AR087418A1 - Inhibidores de replica de virus de influenza - Google Patents
Inhibidores de replica de virus de influenzaInfo
- Publication number
- AR087418A1 AR087418A1 ARP120102809A ARP120102809A AR087418A1 AR 087418 A1 AR087418 A1 AR 087418A1 AR P120102809 A ARP120102809 A AR P120102809A AR P120102809 A ARP120102809 A AR P120102809A AR 087418 A1 AR087418 A1 AR 087418A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently
- alkyl
- structural formula
- inhibitors
- influenza virus
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 241000712461 unidentified influenza virus Species 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 2
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- 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
- 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 Table
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Biochemistry (AREA)
- Emergency Medicine (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
Abstract
Proceso de elaboración e intermediario.Reivindicación 1: Un compuesto representado por la fórmula estructural (1), o una de sus sales farmacéuticamente aceptables, en donde: X1 es -F, -Cl, -CF3, -CN o CH3; X2 es -H, -F o -Cl; Z1 es N o CH; Z2 es N o CR0; Z3 es CH o N; Y es -C(R4R5)-[C(R6R7)]n-Q o -C(R4)=C(R6)-Q; R0 es -H, -F o CN; R1, R2 y R3 son, cada uno y de modo independiente, -CH3, -CH2F, -CF3, -C2H5, -CH2CH2F, -CH2CF3; o, de modo opcional, R2 y R3 o R1, R2 y R3, junto con el átomo de carbono al que están unidos, forman un anillo carbocíclico de 3 - 10 miembros; R4 y R5 son, cada uno y de modo independiente, -H; R6 y R7 son, cada uno y de modo independiente, -H, -OH, -CH3 o -CF3; o de modo opcional, R5 y R7, junto con los átomos de carbono a los que están unidos, forman un anillo ciclopropano; y cada Q es, de modo independiente, -C(O)OR, -OH, -CH2OH, -S(O)R’, -P(O)(OH)2, -S(O)2R’, -S(O)2-NR’’R’’’ o un heterociclo de 5 miembros seleccionado del grupo de formulas (2); JQ es -H, -OH o -CH2OH; R es -H o alquilo C1-4; R’ es -OH, alquilo C1-4 o -CH2C(O)OH; R’’ es -H o -CH3; R’’’ es -H, un anillo carbocíclico de 3 - 6 miembros o alquilo C1-4 sustituido, de modo opcional, con uno o varios sustituyentes seleccionados del grupo que consiste en halógeno, -ORa y -C(O)ORa; Ra es -H o alquilo C1-4; y n es 0 ó 1. Reivindicación 50: Un compuesto representado por la fórmula estructural (3) o una de sus sales farmacéuticamente aceptables, en donde las variables de la fórmula estructural (3) son, cada uno y de modo independiente, tal como se definen en cualquiera de las reivindicaciones 1 - 38; y cuando Z1 es N, G es tritilo; cuando Z1 es CH, G es tosilo o tritilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161513793P | 2011-08-01 | 2011-08-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR087418A1 true AR087418A1 (es) | 2014-03-19 |
Family
ID=46650922
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120102809A AR087418A1 (es) | 2011-08-01 | 2012-08-01 | Inhibidores de replica de virus de influenza |
Country Status (37)
| Country | Link |
|---|---|
| US (5) | US9051319B2 (es) |
| EP (2) | EP2739623B1 (es) |
| JP (3) | JP5917692B2 (es) |
| KR (1) | KR101967172B1 (es) |
| CN (3) | CN105503862B (es) |
| AP (1) | AP3867A (es) |
| AR (1) | AR087418A1 (es) |
| AU (2) | AU2012290127B2 (es) |
| CA (1) | CA2844054C (es) |
| CL (1) | CL2014000245A1 (es) |
| CO (1) | CO6940412A2 (es) |
| CY (1) | CY1118726T1 (es) |
| DK (1) | DK2739623T3 (es) |
| EA (3) | EA037372B1 (es) |
| EC (1) | ECSP14013189A (es) |
| ES (2) | ES2618919T3 (es) |
| GE (2) | GEP201706698B (es) |
| HK (1) | HK1223915A1 (es) |
| HR (1) | HRP20170421T1 (es) |
| HU (1) | HUE033752T2 (es) |
| IL (2) | IL230618A (es) |
| IN (1) | IN2014CN00562A (es) |
| LT (1) | LT2739623T (es) |
| ME (1) | ME02638B (es) |
| MX (1) | MX339149B (es) |
| PE (1) | PE20141209A1 (es) |
| PH (1) | PH12014500257A1 (es) |
| PL (1) | PL2739623T3 (es) |
| PT (1) | PT2739623T (es) |
| RS (1) | RS55858B1 (es) |
| SG (2) | SG10201503835TA (es) |
| SI (1) | SI2739623T1 (es) |
| TW (3) | TWI537268B (es) |
| UA (2) | UA118010C2 (es) |
| UY (1) | UY34234A (es) |
| WO (1) | WO2013019828A1 (es) |
| ZA (2) | ZA201400604B (es) |
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|---|---|---|---|---|
| EP1881983B1 (en) * | 2005-05-20 | 2012-01-11 | Vertex Pharmaceuticals, Inc. | Pyrrolopyridines useful as inhibitors of protein kinase |
| EP2262498A2 (en) * | 2008-03-10 | 2010-12-22 | Vertex Pharmceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| PH12015501678B1 (en) | 2009-06-17 | 2022-07-06 | Vertex Pharma | Inhibitors of influenza viruses replication |
| CN103702998A (zh) | 2011-07-05 | 2014-04-02 | 沃泰克斯药物股份有限公司 | 生产氮杂吲哚类的方法和中间体 |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| US9296727B2 (en) | 2013-10-07 | 2016-03-29 | Vertex Pharmaceuticals Incorporated | Methods of regioselective synthesis of 2,4-disubstituted pyrimidines |
| AU2014348752C1 (en) * | 2013-11-13 | 2019-11-21 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
| JP6615755B2 (ja) | 2013-11-13 | 2019-12-04 | バーテックス ファーマシューティカルズ インコーポレイテッド | インフルエンザウイルスの複製の阻害剤 |
| CN103922966B (zh) * | 2014-04-14 | 2015-10-21 | 武汉大学 | 作为甲型流感病毒抑制剂的甲酰胺和异腈类化合物及其制备与应用 |
| WO2016020526A1 (en) * | 2014-08-08 | 2016-02-11 | Janssen Sciences Ireland Uc | Indoles for use in influenza virus infection |
| KR102531340B1 (ko) * | 2014-09-08 | 2023-05-10 | 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 | 인플루엔자 바이러스 감염에 사용하기 위한 피롤로피리미딘 |
| MA40772A (fr) * | 2014-10-02 | 2017-08-08 | Vertex Pharma | Variants du virus de la grippe a |
| MA40773A (fr) | 2014-10-02 | 2017-08-08 | Vertex Pharma | Variants du virus influenza a |
| JP6704416B2 (ja) * | 2015-05-13 | 2020-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | インフルエンザウイルスの複製の阻害剤を調製する方法 |
| WO2016183120A1 (en) * | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| US10626108B2 (en) | 2015-11-27 | 2020-04-21 | Janssen Sciences Ireland Uc | Heterocyclic indoles for use in influenza virus infection |
| CN106854205B (zh) | 2015-12-09 | 2019-07-09 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其使用方法和用途 |
| DK3400225T3 (da) * | 2016-01-07 | 2022-01-03 | Janssen Sciences Ireland Unlimited Co | Pentansyrederivater substitueret med pyrrolo-[2,3-b]pyrimidinpyridiner til behandling af influenzavirusinfektioner |
| DK3405466T3 (da) | 2016-01-20 | 2021-02-01 | Janssen Sciences Ireland Unlimited Co | Arylsubstituerede pyrimidiner til anvendelse ved influenzavirusinfektion |
| CN109790158B (zh) * | 2016-07-26 | 2022-06-24 | 苏州隆博泰药业有限公司 | 作为jak抑制剂杂环化合物,该化合物的盐类及其治疗用途 |
| WO2018033082A1 (en) | 2016-08-16 | 2018-02-22 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication, application methods and uses thereof |
| CN109641868B (zh) * | 2016-08-30 | 2021-12-03 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其使用方法和用途 |
| CN106478460B (zh) * | 2016-09-28 | 2018-06-12 | 衢州学院 | 一种手性N-Boc-3-氨基-4-芳基-丁酸的合成方法 |
| EP3555095B1 (en) | 2016-12-15 | 2023-04-12 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication and uses thereof |
| US11098042B2 (en) | 2017-01-05 | 2021-08-24 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication and uses thereof |
| CN110446711B (zh) | 2017-03-02 | 2022-02-15 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其用途 |
| CN111511907A (zh) | 2017-03-14 | 2020-08-07 | 加利福尼亚大学董事会 | 对病毒中免疫逃逸功能区域的全基因组鉴定 |
| CN109384783A (zh) * | 2017-08-09 | 2019-02-26 | 银杏树药业(苏州)有限公司 | 新型杂环化合物及其作为抗流感病毒抑制剂的医药用途 |
| KR102813547B1 (ko) * | 2018-07-27 | 2025-05-27 | 코크리스탈 파마, 아이엔씨. | 인플루엔자바이러스 복제 억제제로서의 피롤로[2,3-b]피리딘 유도체 |
| CN112979647B (zh) * | 2021-03-12 | 2022-05-20 | 浙江大学 | 含氮杂氨基酸的氮杂吲哚衍生物及制备和应用 |
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| JP6704416B2 (ja) | 2015-05-13 | 2020-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | インフルエンザウイルスの複製の阻害剤を調製する方法 |
| US10626108B2 (en) | 2015-11-27 | 2020-04-21 | Janssen Sciences Ireland Uc | Heterocyclic indoles for use in influenza virus infection |
| DK3400225T3 (da) | 2016-01-07 | 2022-01-03 | Janssen Sciences Ireland Unlimited Co | Pentansyrederivater substitueret med pyrrolo-[2,3-b]pyrimidinpyridiner til behandling af influenzavirusinfektioner |
| DK3405466T3 (da) | 2016-01-20 | 2021-02-01 | Janssen Sciences Ireland Unlimited Co | Arylsubstituerede pyrimidiner til anvendelse ved influenzavirusinfektion |
| WO2017223231A1 (en) | 2016-06-21 | 2017-12-28 | Alios Biopharma, Inc. | (s)-8-(benzhydryl )-6-isopropyl-3,5-dioxo- 5, 6,7,8,-tetrahydro-3h-pyrazino-[1,2-b]pyridazin-yl-isobutyrate antiviral agent for use in treating influenza |
| WO2018191475A1 (en) | 2017-04-12 | 2018-10-18 | Vertex Pharmaceuticals Incorporated | Combination therapies for treating influenza virus infection |
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