JP2014522860A5 - - Google Patents
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- JP2014522860A5 JP2014522860A5 JP2014520607A JP2014520607A JP2014522860A5 JP 2014522860 A5 JP2014522860 A5 JP 2014522860A5 JP 2014520607 A JP2014520607 A JP 2014520607A JP 2014520607 A JP2014520607 A JP 2014520607A JP 2014522860 A5 JP2014522860 A5 JP 2014522860A5
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- JP
- Japan
- Prior art keywords
- benzamide
- pyrazin
- methylimidazo
- alkyl
- compound according
- 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.)
- Pending
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- -1 pyrazin-1-yl Chemical group 0.000 claims 30
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 26
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 4
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 201000008482 osteoarthritis Diseases 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 2
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 2
- 208000035268 Mast Cell Activation disease Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 2
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 230000001363 autoimmune Effects 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims 2
- 210000003519 mature b lymphocyte Anatomy 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- LCRSPYXMSMVXJE-BDUNBXCCSA-N 4-[3-[(1s)-1-[[(e)-4-methoxybut-2-enoyl]amino]ethyl]-8-methylimidazo[1,5-a]pyrazin-1-yl]-n-[4-(trifluoromethyl)pyridin-2-yl]benzamide Chemical compound C=12C(C)=NC=CN2C([C@H](C)NC(=O)/C=C/COC)=NC=1C(C=C1)=CC=C1C(=O)NC1=CC(C(F)(F)F)=CC=N1 LCRSPYXMSMVXJE-BDUNBXCCSA-N 0.000 claims 1
- CWJRZDWOLHKIIX-HSDHKRTLSA-N 4-[3-[(2s)-1-[(e)-4-(dimethylamino)but-2-enoyl]piperidin-2-yl]-8-methylimidazo[1,5-a]pyrazin-1-yl]-n-(4-propylpyridin-2-yl)benzamide Chemical compound CCCC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCCC3)C(=O)\C=C\CN(C)C)=N2)=C1 CWJRZDWOLHKIIX-HSDHKRTLSA-N 0.000 claims 1
- XLOGIFFPIIBWGJ-HNNXBMFYSA-N 4-[8-methyl-3-[(1s)-1-(prop-2-enoylamino)ethyl]imidazo[1,5-a]pyrazin-1-yl]-n-[4-(trifluoromethyl)pyridin-2-yl]benzamide Chemical compound C=12C(C)=NC=CN2C([C@@H](NC(=O)C=C)C)=NC=1C(C=C1)=CC=C1C(=O)NC1=CC(C(F)(F)F)=CC=N1 XLOGIFFPIIBWGJ-HNNXBMFYSA-N 0.000 claims 1
- ZWHKMEXQEXXCRA-DEOSSOPVSA-N 4-[8-methyl-3-[(2s)-1-prop-2-enoylpiperidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-n-(4-propylpyridin-2-yl)benzamide Chemical compound CCCC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCCC3)C(=O)C=C)=N2)=C1 ZWHKMEXQEXXCRA-DEOSSOPVSA-N 0.000 claims 1
- VLEZQOHBDFVKRP-NRFANRHFSA-N 4-[8-methyl-3-[(2s)-1-prop-2-enoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-n-(4-methylpyridin-2-yl)benzamide Chemical compound CC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCC3)C(=O)C=C)=N2)=C1 VLEZQOHBDFVKRP-NRFANRHFSA-N 0.000 claims 1
- UEVJUPPLOHUVON-QHCPKHFHSA-N 4-[8-methyl-3-[(2s)-1-prop-2-enoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-n-(4-propylpyridin-2-yl)benzamide Chemical compound CCCC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCC3)C(=O)C=C)=N2)=C1 UEVJUPPLOHUVON-QHCPKHFHSA-N 0.000 claims 1
- 208000032467 Aplastic anaemia Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 208000009137 Behcet syndrome Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010006895 Cachexia Diseases 0.000 claims 1
- 206010008909 Chronic Hepatitis Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010010741 Conjunctivitis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010019755 Hepatitis chronic active Diseases 0.000 claims 1
- 206010051645 Idiopathic neutropenia Diseases 0.000 claims 1
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000029523 Interstitial Lung disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 102220517591 Methyl-CpG-binding domain protein 3-like 2B_R11C_mutation Human genes 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000003926 Myelitis Diseases 0.000 claims 1
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 1
- 206010033078 Otitis media Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010065159 Polychondritis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037448 Pulmonary valve incompetence Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 201000010001 Silicosis Diseases 0.000 claims 1
- 206010042033 Stevens-Johnson syndrome Diseases 0.000 claims 1
- 231100000168 Stevens-Johnson syndrome Toxicity 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 206010043781 Thyroiditis chronic Diseases 0.000 claims 1
- 206010048873 Traumatic arthritis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000005000 autoimmune gastritis Diseases 0.000 claims 1
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 231100000321 erythema Toxicity 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 206010023332 keratitis Diseases 0.000 claims 1
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- BOYHADSAXZAUQY-NRFANRHFSA-N n-(4-cyanopyridin-2-yl)-4-[8-methyl-3-[(2s)-1-prop-2-enoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]benzamide Chemical compound C=12C(C)=NC=CN2C([C@H]2N(CCC2)C(=O)C=C)=NC=1C(C=C1)=CC=C1C(=O)NC1=CC(C#N)=CC=N1 BOYHADSAXZAUQY-NRFANRHFSA-N 0.000 claims 1
- ZAXOXFZPTLHJQX-QFIPXVFZSA-N n-(4-ethylpyridin-2-yl)-4-[8-methyl-3-[(2s)-1-prop-2-enoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]benzamide Chemical compound CCC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCC3)C(=O)C=C)=N2)=C1 ZAXOXFZPTLHJQX-QFIPXVFZSA-N 0.000 claims 1
- OPELHLHHRKSOEG-NRFANRHFSA-N n-(4-methoxypyridin-2-yl)-4-[8-methyl-3-[(2s)-1-prop-2-enoylpyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]benzamide Chemical compound COC1=CC=NC(NC(=O)C=2C=CC(=CC=2)C2=C3C(C)=NC=CN3C([C@H]3N(CCC3)C(=O)C=C)=N2)=C1 OPELHLHHRKSOEG-NRFANRHFSA-N 0.000 claims 1
- ACJIPXJQUWPIFD-UHFFFAOYSA-N n-(4-propylpyridin-2-yl)benzamide Chemical compound CCCC1=CC=NC(NC(=O)C=2C=CC=CC=2)=C1 ACJIPXJQUWPIFD-UHFFFAOYSA-N 0.000 claims 1
- BETCAYZPULVFFU-UHFFFAOYSA-N n-[4-(trifluoromethyl)pyridin-2-yl]benzamide Chemical compound FC(F)(F)C1=CC=NC(NC(=O)C=2C=CC=CC=2)=C1 BETCAYZPULVFFU-UHFFFAOYSA-N 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 208000028169 periodontal disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010035653 pneumoconiosis Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 201000010298 pulmonary valve insufficiency Diseases 0.000 claims 1
- 208000002574 reactive arthritis Diseases 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 102200080066 rs122460151 Human genes 0.000 claims 1
- 201000000306 sarcoidosis Diseases 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000004595 synovitis Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 229910052727 yttrium Inorganic materials 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161509376P | 2011-07-19 | 2011-07-19 | |
| US61/509,376 | 2011-07-19 | ||
| EP11174582.4 | 2011-07-19 | ||
| EP11174582 | 2011-07-19 | ||
