AR103566A1 - COMPOUNDS DERIVED FROM CONDENSED HETEROARILO AND HETEROCICLO - Google Patents
COMPOUNDS DERIVED FROM CONDENSED HETEROARILO AND HETEROCICLOInfo
- Publication number
- AR103566A1 AR103566A1 ARP160100258A ARP160100258A AR103566A1 AR 103566 A1 AR103566 A1 AR 103566A1 AR P160100258 A ARP160100258 A AR P160100258A AR P160100258 A ARP160100258 A AR P160100258A AR 103566 A1 AR103566 A1 AR 103566A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- halo
- independently selected
- alkoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente solicitud se refiere a compuestos de heteroarilo y heterociclo condensados, composiciones farmacéuticas que los comprenden, usos de los mismos y métodos para inhibir la actividad de PI₃K para tratar enfermedades inflamatorias, autoinmunes y cáncer. Reivindicación 1: Un compuesto de fórmula (1), o sus solvatos, mezcla racémica, enantiómeros, diastereómeros, tautómeros o sales farmacéuticamente aceptables de los mismos, en donde: Z¹ y Z³ son independientemente N o CH; siempre que Z¹ y Z³ no sean N simultáneamente; Z² y Z⁴ son independientemente N o C, en el cual al menos uno de Z² y Z⁴ es N; R¹ está seleccionado a partir de halo, -CN, C₃₋₆ cicloalquilo, vinilo, etinilo, fenilo, y C₁₋₆ alquilo, en donde el C₁₋₆ alquilo está opcionalmente sustituido con uno o más grupos independientemente seleccionados a partir de halo, OH y C₁₋₆ alcoxilo; R² es C₁₋₆ alquilo opcionalmente sustituido con uno o más grupos independientemente seleccionado a partir de C₃₋₆ cicloalquilo, fenilo y heteroarilo de 5 - 7 miembros; o R² está seleccionado a partir de fenilo, C₃₋₆ cicloalquilo, heterociclo de 4 - 8 miembros, y heteroarilo de 5 - 10 miembros, cada uno de los cuales esta opcionalmente sustituido con uno o más grupos independientemente seleccionados a partir de halo, -CN, C₁₋₆ alquilo, -SRᵃ, -S(O)ₙRᵇ y C₁₋₆ alcoxilo, en donde el C₁₋₆ alquilo y el C₁₋₆ alcoxilo están cada uno opcionalmente sustituidos con uno o más halo; R³ y R⁴ están cada uno independientemente seleccionados a partir de H, C₁₋₆ alcoxilo y C₁₋₄ alquilo, en donde el C₁₋₄ alquilo está opcionalmente sustituido con uno o más -OH; R⁵ es H o un C₁₋₄ alquilo; o R³, R⁵ y los átomos a los cuales están unidos forman un anillo heterocíclico saturado o parcialmente insaturado, mono o bicíclico, de 4 - 6 miembros, que opcionalmente contiene unos 1 - 2 heteroátomos adicionales seleccionados a partir de N, O y S, que están opcionalmente sustituidos con uno o más grupos independientemente seleccionados a partir de halo y C₁₋₆ alquilo, en donde el C₁₋₆ alquilo está opcionalmente sustituido con uno o más halo; Rᵃ y Rᵇ son cada uno independientemente H o un C₁₋₆ alquilo; m es 0 1 ó 2; n es 1 ó 2; W es un resto de fórmula (2) en donde: X¹ es C(O), X² es NR⁷, y X³ es NR⁸ o CHR⁹; X¹ es S(O) o S(O)₂, X² es CH₂ o NR¹⁰, y X³ es CH₂; o X¹ es C(O), X² es CH₂, y X³ es NH, S u O; o W es la fórmulas (3) o la fórmula (4) en donde R⁶ es H, -NH₂ o -NH(C₁₋₆ alquilo); y R⁷, R⁸, R⁹, y R¹⁰ están cada uno independientemente seleccionados a partir de H, C₁₋₆ alquilo, y C₃₋₆ cicloalquilo.The present application relates to condensed heteroaryl and