JP2013056930A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013056930A5 JP2013056930A5 JP2012257150A JP2012257150A JP2013056930A5 JP 2013056930 A5 JP2013056930 A5 JP 2013056930A5 JP 2012257150 A JP2012257150 A JP 2012257150A JP 2012257150 A JP2012257150 A JP 2012257150A JP 2013056930 A5 JP2013056930 A5 JP 2013056930A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- substituted
- unsubstituted
- group
- 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 36
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 27
- 208000035475 disorder Diseases 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 16
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 11
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 6
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 6
- 208000032839 leukemia Diseases 0.000 claims 6
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 5
- 206010061218 Inflammation Diseases 0.000 claims 5
- 108091000080 Phosphotransferase Proteins 0.000 claims 5
- 201000004681 Psoriasis Diseases 0.000 claims 5
- 208000036142 Viral infection Diseases 0.000 claims 5
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 5
- 230000004054 inflammatory process Effects 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 102000020233 phosphotransferase Human genes 0.000 claims 5
- 208000037244 polycythemia vera Diseases 0.000 claims 5
- 230000009385 viral infection Effects 0.000 claims 5
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 230000033115 angiogenesis Effects 0.000 claims 4
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000030533 eye disease Diseases 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 208000003476 primary myelofibrosis Diseases 0.000 claims 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- PKTQHWKZGFKXGT-UHFFFAOYSA-N 3-bromo-n-tert-butylbenzenesulfonamide Chemical compound CC(C)(C)NS(=O)(=O)C1=CC=CC(Br)=C1 PKTQHWKZGFKXGT-UHFFFAOYSA-N 0.000 claims 2
- OTYZNDKWNPQQJP-UHFFFAOYSA-N 4-(2-pyrrolidin-1-ylethoxy)aniline Chemical compound C1=CC(N)=CC=C1OCCN1CCCC1 OTYZNDKWNPQQJP-UHFFFAOYSA-N 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 208000018084 Bone neoplasm Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 102000042838 JAK family Human genes 0.000 claims 2
- 108091082332 JAK family Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000002231 Muscle Neoplasms Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 239000012043 crude product Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 201000002077 muscle cancer Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- -1 cyano, nitro, amino Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000005254 oxyacyl group Chemical group 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 230000012743 protein tagging Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- KSPFHLWLBKZTOF-UHFFFAOYSA-N CC(C)(C)c1cccc(Nc2nc(Cl)ncc2C)c1 Chemical compound CC(C)(C)c1cccc(Nc2nc(Cl)ncc2C)c1 KSPFHLWLBKZTOF-UHFFFAOYSA-N 0.000 description 1
- XIJQDWHJGDTTCL-UHFFFAOYSA-N CC(CCCC1)N1S(c1cccc(Nc2c(C)cnc(Nc(cc3)ccc3N3CCN(C)CC3)n2)c1)(=O)=O Chemical compound CC(CCCC1)N1S(c1cccc(Nc2c(C)cnc(Nc(cc3)ccc3N3CCN(C)CC3)n2)c1)(=O)=O XIJQDWHJGDTTCL-UHFFFAOYSA-N 0.000 description 1
- RBGUWESBYDZRLM-UHFFFAOYSA-N CC[ClH]c1ncc(C)c(N(C)c(cc2OC)ccc2Cl)n1 Chemical compound CC[ClH]c1ncc(C)c(N(C)c(cc2OC)ccc2Cl)n1 RBGUWESBYDZRLM-UHFFFAOYSA-N 0.000 description 1
- AVOXKMWHDSJKEV-UHFFFAOYSA-N Cc(c(Nc(cc1)ccc1Cl)n1)cnc1Cl Chemical compound Cc(c(Nc(cc1)ccc1Cl)n1)cnc1Cl AVOXKMWHDSJKEV-UHFFFAOYSA-N 0.000 description 1
- PFLCSLXLQSDNBS-UHFFFAOYSA-N Cc(c(Nc(cc1C(F)(F)F)ccc1Cl)n1)cnc1Cl Chemical compound Cc(c(Nc(cc1C(F)(F)F)ccc1Cl)n1)cnc1Cl PFLCSLXLQSDNBS-UHFFFAOYSA-N 0.000 description 1
- VPMZIKZXZUQGRU-UHFFFAOYSA-N Cc(c(Nc(cc1F)ccc1Cl)n1)cnc1Cl Chemical compound Cc(c(Nc(cc1F)ccc1Cl)n1)cnc1Cl VPMZIKZXZUQGRU-UHFFFAOYSA-N 0.000 description 1
- QQVVBQCECZMBDI-UHFFFAOYSA-N Cc(c(Nc1cc(OC)cc(OC)c1)n1)cnc1Cl Chemical compound Cc(c(Nc1cc(OC)cc(OC)c1)n1)cnc1Cl QQVVBQCECZMBDI-UHFFFAOYSA-N 0.000 description 1
- OQJZGYXSRKRKLL-UHFFFAOYSA-N Cc(cn1)c(Nc2ccc3[s]ccc3c2)nc1Cl Chemical compound Cc(cn1)c(Nc2ccc3[s]ccc3c2)nc1Cl OQJZGYXSRKRKLL-UHFFFAOYSA-N 0.000 description 1
- ULUSYRCRCJWMKH-UHFFFAOYSA-N Cc1c(NCc(cc2)c(cc[nH]3)c3c2Cl)nc(Nc(cc2)ccc2N2CCN(C)CC2)nc1 Chemical compound Cc1c(NCc(cc2)c(cc[nH]3)c3c2Cl)nc(Nc(cc2)ccc2N2CCN(C)CC2)nc1 ULUSYRCRCJWMKH-UHFFFAOYSA-N 0.000 description 1
- VRYMNQOAQGCOKO-UHFFFAOYSA-N Cc1c(Nc(cc2)c(cc[nH]3)c3c2Cl)nc(Nc(cc2)ccc2OCCN2CCCC2)nc1 Chemical compound Cc1c(Nc(cc2)c(cc[nH]3)c3c2Cl)nc(Nc(cc2)ccc2OCCN2CCCC2)nc1 VRYMNQOAQGCOKO-UHFFFAOYSA-N 0.000 description 1
- KMTZHIZUSJJWHH-UHFFFAOYSA-N Cc1c(Nc2c(cc[nH]3)c3ccc2)nc(Nc2ccc(CN3CCNCC3)cc2)nc1 Chemical compound Cc1c(Nc2c(cc[nH]3)c3ccc2)nc(Nc2ccc(CN3CCNCC3)cc2)nc1 KMTZHIZUSJJWHH-UHFFFAOYSA-N 0.000 description 1
- JQMLLWAZWNUCKB-UHFFFAOYSA-N Cc1c(Nc2c(cc[nH]3)c3ccc2)nc(Nc2ccc(CN3CCOCC3)cc2)nc1 Chemical compound Cc1c(Nc2c(cc[nH]3)c3ccc2)nc(Nc2ccc(CN3CCOCC3)cc2)nc1 JQMLLWAZWNUCKB-UHFFFAOYSA-N 0.000 description 1
- FYEZWBSZYDCHCA-UHFFFAOYSA-N Cc1cc(C)cc(Nc2nc(Cl)ncc2C)c1 Chemical compound Cc1cc(C)cc(Nc2nc(Cl)ncc2C)c1 FYEZWBSZYDCHCA-UHFFFAOYSA-N 0.000 description 1
- HZYKTMNELNYUID-UHFFFAOYSA-N Cc1cnc(Nc(cc2)ccc2N2CCN(C)CC2)nc1Nc1cc(S(N2CCCC2)(=O)=O)ccc1 Chemical compound Cc1cnc(Nc(cc2)ccc2N2CCN(C)CC2)nc1Nc1cc(S(N2CCCC2)(=O)=O)ccc1 HZYKTMNELNYUID-UHFFFAOYSA-N 0.000 description 1
- GOWPYCGEWFYOCQ-UHFFFAOYSA-N Cc1cnc(Nc(cc2)ccc2N2CCN(C)CC2)nc1Nc1cc(S(NC2CCCC2)(=O)=O)ccc1 Chemical compound Cc1cnc(Nc(cc2)ccc2N2CCN(C)CC2)nc1Nc1cc(S(NC2CCCC2)(=O)=O)ccc1 GOWPYCGEWFYOCQ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73262905P | 2005-11-01 | 2005-11-01 | |
| US60/732,629 | 2005-11-01 | ||
| US83800306P | 2006-08-15 | 2006-08-15 | |
| US60/838,003 | 2006-08-15 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008538935A Division JP5191391B2 (ja) | 2005-11-01 | 2006-10-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013056930A JP2013056930A (ja) | 2013-03-28 |
| JP2013056930A5 true JP2013056930A5 (enExample) | 2013-05-30 |
| JP5814903B2 JP5814903B2 (ja) | 2015-11-17 |
Family
ID=38006192
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008538935A Active JP5191391B2 (ja) | 2005-11-01 | 2006-10-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| JP2012257150A Active JP5814903B2 (ja) | 2005-11-01 | 2012-11-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008538935A Active JP5191391B2 (ja) | 2005-11-01 | 2006-10-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US7528143B2 (enExample) |
| EP (1) | EP1951684B1 (enExample) |
| JP (2) | JP5191391B2 (enExample) |
| KR (2) | KR101494468B1 (enExample) |
| CN (1) | CN103626742B (enExample) |
| AU (1) | AU2006309013B2 (enExample) |
| BR (3) | BR122021011788B1 (enExample) |
| CA (1) | CA2628283C (enExample) |
| CY (2) | CY1118330T1 (enExample) |
| DK (1) | DK1951684T3 (enExample) |
| ES (1) | ES2595636T3 (enExample) |
| FI (1) | FIC20210010I1 (enExample) |
| HU (2) | HUE028987T2 (enExample) |
| IL (1) | IL191167A (enExample) |
| LT (2) | LT1951684T (enExample) |
| MX (2) | MX362412B (enExample) |
| MY (1) | MY167260A (enExample) |
| NL (1) | NL301104I2 (enExample) |
| NO (1) | NO342221B1 (enExample) |
| NZ (2) | NZ567851A (enExample) |
| PL (1) | PL1951684T3 (enExample) |
| PT (1) | PT1951684T (enExample) |
| RU (2) | RU2597364C2 (enExample) |
| TW (1) | TWI444368B (enExample) |
| WO (1) | WO2007053452A1 (enExample) |
Families Citing this family (334)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| IL166241A0 (en) | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| EP1549614A4 (en) * | 2002-10-03 | 2008-04-16 | Targegen Inc | VASCULATORY AGENTS AND METHODS FOR THEIR APPLICATION |
| US20050282814A1 (en) * | 2002-10-03 | 2005-12-22 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| US8178671B2 (en) | 2003-07-30 | 2012-05-15 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds |
| EP2543376A1 (en) * | 2004-04-08 | 2013-01-09 | Targegen, Inc. | Benzotriazine inhibitors of kinases |
| PL382308A1 (pl) | 2004-08-25 | 2007-08-20 | Targegen, Inc. | Związki heterocykliczne i sposoby stosowania |
| EP1856135B1 (en) | 2005-01-19 | 2009-12-09 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| CN105348203B (zh) | 2005-06-08 | 2018-09-18 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| JP2008543775A (ja) * | 2005-06-08 | 2008-12-04 | ターゲジェン インコーポレーティッド | 眼の障害を治療するための方法および組成物 |
| US20070203161A1 (en) * | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| DK1951684T3 (en) * | 2005-11-01 | 2016-10-24 | Targegen Inc | BIARYLMETAPYRIMIDIN kinase inhibitors |
