, amino o alquil C1-8-amino; Z es alquilo C1-8, alquenil C2-8-aIquilo C1-8, alquinil C2-8-aIquiIo C1-8, halo- alquilo C1-8, alcoxi C1-8-alquiIo C1-8, alcoxi C1-8-carbonilo, carboxilo, cicloalquilo C3-14, cicloalquenilo C3-14, cicloalquil C3-14-alquilo C1-8, arilo, aril-alquilo C1-8, heteroarilo, heteroaril-alquilo C1-8, heterociclilo o heterociclil-alquilo C1-8, donde en cada caso arilo y heteroarilo son opcionalmente sustituidos con uno, dos, tres o cuatro sustituyentes cada uno seleccionado entre hidroxi, ciano, nitro, halogeno, alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxi-alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, amino, alquil C1-8-amino, alcoxi C1-8-alquiIo C1-8, alquiltio C1-8, alquil C1-8-carbonilo, alcoxi C1-8-carbonilo, alquil C1-8-carboniloxi o amino-sulfonilo; R1 es -N(R3)-SO2-R4, -N(R3)-SO2-N(R5)-R6, -SO2-N(R5)-R6 o -SO2-R7; R2 es uno, dos, tres o cuatro sustituyentes cada uno seleccionado entre hidrogeno, halogeno, hidroxi, ciano, nitro, alquilo C1-8, hidroxi-alquilo C1-8, halo- alquilo C1-8, alquenilo C2-8, halo-alquenilo C2-8, alcoxi C1-8, halo-alcoxi C1-8, alcoxi C1-8-alquilo C1-8, alquil C1-8-carbonilo, alcoxi C1-8-carbonilo, alquil C1-8- carboniloxi, alquil C1-8-carboniloxi-alquilo C1-8, alquil C1-8-carboniloxi-alcoxi C1-8, amino, alquil C1-8-amino, amino-alquilo C1-8, alquil C1-8-amino-alquilo C1-8, amino-alcoxi C1-8, alquil C1-8-amino-alcoxi C1-8, alcoxi C1-8-alquil C1-8-amino- alcoxi C1-8, amino-alquil C1-8-amino-aIcoxi C1-8, alquil C1-8-amino-aIquil C1-8 amino-alcoxi C1-8, alcoxi C1-8-carbonil-amino, carboxil-amino, amino-carbonilo, amino-carbonil-amino, alquil C1-8-amino-carbonil-amino, alquiltio C1-8, alquil C1-8-sulfinilo, alquil C1-8-sulfonilo, alquil C1-8-sulfonil-amino, cicloalquilo C3-14, cicloalquil C3-14-alquilo C1-8, cicloalquil C3-14-alcoxi C1-8, cicloalquiloxi C3-14, arilo, aril-alquilo C1-8, aril-alcoxi C1-8, ariloxi, aril-carbonil-amino, heteroarilo, heteroaril-alquilo C1-8, heteroaril-alcoxi C1-8, heteroariloxi, heterociclil, heterociclil-alquilo C1-8, heterociclil-alcoxi C1-8, heterocicliloxi o heterociclil- carboniloxi, donde cada uno de cicloalquilo C3-14, arilo, heteroarilo y heterociclilo es opcionalmente sustituido con uno, dos, tres o cuatro sustituyentes cada uno seleccionado entre halogeno, ciano, alquilo C1-8, alcoxi C1-8, alcoxi C1-8-alquilo C1-8, amino, alquil C1-8-amino, amino-alquilo C1-8 o alquil C1-8-amino-alquiIo C1-8; R3 es hidrogeno o alquilo C1-8, opcionalmente sustituido en el alquilo C1-8 con uno o más sustituyentes cada uno seleccionado entre halogeno, hidroxi, ciano, alcoxi C1-8, amino o alquil C1-8-amino; R4 es alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, cicloalquilo C3-14, cicloalquil C3-14-alquilo C1-8, arilo, aril-alquilo C1-8, heteroarilo, heteroaril-alquilo C1-8, heterociclilo o heterociclil-alquilo C1-8, donde cada uno de arilo, heteroarilo, heterociclilo y cicloalquilo C3-14 es opcionalmente sustituido con uno o dos sustituyentes cada uno seleccionado entre halogeno, alquilo C1-8, halo- alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, amino o alquil C1-8-amino; R5 es hidrogeno, alquilo C1-8, alquil C1-8-carbonil- o cicloalquilo opcionalmente sustituido en el alquilo C1-8 con uno o más sustituyentes cada uno seleccionado entre halogeno, hidroxi, ciano o alcoxi C1-8; R6 es hidrogeno, alquilo C1-8, hidroxi-alquilo C1-8, halo-alquilo C1-8, ciano- alquilo C1-8, alcoxi C1-8-alquilo C1-8, amino-alquilo C1-8, alquil C1-8-amino-alquilo C1-8, alquil C1-8-carbonilo, alcoxi C1-8-carbonilo, cicloalquilo C3-14, cicloalquil C3-14-alquilo C1-8, arilo, aril-alquilo C1-8, heteroarilo, heteroaril-alquilo C1-8, heterociclilo o heterociclil-alquilo C1-8, donde cada uno de arilo, heteroanilo, heterociclilo y cicloalquilo C3-14 es opcionalmente sustituido con uno o dos sustituyentes cada uno seleccionado entre halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, amino o alquil C1-8-amino; y R7 es alquilo C1-8, cicloalquilo