JP2018516935A5 - - Google Patents
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- JP2018516935A5 JP2018516935A5 JP2017562758A JP2017562758A JP2018516935A5 JP 2018516935 A5 JP2018516935 A5 JP 2018516935A5 JP 2017562758 A JP2017562758 A JP 2017562758A JP 2017562758 A JP2017562758 A JP 2017562758A JP 2018516935 A5 JP2018516935 A5 JP 2018516935A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- lymphoma
- acceptable salt
- cell
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- -1 1- (but-2-ynoyl) piperidin-3-yl Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- ZMGMDXCADSRNCX-UHFFFAOYSA-N 5,6-dihydroxy-1,3-diazepan-2-one Chemical group OC1CNC(=O)NCC1O ZMGMDXCADSRNCX-UHFFFAOYSA-N 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 4
- 208000007465 Giant cell arteritis Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 206010043207 temporal arteritis Diseases 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 208000033808 peripheral neuropathy Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- KOEUOFPEZFUWRF-LJQANCHMSA-N 4-amino-3-(4-phenoxyphenyl)-1-[(3R)-1-prop-2-enoylpiperidin-3-yl]imidazo[4,5-c]pyridin-2-one Chemical compound C(C=C)(=O)N1C[C@@H](CCC1)N1C(N(C=2C(=NC=CC=21)N)C1=CC=C(C=C1)OC1=CC=CC=C1)=O KOEUOFPEZFUWRF-LJQANCHMSA-N 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 208000030939 Chronic inflammatory demyelinating polyneuropathy Diseases 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 206010018691 Granuloma Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 2
- 208000027625 autoimmune inner ear disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 201000005795 chronic inflammatory demyelinating polyneuritis Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 206010028417 myasthenia gravis Diseases 0.000 claims 2
- 201000001119 neuropathy Diseases 0.000 claims 2
- 230000007823 neuropathy Effects 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- FPGGLMIYNLQOID-UHFFFAOYSA-N 3h-pyridin-2-one Chemical compound O=C1CC=CC=N1 FPGGLMIYNLQOID-UHFFFAOYSA-N 0.000 claims 1
- YMALYAHRSSETHN-IBGZPJMESA-N 4-amino-3-(4-phenoxyphenyl)-1-[[(2S)-1-prop-2-enoylpyrrolidin-2-yl]methyl]imidazo[4,5-c]pyridin-2-one Chemical compound C(C=C)(=O)N1[C@@H](CCC1)CN1C(N(C=2C(=NC=CC=21)N)C1=CC=C(C=C1)OC1=CC=CC=C1)=O YMALYAHRSSETHN-IBGZPJMESA-N 0.000 claims 1
- 208000032116 Autoimmune Experimental Encephalomyelitis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000032568 B-cell prolymphocytic leukaemia Diseases 0.000 claims 1
- 208000023611 Burkitt leukaemia Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 208000019758 Hypergammaglobulinemia Diseases 0.000 claims 1
- 201000010743 Lambert-Eaton myasthenic syndrome Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000034800 Leukoencephalopathies Diseases 0.000 claims 1
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims 1
- 201000003791 MALT lymphoma Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000027530 Meniere disease Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000002033 Myoclonus Diseases 0.000 claims 1
- 201000009623 Myopathy Diseases 0.000 claims 1
- 206010029461 Nodal marginal zone B-cell lymphomas Diseases 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 206010048705 Paraneoplastic cerebellar degeneration Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000035416 Prolymphocytic B-Cell Leukemia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 1
- 208000001106 Takayasu Arteritis Diseases 0.000 claims 1
- 208000001435 Thromboembolism Diseases 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 1
- 206010071578 autoimmune retinopathy Diseases 0.000 claims 1
- 210000000467 autonomic pathway Anatomy 0.000 claims 1
- 230000003376 axonal effect Effects 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000003210 demyelinating effect Effects 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 230000002008 hemorrhagic effect Effects 0.000 claims 1
- 125000004476 heterocycloamino group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000002956 necrotizing effect Effects 0.000 claims 1
- 230000001272 neurogenic effect Effects 0.000 claims 1
- 230000002232 neuromuscular Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 210000001541 thymus gland Anatomy 0.000 claims 1
- 208000009174 transverse myelitis Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020001139A JP6985433B2 (ja) | 2015-06-03 | 2020-01-08 | チロシンキナーゼ阻害剤 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562170547P | 2015-06-03 | 2015-06-03 | |
| US62/170,547 | 2015-06-03 | ||
| US201562271689P | 2015-12-28 | 2015-12-28 | |
| US62/271,689 | 2015-12-28 | ||
| PCT/US2016/035588 WO2016196840A1 (en) | 2015-06-03 | 2016-06-02 | Tyrosine kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020001139A Division JP6985433B2 (ja) | 2015-06-03 | 2020-01-08 | チロシンキナーゼ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018516935A JP2018516935A (ja) | 2018-06-28 |
| JP2018516935A5 true JP2018516935A5 (enExample) | 2019-06-27 |
| JP6646072B2 JP6646072B2 (ja) | 2020-02-14 |
Family
ID=56118090
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017562758A Active JP6646072B2 (ja) | 2015-06-03 | 2016-06-02 | チロシンキナーゼ阻害剤 |
| JP2020001139A Active JP6985433B2 (ja) | 2015-06-03 | 2020-01-08 | チロシンキナーゼ阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020001139A Active JP6985433B2 (ja) | 2015-06-03 | 2020-01-08 | チロシンキナーゼ阻害剤 |
Country Status (33)
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20150044271A1 (en) | 2012-02-27 | 2015-02-12 | O-Ray Pharma, Inc. | Solid drug implants for intracochlear delivery of therapeutics for the treatment of otic disorders |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| WO2015080252A1 (ja) | 2013-11-29 | 2015-06-04 | 株式会社ダイゾー | 内容物収容容器、それを用いた内容物収容製品、吐出製品および吐出装置 |
| KR20220027271A (ko) | 2014-02-21 | 2022-03-07 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| CA2970723C (en) | 2014-12-18 | 2023-09-05 | Principia Biopharma Inc. | Treatment of pemphigus |
| KR20240070721A (ko) * | 2015-06-03 | 2024-05-21 | 프린시피아 바이오파마, 인코퍼레이티드 | 티로신 키나제 억제제 |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| CN105753863B (zh) * | 2015-09-11 | 2018-07-31 | 东莞市真兴贝特医药技术有限公司 | 氧代二氢咪唑并吡啶类化合物及其应用 |
| US10358446B2 (en) * | 2015-10-14 | 2019-07-23 | Zibo Biopolar Changsheng Pharmaceutical Co., Ltd. | Bruton's tyrosine kinase inhibitors |
| WO2018005849A1 (en) | 2016-06-29 | 2018-01-04 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| JP6920411B2 (ja) * | 2016-07-25 | 2021-08-18 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | コリンキナーゼ阻害剤としてのプリン及び3−デアザプリンアナログ |
| US10314844B2 (en) * | 2017-02-24 | 2019-06-11 | Gilead Sciences, Inc. | Inhibitors of Bruton's tyrosine kinase |
| EP3789040A4 (en) * | 2018-04-27 | 2022-03-09 | ONO Pharmaceutical Co., Ltd. | PREVENTIVE AND/OR THERAPEUTIC AGENT FOR AUTOIMMUNE DISEASES WITH A COMPOUND WITH BTK INHIBITING ACTIVITY AS AN INGREDIENT |
| BR112021000964A2 (pt) | 2018-07-25 | 2021-04-20 | Novartis Ag | inibidores do inflamassoma de nlrp3 |
| KR102653681B1 (ko) | 2018-07-31 | 2024-04-03 | 록쏘 온콜로지, 인코포레이티드 | (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제 |
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| AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
| TWI877239B (zh) | 2019-10-14 | 2025-03-21 | 美商普林斯匹亞生物製藥公司 | 藉由投予(R)-2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧呾-3-基)哌-1-基]戊-2-烯腈來治療免疫血小板減少症之方法 |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| CN113045484B (zh) * | 2019-12-27 | 2024-01-26 | 南京药石科技股份有限公司 | 一种2-氨基-2-(1-甲基-4-哌啶基)丙烷-1-醇的制备方法 |