| PCT/EP2012/063556 WO2013010869A1 (en) | 2011-07-19 | 2012-07-11 | 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk-inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014522860A JP2014522860A (ja) | 2014-09-08 |
| JP2014522860A5 true JP2014522860A5 (enExample) | 2014-11-13 |
Family
ID=47557678
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014520607A Pending JP2014522860A (ja) | 2011-07-19 | 2012-07-11 | Ｂｔｋ阻害剤としての４−イミダゾピリダジン−１−イル−ベンズアミドおよび４−イミダゾトリアジン−１−イル−ベンズアミド |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20140155406A1 (enExample) |
| EP (1) | EP2734523A1 (enExample) |
| JP (1) | JP2014522860A (enExample) |
| AU (1) | AU2012285988B2 (enExample) |
| CA (1) | CA2841887A1 (enExample) |
| WO (1) | WO2013010869A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8962831B2 (en) | 2011-05-17 | 2015-02-24 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US9376438B2 (en) | 2011-05-17 | 2016-06-28 | Principia Biopharma, Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| CN106243113B (zh) | 2011-07-19 | 2018-12-18 | 默沙东有限责任公司 | 作为btk抑制剂的选择的咪唑并吡嗪类 |
| CA2879570A1 (en) | 2012-07-24 | 2014-01-30 | Pharmacyclics, Inc. | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| AU2013312296B2 (en) | 2012-09-10 | 2017-06-22 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
| CA2887465A1 (en) * | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| TW201441234A (zh) | 2013-01-23 | 2014-11-01 | Merck Sharp & Dohme | Ｂｔｋ抑制劑 |
| WO2014113942A1 (en) | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| AU2014358868A1 (en) | 2013-12-05 | 2016-06-09 | Acerta Pharma B.V. | Therapeutic combination of a PI3K inhibitor and a BTK inhibitor |
| EP3082809B1 (en) | 2013-12-20 | 2021-01-20 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| EP3082811B1 (en) | 2013-12-20 | 2020-01-15 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| US10272083B2 (en) | 2014-01-21 | 2019-04-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor |
| KR20160117614A (ko) | 2014-02-21 | 2016-10-10 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| KR20160127754A (ko) | 2014-03-12 | 2016-11-04 | 노파르티스 아게 | Btk 억제제 및 akt 억제제를 포함하는 조합물 |
| WO2015185998A2 (en) | 2014-04-11 | 2015-12-10 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase |
| US9937171B2 (en) | 2014-04-11 | 2018-04-10 | Acerta Pharma B.V. | Methods of blocking the CXCR-4/SDF-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
| WO2015193740A2 (en) | 2014-06-17 | 2015-12-23 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor and/or a jak-2 inhibitor |
| TW201618783A (zh) | 2014-08-07 | 2016-06-01 | 艾森塔製藥公司 | 以布魯頓(Bruton)氏酪胺酸激酶(BTK)佔據和BTK再合成速率為基礎之治療癌症、免疫和自體免疫疾病及發炎性疾病之方法 |
| TW201618774A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | 使用ｂｔｋ抑制劑透過調變腫瘤微環境來治療實體腫瘤及其他疾病之方法 |
| SI3179992T1 (sl) | 2014-08-11 | 2022-09-30 | Acerta Pharma B.V. | Terapevtske kombinacije zaviralca BTK, zaviralca PD-1 in/ali zaviralca PD-L1 |
| EP3179991B1 (en) | 2014-08-11 | 2021-10-06 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a bcl-2 inhibitor |
| AR101504A1 (es) | 2014-08-11 | 2016-12-21 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6 |
| WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
| EA036269B1 (ru) | 2014-12-18 | 2020-10-21 | Принсипиа Биофарма Инк. | Лечение пузырчатки |
| WO2016106627A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2016161571A1 (en) | 2015-04-08 | 2016-10-13 | Merck Sharp & Dohme Corp. | Indazole and azaindazole btk inhibitors |