C3-14, cicloalquil C3-14-alquilo C1-8, arilo, aril- alquilo C1-8, heteroarilo, heteroaril-alquilo C1-8, heterociclilo o heterociclil-alquilo C1-8, donde cada uno de arilo, heteroarilo, cicloalquilo C3-14 y heterociclilo es opcionalmente sustituido con uno o dos sustituyentes cada uno seleccionado entre halogeno, alquilo C1-8, halo-alquilo C1-8, alcoxi C1-8, halo-alcoxi C1-8, amino o alquil C1-8-amino. Reivindicacion 6: El producto de acuerdo con la reivindicacion 1, donde el inhibidor de la proteasa del VHC se selecciona entre un inhibidor de la NS2 proteasa, un inhibidor de la NS3 proteasa, un inhibidor de la NS3 proteasa peptídico o dipeptídico o un inhibidor del cofactor de la NS4a proteasa.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16692209P | 2009-04-06 | 2009-04-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR076268A1 true AR076268A1 (es) | 2011-06-01 |
Family
ID=42225042
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100101149A AR076268A1 (es) | 2009-04-06 | 2010-04-06 | Combinaciones de inhibidor de vhc y agentes terapeuticos. metodo. uso. |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8841302B2 (es) |
| EP (1) | EP2416765B1 (es) |
| AR (1) | AR076268A1 (es) |
| TW (1) | TW201102062A (es) |
| WO (1) | WO2010117939A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2307419B1 (en) | 2008-06-24 | 2013-11-06 | Codexis, Inc. | Biocatalytic processes for the preparation of substantially stereomerically pure fused bicyclic proline compounds |
| US8703776B2 (en) | 2011-06-15 | 2014-04-22 | Cymabay Therapeutics, Inc. | Agonists of GPR131 and uses thereof |
| WO2013032939A1 (en) * | 2011-08-26 | 2013-03-07 | Metabolex, Inc. | Bicyclic agonists of gpr131 and uses thereof |
| US9310374B2 (en) | 2012-11-16 | 2016-04-12 | Redwood Bioscience, Inc. | Hydrazinyl-indole compounds and methods for producing a conjugate |
| JP6855496B2 (ja) | 2015-11-09 | 2021-04-07 | アール．ピー．シェーラー テクノロジーズ エルエルシー | 抗ｃｄ２２抗体−メイタンシンコンジュゲートおよびその使用方法 |
| KR20190045216A (ko) | 2016-09-16 | 2019-05-02 | 수미토모 케미칼 컴퍼니 리미티드 | 복소환 화합물 및 그것을 함유하는 유해 절족 동물 방제제 |
| RS65335B1 (sr) | 2018-10-05 | 2024-04-30 | Annapurna Bio Inc | Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5922757A (en) | 1996-09-30 | 1999-07-13 | The Regents Of The University Of California | Treatment and prevention of hepatic disorders |
| DE69709671T2 (de) | 1996-10-18 | 2002-08-22 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von serinproteasen, insbesondere von ns3-protease des hepatitis-c-virus |
| DK1663244T3 (da) | 2003-09-12 | 2007-12-03 | 4 Aza Ip Nv | Pteridin-derivater til behandling af TNF-alpha-beslægtede sygdomme |
| KR20070083484A (ko) * | 2004-07-14 | 2007-08-24 | 피티씨 테라퓨틱스, 인크. | Ｃ형 간염 치료 방법 |
| WO2007084413A2 (en) * | 2004-07-14 | 2007-07-26 | Ptc Therapeutics, Inc. | Methods for treating hepatitis c |
| EP1879881A2 (en) | 2005-04-14 | 2008-01-23 | Bristol-Myers Squibb Company | Inhibitors of 11-beta hydroxysteroid dehydrogenase type i |
| US8381971B2 (en) | 2005-06-30 | 2013-02-26 | Capital One Financial Corporation | System and method for point of sale cash rebates |
| EP1981523A2 (en) | 2006-02-09 | 2008-10-22 | Schering Corporation | Novel hcv inhibitor combinations and methods |
-
2010
- 2010-04-05 US US13/259,386 patent/US8841302B2/en not_active Expired - Fee Related
- 2010-04-05 WO PCT/US2010/029933 patent/WO2010117939A1/en not_active Ceased
- 2010-04-05 EP EP10714126.9A patent/EP2416765B1/en not_active Not-in-force
- 2010-04-06 AR ARP100101149A patent/AR076268A1/es not_active Application Discontinuation
- 2010-04-06 TW TW099110615A patent/TW201102062A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2416765B1 (en) | 2016-03-30 |
| TW201102062A (en) | 2011-01-16 |
| US8841302B2 (en) | 2014-09-23 |
| EP2416765A1 (en) | 2012-02-15 |
| WO2010117939A1 (en) | 2010-10-14 |
| US20120070412A1 (en) | 2012-03-22 |
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| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |