JP2014506601A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- 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.)
- Granted
Links
- 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 (83)
| 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 |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| ES2689429T3 (es) | 2012-07-13 | 2018-11-14 | Ucb Biopharma Sprl | Derivados de imidazopiridina como moduladores de actividad de TNF |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| JP6434416B2 (ja) | 2012-11-08 | 2018-12-05 | ライゼン・ファーマシューティカルズ・エスアー | PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| WO2015123437A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| WO2015123408A1 (en) | 2014-02-13 | 2015-08-20 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| TWI664164B (zh) | 2014-02-13 | 2019-07-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| PE20161573A1 (es) | 2014-02-13 | 2017-01-19 | Incyte Corp | Ciclopropilamina como inhibidor de la lsd1 |
| US9695168B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]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 |
| US9695180B2 (en) | 2014-07-10 | 2017-07-04 | Incyte Corporation | Substituted imidazo[1,2-a]pyrazines 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 |
| US20170333435A1 (en) | 2014-11-06 | 2017-11-23 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| WO2016073891A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| KR102662215B1 (ko) | 2014-11-06 | 2024-05-02 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 |
| JP6568588B2 (ja) | 2014-12-19 | 2019-08-28 | ヤンセン ファーマシューティカ エヌ.ベー. | PI3Kβ阻害剤としてのイミダゾピリダジン誘導体 |
| SI3233839T1 (sl) | 2014-12-19 | 2019-12-31 | Janssen Pharmaceutica Nv | Heterociklil vezani derivati imidazopiridazina kot inhibitorji PI3Kbeta |
| JP6385584B2 (ja) | 2014-12-24 | 2018-09-05 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のための縮合ピリミジン化合物 |
| TWI770552B (zh) | 2014-12-24 | 2022-07-11 | 美商基利科學股份有限公司 | 喹唑啉化合物 |
| PT3237397T (pt) | 2014-12-24 | 2019-02-08 | Gilead Sciences Inc | Compostos de isoquinolina para o tratamento de hiv |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MY191796A (en) | 2015-04-03 | 2022-07-15 | Incyte Corp | Heterocyclic compounds as lsd1 inhibitors |
| HK1255074A1 (zh) | 2015-07-01 | 2019-08-02 | Crinetics Pharmaceuticals, Inc. | 生长抑素调节剂及其用途 |
| KR102710120B1 (ko) | 2015-08-12 | 2024-09-27 | 인사이트 홀딩스 코포레이션 | Lsd1 저해제의 염 |
| 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 |
| PT3436461T (pt) | 2016-03-28 | 2024-01-23 | Incyte Corp | Compostos de pirrolotriazina como inibidores de tam |
| US11192892B2 (en) | 2016-04-06 | 2021-12-07 | Bial—R&D Investments, S.A. | Substituted pyrazolo[1,5-a]pyrimidines for the treatment of medical disorders |
| JP7034935B2 (ja) | 2016-04-06 | 2022-03-14 | リソソーマル・セラピューティクス・インコーポレイテッド | ピロロ[1,2-a]ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 |
| WO2017176961A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| PE20190377A1 (es) | 2016-04-22 | 2019-03-08 | Incyte Corp | Formulaciones de un inhibidor de lsd 1 |
| WO2017192930A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| JP7149854B2 (ja) | 2016-06-16 | 2022-10-07 | ヤンセン ファーマシューティカ エヌ.ベー. | Pi3k beta阻害薬としての二環式ピリジン、ピラジンおよびピリミジン誘導体 |
| ES2818620T3 (es) | 2016-06-16 | 2021-04-13 | Janssen Pharmaceutica Nv | Derivados de azabencimidazol como inhibidores de pi3k beta |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| AU2017296289A1 (en) | 2016-07-12 | 2019-01-31 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric SHP2 inhibitors |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ,インコーポレイテッド | アロステリックshp2阻害剤としての二環式化合物 |
| CN110431134A (zh) | 2017-01-23 | 2019-11-08 | 锐新医药公司 | 作为变构shp2抑制剂的吡啶化合物 |
| CN110461827A (zh) | 2017-03-29 | 2019-11-15 | 詹森药业有限公司 | 作为PI3K-β抑制剂的喹喔啉和吡啶并吡嗪衍生物 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2019023278A1 (en) | 2017-07-25 | 2019-01-31 | Crinetics Pharmaceuticals, Inc. | MODULATORS OF SOMATOSTATIN AND USES THEREOF |
| EP3694848A1 (en) | 2017-10-12 | 2020-08-19 | 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 |
| TW201927791A (zh) | 2017-12-15 | 2019-07-16 | 美商銳新醫藥公司 | 作為變構shp2抑制劑的多環化合物 |
| WO2019168847A1 (en) | 2018-02-27 | 2019-09-06 | Incyte Corporation | Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors |
| EP3788046B1 (en) | 2018-05-04 | 2025-12-10 | Incyte Corporation | Salts of an fgfr inhibitor |
| EP4309737A3 (en) | 2018-05-04 | 2024-03-27 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| US11168089B2 (en) | 2018-05-18 | 2021-11-09 | Incyte Corporation | Fused pyrimidine derivatives as A2A / A2B inhibitors |
| JP7768505B2 (ja) | 2018-06-01 | 2025-11-12 | コーネル・ユニバーシティー | Pi3kに関連する疾患または障害に対する併用療法 |
| JOP20200342A1 (ar) | 2018-07-05 | 2020-12-30 | Incyte Corp | مشتقات بيرازين مدمجة كمثبطات a2a/a2b |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11884647B2 (en) | 2019-10-18 | 2024-01-30 | The Regents Of The University Of California | Compounds and methods for targeting pathogenic blood vessels |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021257863A1 (en) | 2020-06-19 | 2021-12-23 | Incyte Corporation | Pyrrolotriazine compounds as jak2 v617f inhibitors |
| US11691971B2 (en) | 2020-06-19 | 2023-07-04 | Incyte Corporation | Naphthyridinone compounds as JAK2 V617F inhibitors |
| US11767323B2 (en) | 2020-07-02 | 2023-09-26 | Incyte Corporation | Tricyclic pyridone compounds as JAK2 V617F inhibitors |
| IL299612A (en) | 2020-07-02 | 2023-03-01 | Incyte Corp | Tricyclic urea compounds as JAK2 V617F inhibitors |
| US11661422B2 (en) | 2020-08-27 | 2023-05-30 | Incyte Corporation | Tricyclic urea compounds as JAK2 V617F inhibitors |
| WO2022140231A1 (en) | 2020-12-21 | 2022-06-30 | Incyte Corporation | Deazaguaine compounds as jak2 v617f inhibitors |
| US11958861B2 (en) | 2021-02-25 | 2024-04-16 | Incyte Corporation | Spirocyclic lactams as JAK2 V617F inhibitors |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4493558A1 (en) | 2022-03-17 | 2025-01-22 | Incyte Corporation | Tricyclic urea compounds as jak2 v617f inhibitors |
| WO2023239846A1 (en) * | 2022-06-10 | 2023-12-14 | Synnovation Therapeutics, Inc. | Heterocyclic compounds as pi3kα inhibitors |
| CN116425743B (zh) * | 2022-12-30 | 2025-06-17 | 贵州医科大学 | 一种作为PI3Kα激酶抑制剂的苯并杂环类化合物及其制备方法与应用 |
Family Cites Families (193)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2313993A (en) | 1939-02-04 | 1943-03-16 | Chromogen Inc | Organic sulphur and selenium compounds |
| GB1219606A (en) | 1968-07-15 | 1971-01-20 | Rech S Et D Applic Scient Soge | Quinuclidinol derivatives and preparation thereof |
| US3657744A (en) | 1970-05-08 | 1972-04-25 | Univ Minnesota | Method for fixing prosthetic implants in a living body |
| FR2102541A5 (enExample) | 1970-08-07 | 1972-04-07 | Aquitaine Total Organico | |
| US4733665C2 (en) | 1985-11-07 | 2002-01-29 | Expandable Grafts Partnership | Expandable intraluminal graft and method and apparatus for implanting an expandable intraluminal graft |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| US5061273A (en) | 1989-06-01 | 1991-10-29 | Yock Paul G | Angioplasty apparatus facilitating rapid exchanges |
| US5350395A (en) | 1986-04-15 | 1994-09-27 | Yock Paul G | Angioplasty apparatus facilitating rapid exchanges |
| US5040548A (en) | 1989-06-01 | 1991-08-20 | Yock Paul G | Angioplasty mehtod |
| US4748982A (en) | 1987-01-06 | 1988-06-07 | Advanced Cardiovascular Systems, Inc. | Reinforced balloon dilatation catheter with slitted exchange sleeve and method |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| CA1322628C (en) | 1988-10-04 | 1993-10-05 | Richard A. Schatz | Expandable intraluminal graft |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| GB8916480D0 (en) | 1989-07-19 | 1989-09-06 | Glaxo Group Ltd | Chemical process |
| US5674278A (en) | 1989-08-24 | 1997-10-07 | Arterial Vascular Engineering, Inc. | Endovascular support device |
| US6344053B1 (en) | 1993-12-22 | 2002-02-05 | Medtronic Ave, Inc. | Endovascular support device and method |
| US5292331A (en) | 1989-08-24 | 1994-03-08 | Applied Vascular Engineering, Inc. | Endovascular support device |
| GB8923590D0 (en) | 1989-10-19 | 1989-12-06 | Pfizer Ltd | Antimuscarinic bronchodilators |
| US5395855A (en) | 1990-05-07 | 1995-03-07 | Ciba-Geigy Corporation | Hydrazones |
| US5614519A (en) | 1991-02-06 | 1997-03-25 | Karl Thomae Gmbh | (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists |
| PT100441A (pt) | 1991-05-02 | 1993-09-30 | Smithkline Beecham Corp | Pirrolidinonas, seu processo de preparacao, composicoes farmaceuticas que as contem e uso |
| US5710158A (en) | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5480883A (en) | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| US5451700A (en) | 1991-06-11 | 1995-09-19 | Ciba-Geigy Corporation | Amidino compounds, their manufacture and methods of treatment |
| NZ243082A (en) | 1991-06-28 | 1995-02-24 | Ici Plc | 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof |
| AU661533B2 (en) | 1992-01-20 | 1995-07-27 | Astrazeneca Ab | Quinazoline derivatives |
| WO1993019749A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating allergic and inflammatory diseases |
| JP3192424B2 (ja) | 1992-04-02 | 2001-07-30 | スミスクライン・ビーチャム・コーポレイション | アレルギーまたは炎症疾患の治療用化合物 |
| WO1993019751A1 (en) | 1992-04-02 | 1993-10-14 | Smithkline Beecham Corporation | Compounds useful for treating inflammatory diseases and inhibiting production of tumor necrosis factor |
| TW225528B (enExample) | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| AU687727B2 (en) | 1992-10-28 | 1998-03-05 | Genentech Inc. | Vascular endothelial cell growth factor antagonists |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| GB9301000D0 (en) | 1993-01-20 | 1993-03-10 | Glaxo Group Ltd | Chemical compounds |
| GB9314893D0 (en) | 1993-07-19 | 1993-09-01 | Zeneca Ltd | Quinazoline derivatives |
| US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
| GB9414193D0 (en) | 1994-07-14 | 1994-08-31 | Glaxo Group Ltd | Compounds |
| GB9414208D0 (en) | 1994-07-14 | 1994-08-31 | Glaxo Group Ltd | Compounds |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| EP0817775B1 (en) | 1995-03-30 | 2001-09-12 | Pfizer Inc. | Quinazoline derivatives |
| FI973974A7 (fi) | 1995-04-20 | 1997-10-16 | Pfizer | Aryylisulfonyylihydroksaamihappojohdannaisia MMP- ja TNF-inhibiittorei na |
| GB9508538D0 (en) | 1995-04-27 | 1995-06-14 | Zeneca Ltd | Quinazoline derivatives |
| US5747498A (en) | 1996-05-28 | 1998-05-05 | Pfizer Inc. | Alkynyl and azido-substituted 4-anilinoquinazolines |
| US5880141A (en) | 1995-06-07 | 1999-03-09 | Sugen, Inc. | Benzylidene-Z-indoline compounds for the treatment of disease |
| ATE212993T1 (de) | 1995-07-06 | 2002-02-15 | Novartis Erfind Verwalt Gmbh | Pyrolopyrimidine und verfahren zu ihrer herstellung |
| DE69624081T2 (de) | 1995-12-20 | 2003-06-12 | Agouron Pharmaceuticals, Inc. | Matrix-metalloprotease Inhibitoren |
| US5760041A (en) | 1996-02-05 | 1998-06-02 | American Cyanamid Company | 4-aminoquinazoline EGFR Inhibitors |
| GB9603095D0 (en) | 1996-02-14 | 1996-04-10 | Zeneca Ltd | Quinazoline derivatives |
| EP0892789B2 (en) | 1996-04-12 | 2009-11-18 | Warner-Lambert Company LLC | Irreversible inhibitors of tyrosine kinases |
| DE69734513T2 (de) | 1996-06-24 | 2006-07-27 | Pfizer Inc. | Phenylamino-substituierte tricyclische derivate zur behandlung hyperproliferativer krankheiten |
| HUP9903014A3 (en) | 1996-07-18 | 2000-08-28 | Pfizer | Phosphinate derivatives having matrix metalloprotease inhibitor effect and medicaments containing the same |
| IL128189A0 (en) | 1996-08-23 | 1999-11-30 | Pfizer | Arylsulfonylamino hydroxamic acid derivatives |
| DE19638745C2 (de) | 1996-09-11 | 2001-05-10 | Schering Ag | Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR) |
| AU4342997A (en) | 1996-09-13 | 1998-04-02 | Sugen, Inc. | Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders |
| EP0837063A1 (en) | 1996-10-17 | 1998-04-22 | Pfizer Inc. | 4-Aminoquinazoline derivatives |
| GB9622386D0 (en) | 1996-10-28 | 1997-01-08 | Sandoz Ltd | Organic compounds |
| TW528755B (en) | 1996-12-24 | 2003-04-21 | Glaxo Group Ltd | 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives |
| ES2224277T3 (es) | 1997-01-06 | 2005-03-01 | Pfizer Inc. | Derivados de sulfonas ciclicas. |
| PT977733E (pt) | 1997-02-03 | 2003-12-31 | Pfizer Prod Inc | Derivados de acido arilsulfonilamino-hidroxamico |
| JP2000507975A (ja) | 1997-02-07 | 2000-06-27 | ファイザー・インク | N−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用 |
| IL131123A0 (en) | 1997-02-11 | 2001-01-28 | Pfizer | Arylsulfonyl hydroxamic acid derivatives |
| CO4950519A1 (es) | 1997-02-13 | 2000-09-01 | Novartis Ag | Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion |
| CO4940418A1 (es) | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
| ES2216293T3 (es) | 1997-08-08 | 2004-10-16 | Pfizer Products Inc. | Derivados de acido ariloxiarilsulfonilamino-hidroxamico. |
| US6166037A (en) | 1997-08-28 | 2000-12-26 | Merck & Co., Inc. | Pyrrolidine and piperidine modulators of chemokine receptor activity |
| WO1999016766A1 (en) | 1997-10-01 | 1999-04-08 | Kyowa Hakko Kogyo Co., Ltd. | Benzodioxole derivatives |
| GB9723566D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB9723590D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB9723589D0 (en) | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| YU44900A (sh) | 1998-01-31 | 2003-01-31 | Glaxo Group Limited | Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola |
| PE20000270A1 (es) | 1998-02-14 | 2000-05-20 | Glaxo Group Ltd | Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| GB9813535D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| GB9813565D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| YU81100A (sh) | 1998-06-23 | 2003-10-31 | Glaxo Group Limited | Derivati 2-(purin-9-il)tetrahidrofuran-3,4 diola |
| GB9813540D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| DE69827673T2 (de) | 1998-06-30 | 2005-04-21 | Dow Global Technologies Inc | Polymerpolyole und ein verfahren zu ihrer darstellung |
| CN1152031C (zh) | 1998-08-11 | 2004-06-02 | 诺瓦提斯公司 | 具有血管生成抑制活性的异喹啉衍生物 |
| EP1121372B1 (en) | 1998-10-16 | 2006-06-28 | Pfizer Limited | Adenine derivatives |
| UA71587C2 (uk) | 1998-11-10 | 2004-12-15 | Шерінг Акцієнгезелльшафт | Аміди антранілової кислоти та їхнє застосування як лікарських засобів |
| GB9824579D0 (en) | 1998-11-10 | 1999-01-06 | Novartis Ag | Organic compounds |
| ATE300957T1 (de) | 1998-12-22 | 2005-08-15 | Genentech Inc | Antagonisten von vaskular-endothelialen zellwachstumsfaktoren und ihre anwendung |
| PT1165085E (pt) | 1999-03-30 | 2006-10-31 | Novartis Ag | Derivados de ftalazina para tratar doencas inflamatorias |
| GB9913083D0 (en) | 1999-06-04 | 1999-08-04 | Novartis Ag | Organic compounds |
| EP1175402B1 (en) | 1999-05-04 | 2005-07-20 | Schering Corporation | Piperidine derivatives useful as ccr5 antagonists |
| CZ20013940A3 (cs) | 1999-05-04 | 2002-04-17 | Schering Corporation | Piperazinové deriváty uľitečné jako CCR5 antagonisté |
| YU25500A (sh) | 1999-05-11 | 2003-08-29 | Pfizer Products Inc. | Postupak za sintezu analoga nukleozida |
| GB9913932D0 (en) | 1999-06-15 | 1999-08-18 | Pfizer Ltd | Purine derivatives |
| US6322771B1 (en) | 1999-06-18 | 2001-11-27 | University Of Virginia Patent Foundation | Induction of pharmacological stress with adenosine receptor agonists |
| ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
| SI1212089T1 (sl) | 1999-08-21 | 2006-08-31 | Altana Pharma Ag | Sinergisticna kombinacija roflumilasta in salmeterola |
| CO5180581A1 (es) | 1999-09-30 | 2002-07-30 | Pfizer Prod Inc | Compuestos para el tratamiento de la isquemia ciones farmaceuticas que los contienen para el tratamiento de la isquemia |
| GB9924363D0 (en) | 1999-10-14 | 1999-12-15 | Pfizer Central Res | Purine derivatives |
| GB9924361D0 (en) | 1999-10-14 | 1999-12-15 | Pfizer Ltd | Purine derivatives |
| GB0003960D0 (en) | 2000-02-18 | 2000-04-12 | Pfizer Ltd | Purine derivatives |
| WO2001081346A2 (en) | 2000-04-25 | 2001-11-01 | Icos Corporation | Inhibitors of human phosphatidyl-inositol 3-kinase delta |
| TWI227240B (en) | 2000-06-06 | 2005-02-01 | Pfizer | 2-aminocarbonyl-9H-purine derivatives |
| BR0112297A (pt) | 2000-06-27 | 2003-05-06 | S A L V A T Lab Sa | Compostos carbamatos derivados de arilalquilaminas |
| GB0015727D0 (en) | 2000-06-27 | 2000-08-16 | Pfizer Ltd | Purine derivatives |
| GB0015876D0 (en) | 2000-06-28 | 2000-08-23 | Novartis Ag | Organic compounds |
| DE10038639A1 (de) | 2000-07-28 | 2002-02-21 | Schering Ag | Nichtsteroidale Entzündungshemmer |
| CO5310534A1 (es) | 2000-08-05 | 2003-08-29 | Glaxo Group Ltd | Nuevos derivados de androstano anti-inflamatorios |
| PE20020354A1 (es) | 2000-09-01 | 2002-06-12 | Novartis Ag | Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda) |
| GB0022695D0 (en) | 2000-09-15 | 2000-11-01 | Pfizer Ltd | Purine Derivatives |
| GB0028383D0 (en) | 2000-11-21 | 2001-01-03 | Novartis Ag | Organic compounds |
| SI1341769T1 (sl) | 2000-12-15 | 2008-02-29 | Vertex Pharma | Inhibitorji bakterijske giraze in njihove uporabe |
| EP1345937B1 (en) | 2000-12-22 | 2005-09-28 | Almirall Prodesfarma AG | Quinuclidine carbamate derivatives and their use as m3 antagonists |
| EE05404B1 (et) | 2000-12-28 | 2011-04-15 | Almirall Prodesfarma Ag | Kinuklidiini derivaat, selle saamine ja kasutamine ravimi valmistamiseks, mis on ette nhtud respiratoorsete, kuseelundite v?i mao-soolte haiguste ravimiseks, ning seda sisaldav ravimkompositsioon |
| EP1241176A1 (en) | 2001-03-16 | 2002-09-18 | Pfizer Products Inc. | Purine derivatives for the treatment of ischemia |
| ES2314052T3 (es) | 2001-04-30 | 2009-03-16 | Glaxo Group Limited | Derivados de ester de 17beta-carbotioato de androstano con un grupo ester ciclico en la posicion 17alfa. |
| AR035885A1 (es) | 2001-05-14 | 2004-07-21 | Novartis Ag | Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica |
| BR0209986A (pt) | 2001-05-25 | 2004-04-06 | Pfizer | Agonista de a2a em combinação com um agente anticolinérgico, para o tratamento de doenças obstrutivas das vias respiratórias |
| US20040248867A1 (en) | 2001-06-12 | 2004-12-09 | Keith Biggadike | Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives |
| DK2327766T3 (en) | 2001-06-21 | 2016-03-07 | Basf Enzymes Llc | nitrilases |
| GB0119249D0 (en) | 2001-08-07 | 2001-10-03 | Novartis Ag | Organic compounds |
| IL160896A0 (en) | 2001-10-17 | 2004-08-31 | Ucb Sa | Quinuclidine derivatives, processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors |
| GB0125259D0 (en) | 2001-10-20 | 2001-12-12 | Glaxo Group Ltd | Novel compounds |
| MY130622A (en) | 2001-11-05 | 2007-07-31 | Novartis Ag | Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (pde4) inhibitors |
| WO2003048181A1 (en) | 2001-12-01 | 2003-06-12 | Glaxo Group Limited | 17.alpha. -cyclic esters of 16-methylpregnan-3,20-dione as anti-inflammatory agents |
| PL211250B1 (pl) | 2001-12-20 | 2012-04-30 | Chiesi Farma Spa | Pochodne karbaminianu 1-alkilo-1-azoniabicyklo [2.2.2] oktanu, jej zastosowania, kompozycja farmaceutyczna zawierająca ten związek oraz związek pośredni |
| WO2003072592A1 (en) | 2002-01-15 | 2003-09-04 | Glaxo Group Limited | 17.alpha-cycloalkyl/cycloylkenyl esters of alkyl-or haloalkyl-androst-4-en-3-on-11.beta.,17.alpha.-diol 17.beta.-carboxylates as anti-inflammatory agents |
| WO2003062259A2 (en) | 2002-01-21 | 2003-07-31 | Glaxo Group Limited | Non-aromatic 17.alpha.-esters of androstane-17.beta.-carboxylate esters as anti-inflammatory agents |
| GB0202216D0 (en) | 2002-01-31 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
| EP1490317A1 (en) | 2002-03-26 | 2004-12-29 | Boehringer Ingelheim Pharmaceuticals Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| HRP20040887A2 (en) | 2002-03-26 | 2005-04-30 | Boehringer Ingelheim Pharmaceuticals Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| US20090170803A1 (en) | 2002-04-10 | 2009-07-02 | Linden Joel M | Adjunctive treatment of biological diseases |
| ES2206021B1 (es) | 2002-04-16 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de pirrolidinio. |
| ES2201907B1 (es) | 2002-05-29 | 2005-06-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de indolilpiperidina como potentes agentes antihistaminicos y antialergicos. |
| DE10224888A1 (de) | 2002-06-05 | 2003-12-24 | Merck Patent Gmbh | Pyridazinderivate |
| US7074806B2 (en) | 2002-06-06 | 2006-07-11 | Boehringer Ingelheim Pharmaceuticals, Inc. | Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof |
| DE10225574A1 (de) | 2002-06-10 | 2003-12-18 | Merck Patent Gmbh | Aryloxime |
| DE10227269A1 (de) | 2002-06-19 | 2004-01-08 | Merck Patent Gmbh | Thiazolderivate |
| AU2003243870B2 (en) | 2002-06-25 | 2008-11-20 | Merck Frosst Canada Ltd | 8-(biaryl) quinoline PDE4 inhibitors |
| AU2003281219A1 (en) | 2002-07-02 | 2004-01-23 | Bernard Cote | Di-aryl-substituted-ethane pyridone pde4 inhibitors |
| ES2204295B1 (es) | 2002-07-02 | 2005-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de quinuclidina-amida. |
| AU2003281355A1 (en) | 2002-07-08 | 2004-01-23 | Pfizer Products Inc. | Modulators of the glucocorticoid receptor |
| AR040962A1 (es) | 2002-08-09 | 2005-04-27 | Novartis Ag | Compuestos derivados de tiazol 1,3-2-ona, composicion farmaceutica y proceso de preparacion del compuesto |
| AU2003260371A1 (en) | 2002-08-10 | 2004-03-11 | Altana Pharma Ag | Piperidine-n-oxide-derivatives |
| AU2003251693A1 (en) | 2002-08-10 | 2004-03-11 | Altana Pharma Ag | Pyridazinone-derivatives as pde4 inhibitors |
| BR0313330A (pt) | 2002-08-10 | 2005-06-14 | Altana Pharma Ag | Piperidina-ftalazonas substituìdas com pirrolidinadiona como inibidores de pde4 |
| WO2004018449A1 (en) | 2002-08-10 | 2004-03-04 | Altana Pharma Ag | Piperidine-derivatives as pde4 inhibitors |
| PL373598A1 (en) | 2002-08-17 | 2005-09-05 | Altana Pharma Ag | Novel benzonaphthyridines |
| WO2004018431A2 (en) | 2002-08-17 | 2004-03-04 | Altana Pharma Ag | Novel phenanthridines |
| SE0202483D0 (sv) | 2002-08-21 | 2002-08-21 | Astrazeneca Ab | Chemical compounds |
| ATE423769T1 (de) | 2002-08-23 | 2009-03-15 | Ranbaxy Lab Ltd | Fluor- und sulfonylaminohaltige, 3,6- disubstituierte azabicyclo 3.1.0 hexanderivate als muscarinrezeptorantagonisten |
| JP4587295B2 (ja) | 2002-08-29 | 2010-11-24 | ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング | Pde4インヒビターとしての3−ヒドロキシ−6−フェニルフェナントリジン |
| AU2003255493B8 (en) | 2002-08-29 | 2009-03-26 | Takeda Gmbh | 2-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors |
| JP2006096662A (ja) | 2002-09-18 | 2006-04-13 | Sumitomo Pharmaceut Co Ltd | 新規6−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| KR20050057408A (ko) | 2002-09-18 | 2005-06-16 | 오노 야꾸힝 고교 가부시키가이샤 | 트리아자스피로[5.5]운데칸 유도체 및 이를 유효 성분으로하는 약제 |
| JP2004107299A (ja) | 2002-09-20 | 2004-04-08 | Japan Energy Corp | 新規1−置換ウラシル誘導体及びアレルギー性疾患の治療剤 |
| DE10246374A1 (de) | 2002-10-04 | 2004-04-15 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Betamimetika mit verlängerter Wirkungsdauer, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| ATE380185T1 (de) | 2002-10-23 | 2007-12-15 | Glenmark Pharmaceuticals Ltd | Tricyclische verbindungen zur behandlung von entzündlichen- und allergischen erkrankungen: verfahren zu deren herstellung und sie enthaltende pharmazeutische zusammensetzungen |
| GB0225535D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| GB0225540D0 (en) | 2002-11-01 | 2002-12-11 | Glaxo Group Ltd | Medicinal compounds |
| DE10253282A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung |
| DE10253220A1 (de) | 2002-11-15 | 2004-05-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Dihydroxy-Methyl-Phenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE10253426B4 (de) | 2002-11-15 | 2005-09-22 | Elbion Ag | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
| AU2004259012C1 (en) | 2003-07-23 | 2012-08-02 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
| AR046845A1 (es) | 2003-11-21 | 2005-12-28 | Novartis Ag | Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas |
| KR100629060B1 (ko) | 2004-08-11 | 2006-09-26 | 주식회사 엘지화학 | 새로운 벤즈이미다졸계 화합물 |
| AU2005293607A1 (en) | 2004-10-07 | 2006-04-20 | Boehringer Ingelheim International Gmbh | PI3 kinases |
| CN101384586A (zh) | 2006-02-14 | 2009-03-11 | 诺华公司 | Pi-3激酶抑制剂及其应用方法 |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| WO2007127175A2 (en) | 2006-04-26 | 2007-11-08 | F. Hoffmann-La Roche Ag | Pharmaceutical compounds |
| PL2057148T3 (pl) | 2006-07-31 | 2010-06-30 | Rottapharm Spa | Amidynowe pochodne 2-heteroarylochinazolin i chinolin, silne środki przeciwbólowe i środki przeciwzapalne |
| JP5095736B2 (ja) | 2006-08-03 | 2012-12-12 | ロッタファルム・ソシエタ・ペル・アチオニ | 6−1h−イミダゾ−キナゾリンおよびキノリン誘導体、新規有効鎮痛剤および抗炎症剤 |
| MX2009002171A (es) | 2006-08-30 | 2009-05-28 | Cellzome Ltd | Derivados de triazol como inhibidores de cinasas. |
| US20080234262A1 (en) | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| WO2008118486A1 (en) | 2007-03-27 | 2008-10-02 | Sandisk 3D, Llc | Memory cell comprising a carbon nanotube fabric element and a steering element and methods of forming the same |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| WO2008152394A1 (en) | 2007-06-12 | 2008-12-18 | F.Hoffmann-La Roche Ag | Pharmaceutical compounds |
| ES2401557T3 (es) | 2007-08-02 | 2013-04-22 | Amgen, Inc | Moduladores de Pl3 cinasas y métodos de uso |
| EP2217601A1 (en) | 2007-11-08 | 2010-08-18 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Imidazopyridazines for use as protein kinase inhibitors |
| WO2009068482A1 (en) | 2007-11-27 | 2009-06-04 | Cellzome Limited | Amino triazoles as pi3k inhibitors |
| US8153813B2 (en) | 2007-12-20 | 2012-04-10 | Abbott Laboratories | Benzothiazole and benzooxazole derivatives and methods of use |
| CN101981037B (zh) | 2008-01-30 | 2013-09-04 | 吉宁特有限公司 | 吡唑并嘧啶pi3k抑制剂化合物及使用方法 |
| US20090192176A1 (en) | 2008-01-30 | 2009-07-30 | Wyeth | 1H-PYRAZOLO[3,4-D]PYRIMIDINE, PURINE, 7H-PURIN-8(9H)-ONE, 3H-[1,2,3]TRIAZOLO[4,5-D]PYRIMIDINE, AND THIENO[3,2-D]PYRIMIDINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES |
| JP2011525535A (ja) * | 2008-06-24 | 2011-09-22 | 武田薬品工業株式会社 | PI3K/mTOR阻害剤 |
| KR20110039558A (ko) * | 2008-07-18 | 2011-04-19 | 사노피-아벤티스 | 신규 트리아졸로(4,3-a)피리딘 유도체, 그의 제조 방법, 의약으로서의 그의 용도, 제약 조성물, 및 특히 met 억제제로서의 신규 용도 |
