JP2016519147A5 - - Google Patents
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- Publication number
- JP2016519147A5 JP2016519147A5 JP2016514126A JP2016514126A JP2016519147A5 JP 2016519147 A5 JP2016519147 A5 JP 2016519147A5 JP 2016514126 A JP2016514126 A JP 2016514126A JP 2016514126 A JP2016514126 A JP 2016514126A JP 2016519147 A5 JP2016519147 A5 JP 2016519147A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound
- bipyrazol
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 68
- 150000003839 salts Chemical class 0.000 claims 54
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 53
- 150000001875 compounds Chemical class 0.000 claims 50
- -1 H 2 N— Chemical group 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 28
- 125000001424 substituent group Chemical group 0.000 claims 20
- 239000003814 drug Substances 0.000 claims 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 12
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 10
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 206010028537 myelofibrosis Diseases 0.000 claims 7
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 6
- 208000003476 primary myelofibrosis Diseases 0.000 claims 6
- MSGYSFWCPOBHEV-AWEZNQCLSA-N 4-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1h-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-2,5-difluoro-n-[(2s)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)N[C@@H](C)C(F)(F)F)=CC(F)=C1N1CC(CC#N)(N2N=CC(=C2)C2=C(NN=C2C)C)C1 MSGYSFWCPOBHEV-AWEZNQCLSA-N 0.000 claims 5
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000006601 (C1-C3) alkylcarbamyl group Chemical group 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 4
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 3
- 208000009527 Refractory anemia Diseases 0.000 claims 3
- 206010072684 Refractory cytopenia with unilineage dysplasia Diseases 0.000 claims 3
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 3
- 208000037244 polycythemia vera Diseases 0.000 claims 3
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 claims 3
- 208000017520 skin disease Diseases 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010058314 Dysplasia Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 229910019142 PO4 Inorganic materials 0.000 claims 2
- 206010033661 Pancytopenia Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 208000024389 cytopenia Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000010452 phosphate Substances 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- IADHQAYOJSDLQB-UHFFFAOYSA-N 4-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylbenzamide Chemical compound CC(C)NC(=O)c1ccc(cc1)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C IADHQAYOJSDLQB-UHFFFAOYSA-N 0.000 claims 1
- WDEZBQCRCIAJPW-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[3-methyl-4-(1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(c(C)n1)-c1cn[nH]c1 WDEZBQCRCIAJPW-UHFFFAOYSA-N 0.000 claims 1
- UVNZXZQWOUVYIS-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[3-methyl-4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(c(C)n1)-c1c[nH]nc1C UVNZXZQWOUVYIS-UHFFFAOYSA-N 0.000 claims 1
- JFFRGYYXQJTLOG-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c(C)n[nH]c1C JFFRGYYXQJTLOG-UHFFFAOYSA-N 0.000 claims 1
- ZNDIFOVCUNVGNF-UHFFFAOYSA-N 5-[3-(cyanomethyl)-3-[4-(5-methyl-1H-pyrazol-4-yl)pyrazol-1-yl]azetidin-1-yl]-N-propan-2-ylpyrazine-2-carboxamide Chemical compound CC(C)NC(=O)c1cnc(cn1)N1CC(CC#N)(C1)n1cc(cn1)-c1c[nH]nc1C ZNDIFOVCUNVGNF-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 206010008805 Chromosomal abnormalities Diseases 0.000 claims 1
- 208000031404 Chromosome Aberrations Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 1
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 101100095974 Mus musculus Smc3 gene Proteins 0.000 claims 1
- AYNNRIXQAVTECA-ZETCQYMHSA-N N-[(2S)-1,1,1-trifluoropropan-2-yl]benzamide Chemical compound C(C1=CC=CC=C1)(=O)N[C@H](C(F)(F)F)C AYNNRIXQAVTECA-ZETCQYMHSA-N 0.000 claims 1
- BISZGLXXDZHLIN-FJXQXJEOSA-N P(O)(O)(O)=O.C(C1=CC=CC=C1)(=O)N[C@H](C(F)(F)F)C Chemical compound P(O)(O)(O)=O.C(C1=CC=CC=C1)(=O)N[C@H](C(F)(F)F)C BISZGLXXDZHLIN-FJXQXJEOSA-N 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms 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
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010070834 Sensitisation Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 206010070835 Skin sensitisation Diseases 0.000 claims 1
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 1
- 208000005485 Thrombocytosis Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 1
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- DDAMPNWYDILDPV-UHFFFAOYSA-N benzamide;phosphoric acid Chemical compound OP(O)(O)=O.NC(=O)C1=CC=CC=C1 DDAMPNWYDILDPV-UHFFFAOYSA-N 0.000 claims 1
- HLWOEQNDJYGYJV-UHFFFAOYSA-N benzamide;sulfuric acid Chemical compound OS(O)(=O)=O.NC(=O)C1=CC=CC=C1 HLWOEQNDJYGYJV-UHFFFAOYSA-N 0.000 claims 1
- 210000000601 blood cell Anatomy 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 208000019664 bone resorption disease Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229910052742 iron Inorganic materials 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm 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
- 210000004165 myocardium Anatomy 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- 230000008313 sensitization Effects 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 231100000370 skin sensitisation Toxicity 0.000 claims 1
- 208000009996 subepithelial mucinous corneal dystrophy Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361824683P | 2013-05-17 | 2013-05-17 | |
| US61/824,683 | 2013-05-17 | ||
| PCT/US2014/038388 WO2014186706A1 (en) | 2013-05-17 | 2014-05-16 | Bipyrazole derivatives as jak inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018187613A Division JP6775560B2 (ja) | 2013-05-17 | 2018-10-02 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016519147A JP2016519147A (ja) | 2016-06-30 |
| JP2016519147A5 true JP2016519147A5 (enExample) | 2017-06-29 |
| JP6415543B2 JP6415543B2 (ja) | 2018-10-31 |
Family
ID=50983151
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016514126A Active JP6415543B2 (ja) | 2013-05-17 | 2014-05-16 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2018187613A Active JP6775560B2 (ja) | 2013-05-17 | 2018-10-02 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2020168950A Active JP7126741B2 (ja) | 2013-05-17 | 2020-10-06 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2022128042A Pending JP2022163162A (ja) | 2013-05-17 | 2022-08-10 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2024079435A Pending JP2024105557A (ja) | 2013-05-17 | 2024-05-15 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018187613A Active JP6775560B2 (ja) | 2013-05-17 | 2018-10-02 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2020168950A Active JP7126741B2 (ja) | 2013-05-17 | 2020-10-06 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2022128042A Pending JP2022163162A (ja) | 2013-05-17 | 2022-08-10 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
| JP2024079435A Pending JP2024105557A (ja) | 2013-05-17 | 2024-05-15 | Ｊａｋ阻害剤としてのビピラゾール誘導体 |
Country Status (36)
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE028588T2 (hu) | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| BRPI1012108B8 (pt) | 2009-05-22 | 2021-05-25 | Incyte Corp | composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico |
| NZ596479A (en) | 2009-05-22 | 2014-01-31 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| MX389479B (es) | 2011-09-02 | 2025-03-20 | Incyte Holdings Corp | Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k) |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| CA2888816A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| KR102242077B1 (ko) | 2012-11-15 | 2021-04-20 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| CR20190156A (es) * | 2013-05-17 | 2019-05-16 | Incyte Corp | Derivados de bipirazol como inhibidores jak |
| MX376856B (es) | 2013-08-07 | 2025-03-07 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| SG11201607083VA (en) * | 2014-02-28 | 2016-09-29 | Incyte Corp | Jak1 inhibitors for the treatment of myelodysplastic syndromes |
| CA3158254C (en) | 2014-04-08 | 2024-05-21 | Incyte Corporation | Treatment of b-cell malignancies by a combination jak and pi3k inhibitors |
| SG11201609016VA (en) | 2014-04-30 | 2016-11-29 | Incyte Corp | Processes of preparing a jak1 inhibitor and new forms thereto |
| WO2015184305A1 (en) * | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US10077277B2 (en) | 2014-06-11 | 2018-09-18 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors |
| US9421199B2 (en) | 2014-06-24 | 2016-08-23 | Sydnexis, Inc. | Ophthalmic composition |
| WO2016172712A2 (en) | 2015-04-23 | 2016-10-27 | Sydnexis, Inc. | Ophthalmic composition |
| WO2016130501A1 (en) | 2015-02-09 | 2016-08-18 | Incyte Corporation | Aza-heteroaryl compounds as pi3k-gamma inhibitors |
| SG10201912302VA (en) | 2015-02-27 | 2020-02-27 | Incyte Corp | Salts of pi3k inhibitor and processes for their preparation |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| WO2016183060A1 (en) | 2015-05-11 | 2016-11-17 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US11052094B2 (en) * | 2015-05-29 | 2021-07-06 | Sydnexis, Inc. | D2O stabilized pharmaceutical formulations |
| RS63359B1 (sr) | 2015-11-06 | 2022-07-29 | Incyte Corp | Heterociklična jedinjenja kao inhibitori pi3k-gama |
| ES2995198T3 (en) | 2016-01-05 | 2025-02-07 | Incyte Corp | Pyridine compounds as pi3k-gamma inhibitors |
| TW201803871A (zh) | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物 |
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