| US8604042B2 (en) * | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| WO2007056023A2 (en) * | 2005-11-02 | 2007-05-18 | Targegen, Inc. | Thiazole inhibitors targeting resistant kinase mutations |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| US8962643B2 (en) | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| WO2007127366A2 (en) * | 2006-04-25 | 2007-11-08 | Targegen, Inc. | Kinase inhibitors and methods of use thereof |
| US8030487B2 (en) * | 2006-07-07 | 2011-10-04 | Targegen, Inc. | 2-amino—5-substituted pyrimidine inhibitors |
| ES2633318T3 (es) | 2006-10-23 | 2017-09-20 | Cephalon, Inc. | Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met |
| JP2010513384A (ja) | 2006-12-22 | 2010-04-30 | エフ．ホフマン−ラ ロシュ アーゲー | スピロ−ピペリジン誘導体 |
| TW200840581A (en) * | 2007-02-28 | 2008-10-16 | Astrazeneca Ab | Novel pyrimidine derivatives |
| KR20090129434A (ko) * | 2007-03-01 | 2009-12-16 | 수퍼젠, 인크. | 피리미딘-2,4-디아민 유도체 및 ｊａｋ2 키나제 억제제로서의 이의 용도 |
| WO2008118822A1 (en) | 2007-03-23 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| 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 |
| JP2010533700A (ja) * | 2007-07-16 | 2010-10-28 | アストラゼネカ アクチボラグ | ピリミジン誘導体 |
| BRPI0814432A2 (pt) | 2007-07-17 | 2017-05-09 | Rigel Pharmaceuticals Inc | pirimidinadiaminas substituídas por amina cíclica como inibidores de pkc |
| US8440681B2 (en) | 2007-08-28 | 2013-05-14 | Irm Llc | 2-biphenylamino-4-aminopyrimidine derivatives as kinase inhibitors |
| EP2219671A4 (en) * | 2007-11-09 | 2011-02-09 | Salk Inst For Biological Studi | USE OF TAM RECEPTOR INHIBITORS AS IMMU ENHANCERS AND TAM ACTIVATORS AS IMMUNOSUPPRESSORS |
| US20100310563A1 (en) * | 2007-11-30 | 2010-12-09 | Bumm Thomas G P | Methods for treating induced cellular proliferative disorders |
| WO2009087127A1 (en) | 2008-01-11 | 2009-07-16 | F. Hoffmann-La Roche Ag | Modulators for amyloid beta |
| AU2009215430B2 (en) * | 2008-02-22 | 2015-02-12 | Rigel Pharmaceuticals, Inc. | Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis |
| ES2428716T3 (es) * | 2008-02-22 | 2013-11-11 | F. Hoffmann-La Roche Ag | Moduladores de beta-amiloide |
| WO2009137052A1 (en) * | 2008-05-05 | 2009-11-12 | Winthrop University Hospital | Method for improving cardiovascular risk profile of cox inhibitors |
| CN102105150B (zh) | 2008-05-21 | 2014-03-12 | 阿里亚德医药股份有限公司 | 用作激酶抑制剂的磷衍生物 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| UY31929A (es) | 2008-06-25 | 2010-01-05 | Irm Llc | Compuestos y composiciones como inhibidores de cinasa |
| NZ624345A (en) | 2008-06-27 | 2016-07-29 | Celgene Avilomics Res Inc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| WO2010011349A2 (en) * | 2008-07-25 | 2010-01-28 | Supergen, Inc. | Pyrimidine-2,4-diamine jak2 kinase inhibiting anti-inflammation use |
| CN102112131A (zh) * | 2008-08-05 | 2011-06-29 | 塔格根公司 | 治疗地中海贫血的方法 |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| JP5502089B2 (ja) | 2008-10-09 | 2014-05-28 | エフ．ホフマン−ラ ロシュ アーゲー | アミロイドβのモジュレーター |
| WO2010052199A1 (en) | 2008-11-10 | 2010-05-14 | F. Hoffmann-La Roche Ag | Heterocyclic gamma secretase modulators |
| US20110245156A1 (en) * | 2008-12-09 | 2011-10-06 | Cytokine Pharmasciences, Inc. | Novel antiviral compounds, compositions, and methods of use |
| WO2010093808A1 (en) | 2009-02-11 | 2010-08-19 | Reaction Biology Corp. | Selective kinase inhibitors |
| CA2757671A1 (en) * | 2009-04-03 | 2010-10-07 | Cellzome Ag | Methods for the identification of kinase interacting molecules and for the purification of kinase proteins |
| CA2758614A1 (en) * | 2009-04-14 | 2010-10-21 | Cellzome Limited | Fluoro substituted pyrimidine compounds as jak3 inhibitors |
| US9908884B2 (en) | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
| TW201040162A (en) * | 2009-05-06 | 2010-11-16 | Portola Pharm Inc | Inhibitors of JAK |
| WO2010135621A1 (en) * | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| ES2487542T3 (es) * | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| PE20120493A1 (es) | 2009-06-29 | 2012-05-20 | Incyte Corp | Pirimidinonas como inhibidores de pi3k |
| JP2012197231A (ja) * | 2009-08-06 | 2012-10-18 | Oncotherapy Science Ltd | Ｔｔｋ阻害作用を有するピリジンおよびピリミジン誘導体 |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| HUE043522T2 (hu) * | 2009-09-04 | 2019-08-28 | Biogen Ma Inc | Bruton tirozinkináz inhibitorok |
| US20120172385A1 (en) * | 2009-09-11 | 2012-07-05 | Richard John Harrison | Ortho substituted pyrimidine compounds as jak inhibitors |
| AU2010295690B2 (en) | 2009-09-16 | 2016-07-28 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| WO2011045702A1 (en) * | 2009-10-15 | 2011-04-21 | Pfizer Inc. | Pyrrolo[2,3-d] pyrimidine compounds |
| EP2501233B1 (en) * | 2009-11-03 | 2014-09-24 | GlaxoSmithKline LLC | Quinazoline compounds |
| WO2011056739A1 (en) * | 2009-11-03 | 2011-05-12 | Glaxosmithkline Llc | Compounds and methods |
| US8772286B2 (en) * | 2009-12-14 | 2014-07-08 | Merck Sharp & Dohme B.V. | MK2 inhibitors |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| CA2782720A1 (en) | 2009-12-18 | 2011-06-23 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine compounds |
| PE20121505A1 (es) * | 2009-12-23 | 2012-11-05 | Medicis Pharmaceutical Corp | Derivados de aminoalquilpirimidina como antagonistas del receptor h4 de histamina |
| KR20130067487A (ko) | 2009-12-30 | 2013-06-25 | 아빌라 테라퓨틱스, 인크. | 단백질의 리간드-지정 공유 변형 |
| MX2012008141A (es) * | 2010-01-13 | 2012-08-03 | Glaxosmithkline Llc | Compuestos y metodos. |
| US8486967B2 (en) | 2010-02-17 | 2013-07-16 | Hoffmann-La Roche Inc. | Heteroaryl substituted piperidines |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| WO2011120911A1 (en) | 2010-03-30 | 2011-10-06 | Novartis Ag | Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| CN103180318B (zh) | 2010-05-14 | 2017-05-10 | 达那-法伯癌症研究所 | 雄性避孕组合物以及使用方法 |
| EP2902030B1 (en) | 2010-05-14 | 2016-09-14 | Dana-Farber Cancer Institute, Inc. | Thienotriazolodiazepine compounds for treating neoplasia |
| WO2011143660A2 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| US8927547B2 (en) | 2010-05-21 | 2015-01-06 | Noviga Research Ab | Pyrimidine derivatives |
| WO2011149827A1 (en) * | 2010-05-24 | 2011-12-01 | Glaxosmithkline Llc | Compounds and methods |
| EP3144298A1 (en) | 2010-08-10 | 2017-03-22 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
| EP2635284B1 (en) | 2010-11-01 | 2019-12-18 | Celgene CAR LLC | Heterocyclic compounds and uses thereof |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| AU2010363329A1 (en) * | 2010-11-07 | 2013-05-09 | Targegen, Inc. | Compositions and methods for treating myelofibrosis |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2012125629A1 (en) * | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| AU2012230229A1 (en) | 2011-03-24 | 2013-10-10 | Noviga Research Ab | Novel pyrimidine derivatives |
| WO2012135009A1 (en) * | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| WO2012135641A2 (en) | 2011-03-30 | 2012-10-04 | H. Lee Moffitt Cancer Center And Research Institute | Aurora kinase inhibitors and methods of making and using thereof |
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| PT2693881T (pt) * | 2011-04-01 | 2019-12-09 | Univ Utah Res Found | Análogos de n-fenilpirimidin-2-amina substituídos como inibidores da axl cinase |
| KR101884010B1 (ko) | 2011-05-04 | 2018-07-31 | 어리어드 파마슈티칼스, 인코포레이티드 | Egfr-유도된 암의 세포 증식을 억제하는 화합물 |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | 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 |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| WO2013059548A1 (en) | 2011-10-19 | 2013-04-25 | Sanofi | Compositions and methods for treating cancer using jak2 inhibitor |
| CA2853498A1 (en) | 2011-10-28 | 2013-05-02 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
| CN102429901B (zh) * | 2011-11-03 | 2013-11-06 | 合肥博太医药生物技术发展有限公司 | 吲哚-3-甲醇、二吲哚甲烷及其衍生物在制备防治肾纤维化药物中的应用 |
| SI2825042T1 (sl) | 2012-03-15 | 2019-01-31 | Celgene Car Llc | Soli inhibitorja kinaze receptorja faktorja epidermalne rasti |
| CN108658873B (zh) | 2012-03-15 | 2021-09-14 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| US20150166591A1 (en) | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| WO2013173720A1 (en) | 2012-05-18 | 2013-11-21 | Incyte Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| EP2858500A4 (en) | 2012-06-08 | 2016-04-06 | Biogen Ma Inc | BRUTON TYROSINE KINASE HEMMER |
| AR091273A1 (es) * | 2012-06-08 | 2015-01-21 | Biogen Idec Inc | Inhibidores de pirimidinil tirosina quinasa |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| SG11201408679XA (en) | 2012-06-26 | 2015-01-29 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| JP6401169B2 (ja) | 2012-10-04 | 2018-10-03 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| 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 |
