JP2014506601A5 - - Google Patents
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- JP2014506601A5 JP2014506601A5 JP2013555580A JP2013555580A JP2014506601A5 JP 2014506601 A5 JP2014506601 A5 JP 2014506601A5 JP 2013555580 A JP2013555580 A JP 2013555580A JP 2013555580 A JP2013555580 A JP 2013555580A JP 2014506601 A5 JP2014506601 A5 JP 2014506601A5
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- JP
- Japan
- Prior art keywords
- item
- alkyl
- halo
- heterocycloalkyl
- aryl
- 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 description 53
- 150000003839 salts Chemical class 0.000 claims description 11
- 206010012601 diabetes mellitus Diseases 0.000 claims description 8
- 201000004681 Psoriasis Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 206010002198 Anaphylactic reaction Diseases 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 201000004624 Dermatitis Diseases 0.000 claims description 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 3
- 206010014561 Emphysema Diseases 0.000 claims description 3
- 208000032612 Glial tumor Diseases 0.000 claims description 3
- 206010018338 Glioma Diseases 0.000 claims description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 claims description 3
- 206010020751 Hypersensitivity Diseases 0.000 claims description 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 3
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 206010033645 Pancreatitis Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims description 3
- 206010039710 Scleroderma Diseases 0.000 claims description 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 3
- 208000026935 allergic disease Diseases 0.000 claims description 3
- 230000007815 allergy Effects 0.000 claims description 3
- 230000036783 anaphylactic response Effects 0.000 claims description 3
- 208000003455 anaphylaxis Diseases 0.000 claims description 3
- 208000010668 atopic eczema Diseases 0.000 claims description 3
- 206010006451 bronchitis Diseases 0.000 claims description 3
- 201000000493 colon squamous cell carcinoma Diseases 0.000 claims description 3
- 208000029742 colonic neoplasm Diseases 0.000 claims description 3
- 208000024908 graft versus host disease Diseases 0.000 claims description 3
- 201000011066 hemangioma Diseases 0.000 claims description 3
- 208000017169 kidney disease Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 206010025135 lupus erythematosus Diseases 0.000 claims description 3
- 208000002780 macular degeneration Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 3
- 208000012972 squamous cell carcinoma of colon Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 description 81
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 76
- -1 heterocycloalkyloxy Chemical class 0.000 description 66
- 125000000217 alkyl group Chemical group 0.000 description 44
- 125000005843 halogen group Chemical group 0.000 description 40
- 125000003118 aryl group Chemical group 0.000 description 38
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 38
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 38
- 125000001072 heteroaryl group Chemical group 0.000 description 37
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 description 36
- 229910019142 PO4 Inorganic materials 0.000 description 36
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 36
- 125000002252 acyl group Chemical group 0.000 description 36
- 125000004423 acyloxy group Chemical group 0.000 description 36
- 125000003342 alkenyl group Chemical group 0.000 description 36
- 125000003545 alkoxy group Chemical group 0.000 description 36
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 36
- 125000000304 alkynyl group Chemical group 0.000 description 36
- 150000001408 amides Chemical class 0.000 description 36
- 125000003710 aryl alkyl group Chemical group 0.000 description 36
- 239000004202 carbamide Substances 0.000 description 36
- 125000004122 cyclic group Chemical group 0.000 description 36
- 125000000753 cycloalkyl group Chemical group 0.000 description 36
- 125000004404 heteroalkyl group Chemical group 0.000 description 36
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 36
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 36
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 36
- 239000010452 phosphate Substances 0.000 description 36
- 229940124530 sulfonamide Drugs 0.000 description 36
- 150000003456 sulfonamides Chemical class 0.000 description 36
- 229910052739 hydrogen Inorganic materials 0.000 description 30
- 239000001257 hydrogen Substances 0.000 description 30
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 30
- 0 *c1c2nc(N)[o]c2c(*)c(*)c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O Chemical compound *c1c2nc(N)[o]c2c(*)c(*)c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O 0.000 description 10
- 229910052799 carbon Inorganic materials 0.000 description 10
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 description 9
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 description 9
- 238000000034 method Methods 0.000 description 9
- 229910052717 sulfur Inorganic materials 0.000 description 8
- 229910052760 oxygen Inorganic materials 0.000 description 6
- 201000010099 disease Diseases 0.000 description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 description 4
- 208000006673 asthma Diseases 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 201000008171 proliferative glomerulonephritis Diseases 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- QQESVQNMQDZQHT-UHFFFAOYSA-N CN(C1)CC(C2)C1CN2C(c1cnc(cc2)[n]1cc2-c(cc1)cc2c1[o]c(N)n2)=O Chemical compound CN(C1)CC(C2)C1CN2C(c1cnc(cc2)[n]1cc2-c(cc1)cc2c1[o]c(N)n2)=O QQESVQNMQDZQHT-UHFFFAOYSA-N 0.000 description 1
- MXAVXHBXUHXKAM-UHFFFAOYSA-N CN(CC1)CCN1c1nnc(cc2)[n]1cc2-c(cc1)cc2c1nc(N)[o]2 Chemical compound CN(CC1)CCN1c1nnc(cc2)[n]1cc2-c(cc1)cc2c1nc(N)[o]2 MXAVXHBXUHXKAM-UHFFFAOYSA-N 0.000 description 1
- JFQKQWJUCNSORA-UHFFFAOYSA-N CN1CCN(CCc2nnc(cc3)[n]2cc3-c(cc2)cc3c2nc(N)[o]3)CC1 Chemical compound CN1CCN(CCc2nnc(cc3)[n]2cc3-c(cc2)cc3c2nc(N)[o]3)CC1 JFQKQWJUCNSORA-UHFFFAOYSA-N 0.000 description 1
- IPGGRBSJXVRDMH-UHFFFAOYSA-N CN1CCN(Cc2nnc(cc3)[n]2cc3-c(cc2)cc3c2nc(N)[o]3)CC1 Chemical compound CN1CCN(Cc2nnc(cc3)[n]2cc3-c(cc2)cc3c2nc(N)[o]3)CC1 IPGGRBSJXVRDMH-UHFFFAOYSA-N 0.000 description 1
- FROLFXUNNJXSCM-UHFFFAOYSA-N C[n]1ncc2c1cncc2-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O Chemical compound C[n]1ncc2c1cncc2-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O FROLFXUNNJXSCM-UHFFFAOYSA-N 0.000 description 1
- SSUJNFTULPBNSD-UHFFFAOYSA-N Cc(nc1)c2[nH]ccc2c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O Chemical compound Cc(nc1)c2[nH]ccc2c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O SSUJNFTULPBNSD-UHFFFAOYSA-N 0.000 description 1
- NOFBWFALVUWQFU-UHFFFAOYSA-N Cc(nc1)c2[nH]ncc2c1-c(cc1)c[n]2c1ncc2C(N1C2COCC1CC2)=O Chemical compound Cc(nc1)c2[nH]ncc2c1-c(cc1)c[n]2c1ncc2C(N1C2COCC1CC2)=O NOFBWFALVUWQFU-UHFFFAOYSA-N 0.000 description 1
- GCQBQPXYJIEDOP-UHFFFAOYSA-N Cc(nc1)c2[nH]ncc2c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O Chemical compound Cc(nc1)c2[nH]ncc2c1-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O GCQBQPXYJIEDOP-UHFFFAOYSA-N 0.000 description 1
- MSXFZTVVGNYKDM-UHFFFAOYSA-N Cc1cc(-c(cc2)cc3c2nc(N)[o]3)c[n]2c(-c3ccncc3)nnc12 Chemical compound Cc1cc(-c(cc2)cc3c2nc(N)[o]3)c[n]2c(-c3ccncc3)nnc12 MSXFZTVVGNYKDM-UHFFFAOYSA-N 0.000 description 1
- JZDCENLTEHAJLS-UHFFFAOYSA-N Nc1nc(cc(cc2)-c3cnc(cc4)[n]3cc4C(N3CCOCC3)=O)c2[o]1 Chemical compound Nc1nc(cc(cc2)-c3cnc(cc4)[n]3cc4C(N3CCOCC3)=O)c2[o]1 JZDCENLTEHAJLS-UHFFFAOYSA-N 0.000 description 1
- BSPHZKKRWHTGAQ-UHFFFAOYSA-N Nc1nc(ccc(-c(cc2)c[n]3c2ncc3C(N2CCOCC2)=O)c2)c2[nH]1 Chemical compound Nc1nc(ccc(-c(cc2)c[n]3c2ncc3C(N2CCOCC2)=O)c2)c2[nH]1 BSPHZKKRWHTGAQ-UHFFFAOYSA-N 0.000 description 1
- WVSALGROVPJFFB-UHFFFAOYSA-N Nc1nc2cc(-c3cnc(cc4)[n]3cc4C(N3C4COCC3CC4)=O)ccc2[o]1 Chemical compound Nc1nc2cc(-c3cnc(cc4)[n]3cc4C(N3C4COCC3CC4)=O)ccc2[o]1 WVSALGROVPJFFB-UHFFFAOYSA-N 0.000 description 1
- OMMRCYUMEZEGJN-UHFFFAOYSA-N O=C(c1cnc(cc2)[n]1cc2-c1cc([nH]cc2)c2nc1)N1CCOCC1 Chemical compound O=C(c1cnc(cc2)[n]1cc2-c1cc([nH]cc2)c2nc1)N1CCOCC1 OMMRCYUMEZEGJN-UHFFFAOYSA-N 0.000 description 1
- OEFNXIPQCPFMDJ-UHFFFAOYSA-N O=C(c1cnc(cc2)[n]1cc2-c1ccnc2c1cn[nH]2)N1CCOCC1 Chemical compound O=C(c1cnc(cc2)[n]1cc2-c1ccnc2c1cn[nH]2)N1CCOCC1 OEFNXIPQCPFMDJ-UHFFFAOYSA-N 0.000 description 1
- HGTBLURUMIBMAP-UHFFFAOYSA-N O=C(c1cnc(cc2)[n]1cc2-c1cnc(cn[nH]2)c2c1)N1CCOCC1 Chemical compound O=C(c1cnc(cc2)[n]1cc2-c1cnc(cn[nH]2)c2c1)N1CCOCC1 HGTBLURUMIBMAP-UHFFFAOYSA-N 0.000 description 1
- VXMPYADDRAZEHW-UHFFFAOYSA-N OCC[n]1ncc2c1cncc2-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O Chemical compound OCC[n]1ncc2c1cncc2-c(cc1)c[n]2c1ncc2C(N1CCOCC1)=O VXMPYADDRAZEHW-UHFFFAOYSA-N 0.000 description 1
- 108091007960 PI3Ks Proteins 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 201000004240 prostatic hypertrophy Diseases 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161445999P | 2011-02-23 | 2011-02-23 | |
| US61/445,999 | 2011-02-23 | ||
| PCT/US2012/026406 WO2012116237A2 (en) | 2011-02-23 | 2012-02-23 | Heterocyclic compounds and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014506601A JP2014506601A (ja) | 2014-03-17 |
| JP2014506601A5 true JP2014506601A5 (enExample) | 2015-07-02 |
| JP5808826B2 JP5808826B2 (ja) | 2015-11-10 |
Family
ID=46721464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013555580A Expired - Fee Related JP5808826B2 (ja) | 2011-02-23 | 2012-02-23 | 複素環化合物およびその使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US9127000B2 (enExample) |
| EP (1) | EP2678016B1 (enExample) |
| JP (1) | JP5808826B2 (enExample) |
| WO (1) | WO2012116237A2 (enExample) |
Families Citing this family (84)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| LT3495367T (lt) | 2012-06-13 | 2021-02-25 | Incyte Holdings Corporation | Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai |
| US9309243B2 (en) | 2012-07-13 | 2016-04-12 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of TNF activity |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| WO2014072937A1 (en) | 2012-11-08 | 2014-05-15 | Rhizen Pharmaceuticals Sa | Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| KR102421235B1 (ko) | 2014-02-13 | 2022-07-15 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| NZ723203A (en) | 2014-02-13 | 2020-08-28 | Incyte Corp | Cyclopropylamines as lsd1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| CN105503877A (zh) * | 2014-09-24 | 2016-04-20 | 和记黄埔医药(上海)有限公司 | 咪唑并哒嗪类化合物及其用途 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| AU2015342883B2 (en) | 2014-11-06 | 2020-07-02 | Bial - R&D Investments, S.A. | Substituted pyrrolo(1,2-a)pyrimidines and their use in the treatment of medical disorders |
| CN107001379B (zh) | 2014-11-06 | 2022-11-01 | Bial研发投资股份有限公司 | 取代的吡唑并[1,5-a]嘧啶以及它们在治疗医学障碍中的用途 |
| HUE045220T2 (hu) | 2014-12-19 | 2019-12-30 | Janssen Pharmaceutica Nv | Imidazopiridazin-származékok mint PI3Kbéta inhibitorok |
| MX2017008076A (es) | 2014-12-19 | 2018-01-09 | Janssen Pharmaceutica Nv | DERIVADOS DE IMIDAZOPIRIDAZINA ENLAZADOS A HETEROCICLILO COMO INHIBIDORES DE PI3Kß. |
| EP3237397B1 (en) | 2014-12-24 | 2018-11-21 | Gilead Sciences, Inc. | Isoquinoline compounds for the treatment of hiv |
| TW202237569A (zh) | 2014-12-24 | 2022-10-01 | 美商基利科學股份有限公司 | 喹唑啉化合物 |
| ES2735087T3 (es) | 2014-12-24 | 2019-12-16 | Gilead Sciences Inc | Compuestos de pirimidina fusionados para el tratamiento de VIH |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| SG11201706287PA (en) | 2015-02-20 | 2017-09-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| UA122688C2 (uk) | 2015-04-03 | 2020-12-28 | Інсайт Корпорейшн | Гетероциклічні сполуки як інгібітори lsd1 |
| EP3317278B1 (en) | 2015-07-01 | 2021-04-14 | Crinetics Pharmaceuticals, Inc. | Somatostatin modulators and uses thereof |
| JP7427363B2 (ja) | 2015-08-12 | 2024-02-05 | インサイト・ホールディングス・コーポレイション | Lsd1阻害剤の塩 |
| CN105130984B (zh) * | 2015-09-23 | 2017-03-29 | 前湾医药科技(深圳)有限公司 | 一种咪唑并吡啶类化合物与在制备pi3k抑制剂中的应用 |
| JP6912460B2 (ja) | 2015-10-09 | 2021-08-04 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのキノキサリンおよびピリドピラジン誘導体 |
| CN114456176B (zh) | 2016-03-28 | 2024-08-30 | 因赛特公司 | 作为tam抑制剂的吡咯并三嗪化合物 |
| WO2017176962A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics, Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| WO2017176960A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US10787454B2 (en) | 2016-04-06 | 2020-09-29 | BIAL—BioTech Investments, Inc. | Imidazo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| US10166221B2 (en) | 2016-04-22 | 2019-01-01 | Incyte Corporation | Formulations of an LSD1 inhibitor |
| MX389579B (es) | 2016-05-05 | 2025-03-20 | Bial R&D Invest S A | IMIDAZO[1,2-b]PIRIDAZINAS SUSTITUIDAS, IMIDAZO[1,5-b]PIRIDAZINAS SUSTITUIDAS, COMPUESTOS RELACIONADOS Y SU USO EN EL TRATAMIENTO DE TRASTORNOS MÉDICOS |
| WO2017192931A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| KR102472453B1 (ko) | 2016-06-16 | 2022-11-29 | 얀센 파마슈티카 엔.브이. | Pi3k 베타 저해제로서의 이환식 피리딘, 피라진, 및 피리미딘 유도체 |
| US20190263804A1 (en) | 2016-06-16 | 2019-08-29 | Janssen Pharmaceutica Nv | Azabenzimidazole derivatives as pi3k beta inhibitors |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| PH12019500056B1 (en) | 2016-07-12 | 2024-01-31 | Revolution Medicines Inc | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| BR112019015075A2 (pt) | 2017-01-23 | 2020-03-10 | Revolution Medicines, Inc. | Compostos bicíclicos como inibidores de shp2 alostéricos |
| SG11201906412SA (en) | 2017-01-23 | 2019-08-27 | Revolution Medicines Inc | Pyridine compounds as allosteric shp2 inhibitors |
| EP3601254B1 (en) | 2017-03-29 | 2022-05-25 | Janssen Pharmaceutica NV | Quinoxaline and pyridopyrazine derivatives as pi3k-beta inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EP3658560A4 (en) | 2017-07-25 | 2021-01-06 | Crinetics Pharmaceuticals, Inc. | SOMATOSTAT IN MODULATORS AND USES THEREOF |
| SG11202002941WA (en) | 2017-10-12 | 2020-04-29 | Revolution Medicines Inc | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| CN107935918A (zh) * | 2017-11-15 | 2018-04-20 | 山东潍坊润丰化工股份有限公司 | 一种百草枯的制备方法 |
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-
2012
- 2012-02-23 EP EP12749668.5A patent/EP2678016B1/en not_active Not-in-force
- 2012-02-23 WO PCT/US2012/026406 patent/WO2012116237A2/en not_active Ceased
- 2012-02-23 US US14/001,143 patent/US9127000B2/en not_active Expired - Fee Related
- 2012-02-23 JP JP2013555580A patent/JP5808826B2/ja not_active Expired - Fee Related
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