| CN113149891B (zh) * | 2020-01-07 | 2024-02-02 | 南京药石科技股份有限公司 | 一种2-氨基-2-(1-甲基-4-哌啶基)乙醇的制备方法 |
| US11969418B2 (en) | 2020-01-20 | 2024-04-30 | Genzyme Corporation | Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (RMS) |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| BR112022014149A2 (pt) | 2020-01-22 | 2022-09-27 | Principia Biopharma Inc | Formas cristalinas de 2-[3-[4-amino-3-(2-fluoro-4-fenóxi-fenil)-1h-pirazolo[3,4-d]pirimidina-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrila |
| CN115397427A (zh) * | 2020-03-30 | 2022-11-25 | Igia制药有限公司 | 酪氨酸激酶抑制剂的儿科制剂 |
| KR20230050363A (ko) * | 2020-08-10 | 2023-04-14 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 질환의 치료에 있어서 btk 저해제의 용도 |
| AU2021325431B2 (en) | 2020-08-14 | 2024-01-18 | Novartis Ag | Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof |
| JP2023550591A (ja) | 2020-11-02 | 2023-12-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | EGFR阻害薬としての置換1H-ピラゾロ[4,3-c]及び誘導体 |
| MX2023006854A (es) * | 2020-12-10 | 2023-07-20 | Genzyme Corp | Forma cristalina de tolebrutinib, metodo de preparacion y uso de la misma. |
| CN116710452A (zh) * | 2020-12-23 | 2023-09-05 | 建新公司 | 4-氨基-3-(4-苯氧基苯基)-1,3-二氢-2h-咪唑并[4,5-c]吡啶-2-酮衍生物及其盐类 |
| EP4267572A1 (en) * | 2020-12-23 | 2023-11-01 | Genzyme Corporation | 4-amino-3-(4-phenoxyphenyl)-1,3- dihydro-2h-imidazo[4,5-c]pyridin-2-one derivatives and salts thereof |
| WO2022212893A1 (en) | 2021-04-02 | 2022-10-06 | Biogen Ma Inc. | Combination treatment methods of multiple sclerosis |
| WO2022218430A1 (zh) * | 2021-04-16 | 2022-10-20 | 南京明德新药研发有限公司 | 咪唑并吡啶类化合物及其应用 |
| WO2022223027A1 (zh) * | 2021-04-23 | 2022-10-27 | 杭州领业医药科技有限公司 | Tolebrutinib晶型、无定型及其制备方法和用途 |
| CN117412749A (zh) * | 2021-05-21 | 2024-01-16 | 杭州领业医药科技有限公司 | Tolebrutinib盐及其晶型、其制备方法、其药物组合物和用途 |
| CN117897381A (zh) | 2021-06-11 | 2024-04-16 | 建新公司 | Tolebrutinib的晶型及其制备方法和用途 |
| WO2023280132A1 (zh) * | 2021-07-06 | 2023-01-12 | 苏州晶云药物科技股份有限公司 | 氧代二氢咪唑并吡啶类化合物的晶型及其制备方法 |
| US11793820B2 (en) * | 2021-09-24 | 2023-10-24 | Chadwick Donaldson | Dry powder foamable formulations for delivery of medicaments through the mucosa |
| KR20240125005A (ko) | 2021-12-21 | 2024-08-19 | 프린시피아 바이오파마, 인코퍼레이티드 | (r)-1-(1-아크릴로일피페리딘-3-일)-4-아미노-3-(4-페녹시페닐)-1h-이미다조[4,5-c]피리딘-2(3h)-온의결정질 형태 및 이의 염 |
| WO2023172663A1 (en) * | 2022-03-09 | 2023-09-14 | Teva Pharmaceuticals International Gmbh | Solid state forms of tolebrutinib and of tolebrutinib salts |
| US20230399313A1 (en) * | 2022-06-10 | 2023-12-14 | Advenchen Pharmaceuticals, LLC | Biological activities of 5-(2-(4-(4-fluoro-2-methyl-1h-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)ethyl)-5-azaspiro[2.4]-heptan-7-ol crystalline, phosphoric acid salt and its enantiomers |
| AU2023294689A1 (en) * | 2022-06-14 | 2025-01-30 | Principia Biopharma Inc. | Methods of making tolebrutinib |
| CA3259743A1 (en) * | 2022-06-22 | 2023-12-28 | Principia Biopharma Inc. | METHODS FOR MANUFACTURING MODIFIED BTK INHIBITORS |
| CN119421712A (zh) | 2022-06-30 | 2025-02-11 | 普林斯匹亚生物制药公司 | 用于多发性硬化和重症肌无力的治疗性酪氨酸激酶抑制剂 |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
| KR20250084183A (ko) | 2022-10-11 | 2025-06-10 | 프린시피아 바이오파마, 인코퍼레이티드 | 다발성 경화증에 대한 치료용 티로신 키나제 저해제 |
| WO2024099242A1 (zh) * | 2022-11-07 | 2024-05-16 | 天津征程医药科技有限公司 | 氘代的氨基吡啶衍生物以及包含该化合物的药物组合物 |
| AU2023408758A1 (en) | 2022-12-20 | 2025-07-31 | Principia Biopharma Inc. | Drug formulations of (r)-1-(1-acryloylpiperidin-3-yl)-4-amino-3-(4- phenoxyphenyl)-1h-imidazo[4,5-c]pyridin-2(3h)-one |
| WO2024163542A2 (en) | 2023-02-01 | 2024-08-08 | Principia Biopharma Inc. | Methods of diagnosing and treating multiple sclerosis |
| WO2025188862A1 (en) | 2024-03-06 | 2025-09-12 | Principia Biopharma Inc. | Methods of making tolebrutinib |
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