heterocycle compounds, pharmaceutical compositions comprising them, uses thereof and methods to inhibit PI₃K activity to treat inflammatory, autoimmune and cancer diseases. Claim 1: A compound of formula (1), or its solvates, racemic mixture, enantiomers, diastereomers, tautomers or pharmaceutically acceptable salts thereof, wherein: Z¹ and Z³ are independently N or CH; provided that Z¹ and Z³ are not N simultaneously; Z² and Z⁴ are independently N or C, in which at least one of Z² and Z⁴ is N; R¹ is selected from halo, -CN, C₃₋₆ cycloalkyl, vinyl, ethynyl, phenyl, and C₁₋₆ alkyl, wherein the C₁₋₆ alkyl is optionally substituted with one or more groups independently selected from halo, OH and C₁₋₆ alkoxy; R² is C₁₋₆ alkyl optionally substituted with one or more groups independently selected from C₃₋₆ 5-7 membered cycloalkyl, phenyl and heteroaryl; or R² is selected from phenyl, C₃₋₆ cycloalkyl, 4-8 membered heterocycle, and 5-10 membered heteroaryl, each of which is optionally substituted with one or more groups independently selected from halo, - CN, C₁₋₆ alkyl, -SRᵃ, -S (O) ₙRᵇ and C₁₋₆ alkoxy, wherein the C₁₋₆ alkyl and the C₁₋₆ alkoxy are each optionally substituted with one or more halo; R³ and R⁴ are each independently selected from H, C₁₋₆ alkoxy and C₁₋₄ alkyl, wherein the C₁₋₄ alkyl is optionally substituted with one or more -OH; R⁵ is H or a C₁₋₄ alkyl; or R³, R⁵ and the atoms to which they are attached form a saturated or partially unsaturated, mono or bicyclic, 4-6 membered heterocyclic ring, which optionally contains about 1-2 additional heteroatoms selected from N, O and S, which are optionally substituted with one or more groups independently selected from halo and C₁₋₆ alkyl, wherein the C₁₋₆ alkyl is optionally substituted with one or more halo; Rᵃ and Rᵇ are each independently H or a C₁₋₆ alkyl; m is 0 1 or 2; n is 1 or 2; W is a remainder of formula (2) where: X¹ is C (O), X² is NR⁷, and X³ is NR⁸ or CHR⁹; X¹ is S (O) or S (O) ₂, X² is CH₂ or NR¹⁰, and X³ is CH₂; or X¹ is C (O), X² is CH₂, and X³ is NH, S or O; or W is the formulas (3) or the formula (4) wherein R⁶ is H, -NH₂ or -NH (C₁₋₆ alkyl); and R⁷, R⁸, R⁹, and R¹⁰ are each independently selected from H, C₁₋₆ alkyl, and C₃₋₆ cycloalkyl.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562109471P | 2015-01-29 | 2015-01-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103566A1 true AR103566A1 (en) | 2017-05-17 |
Family
ID=56542439
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160100258A AR103566A1 (en) | 2015-01-29 | 2016-01-29 | COMPOUNDS DERIVED FROM CONDENSED HETEROARILO AND HETEROCICLO |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR103566A1 (en) |
| TW (1) | TW201639845A (en) |
| WO (1) | WO2016119707A1 (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3419978T3 (en) | 2016-02-24 | 2020-06-02 | Pfizer | Pyrazolo [1,5-A] pyrazin-4-yl derivatives as JAK inhibitors |
| JP7071389B2 (en) * | 2017-03-07 | 2022-05-18 | グアンジョウ マキシノベル ファーマシューティカルズ カンパニー リミテッド | Aminopyrimidine Condensation 5-membered heterocyclic compound, its intermediate, manufacturing method, drug composition and use |
| WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | Pfizer Inc. | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
| CN109422730B (en) * | 2017-08-27 | 2020-04-21 | 中南民族大学 | Non-natural amino acid derivatives containing azetidine skeleton and synthetic method thereof |
| WO2022266015A1 (en) * | 2021-06-14 | 2022-12-22 | Kumquat Biosciences Inc. | Fused heteroaryl compounds useful as anticancer agents |
| WO2023104165A1 (en) * | 2021-12-08 | 2023-06-15 | 上海维申医药有限公司 | Pyridine[4,3-d]pyrimidine compound as tlr7/8 agonist |
| WO2024055879A1 (en) * | 2022-09-16 | 2024-03-21 | 四川科伦博泰生物医药股份有限公司 | Class of fused bicyclic compounds, method for preparing same, and use thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014015523A1 (en) * | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
-
2016
- 2016-01-28 TW TW105102649A patent/TW201639845A/en unknown
- 2016-01-28 WO PCT/CN2016/072474 patent/WO2016119707A1/en active Application Filing
- 2016-01-29 AR ARP160100258A patent/AR103566A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201639845A (en) | 2016-11-16 |
| WO2016119707A1 (en) | 2016-08-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR103566A1 (en) | COMPOUNDS DERIVED FROM CONDENSED HETEROARILO AND HETEROCICLO | |
| AR087760A1 (en) | HETEROCICLILAMINAS AS PI3K INHIBITORS | |
| AR121879A2 (en) | INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF SERINE/THREONINE KINASE INHIBITORS | |
| AR106595A1 (en) | HETEROCYCLIC COMPOUNDS AS PI3K-g INHIBITORS | |
| AR100438A1 (en) | PIRAZOLOPIRIDINAS AND PIRAZOLOPIRIMIDINAS | |
| AR120338A1 (en) | PYRIDAZINONES AS PARP7 INHIBITORS | |
| AR105845A1 (en) | BICYCLIC HETEROARIL COMPOUNDS FUSED AS MODULATORS OF THE IRAK4 FUNCTION | |
| AR086817A1 (en) | INHIBITING COMPOUNDS OF PHOSPHODESTERASE TYPE 10A | |
| AR108388A2 (en) | OXAZOL COMPOUNDS REPLACED WITH INDAZOL AS INHIBITORS OF PI3-KINASES | |
| AR100033A1 (en) | COMPOUNDS AND COMPOSITIONS TO INHIBIT THE ACTIVITY OF SHP2 | |
| AR096979A1 (en) | DERIVATIVES OF PIRROL, ITS PREPARATION PROCEDURE AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | |
| AR094346A1 (en) | DERIVATIVES OF AZAINDOL AS INHIBITORS OF PROTEIN KINASES | |
| AR103833A1 (en) | BICYCLIC COMPOUNDS OF SULFONAMIDE KETONE | |
| AR099228A1 (en) | FXIA MACROCYCLIC INHIBITORS THAT HAVE HETEROCYCLIC GROUPS | |
| AR112834A1 (en) | RAPAMYCIN DERIVATIVES | |
| AR106865A1 (en) | PIRIDINES REPLACED AND METHODS OF USE | |
| AR107042A1 (en) | INHIBITORS OF BRUTON TYROSINE KINASE AND METHODS OF USE | |
| AR090548A1 (en) | BICYCLIC AZAHETEROCICLOBENCILAMINS AS PI3K INHIBITORS | |
| AR107032A1 (en) | PAD4 BICYCLIC INHIBITORS | |
| AR088748A1 (en) | MACROCICLES AS INHIBITORS OF THE XIA FACTOR | |
| RS54358B1 (en) | Pyrrolopyridines as kinase inhibitors | |
| AR090293A1 (en) | ARILETER-BASED KINASE INHIBITORS | |
| AR091654A1 (en) | COMPOUNDS CONTAINING BIARILO AS INVESTED AGONISTS OF ROR-g RECEIVERS | |
| AR096846A1 (en) | DIHYDROCHINOXALINONES AND MODIFIED DIHYDROPIRIDOPIRAZINONES AS INHIBITORS OF BET PROTEIN | |
| AR062011A1 (en) | DERIVATIVES OF DIAZOL AND ITS COMPOSITIONS AS ITPKB INHIBITORS |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |