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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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 (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012278976B2 (en) | 2011-07-06 | 2017-05-11 | Gilead Sciences, Inc. | Compounds for the treatment of HIV |
| TWI770552B (zh) | 2014-12-24 | 2022-07-11 | 美商基利科學股份有限公司 | 喹唑啉化合物 |
| EP3237414B1 (en) | 2014-12-24 | 2019-05-08 | Gilead Sciences, Inc. | Fused pyrimidine compounds for the tratment of hiv |
| SG11201705184PA (en) | 2014-12-24 | 2017-07-28 | Gilead Sciences Inc | Isoquinoline compounds for the treatment of hiv |
| US20190022116A1 (en) | 2014-12-26 | 2019-01-24 | Emory University | N4-Hydroxycytidine and Derivatives and Anti-Viral Uses Related Thereto |
| 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 |
| DK3706762T3 (da) | 2017-12-07 | 2024-12-16 | Univ Emory | N4-hydroxycytidin og derivater og antivirale anvendelser relateret dertil |
| US10836746B2 (en) | 2018-02-15 | 2020-11-17 | Gilead Sciences, Inc. | Therapeutic compounds |
| JP7038843B2 (ja) | 2018-02-16 | 2022-03-18 | ギリアード サイエンシーズ， インコーポレイテッド | Ｒｅｔｒｏｖｉｒｉｄａｅウイルス感染の処置において有用な治療用化合物を調製するための方法および中間体 |
| US20210353626A1 (en) * | 2018-04-20 | 2021-11-18 | The Regents Of The University Of California | Beta-adrenergic receptor allosteric modulators |
| KR20230141905A (ko) | 2018-07-16 | 2023-10-10 | 길리애드 사이언시즈, 인코포레이티드 | Hiv의 치료를 위한 캡시드 억제제 |
| CA3124569A1 (en) | 2018-12-28 | 2020-07-02 | Spv Therapeutics Inc. | Cyclin-dependent kinase inhibitors |
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| 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 |
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| CA3176531A1 (en) | 2020-04-24 | 2021-10-28 | Sumitomo Pharma Co., Ltd. | 2-heteroarylaminoquinazolinone derivative |
| CA3181690A1 (en) | 2020-06-25 | 2021-12-30 | Chienhung CHOU | 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 |
| US12084467B2 (en) | 2021-12-03 | 2024-09-10 | Gilead Sciences, Inc. | Therapeutic compounds for HIV virus infection |
| PL4445900T3 (pl) | 2021-12-03 | 2025-09-22 | Gilead Sciences, Inc. | Związki terapeutyczne przeciwko zakażeniu wirusem hiv |
| CN118369316A (zh) | 2021-12-03 | 2024-07-19 | 吉利德科学公司 | Hiv病毒感染的治疗性化合物 |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 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 |
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