| PE20151157A1 (es) | 2012-11-15 | 2015-08-19 | Incyte Corp | Formas de dosificacion de ruxolitinib de liberacion sostenida |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EA201591051A1 (ru) | 2013-02-08 | 2016-06-30 | Селджен Авиломикс Рисерч, Инк. | Ингибиторы erk и варианты их применения |
| LT3489239T (lt) | 2013-03-06 | 2022-03-10 | Incyte Holdings Corporation | Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai |
| AU2014236820B2 (en) | 2013-03-14 | 2018-08-02 | Sumitomo Pharma Oncology, Inc. | JAK2 and ALK2 inhibitors and methods for their use |
| WO2014159392A1 (en) | 2013-03-14 | 2014-10-02 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| EP2968358A4 (en) * | 2013-03-15 | 2016-08-10 | Ariad Pharma Inc | NOVEL CHOLINKINASE INHIBITORS |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| US9210831B2 (en) | 2013-04-15 | 2015-12-08 | International Business Machines Corporation | Separable and integrated heat sinks facilitating cooling multi-compnent electronic assembly |
| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| CN105263923B (zh) * | 2013-06-04 | 2017-06-23 | 阿克图拉姆生命科学股份公司 | 嘧啶化合物及它们作为γ分泌酶调节剂的用途 |
| CA2918910A1 (en) | 2013-07-25 | 2015-01-29 | Dana-Farber Cancer Institute, Inc. | Inhibitors of transcription factors and uses thereof |
| CN105592850B (zh) * | 2013-08-06 | 2019-11-15 | H·李·莫菲特癌症中心研究所公司 | Ack1/tnk2酪氨酸激酶的抑制剂 |
| UA120499C2 (uk) | 2013-08-07 | 2019-12-26 | Інсайт Корпорейшн | Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1 |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| EP3066101B1 (en) | 2013-11-08 | 2020-07-29 | Dana-Farber Cancer Institute, Inc. | Combination therapy for cancer using bromodomain and extra-terminal (bet) protein inhibitors |
| KR102413253B1 (ko) | 2013-12-11 | 2022-06-27 | 바이오젠 엠에이 인코포레이티드 | 종양, 신경 및 면역에서 인간 질환을 치료하는데 유용한 바이아릴 화합물 |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| JP2017504650A (ja) | 2014-01-31 | 2017-02-09 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | ジアゼパン誘導体およびその使用 |
| JP2017504651A (ja) | 2014-01-31 | 2017-02-09 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | ジアゼパン誘導体の使用 |
| KR20160115953A (ko) | 2014-01-31 | 2016-10-06 | 다나-파버 캔서 인스티튜트 인크. | 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도 |
| CN106456653A (zh) | 2014-02-28 | 2017-02-22 | 腾沙治疗公司 | 高胰岛素血症相关病症的治疗 |
| ES2921874T3 (es) | 2014-02-28 | 2022-09-01 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
| 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 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| WO2016022460A1 (en) * | 2014-08-03 | 2016-02-11 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Potent dual brd4-kinase inhibitors as cancer therapeutics |
| JP2017526741A (ja) | 2014-08-08 | 2017-09-14 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | ジアゼパン誘導体およびその使用 |
| CN106793775B (zh) | 2014-08-08 | 2020-06-02 | 达纳-法伯癌症研究所股份有限公司 | 二氢碟啶酮衍生物及其用途 |
| EP4578865A3 (en) | 2014-08-12 | 2025-07-30 | Monash University | Lymph directing prodrugs |
| EP3179858B1 (en) | 2014-08-13 | 2019-05-15 | Celgene Car Llc | Forms and compositions of an erk inhibitor |
| TWI679205B (zh) * | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| SG11201703414VA (en) | 2014-10-27 | 2017-05-30 | Tensha Therapeutics Inc | Bromodomain inhibitors |
| US10480375B2 (en) | 2014-10-28 | 2019-11-19 | Cummins Emission Solutions Inc. | SCR conversion efficiency diagnostics |
| CA3220466A1 (en) | 2014-10-29 | 2016-05-06 | Bicyclerd Limited | Bicyclic peptide ligands specific for mt1-mmp |
| 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 |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| PH12017501538B1 (en) | 2015-02-27 | 2024-02-14 | Incyte Holdings Corp | Salts of p13k inhibitor and processes for their preparation |
| ES2930585T3 (es) | 2015-02-27 | 2022-12-19 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| WO2016201370A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| WO2017012559A1 (zh) * | 2015-07-21 | 2017-01-26 | 广州再极医药科技有限公司 | 稠环嘧啶类化合物、中间体、其制备方法、组合物和应用 |
| US10023571B2 (en) | 2015-09-02 | 2018-07-17 | Nimbus Lakshimi, Inc. | TYK2 inhibitors and uses thereof |
| CN108137482B (zh) | 2015-09-08 | 2024-03-15 | 莫纳什大学 | 定向淋巴的前药 |
| WO2017044720A1 (en) | 2015-09-11 | 2017-03-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| PE20181287A1 (es) | 2015-09-11 | 2018-08-07 | Dana Farber Cancer Inst Inc | Ciano tienotriazolpirazinas y usos de las mismas |
| HK1256419A1 (zh) | 2015-09-11 | 2019-09-20 | 达纳-法伯癌症研究所股份有限公司 | 乙酰胺噻吩並三唑並二氮雜環庚三烯及其用途 |
| WO2017066428A1 (en) | 2015-10-13 | 2017-04-20 | H. Lee Moffitt Cancer Center & Research Institute, Inc. | Brd4-kinase inhibitors as cancer therapeutics |
| SI3364958T1 (sl) | 2015-10-23 | 2023-05-31 | Navitor Pharmaceuticals, Inc. | Modulatorji interakcije sestrina in gator2 ter njihova uporaba |
| WO2017091681A1 (en) | 2015-11-24 | 2017-06-01 | Aclaris Therapeutics, Inc. | Selective kinase inhibitors |
| SG10201913450PA (en) | 2015-11-25 | 2020-03-30 | Dana Farber Cancer Inst Inc | Bivalent bromodomain inhibitors and uses thereof |
| GB201521919D0 (en) | 2015-12-11 | 2016-01-27 | Electrophoretics Ltd | Isobaric mass labels |
| WO2017106352A1 (en) | 2015-12-14 | 2017-06-22 | Raze Therapeutics, Inc. | Caffeine inhibitors of mthfd2 and uses thereof |
| EP4234552A3 (en) | 2016-03-09 | 2023-10-18 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| PL3426243T3 (pl) | 2016-03-09 | 2021-10-04 | Raze Therapeutics, Inc. | Inhibitory dehydrogenazy 3-fosfoglicerynianowej i ich zastosowania |
| WO2017177230A1 (en) | 2016-04-08 | 2017-10-12 | X4 Pharmaceuticals, Inc. | Methods for treating cancer |
| LT3442947T (lt) * | 2016-04-15 | 2023-09-11 | Epizyme, Inc. | Aminu pakeisti arilo arba heteroarilo junginiai, kaip ehmt1 ir ehmt2 inhibitoriai |
| EP3808748A1 (en) | 2016-06-21 | 2021-04-21 | X4 Pharmaceuticals, Inc. | Substituted piperidines as cxcr4-inhibitors |
| CN109640988A (zh) | 2016-06-21 | 2019-04-16 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
| CA3027500A1 (en) | 2016-06-21 | 2017-12-28 | X4 Pharmaceuticals, Inc. | Cxcr4 inhibitors and uses thereof |
| EP3487852A1 (en) | 2016-07-21 | 2019-05-29 | Biogen MA Inc. | Succinate forms and compositions of bruton's tyrosine kinase inhibitors |
| TWI825663B (zh) | 2016-10-14 | 2023-12-11 | 美商林伯士拉克許米公司 | Tyk2抑制劑及其用途 |
| EP3528816A4 (en) | 2016-10-21 | 2020-04-08 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| WO2018089499A1 (en) | 2016-11-08 | 2018-05-17 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF |
| JP2019535839A (ja) | 2016-11-29 | 2019-12-12 | ピュアテック ヘルス エルエルシー | 治療剤の送達のためのエクソソーム |
| WO2018106636A1 (en) | 2016-12-05 | 2018-06-14 | Raze Therapeutics, Inc. | Shmt inhibitors and uses thereof |
| US11730819B2 (en) | 2016-12-23 | 2023-08-22 | Bicycletx Limited | Peptide derivatives having novel linkage structures |
| EP3565638B8 (en) | 2017-01-06 | 2024-04-10 | BicycleRD Limited | Bicycle conjugate for treating cancer |
| US10336752B2 (en) | 2017-03-08 | 2019-07-02 | Nimbus Lakshmi, Inc. | TYK2 inhibitors, uses, and methods for production thereof |
| EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
| EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine derivatives |
| US10363230B2 (en) | 2017-03-23 | 2019-07-30 | North Carolina Agricultural And Technical State University | 6-shogaol derivatives and activities thereof |
| WO2018191146A1 (en) | 2017-04-10 | 2018-10-18 | Navitor Pharmaceuticals, Inc. | Heteroaryl rheb inhibitors and uses thereof |
| CA3060416A1 (en) | 2017-04-21 | 2018-10-25 | Epizyme, Inc. | Combination therapies with ehmt2 inhibitors |
| WO2018200625A1 (en) | 2017-04-26 | 2018-11-01 | Navitor Pharmaceuticals, Inc. | Modulators of sestrin-gator2 interaction and uses thereof |
| EP3615550A1 (en) | 2017-04-27 | 2020-03-04 | BicycleTx Limited | Bicyclic peptide ligands and uses thereof |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EP3645549A1 (en) | 2017-06-26 | 2020-05-06 | BicycleRD Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
| MY205416A (en) | 2017-07-28 | 2024-10-21 | Takeda Pharmaceuticals Co | Tyk2 inhibitors and uses thereof |
| US11261214B2 (en) | 2017-08-04 | 2022-03-01 | Bicycletx Limited | Bicyclic peptide ligand specific for CD137 |
| EP3668550A1 (en) | 2017-08-14 | 2020-06-24 | Bicyclerd Limited | Bicyclic peptide ligand prr-a conjugates and uses thereof |
| US20200291096A1 (en) | 2017-08-14 | 2020-09-17 | Bicyclerd Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
| US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
| EP4306524A3 (en) | 2017-08-29 | 2024-09-11 | PureTech LYT, Inc. | Lymphatic system-directing lipid prodrugs |
| EP3684366A4 (en) | 2017-09-22 | 2021-09-08 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES OF THE LATEST |
| EP3684365A4 (en) | 2017-09-22 | 2021-09-08 | Kymera Therapeutics, Inc. | PROTEIN DEGRADATION AGENTS AND USES OF SUCH |
| AU2018353122B2 (en) * | 2017-10-18 | 2023-11-23 | Epizyme, Inc. | Amine-substituted heterocyclic compounds as EHMT2 inhibitors, salts thereof, and methods of synthesis thereof |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3727362A4 (en) | 2017-12-19 | 2021-10-06 | PureTech LYT, Inc. | MYCOPHENOLIC ACID LIPID MEDICINAL PRODUCTS AND THEIR USES |
| GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
| TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
| US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
| US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| EP3737675A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| EP3737666A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES |
| WO2019140953A1 (zh) * | 2018-01-16 | 2019-07-25 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制激酶活性的二苯氨基嘧啶类化合物 |
| US10793563B2 (en) | 2018-01-29 | 2020-10-06 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
| KR20200116481A (ko) | 2018-01-29 | 2020-10-12 | 메르크 파텐트 게엠베하 | Gcn2 억제제 및 이의 용도 |
| IL276302B2 (en) | 2018-01-30 | 2023-11-01 | Incyte Corp | Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one) |
| US11453676B2 (en) * | 2018-02-02 | 2022-09-27 | Forward Therapeutics, Inc. | Inhibitors of protein arginine deiminases |
| MX2020008791A (es) | 2018-02-23 | 2021-01-08 | Bicycletx Ltd | Ligandos de peptidos biciclicos multimericos. |
| CN117304157A (zh) | 2018-02-27 | 2023-12-29 | 阿塔克斯生物制药有限公司 | 作为tcr-nck相互作用的抑制剂的色烯衍生物 |
| SMT202400306T1 (it) | 2018-03-30 | 2024-09-16 | Incyte Corp | Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak. |
| EP3773591A4 (en) | 2018-04-05 | 2021-12-22 | Sumitomo Dainippon Pharma Oncology, Inc. | AXL KINASE INHIBITORS AND THEIR USE |
| KR102063155B1 (ko) | 2018-04-11 | 2020-01-08 | 한국과학기술연구원 | 우수한 카이네이즈 저해 활성을 보이는 다양한 치환기를 갖는 피리미딘 유도체 |
| IL301501B2 (en) | 2018-04-24 | 2024-10-01 | Vertex Pharma | Antiproliferation compounds and uses thereof |
| ES2969982T3 (es) | 2018-04-24 | 2024-05-23 | Vertex Pharma | Compuestos de pteridinona y usos de los mismos |
| EP4309737A3 (en) | 2018-05-04 | 2024-03-27 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| EP3788046B1 (en) | 2018-05-04 | 2025-12-10 | Incyte Corporation | Salts of an fgfr inhibitor |
| CN112469418A (zh) | 2018-06-01 | 2021-03-09 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| EA202092692A1 (ru) | 2018-06-15 | 2021-04-21 | Навитор Фармасьютикалз, Инк. | Аналоги рапамицина и их применения |
| GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
| IL279489B2 (en) | 2018-06-22 | 2025-10-01 | Bicycletx Ltd | Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate |
| EP3817822A4 (en) | 2018-07-06 | 2022-07-27 | Kymera Therapeutics, Inc. | PROTEIN DEGRADANTS AND USES THEREOF |
| WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
| CN112512597A (zh) | 2018-07-26 | 2021-03-16 | 大日本住友制药肿瘤公司 | 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂 |
| US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
| EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| US20220031699A1 (en) * | 2018-09-25 | 2022-02-03 | Impact Biomedicines, Inc. | Methods of treating myeloproliferative disorders |
| CN113271940A (zh) | 2018-10-15 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| WO2020084305A1 (en) | 2018-10-23 | 2020-04-30 | Bicycletx Limited | Bicyclic peptide ligands and uses thereof |
| EP3870158A4 (en) | 2018-10-24 | 2022-08-10 | Navitor Pharmaceuticals, Inc. | Polymorphic compounds and uses thereof |
| WO2020092015A1 (en) * | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| SG11202105424PA (en) | 2018-11-30 | 2021-06-29 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| CN113271938A (zh) | 2018-11-30 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| GB201820325D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for psma |
| GB201820288D0 (en) | 2018-12-13 | 2019-01-30 | Bicycle Tx Ltd | Bicycle peptide ligaands specific for MT1-MMP |
| EP3670659A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Biomarkers, and uses in treatment of viral infections, inflammations, or cancer |
| CN111362922A (zh) * | 2018-12-26 | 2020-07-03 | 上海喆邺生物科技有限公司 | 2,4-二氨基嘧啶衍生物及其用途 |
| WO2020154474A1 (en) | 2019-01-23 | 2020-07-30 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| FR3092581A1 (fr) * | 2019-02-12 | 2020-08-14 | Impact Biomedicines, Inc | Formes cristallines d'un inhibiteur de jak2 |
| JP2022519885A (ja) * | 2019-02-12 | 2022-03-25 | インパクト バイオメディシンズ インコーポレイテッド | Ｊａｋ２阻害剤の結晶形態 |
| WO2020165600A1 (en) | 2019-02-14 | 2020-08-20 | Bicycletx Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| EP3937943A4 (en) | 2019-03-15 | 2022-12-07 | The General Hospital Corporation | NEW SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS |
| US20220184222A1 (en) | 2019-04-02 | 2022-06-16 | Bicycletx Limited | Bicycle toxin conjugates and uses thereof |
| SG11202110829YA (en) | 2019-04-05 | 2021-10-28 | Kymera Therapeutics Inc | Stat degraders and uses thereof |
| TW202108559A (zh) | 2019-05-31 | 2021-03-01 | 美商醫肯納腫瘤學公司 | Tead抑制劑及其用途 |
| WO2020256739A1 (en) | 2019-06-21 | 2020-12-24 | Constellation Pharmaceuticals, Inc. | Methods of treating myeloproliferative disorders |
| WO2020257644A1 (en) | 2019-06-21 | 2020-12-24 | Constellation Pharmaceuticals, Inc. | Methods of treating myeloproliferative disorders |
| WO2021091535A1 (en) | 2019-11-05 | 2021-05-14 | Constellation Pharmaceuticals, Inc. | Treating myeloproliferative disorders with cpi-0610 and a jak inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI860386B (zh) | 2019-07-30 | 2024-11-01 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
| AU2020345962A1 (en) | 2019-09-11 | 2022-03-31 | Vincere Biosciences, Inc. | USP30 inhibitors and uses thereof |
| EP4027995A4 (en) | 2019-09-13 | 2023-08-23 | Nimbus Saturn, Inc. | HPK1 ANTAGONISTS AND THEIR APPLICATIONS |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| 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 |
| US11306062B2 (en) | 2019-10-29 | 2022-04-19 | Johnson Matthey Public Limited | Forms of fedratinib dihydrochloride |
| TWI870497B (zh) | 2019-11-01 | 2025-01-21 | 美商奈維特製藥公司 | 使用mtorc1調節劑的治療方法 |
| 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 |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| AU2020397938A1 (en) | 2019-12-05 | 2022-06-23 | Janssen Pharmaceutica Nv | Rapamycin analogs and uses thereof |
| EP4076524A4 (en) | 2019-12-17 | 2023-11-29 | Kymera Therapeutics, Inc. | IRAQ DEGRADERS AND USES THEREOF |
| MX2022007576A (es) | 2019-12-17 | 2022-09-23 | Kymera Therapeutics Inc | Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos. |
| IL294150A (en) | 2019-12-23 | 2022-08-01 | Kymera Therapeutics Inc | Smarca joints and their uses |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN111423419B (zh) * | 2020-01-17 | 2021-12-17 | 温州医科大学 | 一种小分子化合物cyy-260及其在制备抗肿瘤药物中的应用 |
| JP2023514147A (ja) | 2020-02-05 | 2023-04-05 | ピュアテック・エル・ワイ・ティ・インコーポレイテッド | 神経ステロイドの脂質プロドラッグ |
| AU2021230289A1 (en) | 2020-03-03 | 2022-09-29 | PIC Therapeutics, Inc. | eIF4E inhibitors and uses thereof |
| MX2022011602A (es) | 2020-03-19 | 2023-01-04 | Kymera Therapeutics Inc | Degradadores de la proteína de homólogo de ratón de minuto 2 (mdm2) y usos de los mismos. |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| EP4161521A4 (en) | 2020-06-03 | 2024-07-10 | Kymera Therapeutics, Inc. | DEUTERED IRAQ DEGRADERS AND USES THEREOF |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| CN113754591B (zh) * | 2020-06-05 | 2024-01-05 | 山东大学 | 一种hdac、jak和bet三靶点抑制剂及其制备方法和应用 |
| EP3944859A1 (en) | 2020-07-30 | 2022-02-02 | Assistance Publique Hôpitaux de Paris | Method for treating immune toxicities induced by immune checkpoint inhibitors |
| EP4196792A1 (en) | 2020-08-17 | 2023-06-21 | BicycleTX Limited | Bicycle conjugates specific for nectin-4 and uses thereof |
| CN112225703B (zh) * | 2020-09-28 | 2022-03-11 | 广州智睿医药科技有限公司 | 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物 |
| EP4232425A4 (en) | 2020-10-23 | 2024-07-24 | Nimbus Clotho, Inc. | Ctps1 inhibitors and uses thereof |
| KR20230091150A (ko) * | 2020-10-29 | 2023-06-22 | 수저우 야바오 파마슈티걸 알앤디 컴퍼니 리미티드 | 치환된 디아릴아민 화합물 및 이의 약학적 조성물, 제조 방법과 용도 |
| TWI750905B (zh) * | 2020-11-19 | 2021-12-21 | 財團法人國家衛生研究院 | 噻唑化合物作為蛋白質激酶抑制劑 |
| CA3200814A1 (en) | 2020-12-02 | 2022-06-09 | Alfredo C. Castro | Tead inhibitors and uses thereof |
| WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| TW202237119A (zh) | 2020-12-10 | 2022-10-01 | 美商住友製藥腫瘤公司 | Ａｌｋ﹘５抑制劑和彼之用途 |
| IL303118A (en) | 2020-12-16 | 2023-07-01 | Impact Biomedicines Inc | Dosing of fedratinib |
| CN116710141A (zh) * | 2020-12-29 | 2023-09-05 | 上海岸阔医药科技有限公司 | 预防或治疗抗肿瘤剂相关疾病或病症的方法 |
| AU2021413371A1 (en) | 2020-12-30 | 2023-07-13 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| CN112778282B (zh) | 2021-01-06 | 2022-07-22 | 温州医科大学 | 一种嘧啶类小分子化合物及其应用 |
| AU2022215844A1 (en) | 2021-02-02 | 2023-09-14 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
| CN117098757A (zh) | 2021-02-02 | 2023-11-21 | 里米诺生物科学有限公司 | Gpr84拮抗剂和其用途 |
| CN117120090A (zh) | 2021-02-12 | 2023-11-24 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
| AU2022220043A1 (en) | 2021-02-15 | 2023-08-31 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| AU2022220869A1 (en) | 2021-02-15 | 2023-08-24 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| EP4297750A1 (en) | 2021-02-25 | 2024-01-03 | Impact Biomedicines, Inc. | Use of a bet inhibitor alone or in combination with fedratinib or ruxolitinib for treating a hematological malignancy such as myelofibrosis |
| US11926625B2 (en) | 2021-03-05 | 2024-03-12 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
| IL307165A (en) * | 2021-03-26 | 2023-11-01 | Sumitomo Pharma Oncology Inc | ALK-5 inhibitors and their uses |
| KR102585194B1 (ko) * | 2021-03-26 | 2023-10-10 | 주식회사 스탠다임 | Lrrk2에 대해 저해 활성을 갖는 신규한 페닐아미노피리미딘화합물 및 이의 용도 |
| EP4313989A4 (en) | 2021-03-29 | 2025-03-05 | Nimbus Saturn, Inc. | HPK1 ANTAGONISTS AND USES THEREOF |
| EP4319756A4 (en) | 2021-04-09 | 2025-02-26 | Nimbus Clio, Inc. | CBL-B MODULATORS AND USES THEREOF |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| JP2024514879A (ja) | 2021-04-16 | 2024-04-03 | イケナ オンコロジー， インコーポレイテッド | Ｍｅｋ阻害剤及びその使用 |
| US12097261B2 (en) | 2021-05-07 | 2024-09-24 | Kymera Therapeutics, Inc. | CDK2 degraders and uses thereof |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CA3229560A1 (en) | 2021-08-25 | 2023-03-02 | Christopher L. Vandeusen | Eif4e inhibitors and uses thereof |
| JP2024532276A (ja) | 2021-08-25 | 2024-09-05 | ピク セラピューティクス， インコーポレイテッド | ｅＩＦ４Ｅ阻害剤及びその使用 |
| WO2023044297A1 (en) | 2021-09-14 | 2023-03-23 | Impact Biomedicines, Inc. | Fedratinib for treating myeloproliferative disorders |
| EP4401735A4 (en) * | 2021-09-16 | 2025-07-16 | Lomond Therapeutics Inc | COMPOUNDS COMPRISING N-ARYLPYRIMIDIN-2-AMINE DERIVATIVES AS THERAPEUTIC AGENTS |
| CN118302168A (zh) | 2021-10-29 | 2024-07-05 | 凯麦拉医疗公司 | Irak4降解剂和其制备 |
| WO2023114984A1 (en) | 2021-12-17 | 2023-06-22 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| EP4472967A2 (en) | 2022-01-31 | 2024-12-11 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP4238564A1 (en) * | 2022-03-02 | 2023-09-06 | Bash Biotech Inc | New treatments of renal cell carcinoma |
| WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| WO2023211889A1 (en) | 2022-04-25 | 2023-11-02 | Ikena Oncology, Inc. | Polymorphic compounds and uses thereof |
| WO2023230205A1 (en) | 2022-05-25 | 2023-11-30 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| KR20250057800A (ko) | 2022-08-02 | 2025-04-29 | 리미널 바이오사이언시스 리미티드 | 헤테로아릴 카복스아마이드 및 관련 gpr84 길항제 및 이의 용도 |
| WO2024028364A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Aryl-triazolyl and related gpr84 antagonists and uses thereof |
| IL318576A (en) | 2022-08-02 | 2025-03-01 | Liminal Biosciences Ltd | Pyridoxine-substituted GPR84 antagonists and their uses |
| CN115745896B (zh) * | 2022-11-18 | 2024-08-06 | 合肥医工医药股份有限公司 | 一种jak2激酶选择性抑制剂及其制备方法和用途 |
| US20240208961A1 (en) | 2022-11-22 | 2024-06-27 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| WO2024179699A1 (en) * | 2023-03-02 | 2024-09-06 | Bash Biotech Inc. | New compounds and treatment of renal cell carcinoma |
| WO2024264017A2 (en) | 2023-06-23 | 2024-12-26 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| TW202529769A (zh) | 2023-09-21 | 2025-08-01 | 日商武田藥品工業股份有限公司 | Ｔｙｋ２抑制劑及其用途 |
Family Cites Families (231)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2A (en) * | 1826-12-15 | 1836-07-29 | John Goulding | Mode of manufacturing wool or other fibrous materials |
| US2003199A (en) | 1930-05-31 | 1935-05-28 | Johnson Frank James | Automatic coal stoker |
| US2003149A (en) | 1931-05-22 | 1935-05-28 | Autographic Register Co | Manifolding |
| US2003065A (en) | 1931-06-20 | 1935-05-28 | John R Ditmars | Composition for coating sheets, fibrous stocks, and the like |
| US2004102A (en) | 1932-02-24 | 1935-06-11 | Daniel A Dickey | Hollow steel propeller construction |
| US2004138A (en) | 1932-11-30 | 1935-06-11 | Byers A M Co | Method of making wrought iron pipe |
| US2002165A (en) | 1933-07-08 | 1935-05-21 | Charles A Winslow | Air cleaner |
| US2003187A (en) | 1933-10-02 | 1935-05-28 | Frederick H Shaw | Automobile radio device |
| US2003166A (en) | 1933-10-26 | 1935-05-28 | Zancan Ottavio | Front drive for motor cars |
| US2001051A (en) | 1933-12-01 | 1935-05-14 | Angelina Mariani | Tamperproof meter box with cutout control and fuse drawer for electric meters |
| US2004092A (en) | 1933-12-15 | 1935-06-11 | John L Chaney | Device for indicating the temperature of liquids |
| US2003060A (en) | 1934-04-02 | 1935-05-28 | Ernest L Heckert | Thermostatic controlling device |
| US2667486A (en) | 1951-05-24 | 1954-01-26 | Research Corp | 2,4-diamino pteridine and derivatives |
| IL44058A (en) | 1973-02-02 | 1978-10-31 | Ciba Geigy Ag | 3amino-1,2,4-benzotriazine 1,4-di-noxide derivatives, their preparation and compositions for the control of microorganisms containing them |
| AU535258B2 (en) | 1979-08-31 | 1984-03-08 | Ici Australia Limited | Benzotriazines |
| DE3205638A1 (de) | 1982-02-17 | 1983-08-25 | Hoechst Ag, 6230 Frankfurt | Trisubstituierte pyrimidin-5-carbonsaeuren und deren derivate, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel |
| US4490289A (en) | 1982-09-16 | 1984-12-25 | Hoffmann-La Roche Inc. | Homogeneous human interleukin 2 |
| DE3518887C1 (de) | 1985-05-25 | 1986-09-18 | Ernst Leitz Wetzlar Gmbh, 6330 Wetzlar | Verfahren und Anordnung zur automatischen Bestimmung und Einstellung von Aufnahmeparametern bei einer fotografischen Aufnahmekamera |
| US5624925A (en) | 1986-09-25 | 1997-04-29 | Sri International | 1,2,4-benzotriazine oxides as radiosensitizers and selective cytotoxic agents |
| JPH0741461B2 (ja) | 1987-06-01 | 1995-05-10 | 株式会社日立製作所 | 剪断機 |
| JP2598100B2 (ja) | 1988-08-31 | 1997-04-09 | キヤノン株式会社 | 電子写真感光体 |
| US5214059A (en) | 1989-07-03 | 1993-05-25 | Hoechst-Roussel Pharmaceuticals Incorporated | 2-(aminoaryl) indoles and indolines as topical antiinflammatory agents for the treatment of skin disorders |
| US5665543A (en) | 1989-07-18 | 1997-09-09 | Oncogene Science, Inc. | Method of discovering chemicals capable of functioning as gene expression modulators |
| US5776502A (en) | 1989-07-18 | 1998-07-07 | Oncogene Science, Inc. | Methods of transcriptionally modulating gene expression |
| GB9003553D0 (en) | 1990-02-16 | 1990-04-11 | Ici Plc | Herbicidal compositions |
| JP2839106B2 (ja) | 1990-02-19 | 1998-12-16 | キヤノン株式会社 | 電子写真感光体 |
| JPH03127790U (enExample) | 1990-04-06 | 1991-12-24 | ||
| GB9012592D0 (en) | 1990-06-06 | 1990-07-25 | Smithkline Beecham Intercredit | Compounds |
| FR2665159B1 (fr) | 1990-07-24 | 1992-11-13 | Rhone Poulenc Sante | Nouveaux derives de la pyridine et de la quinoleine, leur preparation et les compositions pharmaceutiques qui les contiennent. |
| IE74711B1 (en) | 1990-07-27 | 1997-07-30 | Ici Plc | Fungicides |
| GB9016800D0 (en) | 1990-07-31 | 1990-09-12 | Shell Int Research | Tetrahydropyrimidine derivatives |
| DE4025891A1 (de) | 1990-08-16 | 1992-02-20 | Bayer Ag | Pyrimidyl-substituierte acrylsaeureester |
| DE69127207T2 (de) * | 1991-05-03 | 1998-01-22 | Raision Tehtaat Oy Ab | Substanz zur absenkung eines hohen cholesterolspiegels im serum und verfahren zu ihrer herstellung |
| JPH05345780A (ja) | 1991-12-24 | 1993-12-27 | Kumiai Chem Ind Co Ltd | ピリミジンまたはトリアジン誘導体及び除草剤 |
| HUT63941A (en) | 1992-05-15 | 1993-11-29 | Hoechst Ag | Process for producing 4-alkyl-substituted pyrimidine-5-carboxanilide derivatives, and fungicidal compositions comprising same |
| US5438130A (en) | 1993-01-15 | 1995-08-01 | Cambridge Neuroscience, Inc. | Fucosylated guanosine disulfates as excitatory amino acid antagonists |
| DE4338704A1 (de) | 1993-11-12 | 1995-05-18 | Hoechst Ag | Stabilisierte Oligonucleotide und deren Verwendung |
| US5530000A (en) | 1993-12-22 | 1996-06-25 | Ortho Pharmaceutical Corporation | Substituted pyrimidinylaminothiazole derivatives useful as platelet aggreggation inhibitors |
| GB9506466D0 (en) | 1994-08-26 | 1995-05-17 | Prolifix Ltd | Cell cycle regulated repressor and dna element |
