AR111594A1 - Agentes inhibidores de la tirosina quinasa de bruton - Google Patents
Agentes inhibidores de la tirosina quinasa de brutonInfo
- Publication number
- AR111594A1 AR111594A1 ARP180100935A ARP180100935A AR111594A1 AR 111594 A1 AR111594 A1 AR 111594A1 AR P180100935 A ARP180100935 A AR P180100935A AR P180100935 A ARP180100935 A AR P180100935A AR 111594 A1 AR111594 A1 AR 111594A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- membered monocyclic
- alkynyl
- alkenyl
- carbocyclyl
- Prior art date
Links
- 230000002401 inhibitory effect Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 22
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 11
- 125000005843 halogen group Chemical group 0.000 abstract 7
- -1 2 - ((1-methyl-1 H -pyrazol-4-yl) amino) pyrimidin-4-yl Chemical group 0.000 abstract 4
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000006299 oxetan-3-yl group Chemical group [H]C1([H])OC([H])([H])C1([H])* 0.000 abstract 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
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- 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
- C07D401/14—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 three or more hetero rings
-
- 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
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- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
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- 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
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- 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
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable, en donde: el anillo A es un heteroarilo monocíclico de 5 miembros que contiene 3 heteroátomos seleccionados independientemente entre N, O y S, en donde dicho heteroarilo monocíclico de 5 miembros está opcionalmente sustituido con uno o más R¹; Q¹, Q² y Q³ son cada uno, independientemente, seleccionados de O, N(R²) y CH-R³, en donde al menos dos de Q¹, Q² y Q³ son C-R³; W se selecciona de CH y N; Y se selecciona de CH y N; R¹ en cada caso se selecciona independientemente de alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros, en donde dicho alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros están opcionalmente sustituidos con uno o más R¹⁰; R¹⁰ en cada caso se selecciona independientemente de halo, -CN, alquilo C₁₋₆ y carbociclilo de 3 a 5 miembros; R² se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, -CN, -C(O)R²ᵃ, -C(O)₂R²ᵃ, -C(O)N(R²ᵃ)₂, -S(O)₂R²ᵃ, y -S(O)₂N(R²ᵃ)₂, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros están opcionalmente sustituidos con uno o más R²⁰; R²ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros en cada aparición están opcionalmente e independientemente sustituidos con uno o más R²⁰; R²⁰ en cada aparición se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R²⁰ᵃ, -C(O)₂R²⁰ᵃ, -C(O)N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)C(O)R²⁰ᵃ, -N(R²⁰ᵃ)C(O)₂R²⁰ᵃ, -N(R²⁰ᵃ)C(O)N(R²⁰ᵃ)₂, -N(R²⁰ᵃ)S(O)₂R²⁰ᵃ, -OR²⁰ᵃ, -OC(O)R²⁰ᵃ, -OC(O)N(R²⁰ᵃ)₂, -SR²⁰ᵃ, -S(O)R²⁰ᵃ, -S(O)₂R²⁰ᵃ, -S(O)N(R²⁰ᵃ)₂, y -S(O)₂N(R²⁰ᵃ)₂; R²⁰ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros; R³ se selecciona de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R³ᵃ, -C(O)₂R³ᵃ, -C(O)N(R³ᵃ)₂, -N(R³ᵃ)₂, -N(R³ᵃ)C(O)R³ᵃ, -N(R³ᵃ)C(O)₂R³ᵃ, -N(R³ᵃ)C(O)N(R³ᵃ)₂, -N(R³ᵃ)S(O)₂R³ᵃ, -OR³ᵃ, -OC(O)R³ᵃ, -OC(O)N(R³ᵃ)₂, -SR³ᵃ, -S(O)R³ᵃ, -S(O)₂R³ᵃ, -S(O)N(R³ᵃ)₂, y -S(O)₂N(R³ᵃ)₂, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros están opcionalmente sustituidos con uno o más R³⁰; R³ᵃ en cada aparición se selecciona independientemente de H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros, y heterociclilo monocíclico de 4 a 6 miembros, en donde dicho alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros en cada aparición están opcional e independientemente sustituidos con uno o más R³⁰; R³⁰ en cada aparición se selecciona independientemente de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico de 4 a 6 miembros heterociclilo monocíclico de 4 a 6 miembros, halo, -CN, -C(O)R³⁰ᵃ, -C(O)₂R³⁰ᵃ, -C(O)N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)C(O)R³⁰ᵃ, -N(R³⁰ᵃ)C(O)₂R³⁰ᵃ, -N(R³⁰ᵃ)C(O)N(R³⁰ᵃ)₂, -N(R³⁰ᵃ)S(O)₂R³⁰ᵃ, -OR³⁰ᵃ, -OC(O)R³⁰ᵃ, -OC(O)N(R³⁰ᵃ)₂, -SR³⁰ᵃ, -S(O)R³⁰ᵃ, -S(O)₂R³⁰ᵃ, -S(O)N(R³⁰ᵃ)₂, y -S(O)₂N(R³⁰ᵃ)₂; R³⁰ᵃ en cada aparición se selecciona independientemente de; H, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, carbociclilo monocíclico do 4 a 6 miembros y heterociclilo monocíclico de 4 a 6 miembros; R⁴ se selecciona de H y alquilo C₁₋₆, en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; R⁵ se selecciona de H y alquilo C₁₋₆ en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; R⁶ se selecciona de H y alquilo C₁₋₆, en donde dicho alquilo C₁₋₆ está opcionalmente sustituido con uno o más halo; o R⁵ y R⁶, junto con los átomos a los que están unidos, forman un anillo que contiene uno o dos heteroátomos seleccionados de O, N y S, en donde el anillo está opcionalmente sustituido con uno o mas R⁵⁰; y R⁵⁰ es alquilo C₁₋₆. Reivindicación 38: La forma A cristalina de (R)-1-(terc-butil)-N-(8-(2-((1-metil-1H-pirazol-4-il)amino)pirimidin-4-il)-2-(oxetan-3-il)-2,3,4,5-tetrahidro-1H-benzo[c]azepin-5-il)-1H-1,2,3-triazol-4-carboxamida. Reivindicación 48: La forma G cristalina de (R)-1-(terc-butil)-N-(8-(2-((1-metil-1H-pirazol-4-il)amino)pirimidin-4-il)-2-(oxetan-3-il)-2,3,4,5-tetrahidro-1H-benzo[c]azepin-5-il)-1H-1,2,3-triazol-4-carboxamida.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762485745P | 2017-04-14 | 2017-04-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR111594A1 true AR111594A1 (es) | 2019-07-31 |
Family
ID=62092333
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180100935A AR111594A1 (es) | 2017-04-14 | 2018-04-13 | Agentes inhibidores de la tirosina quinasa de bruton |
Country Status (30)
| Country | Link |
|---|---|
| US (5) | US10227341B2 (es) |
| EP (2) | EP3609886B1 (es) |
| JP (2) | JP7145874B2 (es) |
| KR (2) | KR102607900B1 (es) |
| CN (2) | CN110621670B (es) |
| AR (1) | AR111594A1 (es) |
| AU (2) | AU2018253209B2 (es) |
| BR (1) | BR112019021399A2 (es) |
| CA (1) | CA3058774A1 (es) |
| CL (1) | CL2019002900A1 (es) |
| CO (1) | CO2019012571A2 (es) |
| CR (1) | CR20190517A (es) |
| DK (1) | DK3609886T3 (es) |
| EA (1) | EA201992354A1 (es) |
| FI (1) | FI3609886T3 (es) |
| IL (2) | IL269933B (es) |
| JO (1) | JOP20190233A1 (es) |
| LT (1) | LT3609886T (es) |
| MA (1) | MA50013A (es) |
| MX (1) | MX2023000812A (es) |
| PE (2) | PE20200740A1 (es) |
| PH (1) | PH12019502334A1 (es) |
| PL (1) | PL3609886T3 (es) |
| PT (1) | PT3609886T (es) |
| RS (1) | RS65386B1 (es) |
| SA (1) | SA519410292B1 (es) |
| SG (1) | SG11201909224QA (es) |
| TW (2) | TW202315870A (es) |
| UA (1) | UA127347C2 (es) |
| WO (1) | WO2018191577A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI744672B (zh) | 2013-12-11 | 2021-11-01 | 美商百健Ｍａ公司 | 布魯頓氏(bruton's)酪胺酸激酶之聯芳基抑制劑 |
| JOP20190233A1 (ar) | 2017-04-14 | 2019-10-02 | Biogen Ma Inc | نظائر بنزوازيبين بوصفها عوامل مثبطة لتيروزين كيناز بروتون |
| US11820760B2 (en) | 2018-10-15 | 2023-11-21 | Biogen Ma Inc. | Crystalline polymorphs of Bruton's tyrosine kinase inhibitors |
| CN117146007A (zh) | 2018-10-22 | 2023-12-01 | 株式会社村田制作所 | 阀以及气体控制装置 |
| US20220259194A1 (en) * | 2019-05-15 | 2022-08-18 | Biogen Ma Inc. | Inhibiting agents for bruton's tyrosine kinase |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| EP4313023A1 (en) | 2021-04-02 | 2024-02-07 | Biogen MA Inc. | Combination treatment methods of multiple sclerosis |
| WO2023086521A1 (en) | 2021-11-10 | 2023-05-19 | Biogen Ma Inc. | Btk inhibitors |
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| CN101730699A (zh) | 2007-03-21 | 2010-06-09 | 百时美施贵宝公司 | 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物 |
| RU2681081C2 (ru) | 2007-10-05 | 2019-03-04 | Верастэм, Инк. | Пиримидинзамещенные производные пурина, фармацевтическая композиция на их основе, способ ингибирования протеинкиназ, способ лечения или профилактики заболеваний, чувствительных к ингибированию протеинкиназ, и способ лечения пролиферативных заболеваний |
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| TWI744672B (zh) * | 2013-12-11 | 2021-11-01 | 美商百健Ｍａ公司 | 布魯頓氏(bruton's)酪胺酸激酶之聯芳基抑制劑 |
| CA2960401C (en) * | 2014-10-06 | 2022-07-26 | Merck Patent Gmbh | Heteroaryl compounds as btk inhibitors and uses thereof |
| JOP20190233A1 (ar) | 2017-04-14 | 2019-10-02 | Biogen Ma Inc | نظائر بنزوازيبين بوصفها عوامل مثبطة لتيروزين كيناز بروتون |
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