AR101106A1 - Inhibidores de tirosina quinasa de bruton - Google Patents
Inhibidores de tirosina quinasa de brutonInfo
- Publication number
- AR101106A1 AR101106A1 ARP150102136A ARP150102136A AR101106A1 AR 101106 A1 AR101106 A1 AR 101106A1 AR P150102136 A ARP150102136 A AR P150102136A AR P150102136 A ARP150102136 A AR P150102136A AR 101106 A1 AR101106 A1 AR 101106A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- cycloalkyl
- pr10a
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000002947 alkylene group Chemical group 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 229940124291 BTK inhibitor Drugs 0.000 abstract 3
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 3
- -1 nitro, oxo, thioxo Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 abstract 2
- 125000004450 alkenylene group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 abstract 1
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 abstract 1
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010025323 Lymphomas Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical group C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- CBOIHMRHGLHBPB-UHFFFAOYSA-N hydroxymethyl Chemical compound O[CH2] CBOIHMRHGLHBPB-UHFFFAOYSA-N 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002427 irreversible effect Effects 0.000 abstract 1
- 230000000155 isotopic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 230000002441 reversible effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- 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
-
- 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
- C07D471/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
En la presente se describen compuestos que inhiben la tirosina quinasa de Bruton (Btk). Se describen, además, inhibidores irreversibles de Btk. Adicionalmente, se describen los inhibidores reversibles de Btk. Se describen, además, composiciones farmacéuticas que incluyen los compuestos. Los métodos de uso de los inhibidores de Btk se describen, solos o en combinación con otros agentes terapéuticos, para el tratamiento de enfermedades o afecciones autoinmunes, enfermedades o afecciones heteroinmunes, cáncer, que incluye linfoma, y enfermedades y afecciones inflamatorias. Reivindicación 2: Un compuesto de la fórmula [1] caracterizado porque tiene la estructura de fórmula [1]; o un solvato, sal farmacéuticamente aceptable, o profármaco de este; o un estereoisómero o una variante isotópica de este; en donde: uno de W¹ y W² es =C(R⁹)-, o =N-; y el otro es =C(R⁹)-; Z es =C(R⁹), o =N-; L¹ es -N(R⁵)-, -O-, -S-, un enlace simple, -CH₂-, o -NH-CH₂-; T¹ es -O-, -S-, -N(R⁵)-, un enlace simple, o alquileno de C₁₋₃; Cy¹ es arilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; Cy² es heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; R¹ es -C(O)-R¹ᵃ, H, halo, alquilo, OH, alcoxialquilo, hidroxialquilo, haloalquilo, ciano, -O-R¹ᵃ, -C(S)-R¹ᵃ, -C(O)-O-R¹ᵇ, -C(O)-C(O)-N(R¹ᶜ)R¹ᵈ, -N(R¹ᶜ)-O(O)R¹ᵈ, -C(O)-N(R¹ᶜ)R¹ᵈ, -S(O)ₚ-R¹ᵃ, o -S(O)ₚ-N(R¹ᶜ)R¹ᵈ; R¹⁰ es -R¹⁰ᵇ-C(O)R¹⁰ᵃ, halo, nitro, oxo, tioxo, -R¹⁰ᵇ-R¹⁰ᶜ, alcoxialquilo, hidroxialquilo, haloalquilo, ciano, -R¹⁰ᵇ-OR¹⁰ᵃ, -R¹⁰ᵇ-OC(O)R¹⁰ᵃ, -R¹⁰ᵇ-SR¹⁰ᵃ, -R¹⁰ᵇ-C(S)R¹⁰ᵃ, -R¹⁰ᵇ-C(O)OR¹⁰ᵃ, -R¹⁰ᵇ-C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-O-R¹⁰ᵉ-C(O)N(R¹⁰ᵃ)₂, -R¹⁰ᵇ-OCH₂R¹⁰ᵃ, -R¹⁰ᵇ-SCH₂R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)R¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)OR¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵈ)S(O)ₚR¹⁰ᵃ; -S(O)ₚR¹⁰ᵃ, -R¹⁰ᵇ-S(O)ₚOR¹⁰ᵃ, o -R¹⁰ᵇ-S(O)ₚN(R¹⁰ᵃ)R¹⁰ᵃ; p es 1 ó 2; cada uno de R¹ᵃ, R¹ᵇ, R¹ᶜ, R¹ᵈ, y R¹⁰ᵃ es independientemente H, ciano, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; R¹⁰ᵇ es un enlace simple o una cadena de