AR103252A1 - Compuestos de quinazolina - Google Patents
Compuestos de quinazolinaInfo
- Publication number
- AR103252A1 AR103252A1 ARP150104262A ARP150104262A AR103252A1 AR 103252 A1 AR103252 A1 AR 103252A1 AR P150104262 A ARP150104262 A AR P150104262A AR P150104262 A ARP150104262 A AR P150104262A AR 103252 A1 AR103252 A1 AR 103252A1
- Authority
- AR
- Argentina
- Prior art keywords
- cycloalkyl
- alkyl
- heteroalkyl
- nrarb
- ora
- Prior art date
Links
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 26
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 25
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 abstract 20
- 229910003827 NRaRb Inorganic materials 0.000 abstract 19
- 229910052736 halogen Inorganic materials 0.000 abstract 11
- 150000002367 halogens Chemical class 0.000 abstract 11
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 -ORa Chemical group 0.000 abstract 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 3
- MPVDXIMFBOLMNW-UHFFFAOYSA-N chembl1615565 Chemical compound OC1=CC=C2C=C(S(O)(=O)=O)C=C(S(O)(=O)=O)C2=C1N=NC1=CC=CC=C1 MPVDXIMFBOLMNW-UHFFFAOYSA-N 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen en el presente documento compuestos de fórmula (1) y tautómeros y sales farmacéuticas de los mismos, composiciones y formulaciones que contienen dichos compuestos y métodos para usar y preparar dichos compuestos. Reivindicación 1: Un compuesto de fórmula (1), en donde Q es un resto de fórmula (2) ó (3); X¹, X², y X³ son cada uno independientemente N o C(R¹¹), provisto que, a lo sumo 2 de X¹, X², y X³ son N; R¹ es -H, -CN, -ORᵃ, -C(O)ORᵃ, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R² es -H, -CN, -ORᵃ, -NRᵃRᵇ, -C(O)ORᵃ, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀ y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R³ es -H, -ORᵃ, -SRᵃ, -NRᵃRᵇ, -NHC(O)NRᵃRᵇ, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁴ es -H, -ORᵃ, halógeno, -NO₂, -CN, -NRᵃRᵇ, -NHC(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -CH₂C(O)NRᵃRᵇ, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁵ es -H, -ORᵃ, halógeno, -NO₂, -CN, -NRᵃRᵇ, -NHC(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -CH₂C(O)NRᵃRᵇ, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁶ es -H, -ORᵃ, halógeno, -NO₂, -CN, -NRᵃRᵇ, -NHC(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -CH₂C(O)NRᵃRᵇ, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₃, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀ y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁷ es alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, halógeno, -ORᵃ, -CN, o -NO₂, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁸ es alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₃, halógeno, -ORᵃ, -CN, o -NO₂, en donde cada alquilo C₁₋₆, cicloalquilo, C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R⁹ es -H, alquilo C₁₋₆, o cicloalquilo C₃₋₁₀, en donde cada alquilo C₁₋₆ y cicloalquilo C₃₋₁₀ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; R¹⁰ es -H, alquilo C₁₋₆, o cicloalquilo C₃₋₁₀, en donde cada alquilo C₁₋₆ y cicloalquilo C₃₋₁₀ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; cada R¹¹ es independientemente -H, -CN, -ORᵃ, -C(O)ORᵃ, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, o heteroalquilo C₁₋₆, que, pueden ser los mismos o diferentes, en donde cada alquilo C₁₋₃, cicloalquilo C₃₋₁₀, y heteroalquilo C₁₋₆ está opcionalmente sustituido con 1, 2, 3, 4, ó 5 Grupos R¹², que pueden ser los mismos o diferentes; cada R¹² es independientemente alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, heterociclilo de 5 - 10 miembros, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros, halógeno, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)ORᵇ, -SRᵃ, -S(O)₁₋₂Rᵃ, -S(O)₂F, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, o -NO₂; en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, y heterociclilo de 5 - 10 miembros está opcionalmente sustituido con 1, 2, 3, 4, ó 5 sustituyentes seleccionados de halógeno, -ORᵃ, -C(O)Rᵃ, -C(O)ORᵃ, -C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃC(O)ORᵇ, -SRᵃ, -S(O)₁₋₂Rᵃ, -S(O)₂F, -S(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵇ, -N₃, -CN, y -NO₂, grupos, que pueden ser los mismos o diferentes; cada Rᵃ y Rᵇ es independientemente -H, -NH₂, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, heterociclilo de 5 - 10 miembros, arilo C₆₋₁₀, o heteroarilo de 5 - 10 miembros, en donde cada alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, heterociclilo de 5 - 10 miembros, arilo C₆₋₁₀, y heteroarilo de 5 - 10 miembros está opcionalmente sustituido con 1, 2, 3, 4, ó 5 grupos R¹³, que pueden ser los mismos o diferentes; o Rᵃ y Rᵇ junto con los átomos a los que están unidos forman un heterociclo de 5 - 10 miembros; y cada R¹³ es independientemente -CN, halógeno, alquilo C₁₋₆, cicloalquilo C₃₋₁₀, heteroalquilo C₁₋₆, o heterociclilo de 5 - 10 miembros; o un tautómero o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462096748P | 2014-12-24 | 2014-12-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103252A1 true AR103252A1 (es) | 2017-04-26 |
Family
ID=55305044
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150104262A AR103252A1 (es) | 2014-12-24 | 2015-12-22 | Compuestos de quinazolina |
Country Status (41)
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2729448E (pt) | 2011-07-06 | 2015-12-02 | Gilead Sciences Inc | Compostos para o tratamento de vih |
| KR101960624B1 (ko) | 2014-12-24 | 2019-03-20 | 길리애드 사이언시즈, 인코포레이티드 | Hiv의 치료를 위한 이소퀴놀린 화합물 |
| WO2016105532A1 (en) | 2014-12-24 | 2016-06-30 | Gilead Sciences, Inc. | Fused pyrimidine compounds for the treatment of hiv |
| TW202237569A (zh) | 2014-12-24 | 2022-10-01 | 美商基利科學股份有限公司 | 喹唑啉化合物 |
| KR20170123308A (ko) | 2014-12-26 | 2017-11-07 | 에모리 유니버시티 | Ｎ4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도 |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| PL3347352T3 (pl) | 2016-08-19 | 2019-12-31 | Gilead Sciences, Inc. | Związki terapeutyczne użyteczne do profilaktycznego lub terapeutycznego leczenia zakażenia wirusem HIV |
| AR112412A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas de sal de colina de un inhibidor de la cápside del vih |
| AR112413A1 (es) | 2017-08-17 | 2019-10-23 | Gilead Sciences Inc | Formas sólidas de un inhibidor de la cápside del vih |
| US11331331B2 (en) | 2017-12-07 | 2022-05-17 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| JP7083398B2 (ja) | 2018-02-15 | 2022-06-10 | ギリアード サイエンシーズ， インコーポレイテッド | ピリジン誘導体およびｈｉｖ感染を処置するためのその使用 |
| CA3175557A1 (en) | 2018-02-16 | 2019-08-22 | Gilead Sciences, Inc. | Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection |
| EP3823621A1 (en) | 2018-07-16 | 2021-05-26 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of hiv |
| TW202104210A (zh) | 2019-04-17 | 2021-02-01 | 美商基利科學股份有限公司 | Hiv蛋白酶抑制劑 |
| WO2020214647A1 (en) | 2019-04-17 | 2020-10-22 | Gilead Sciences, Inc. | Solid forms of an hiv protease inhibitor |
| AU2020391466B2 (en) | 2019-11-26 | 2024-05-23 | Gilead Sciences, Inc. | Capsid inhibitors for the prevention of HIV |
| CA3169348A1 (en) | 2020-03-20 | 2021-09-23 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
| WO2021215537A1 (ja) | 2020-04-24 | 2021-10-28 | 大日本住友製薬株式会社 | ２－ヘテロアリールアミノキナゾリノン誘導体 |
| EP4172157A1 (en) | 2020-06-25 | 2023-05-03 | Gilead Sciences, Inc. | Capsid inhibitors for the treatment of hiv |
| US20220144923A1 (en) | 2020-11-11 | 2022-05-12 | Gilead Sciences, Inc. | METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES |
| CA3237155A1 (en) | 2021-12-03 | 2023-06-08 | Zhimin Du | Therapeutic compounds for hiv virus infection |
| WO2023102239A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| WO2023102523A1 (en) | 2021-12-03 | 2023-06-08 | Gilead Sciences, Inc. | Therapeutic compounds for hiv virus infection |
| TW202400172A (zh) | 2022-04-06 | 2024-01-01 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| TW202402280A (zh) | 2022-07-01 | 2024-01-16 | 美商基利科學股份有限公司 | 可用於ｈｉｖ病毒感染之疾病預防性或治療性治療的治療性化合物 |
| WO2024044477A1 (en) | 2022-08-26 | 2024-02-29 | Gilead Sciences, Inc. | Dosing and scheduling regimen for broadly neutralizing antibodies |
| WO2024076915A1 (en) | 2022-10-04 | 2024-04-11 | Gilead Sciences, Inc. | 4'-thionucleoside analogues and their pharmaceutical use |
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