| CA2738429C (en) * | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| US8476282B2 (en) | 2008-11-03 | 2013-07-02 | Intellikine Llc | Benzoxazole kinase inhibitors and methods of use |
| EP3123864A1 (en) | 2008-12-08 | 2017-02-01 | Gilead Connecticut, Inc. | Imidazopyrazine syk inhibitors |
| US8491869B2 (en) | 2009-03-23 | 2013-07-23 | Eli Lilly And Company | Imaging agents for detecting neurological disorders |
| JP2012526836A (ja) * | 2009-05-13 | 2012-11-01 | アムジエン・インコーポレーテツド | Pikk阻害薬としてのヘテロアリール化合物 |
| CN102459248A (zh) * | 2009-05-26 | 2012-05-16 | 埃克塞里艾克西斯公司 | 作为PI3K/mTOR抑制剂的苯并氧杂环庚三烯以及它们使用与制造方法 |
| UA111579C2 (uk) | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
| CN103153062B (zh) | 2010-05-24 | 2015-07-15 | 因特利凯有限责任公司 | 杂环化合物及其用途 |
| TWI592411B (zh) | 2011-02-23 | 2017-07-21 | 英特爾立秦有限責任公司 | 激酶抑制劑之組合及其用途 |
-
2012
- 2012-02-23 EP EP12749668.5A patent/EP2678016B1/en not_active Not-in-force
- 2012-02-23 JP JP2013555580A patent/JP5808826B2/ja not_active Expired - Fee Related
- 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
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014506601A5 (enExample) | ||
| JP2013502423A5 (enExample) | ||
| JP2012526143A5 (enExample) | ||
| Paul et al. | Synthesis and in vitro antitumor evaluation of primary amine substituted quinazoline linked benzimidazole | |
| KR101958501B1 (ko) | 설폭시민기 함유 4-아릴-n-페닐-1,3,5-트리아진-2-아민 | |
| Al-Sanea et al. | Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights | |
| Ferroni et al. | 1, 4-Substituted triazoles as nonsteroidal anti-androgens for prostate cancer treatment | |
| Amin et al. | New series of 6-substituted coumarin derivatives as effective factor Xa inhibitors: Synthesis, in vivo antithrombotic evaluation and molecular docking | |
| Li et al. | Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines | |
| Vasbinder et al. | Discovery and optimization of a novel series of potent mutant B-RafV600E selective kinase inhibitors | |
| GEP201706639B (en) | Heterocyclic compounds and uses thereof | |
| AU2019372121A1 (en) | Heterocyclic compounds as BET inhibitors | |
| Yu et al. | Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines | |
| Raghav et al. | Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H | |
| ATE532780T1 (de) | Chinoline und ihre therapeutische verwendung | |
| Czako et al. | Discovery of IACS-9439, a potent, exquisitely selective, and orally bioavailable inhibitor of CSF1R | |
| Saidahmatov et al. | Discovery of Novel 2-Aminopyridine-Based and 2-Aminopyrimidine-Based Derivatives as Potent CDK/HDAC Dual Inhibitors for the Treatment of Refractory Solid Tumors and Hematological Malignancies | |
| Ochiana et al. | Repurposing Human PDE 4 Inhibitors for Neglected Tropical Diseases. Evaluation of Analogs of the Human PDE 4 Inhibitor GSK‐256066 as Inhibitors of PDEB 1 of Trypanosoma brucei | |
| Feng et al. | Synthesis and biological evaluation of 4-(piperid-3-yl) amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors | |
| WO2014086964A1 (en) | New derivatives of indole for the treatment of cancer, viral infections and lung diseases | |
| Jawed Ahsan et al. | Synthesis of 2, 5-disubstituted-1, 3, 4-oxadiazole analogs as novel anticancer and antimicrobial agents | |
| CA2964696C (en) | Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfoximine group | |
| Sun et al. | Synthesis and primary anticonvulsant activity evaluation of 6-alkyoxyl-tetrazolo [5, 1-a] phthalazine derivatives | |
| Nilewski et al. | 1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties | |
| Bondock et al. | Tandem synthesis and computational insights into triazole and pyrazole-based pyridine derivatives targeting EGFR-TK in cancer therapy |