alquenileno o alquileno lineal o ramificada; R¹⁰ᶜ es alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; R¹⁰ᵈ es alquilo C₁₋₆ H, sustituido o no sustituido, o cicloalquilo C₃₋₈ sustituido o no sustituido; R¹⁰ᵉ es una cadena de alquenileno o alquileno lineal o ramificada; cada uno de R⁵ es independientemente H, -C(O)-R⁵ᵃ, alquilo C₁₋₆, o heteroalquilo C₁₋₆; o cuando cada uno de L¹ y T¹ es independientemente -N(R⁵)-, entonces los dos R⁵s pueden unirse para formar un heterociclo sustituido o no sustituido; R⁵ᵃ es alquilo C₁₋₄ sustituido o no sustituido, alquenilo de C₂₋₄ sustituido o no sustituido, o alquinilo de C₂₋₄ sustituido o no sustituido; y cada R⁹ es independientemente H, halógeno, -CN, -OH, -NH₂, -SH, alquilo C₁₋₆ sustituido o no sustituido, alcoxi C₁₋₄ sustituido o no sustituido, heteroalquilo C₁₋₆ sustituido o no sustituido, fenilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, o cicloalquilo C₃₋₈ sustituido o no sustituido siempre que: (1) cuando L¹ es un enlace simple, entonces Cy² es heterocicloalquilo sustituido o no sustituido completamente saturado, R¹ es ciano, -C(O)-R¹ᵃ o -N(R¹ᶜ)-C(O)R¹ᵈ, y T¹ es alquileno de C₁₋₃, -O-, o -S; y (2) cuando L¹ es -NH-CH₂-, entonces Cy² es heterocicloalquilo sustituido o no sustituido completamente saturado y R¹ es C(O)-R¹ᵃ, C(S)-R¹ᵃ, C(O)-O-R¹ᵇ, C(O)-N(R¹ᶜ)R¹ᵈ, S(O)ₚR¹ᵃ, o S(O)ₚ-N(R¹ᶜ)R¹ᵈ; (3) cuando L¹ es CH₂-, entonces R¹ es distinto de H; (4) cuando T¹ es un enlace sencillo, entonces R¹⁰ es -R¹⁰ᵇ-C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-O-R¹⁰ᵉ-C(O)N(R¹⁰ᵃ)₂, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)R¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)OR¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵈ)S(O)ₚR¹⁰ᵃ, -S(O)ₚR¹⁰ᵃ, -R¹⁰ᵇ-S(O)ₚOR¹⁰ᵃ, o -R¹⁰ᵇ-S(O)ₚN(R¹⁰ᵃ)R¹⁰ᵃ; (5) cuando T¹ es un -CH₂-CH₂-, y L¹ y O, entonces Cy² es diferente que tetrahidropiran sustituido con tres o más sustituyentes independientemente seleccionados de OH, CH₂OH, OC(O)-t-Bu y CH₂OC(O)-t-Bu; (6) cuando W¹ es =N-, L¹ y T¹ son ambos -N(R⁵)-, Cy¹ y Cy² son ambos fenilo, y R¹ es H, halo, alquilo, OH, alcoxialquilo, hidroxialquilo, haloalquilo o ciano, entonces R¹⁰ es -R¹⁰ᵇ-R¹⁰ᶜ, -R¹⁰ᵇ-OR¹⁰ᵃ, -R¹⁰ᵇ-OC(O)R¹⁰ᵃ, -R¹⁰ᵇ-SR¹⁰ᵃ, R¹⁰ᵇ-C(O)R¹⁰ᵃ, -R¹⁰ᵇ-C(S)R¹⁰ᵃ, -R¹⁰ᵇ-C(O)OR¹⁰ᵃ, -R¹⁰ᵇ-C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-O-R¹⁰ᵉ-C(O)N(R¹⁰ᵃ)₂, -R¹⁰ᵇ-OCH₂R¹⁰ᵃ, -R¹⁰ᵇ-SCH₂R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)R¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)OR¹⁰ᶜ, -R¹⁰ᵇ-N(R¹⁰ᵈ)C(O)N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ-N(R¹⁰ᵃ)R¹⁰ᵃ, -R¹⁰ᵇ N(R¹⁰ᵈ)S(O)ₚR¹⁰ᵃ, -S(O)ₚR¹⁰ᵃ, -R¹⁰ᵇ-S(O)ₚOR¹⁰ᵃ, o -R¹⁰ᵇ-S(O)ₚN(R¹⁰ᵃ)R¹⁰ᵃ, y en donde al menos uno de R¹⁰ᵃ y R¹⁰ᶜ es alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, heterocicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; (7) cuando W¹ es =N-, entonces -Cy¹-R¹⁰ juntos son diferentes que 3-Cl-fenilo no sustituido; (8) -Cy¹-R¹⁰ juntos son diferentes que 2-F-fenilo sustituido o no sustituido; y (9) cuando Cy¹ es cicloalquilo sustituido o no sustituido, entonces T¹ es alquileno C₁₋₃, -N(R⁵)-, -O-, o -S-, y R¹⁰ es -C(O)R¹⁰ᵃ o -C(O)NHR¹⁰ᵃ.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462019961P | 2014-07-02 | 2014-07-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR101106A1 true AR101106A1 (es) | 2016-11-23 |
Family
ID=55016546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150102136A AR101106A1 (es) | 2014-07-02 | 2015-07-02 | Inhibidores de tirosina quinasa de bruton |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9580416B2 (es) |
| AR (1) | AR101106A1 (es) |
| TW (1) | TW201613919A (es) |
| WO (2) | WO2016004305A2 (es) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2939286A1 (en) * | 2016-08-17 | 2018-02-17 | Pharmascience Inc. | Spirocyclic containing compounds and pharmaceutical uses thereof |