| US5597826A (en) | 1994-09-14 | 1997-01-28 | Pfizer Inc. | Compositions containing sertraline and a 5-HT1D receptor agonist or antagonist |
| DE19502912A1 (de) | 1995-01-31 | 1996-08-01 | Hoechst Ag | G-Cap Stabilisierte Oligonucleotide |
| US6326487B1 (en) | 1995-06-05 | 2001-12-04 | Aventis Pharma Deutschland Gmbh | 3 modified oligonucleotide derivatives |
| CA2230894A1 (en) | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxamides and related compounds and methods for treating inflammatory conditions |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| EP0895475A4 (en) | 1995-12-29 | 2000-08-23 | Smithkline Beecham Corp | VITRONECTIN RECEPTOR ANTAGONISTS |
| JPH09274290A (ja) | 1996-02-07 | 1997-10-21 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料用の現像液および処理方法 |
| US6204260B1 (en) | 1996-02-23 | 2001-03-20 | Eli Lilly And Company | Non-peptidyl vasopressin V1a antagonists |
| DE59707681D1 (de) | 1996-10-28 | 2002-08-14 | Rolic Ag Zug | Vernetzbare, photoaktive Silanderivate |
| DE69737107T2 (de) | 1996-11-20 | 2007-07-12 | Introgen Therapeutics Inc., Austin | Ein verbessertes verfahren zur produktion und reinigung von adenoviralen vektoren |
| JP3734903B2 (ja) | 1996-11-21 | 2006-01-11 | 富士写真フイルム株式会社 | 現像処理方法 |
| JPH10153838A (ja) | 1996-11-22 | 1998-06-09 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料の処理方法 |
| JP3720931B2 (ja) | 1996-11-26 | 2005-11-30 | 富士写真フイルム株式会社 | ハロゲン化銀写真感光材料の処理方法 |
| CN1240010A (zh) | 1996-12-04 | 1999-12-29 | 金伯利-克拉克环球有限公司 | 湿强度纸的制备方法 |
| US5935383A (en) | 1996-12-04 | 1999-08-10 | Kimberly-Clark Worldwide, Inc. | Method for improved wet strength paper |
| ES2196396T3 (es) | 1996-12-23 | 2003-12-16 | Bristol Myers Squibb Pharma Co | Compuestos heteroaromaticos de 5 miembros conteniendo oxigeno o azufre como inhibidores del factor xa. |
| JPH10207019A (ja) | 1997-01-22 | 1998-08-07 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料の処理方法 |
| JPH10213820A (ja) | 1997-01-31 | 1998-08-11 | Canon Inc | 液晶素子及び液晶装置 |
| DE59807348D1 (de) | 1997-02-05 | 2003-04-10 | Rolic Ag Zug | Photovernetzbare Silanderivate |
| GB9705361D0 (en) * | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
| JPH10260512A (ja) | 1997-03-19 | 1998-09-29 | Fuji Photo Film Co Ltd | ハロゲン化銀感光材料の処理方法 |
| JPH10310583A (ja) | 1997-05-09 | 1998-11-24 | Mitsubishi Chem Corp | ピリドンアゾ系化合物、感熱転写用色素およびそれを使用した感熱転写材料 |
| US6070126A (en) | 1997-06-13 | 2000-05-30 | William J. Kokolus | Immunobiologically-active linear peptides and method of identification |
| TW436485B (en) | 1997-08-01 | 2001-05-28 | American Cyanamid Co | Substituted quinazoline derivatives |
| US6635626B1 (en) | 1997-08-25 | 2003-10-21 | Bristol-Myers Squibb Co. | Imidazoquinoxaline protein tyrosine kinase inhibitors |
| US6022884A (en) | 1997-11-07 | 2000-02-08 | Amgen Inc. | Substituted pyridine compounds and methods of use |
| EP1054004B1 (en) | 1997-12-15 | 2008-07-16 | Astellas Pharma Inc. | Novel pyrimidine-5-carboxamide derivatives |
| IL136637A0 (en) | 1997-12-22 | 2001-06-14 | Du Pont Pharm Co | Nitrogen containing heteroaromatics with ortho-substituted pi's as factor xa inhibitors |
| KR20010041015A (ko) | 1998-02-17 | 2001-05-15 | 윌리엄 제이. 리플린 | 항바이러스성 피리미딘 유도체 |
| KR100643419B1 (ko) | 1998-03-27 | 2006-11-10 | 얀센 파마슈티카 엔.브이. | Ｈｉｖ를 억제하는 피리미딘 유도체 |
| US6685938B1 (en) | 1998-05-29 | 2004-02-03 | The Scripps Research Institute | Methods and compositions useful for modulation of angiogenesis and vascular permeability using SRC or Yes tyrosine kinases |
| US6136971A (en) | 1998-07-17 | 2000-10-24 | Roche Colorado Corporation | Preparation of sulfonamides |
| US6378526B1 (en) | 1998-08-03 | 2002-04-30 | Insite Vision, Incorporated | Methods of ophthalmic administration |
| ES2274634T3 (es) * | 1998-08-29 | 2007-05-16 | Astrazeneca Ab | Compuestos de pirimidina. |
| US6297258B1 (en) | 1998-09-29 | 2001-10-02 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| US6288082B1 (en) | 1998-09-29 | 2001-09-11 | American Cyanamid Company | Substituted 3-cyanoquinolines |
| KR100736502B1 (ko) | 1998-09-29 | 2007-07-06 | 와이어쓰 홀딩스 코포레이션 | 단백질 티로신 키나제 억제제로서 치환된 3-시아노퀴놀린 |
| EA004436B1 (ru) | 1998-09-29 | 2004-04-29 | Уайт Холдингз Корпорейшн | Замещенные 3-цианохинолины в качестве ингибиторов протеинтирозинкиназ |
| EP1058549A4 (en) | 1998-12-23 | 2003-11-12 | Bristol Myers Squibb Pharma Co | FACTOR Xa OR THROMBIN INHIBITORS |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| WO2000046203A2 (en) | 1999-02-04 | 2000-08-10 | Millennium Pharmaceuticals, Inc. | G-protein coupled heptahelical receptor binding compounds and methods of use thereof |
| EP2308833A3 (en) | 1999-04-15 | 2011-09-28 | Bristol-Myers Squibb Company | Cyclic protein tyrosine kinase inhibitors |
| NZ514576A (en) | 1999-04-21 | 2004-02-27 | Wyeth Corp | Substituted 3-cyano-[1.7], [1.5], and [1.8]- naphthyridine inhibitors of tyrosine kinases |
| AU5020400A (en) | 1999-05-20 | 2000-12-12 | E.I. Du Pont De Nemours And Company | Heteroaryloxypyrimidine insecticides and acaricides |
| CA2377771A1 (en) | 1999-07-01 | 2001-01-11 | Ajinomoto Co., Inc. | Heterocyclic compounds and medical use thereof |
| WO2001007027A2 (en) | 1999-07-22 | 2001-02-01 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives for the treatment of viral diseases |
| WO2001007401A1 (en) | 1999-07-23 | 2001-02-01 | Shionogi & Co., Ltd. | Tricyclic compounds and drug compositions containing the same |
| EP1206935A4 (en) | 1999-07-23 | 2008-07-30 | Shionogi & Co | TH2 DIFFERENTIAL INHIBITION |
| IL147913A0 (en) | 1999-08-12 | 2002-08-14 | American Cyanamid Co | Nsaid and efgr kinase inhibitor containing composition for the treatment or inhibition of colonic polyps and colorectal cancer |
| US6093838A (en) | 1999-08-16 | 2000-07-25 | Allergan Sales, Inc. | Amines substituted with a dihydro-benzofuranyl or with a dihydro-isobenzofuranyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| US6127382A (en) | 1999-08-16 | 2000-10-03 | Allergan Sales, Inc. | Amines substituted with a tetrahydroquinolinyl group an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| HUP0202682A3 (en) | 1999-09-10 | 2003-03-28 | Merck & Co Inc | Tyrosine kinase inhibitors, pharmaceutical compositions containing them and their use |
| GB9922171D0 (en) | 1999-09-21 | 1999-11-17 | Zeneca Ltd | Chemical compounds |
| JP2001089412A (ja) | 1999-09-22 | 2001-04-03 | Otsuka Pharmaceut Co Ltd | ベンゼン誘導体またはその医薬的に許容される塩 |
| US6506769B2 (en) | 1999-10-06 | 2003-01-14 | Boehringer Ingelheim Pharmaceuticals, Inc. | Heterocyclic compounds useful as inhibitors of tyrosine kinases |
| WO2001027105A1 (en) | 1999-10-12 | 2001-04-19 | Takeda Chemical Industries, Ltd. | Pyrimidine-5-carboxamide compounds, process for producing the same and use thereof |
| GB9924092D0 (en) * | 1999-10-13 | 1999-12-15 | Zeneca Ltd | Pyrimidine derivatives |
| WO2001032628A1 (en) | 1999-11-03 | 2001-05-10 | Bristol-Myers Squibb Pharma Company | Cyano compounds as factor xa inhibitors |
| GB9929988D0 (en) | 1999-12-17 | 2000-02-09 | Celltech Therapeutics Ltd | Chemical compounds |
| ATE353320T1 (de) | 1999-12-29 | 2007-02-15 | Wyeth Corp | Tricyclische proteinkinasehemmer |
| US6638929B2 (en) | 1999-12-29 | 2003-10-28 | Wyeth | Tricyclic protein kinase inhibitors |
| JP2003520855A (ja) | 2000-01-28 | 2003-07-08 | アストラゼネカ アクチボラグ | 化学的化合物 |
| US6153752A (en) | 2000-01-28 | 2000-11-28 | Creanova, Inc. | Process for preparing heterocycles |
| US20020165244A1 (en) | 2000-01-31 | 2002-11-07 | Yuhong Zhou | Mucin synthesis inhibitors |
| WO2001060816A1 (en) | 2000-02-17 | 2001-08-23 | Amgen Inc. | Kinase inhibitors |
| RU2277911C2 (ru) | 2000-02-25 | 2006-06-20 | Ф.Хоффманн-Ля Рош Аг | Модуляторы аденозиновых рецепторов |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| ATE414079T1 (de) | 2000-03-01 | 2008-11-15 | Janssen Pharmaceutica Nv | 2,4-disubstituierte thiazolyl derivate |
| GB0004890D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004887D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| WO2001064646A2 (en) | 2000-03-01 | 2001-09-07 | Tularik Inc. | Hydrazones and analogs as cholesterol lowering agents |
| JP2001247411A (ja) | 2000-03-09 | 2001-09-11 | Tomono Agrica Co Ltd | 有害生物防除剤 |
| KR20080009294A (ko) | 2000-03-13 | 2008-01-28 | 와이어쓰 홀딩스 코포레이션 | 시아노퀴놀린을 포함하는 결장 폴립의 치료 또는 억제를위한 약제학적 조성물 |
| US6613917B1 (en) | 2000-03-23 | 2003-09-02 | Allergan, Inc. | Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| AR028261A1 (es) | 2000-03-28 | 2003-04-30 | Wyeth Corp | Inhibidores triciclicos de la proteina quinasa |
| US6608048B2 (en) | 2000-03-28 | 2003-08-19 | Wyeth Holdings | Tricyclic protein kinase inhibitors |
| AU2001244614A1 (en) | 2000-04-04 | 2001-10-15 | Shionogi & Co., Ltd. | Oily compositions containing highly fat-soluble drugs |
| WO2001076582A1 (fr) | 2000-04-05 | 2001-10-18 | Shionogi & Co., Ltd. | Micro-emulsions huile dans eau contenant des composes tricycliques ou des preconcentres de ceux-ci |
| FR2808163B1 (fr) * | 2000-04-19 | 2002-11-08 | Celes | Dispositif de chauffage par induction a flux transverse a circuit magnetique de largeur variable |
| US6471968B1 (en) | 2000-05-12 | 2002-10-29 | Regents Of The University Of Michigan | Multifunctional nanodevice platform |
| DE10024622A1 (de) | 2000-05-18 | 2001-11-22 | Piesteritz Stickstoff | N-(2-Pyrimidinyl)(thio)phosphorsäuretriamide, Verfahren zu ihrer Herstellung und deren Verwendung als Mittel zur Regulierung bzw. Hemmung der enzymatischen Harnstoff-Hydrolyse |
| EP1170353B1 (en) | 2000-07-06 | 2005-11-02 | Fuji Photo Film Co., Ltd. | Liquid crystal composition comprising liquid crystal molecules and aligment promoter |
| DE60132702T2 (de) | 2000-08-11 | 2009-03-19 | Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield | Heterozyklische verbindungen als inhibitoren von tyrosin-kinasen |
| US6638926B2 (en) | 2000-09-15 | 2003-10-28 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2002030358A2 (en) | 2000-10-11 | 2002-04-18 | Tularik Inc. | Modulation of ccr4 function |
| AU2001295791A1 (en) | 2000-11-02 | 2002-05-15 | Astrazeneca Ab | 4-substituted quinolines as antitumor agents |
| WO2002044166A1 (en) | 2000-11-02 | 2002-06-06 | Astrazeneca Ab | Substituted quinolines as antitumor agents |
| WO2002042272A2 (en) | 2000-11-20 | 2002-05-30 | Pharmacia Corporation | Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade |
| WO2002053160A1 (en) | 2000-12-29 | 2002-07-11 | Alteon, Inc. | Method for treating glaucoma ivb |
| WO2002053101A2 (en) | 2000-12-29 | 2002-07-11 | Alteon, Inc. | Method for treating fibrotic diseases or other indications |
| JP2002221770A (ja) | 2001-01-24 | 2002-08-09 | Fuji Photo Film Co Ltd | ハロゲン化銀写真感光材料およびその処理方法 |
| US20030130264A1 (en) | 2001-02-16 | 2003-07-10 | Tularik Inc. | Methods of using pyrimidine-based antiviral agents |
| UA75392C2 (en) | 2001-02-23 | 2006-04-17 | Merck & Co Inc | N-substituted non-aryl heterocyclic antagonists nmda/nr2b |
| JP2004525139A (ja) | 2001-03-23 | 2004-08-19 | 中外製薬株式会社 | Ｆｌｔ−１リガンド、および血管形成により調節可能な疾患の治療におけるそれらの使用 |
| EP1389206B1 (en) | 2001-04-13 | 2006-09-13 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| NZ528961A (en) * | 2001-04-20 | 2005-04-29 | Bayer Cropscience Ag | Novel insecticidal azoles |
| EP1383760A1 (en) | 2001-04-30 | 2004-01-28 | Fujisawa Pharmaceutical Co., Ltd. | Biarylcarboxamide compounds as apolipoprotein b inhibitors |
| MXPA03010269A (es) | 2001-05-11 | 2004-05-05 | Vertex Pharma | Derivados de 2,5-disubstituida piridina, pirimidina, piridazina y 1,2,4-triazina para usarse como inhibidores de p38. |
| WO2002094766A1 (en) | 2001-05-18 | 2002-11-28 | Nihon Nohyaku Co., Ltd. | Phthalamide derivative, agricultural or horticultural insecticide, and use thereof |
| WO2002096903A2 (fr) | 2001-05-28 | 2002-12-05 | Aventis Pharma S.A. | Derives chimiques et leur application comme agent antitelomerase |
| CA2449118A1 (en) | 2001-05-29 | 2002-12-05 | Schering Aktiengesellschaft | Cdk inhibiting pyrimidines, production thereof and their use as medicaments |
| CN100384480C (zh) | 2001-05-30 | 2008-04-30 | 斯克里普斯研究学院 | 核酸传递系统 |
| US6689778B2 (en) | 2001-07-03 | 2004-02-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and Lck protein kinases |
| US6861529B2 (en) | 2001-07-06 | 2005-03-01 | Pfizer Inc | Cycloalkypyrrole-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| MXPA04002397A (es) | 2001-09-14 | 2004-12-02 | Methylgene Inc | Inhibidores de histona deacetilasa. |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| DE10150614A1 (de) | 2001-10-12 | 2003-04-30 | Clariant Gmbh | Verfahren zur metallorganischen Herstellung organischer Zwischenprodukte über Halogen-Metall-Austauschreaktionen |
| DE10150610A1 (de) | 2001-10-12 | 2003-04-30 | Clariant Gmbh | Verfahren zur metallorganischen Herstellung organischer Zwischenprodukte über Amidbasen |
| DE10150615A1 (de) | 2001-10-12 | 2003-04-30 | Clariant Gmbh | Verfahren zur metallorganischen Herstellung organischer Zwischenprodukte |
| EP1453516A2 (de) | 2001-10-17 | 2004-09-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | 5-substituierte 4-amino-2-phenylamino-pyrimdinderivate und ihre verwendung als beta-amyloid modulatoren |
| US7183288B2 (en) | 2001-11-01 | 2007-02-27 | Herwig Josephus Margareta Janssen, legal representative | Amide derivatives as glycogen synthase kinase 3-β inhibitors |
| NZ531853A (en) | 2001-11-01 | 2006-02-24 | Janssen Pharmaceutica Nv | Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) |
| US6821988B2 (en) | 2001-11-27 | 2004-11-23 | Wyeth Holdings Corporation | 3-cyanoquinolines as inhibitors of EGF-R and HER2 kinases |
| US20050038035A1 (en) | 2001-11-28 | 2005-02-17 | Hisashi Takasugi | Heterocyclic amide compounds as apolipoprotein b inhibitors |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| AU2003206397B2 (en) | 2002-01-04 | 2008-07-17 | The Rockefeller University | Compositions and methods for prevention and treatment of amyloid-beta peptide-related disorders |
| US20030166932A1 (en) | 2002-01-04 | 2003-09-04 | Beard Richard L. | Amines substituted with a dihydronaphthalenyl, chromenyl, or thiochromenyl group, an aryl or heteroaryl group and an alkyl group, having retinoid-like biological activity |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| DE60332915D1 (de) | 2002-02-05 | 2010-07-22 | Wyeth Llc | Verfahren zur herstellung von n-acyl-2-amino-4-alkoxy-5-nitrobenzoesäuren |
| AU2003220970A1 (en) | 2002-03-01 | 2003-09-16 | Smithkline Beecham Corporation | Diamino-pyrimidines and their use as angiogenesis inhibitors |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| AU2003231231A1 (en) | 2002-05-06 | 2003-11-11 | Bayer Pharmaceuticals Corporation | Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders |
| PE20040522A1 (es) | 2002-05-29 | 2004-09-28 | Novartis Ag | Derivados de diarilurea dependientes de la cinasa de proteina |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| JP4570955B2 (ja) | 2002-07-09 | 2010-10-27 | バーテクス ファーマスーティカルズ インコーポレイテッド | プロテインキナーゼ阻害活性を持つイミダゾール類 |
| IL166241A0 (en) | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| MXPA05001277A (es) | 2002-08-02 | 2005-10-06 | Ab Science | 2-(3-aminoaril)amino-4-aril-tiazoles y su uso como inhibidores del c-kit. |
| MXPA05001804A (es) | 2002-08-14 | 2005-05-27 | Vertex Pharma | Inhibidores de proteinas cinasas y usos de los mismos. |
| UY27939A1 (es) | 2002-08-21 | 2004-03-31 | Glaxo Group Ltd | Compuestos |
| DE10240262A1 (de) | 2002-08-31 | 2004-03-11 | Clariant Gmbh | Verfahren zur metallorganischen Herstellung organischer Zwischenprodukte über Aryllithium-Basen |
| DE10240261A1 (de) | 2002-08-31 | 2004-03-11 | Clariant Gmbh | Verfahren zur metallorganischen Herstellung organischer Zwischenprodukte über Halogen-Metall-Austauschreaktionen |
| EP1549614A4 (en) | 2002-10-03 | 2008-04-16 | Targegen Inc | VASCULATORY AGENTS AND METHODS FOR THEIR APPLICATION |
| US20050282814A1 (en) | 2002-10-03 | 2005-12-22 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| WO2004032709A2 (en) | 2002-10-04 | 2004-04-22 | Caritas St.Elisabeth's Medical Center Of Boston, Inc. | Inhibition of src for treatment of reperfusion injury related to revascularization |
| WO2004037176A2 (en) | 2002-10-21 | 2004-05-06 | Bristol-Myers Squibb Company | Quinazolinones and derivatives thereof as factor xa inhibitors |
| AU2003286711A1 (en) | 2002-10-25 | 2004-05-13 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| US7452911B2 (en) | 2002-10-31 | 2008-11-18 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds |
| DE10250708A1 (de) | 2002-10-31 | 2004-05-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| US7129351B2 (en) * | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| ATE371656T1 (de) | 2002-11-04 | 2007-09-15 | Vertex Pharma | Heteroaryl-pyrimidinderivate als jak-inhibitoren |
| US20050101576A1 (en) | 2003-11-06 | 2005-05-12 | Novacea, Inc. | Methods of using vitamin D compounds in the treatment of myelodysplastic syndromes |
| JP2006510661A (ja) | 2002-12-06 | 2006-03-30 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | Ｐｉ３ｋの阻害剤としてのベンズオキサジン−３−オン類及びその誘導体 |
| WO2004054186A1 (ja) | 2002-12-12 | 2004-06-24 | Fujitsu Limited | データ中継装置、連想メモリデバイス、および連想メモリデバイス利用情報検索方法 |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| BR0317487A (pt) | 2002-12-20 | 2005-11-29 | Pharmacia Corp | O r-isÈmero de compostos de aminoácido beta como derivados de antagonistas de receptores de integrina |
| JP2006518333A (ja) | 2002-12-20 | 2006-08-10 | ファルマシア・コーポレーション | インテグリン受容体アンタゴニストとしてのヘテロアリールアルカン酸 |
| ES2314271T3 (es) | 2002-12-24 | 2009-03-16 | Astrazeneca Ab | Derivados de quinazolina terapeuticos. |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| CA2513527C (en) | 2003-02-07 | 2012-08-14 | Janssen Pharmaceutica N.V. | Pyrimidine derivatives for the prevention of hiv infection |
| WO2004074266A1 (en) | 2003-02-07 | 2004-09-02 | Janssen Pharmaceutica N.V. | Hiv inhibiting 1,2,4-triazines |
| EP1594512A4 (en) | 2003-02-11 | 2007-07-11 | Kemia Inc | COMPOUNDS FOR THE TREATMENT OF VIRUS INFECTIONS |
| CL2004000303A1 (es) | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih. |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| US20040214914A1 (en) | 2003-04-24 | 2004-10-28 | Ocular Sciences, Inc. | Hydrogel contact lenses and package systems and production methods for same |
| US8178671B2 (en) | 2003-07-30 | 2012-05-15 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds |
| PT2287156E (pt) | 2003-08-15 | 2013-08-26 | Novartis Ag | 2,4-di(fenilamino)-pirimidinas úteis no tratamento de doenças neoplásicas, desordens inflamatórias e do sistema imunitário |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| CA2538413A1 (en) | 2003-09-18 | 2005-03-24 | Novartis Ag | 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
| EP2543376A1 (en) | 2004-04-08 | 2013-01-09 | Targegen, Inc. | Benzotriazine inhibitors of kinases |
| PL382308A1 (pl) | 2004-08-25 | 2007-08-20 | Targegen, Inc. | Związki heterocykliczne i sposoby stosowania |
| US7210697B2 (en) | 2004-12-16 | 2007-05-01 | Tricam International, Inc. | Convertible handle |
| WO2006074057A2 (en) * | 2004-12-30 | 2006-07-13 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| MX2007011500A (es) * | 2005-03-16 | 2007-11-21 | Targegen Inc | Compuestos pirimidina y metodos de uso. |
| US7389455B2 (en) * | 2005-05-16 | 2008-06-17 | Texas Instruments Incorporated | Register file initialization to prevent unknown outputs during test |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| US20070032493A1 (en) | 2005-05-26 | 2007-02-08 | Synta Pharmaceuticals Corp. | Method for treating B cell regulated autoimmune disorders |
| CN105348203B (zh) * | 2005-06-08 | 2018-09-18 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| JP2008543775A (ja) | 2005-06-08 | 2008-12-04 | ターゲジェン インコーポレーティッド | 眼の障害を治療するための方法および組成物 |
| KR100848205B1 (ko) | 2005-06-20 | 2008-07-24 | 주식회사 동부하이텍 | 면역 억제 및 염증 억제 활성을 갖는 신규한 치환된1,3-티아졸 유도체 또는 이의 약학적으로 허용가능한 염,중간체 화합물 또는 이의 약학적으로 허용가능한 염, 이의제조방법, 및 이를 포함하는 약학적 조성물 |
| WO2007008541A2 (en) * | 2005-07-08 | 2007-01-18 | Kalypsys, Inc. | Cellular cholesterol absorption modifiers |
| US7754717B2 (en) | 2005-08-15 | 2010-07-13 | Amgen Inc. | Bis-aryl amide compounds and methods of use |
| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| US20070072682A1 (en) | 2005-09-29 | 2007-03-29 | Crawford James T Iii | Head to head electronic poker game assembly and method of operation |
| US8133900B2 (en) | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| DK1951684T3 (en) * | 2005-11-01 | 2016-10-24 | Targegen Inc | BIARYLMETAPYRIMIDIN kinase inhibitors |
| WO2007056023A2 (en) | 2005-11-02 | 2007-05-18 | Targegen, Inc. | Thiazole inhibitors targeting resistant kinase mutations |
| JP2009519218A (ja) | 2005-11-03 | 2009-05-14 | エスジーエックス ファーマシューティカルズ、インコーポレイテッド | ピリミジニル−チオフェンキナーゼモジュレータ |
| PH12012501003B1 (en) | 2005-11-16 | 2018-04-06 | Cti Biopharma Corp | Oxygen linked pyrimidine derivatives |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| US8962643B2 (en) | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| WO2007127366A2 (en) | 2006-04-25 | 2007-11-08 | Targegen, Inc. | Kinase inhibitors and methods of use thereof |
| US8030487B2 (en) | 2006-07-07 | 2011-10-04 | Targegen, Inc. | 2-amino—5-substituted pyrimidine inhibitors |
| US20080021013A1 (en) | 2006-07-21 | 2008-01-24 | Cephalon, Inc. | JAK inhibitors for treatment of myeloproliferative disorders |
| EP2046759A1 (en) | 2006-07-21 | 2009-04-15 | Novartis AG | 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors |
| 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 |
| WO2009046416A1 (en) | 2007-10-05 | 2009-04-09 | Targegen Inc. | Anilinopyrimidines as jak kinase inhibitors |
| EP2296632A4 (en) | 2008-07-14 | 2014-11-12 | Otonomy Inc | COMPOSITIONS AND METHODS FOR MODULATING CONTROLLED RELEASE APOPTOSIS FOR THE TREATMENT OF OTIC DISORDERS |
| CN102112131A (zh) | 2008-08-05 | 2011-06-29 | 塔格根公司 | 治疗地中海贫血的方法 |
| US8987243B2 (en) | 2008-12-11 | 2015-03-24 | Cti Biopharma Corp. | 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-maleate salt |
| US20100278921A1 (en) | 2009-04-30 | 2010-11-04 | Fischer Cristina M | Solid oral formulation of abt-263 |
-
2006
- 2006-10-26 DK DK06836583.2T patent/DK1951684T3/en active
- 2006-10-26 US US11/588,638 patent/US7528143B2/en active Active
- 2006-10-26 RU RU2012103851/04A patent/RU2597364C2/ru active
- 2006-10-26 ES ES06836583.2T patent/ES2595636T3/es active Active
- 2006-10-26 NZ NZ567851A patent/NZ567851A/en unknown
- 2006-10-26 PT PT68365832T patent/PT1951684T/pt unknown
- 2006-10-26 MY MYPI20081381A patent/MY167260A/en unknown
- 2006-10-26 BR BR122021011788-8A patent/BR122021011788B1/pt active IP Right Grant
- 2006-10-26 MX MX2010010772A patent/MX362412B/es unknown
- 2006-10-26 PL PL06836583T patent/PL1951684T3/pl unknown
- 2006-10-26 EP EP06836583.2A patent/EP1951684B1/en active Active
- 2006-10-26 HU HUE06836583A patent/HUE028987T2/en unknown
- 2006-10-26 MX MX2018008723A patent/MX391408B/es unknown
- 2006-10-26 NZ NZ592990A patent/NZ592990A/xx unknown
- 2006-10-26 KR KR1020087013115A patent/KR101494468B1/ko active Active
- 2006-10-26 CN CN201310043377.0A patent/CN103626742B/zh active Active
- 2006-10-26 WO PCT/US2006/042044 patent/WO2007053452A1/en not_active Ceased
- 2006-10-26 JP JP2008538935A patent/JP5191391B2/ja active Active
- 2006-10-26 AU AU2006309013A patent/AU2006309013B2/en active Active
- 2006-10-26 RU RU2012103850/04A patent/RU2589878C2/ru active
- 2006-10-26 KR KR1020137021980A patent/KR101467723B1/ko active Active
- 2006-10-26 CA CA2628283A patent/CA2628283C/en not_active Expired - Fee Related
- 2006-10-26 LT LTEP06836583.2T patent/LT1951684T/lt unknown
- 2006-10-26 BR BRPI0618179-1A patent/BRPI0618179A2/pt not_active Application Discontinuation
- 2006-10-26 BR BR122021011787-0A patent/BR122021011787B1/pt active IP Right Grant
- 2006-11-01 TW TW095140348A patent/TWI444368B/zh active
-
2007
- 2007-04-26 US US11/796,717 patent/US7825246B2/en active Active
-
2008
- 2008-04-30 IL IL191167A patent/IL191167A/en active IP Right Grant
- 2008-05-30 NO NO20082447A patent/NO342221B1/no active Protection Beyond IP Right Term
- 2008-10-17 US US12/253,374 patent/US8138199B2/en active Active
-
2012
- 2012-11-26 JP JP2012257150A patent/JP5814903B2/ja active Active
-
2016
- 2016-10-12 CY CY20161101021T patent/CY1118330T1/el unknown
-
2021
- 2021-05-12 FI FIC20210010C patent/FIC20210010I1/fi unknown
- 2021-05-17 CY CY2021013C patent/CY2021013I2/el unknown
- 2021-05-17 NL NL301104C patent/NL301104I2/nl unknown
- 2021-05-18 HU HUS2100020C patent/HUS2100020I1/hu unknown
- 2021-05-21 LT LTPA2021509C patent/LTC1951684I2/lt unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013056930A5 (enExample) | ||
| JP2009513703A5 (enExample) | ||
| JP2021502387A5 (enExample) | ||
| RU2477723C2 (ru) | Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе | |
| RU2468021C2 (ru) | Гетероциклические соединения и их применение | |
| JP5881705B2 (ja) | Ｎａｍｐｔの阻害のための新規化合物及び組成物 | |
| RU2020123151A (ru) | Антагонисты tlr7/8 и их применение | |
| JP2019517487A5 (enExample) | ||
| RU2013144571A (ru) | Алинзамещенные хиназолины и способы их применения | |
| JP2009536620A5 (enExample) | ||
| JP2014518544A5 (enExample) | ||
| KR102796209B1 (ko) | 키나아제 억제제로서의 시클릭 이미노피리미딘 유도체 | |
| JP2018519245A5 (enExample) | ||
| JP2018516238A5 (enExample) | ||
| JP2016513661A5 (enExample) | ||
| HRP20141094T1 (hr) | 1,2,5-oksadiazoli kao inhibitori indolamin 2,3-dioksigenaze | |
| JP2013010792A5 (enExample) | ||
| JP2016518324A5 (enExample) | ||
| RU2016101548A (ru) | Соединения амидов гетероарилпиридона и азапиридона | |
| JP2020536971A5 (enExample) | ||
| WO2016082713A1 (zh) | 2-氨基嘧啶类化合物及其药物组合物和应用 | |
| RU2015107803A (ru) | Производные дигидроксипиримидинкарбоновой кислоты и их применение в лечении, облегчении или предотвращении вирусного заболевания | |
| JP2016506387A5 (enExample) | ||
| RU2003114740A (ru) | Азотсодержащие ароматические производные | |
| RU2015143542A (ru) | Ингибиторы jak2 и alk2 и способы их использования |