| WO2016192074A1 (en) * | 2015-06-04 | 2016-12-08 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2016210165A1 (en) | 2015-06-24 | 2016-12-29 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| DK3954690T3 (da) | 2015-07-02 | 2023-06-06 | Acerta Pharma Bv | Faste former og formuleringer af (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamid |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| US20190022092A1 (en) | 2015-09-15 | 2019-01-24 | Acerta Pharma B.V. | Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist |
| HUE066644T2 (hu) | 2015-09-15 | 2024-08-28 | Acerta Pharma Bv | CD19-inhibitor és BTK-inhibitor terápiás kombinációi |
| WO2017122175A1 (en) | 2016-01-13 | 2017-07-20 | Acerta Pharma B.V. | Therapeutic combinations of an antifolate and a btk inhibitor |
| CN107021963A (zh) | 2016-01-29 | 2017-08-08 | 北京诺诚健华医药科技有限公司 | 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用 |
| EP3478273A1 (en) | 2016-06-29 | 2019-05-08 | 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 |
| CA3046578A1 (en) * | 2016-12-21 | 2018-06-28 | Acerta Pharma B.V. | Imidazopyrazine inhibitors of bruton's tyrosine kinase |
| US20190376971A1 (en) | 2017-01-19 | 2019-12-12 | Acerta Pharma B.V. | Compositions and Methods for the Assessment of Drug Target Occupancy for Bruton's Tyrosine Kinase |
| JP2020508326A (ja) | 2017-02-24 | 2020-03-19 | ギリアド サイエンシズ， インコーポレイテッド | ブルトン型チロシンキナーゼの阻害剤 |
| AR110998A1 (es) | 2017-02-24 | 2019-05-22 | Gilead Sciences Inc | Inhibidores de la tirosina cinasa de bruton |
| AU2018237123B2 (en) * | 2017-03-22 | 2022-08-04 | Xibin Liao | Bruton's tyrosine kinase inhibitors |
| EA037031B1 (ru) * | 2017-10-06 | 2021-01-28 | Асерта Фарма Б.В. | Имидазопиразиновые ингибиторы тирозинкиназы брутона |
| WO2019090269A1 (en) * | 2017-11-06 | 2019-05-09 | Peng Wang | Processes to produce acalabrutinib |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| EP4045051A1 (en) | 2019-10-14 | 2022-08-24 | Principia Biopharma Inc. | Methods for treating immune thrombocytopenia by administering (r)-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 |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| PH12022551787A1 (en) | 2020-01-22 | 2024-02-12 | Principia Biopharma Inc | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| PT4426434T (pt) | 2021-11-02 | 2025-11-24 | Flare Therapeutics Inc | Agonistas inversos de pparg e suas utilizações |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006316605B2 (en) * | 2005-11-17 | 2012-04-26 | Osi Pharmaceuticals, Inc. | Fused bicyclic mTOR inhibitors |
| SG10201508035TA (en) * | 2007-03-28 | 2015-10-29 | Pharmacyclics Inc | Inhibitors of bruton's tyrosine kinase |
| JP5656976B2 (ja) * | 2009-04-29 | 2015-01-21 | ローカス ファーマシューティカルズ インコーポレイテッド | ピロロトリアジン化合物 |
| EP2534151B1 (en) * | 2010-02-08 | 2018-11-14 | Merck Sharp & Dohme B.V. | 8-methyl-1-phenyl-imidazol[1,5-a]pyrazine compounds |
-
2012
- 2012-07-11 AU AU2012285988A patent/AU2012285988B2/en not_active Expired - Fee Related
- 2012-07-11 WO PCT/EP2012/063556 patent/WO2013010869A1/en not_active Ceased
- 2012-07-11 US US14/233,429 patent/US20140155406A1/en not_active Abandoned
- 2012-07-11 EP EP12735138.5A patent/EP2734523A1/en not_active Withdrawn
- 2012-07-11 CA CA2841887A patent/CA2841887A1/en not_active Abandoned
- 2012-07-11 JP JP2014520607A patent/JP2014522860A/ja active Pending
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