| JP2019530650A (ja) * | 2016-08-24 | 2019-10-24 | アークル インコーポレイテッド | アミノ−ピロロピリミジノン化合物およびその使用方法 |
| NZ750781A (en) * | 2016-09-09 | 2025-06-27 | Novartis Ag | Compounds and compositions as inhibitors of endosomal toll-like receptors |
| GB201616627D0 (en) | 2016-09-30 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| EP3556761B1 (en) * | 2017-02-08 | 2021-03-03 | The National Institutes Of Pharmaceutical Research | Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof |
| US11427578B1 (en) | 2017-07-18 | 2022-08-30 | Bayer Pharma Aktiengesellschaft | Substituted pyrrolopyridine-derivatives |
| CN115819359B (zh) * | 2018-05-03 | 2025-04-18 | 江苏裕事达新材料科技有限责任公司 | 一种防蓝光化合物、制备方法及其组合物 |
| CN112533923B (zh) | 2018-06-04 | 2024-07-09 | 爱克思科技有限公司 | 作为腺苷受体拮抗剂的吡唑并嘧啶化合物 |
| IL259810A (en) | 2018-06-04 | 2018-07-31 | Yeda Res & Dev | Mitogen-activated protein kinase kinase 7 inhibitors |
| UY38349A (es) | 2018-08-30 | 2020-03-31 | Array Biopharma Inc | Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met |
| AU2019372046B2 (en) | 2018-10-31 | 2022-05-26 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as HPK1 inhibitors |
| EP3873608A1 (en) | 2018-10-31 | 2021-09-08 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
| US20220047603A1 (en) | 2018-12-11 | 2022-02-17 | Bayer Aktiengesellschaft | Substituted pyrrolopyridine-derivatives |
| CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药（上海）有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
| WO2020237025A1 (en) | 2019-05-23 | 2020-11-26 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| SG11202110085TA (en) * | 2019-05-31 | 2021-10-28 | Sichuan Haisco Pharmaceutical Co Ltd | Btk inhibitor ring derivative, preparation method therefor and pharmaceutical application thereof |
| CN111116593B (zh) * | 2019-11-27 | 2020-11-24 | 河北合佳医药科技集团股份有限公司 | 一种连续的伊鲁替尼的制备方法 |
| TW202140478A (zh) * | 2020-03-11 | 2021-11-01 | 英屬開曼群島商百濟神州有限公司 | 藉由軛合btk抑制劑與e3連接酶配位基降解布魯頓氏酪胺酸激酶（btk）及其使用方法 |
| WO2021249913A1 (en) | 2020-06-09 | 2021-12-16 | Bayer Aktiengesellschaft | 2'-(quinolin-3-yl)-5',6'-dihydrospiro[azetidine-3,4'-pyrrolo[1,2-b]pyrazole]-1-carboxylate derivatives and related compounds as map4k1 (hpk1) inhibitors for the treatment of cancer |
| US20240174683A1 (en) | 2021-02-05 | 2024-05-30 | Bayer Aktiengesellschaft | Map4k1 inhibitors |
| CN112574200B (zh) * | 2021-02-26 | 2021-06-11 | 安润医药科技（苏州）有限公司 | Btk和/或btk的突变体c481s的小分子抑制剂 |
| TW202415651A (zh) | 2022-07-29 | 2024-04-16 | 日商住友製藥股份有限公司 | 含氮飽和雜環衍生物 |
| TWI899933B (zh) | 2023-04-06 | 2025-10-01 | 美商輝瑞大藥廠 | 經取代吲唑丙酸衍生化合物及其用途 |
| CN118834163B (zh) * | 2024-06-26 | 2025-09-16 | 安徽大学 | 一种4-(叔丁基)-2-氯吡啶的合成方法 |
| WO2026013291A1 (en) * | 2024-07-11 | 2026-01-15 | University Of Dundee | Inhibitors of rna methyltransferase |
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| ATE195123T1 (de) * | 1995-04-03 | 2000-08-15 | Novartis Erfind Verwalt Gmbh | Pyrazolderivate und verfahren zu deren herstellung |
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2015
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- 2015-07-02 US US14/790,978 patent/US9580416B2/en active Active
- 2015-07-02 AR ARP150102136A patent/AR101106A1/es unknown
- 2015-07-02 WO PCT/US2015/038937 patent/WO2016004272A1/en not_active Ceased
- 2015-07-02 TW TW104121464A patent/TW201613919A/zh unknown
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| US9580416B2 (en) | 2017-02-28 |
| WO2016004305A2 (en) | 2016-01-07 |
| WO2016004305A3 (en) | 2016-03-03 |
| US20160002225A1 (en) | 2016-01-07 |
| TW201613919A (en) | 2016-04-16 |
| WO2016004272A1 (en) | 2016-01-07 |
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