JP2005508300A5 - - Google Patents
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- Publication number
- JP2005508300A5 JP2005508300A5 JP2003507098A JP2003507098A JP2005508300A5 JP 2005508300 A5 JP2005508300 A5 JP 2005508300A5 JP 2003507098 A JP2003507098 A JP 2003507098A JP 2003507098 A JP2003507098 A JP 2003507098A JP 2005508300 A5 JP2005508300 A5 JP 2005508300A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- effective amount
- pharmaceutically effective
- heteroaryl
- 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 27
- 239000000203 mixture Substances 0.000 claims description 12
- 239000003112 inhibitor Substances 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- -1 cyclic acetal Chemical class 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 6
- 239000000651 prodrug Substances 0.000 claims 6
- 229940002612 prodrugs Drugs 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000011780 sodium chloride Substances 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 230000003197 catalytic Effects 0.000 claims 4
- 230000024881 catalytic activity Effects 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- 200000000018 inflammatory disease Diseases 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 208000002205 Allergic Conjunctivitis Diseases 0.000 claims 2
- 206010003246 Arthritis Diseases 0.000 claims 2
- 208000006673 Asthma Diseases 0.000 claims 2
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 2
- 206010039085 Rhinitis allergic Diseases 0.000 claims 2
- 125000003302 alkenyloxy group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 201000010105 allergic rhinitis Diseases 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 101700007619 AURKA Proteins 0.000 claims 1
- 102100010552 AURKA Human genes 0.000 claims 1
- 206010061430 Arthritis allergic Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010048768 Dermatosis Diseases 0.000 claims 1
- 208000005679 Eczema Diseases 0.000 claims 1
- 206010062639 Herpes dermatitis Diseases 0.000 claims 1
- 206010037162 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 208000006641 Skin Disease Diseases 0.000 claims 1
- 206010047124 Vasculitis necrotising Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000005530 alkylenedioxy group Chemical group 0.000 claims 1
- 201000011231 colorectal cancer Diseases 0.000 claims 1
- 201000004624 dermatitis Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 231100001003 eczema Toxicity 0.000 claims 1
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920000728 polyester Polymers 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 201000001263 psoriatic arthritis Diseases 0.000 claims 1
- 201000005404 rubella Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 102000016621 Focal Adhesion Protein-Tyrosine Kinases Human genes 0.000 description 10
- 108010067715 Focal Adhesion Protein-Tyrosine Kinases Proteins 0.000 description 10
- 210000004027 cells Anatomy 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 102000006495 integrins Human genes 0.000 description 3
- 108010044426 integrins Proteins 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 230000000240 adjuvant Effects 0.000 description 2
- 239000007900 aqueous suspension Substances 0.000 description 2
- 230000027455 binding Effects 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- 230000010261 cell growth Effects 0.000 description 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 230000005012 migration Effects 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical group CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- XJKJWTWGDGIQRH-BFIDDRIFSA-N Alginic acid Chemical compound O1[C@@H](C(O)=O)[C@@H](OC)[C@H](O)[C@H](O)[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](C)[C@@H](O)[C@H]1O XJKJWTWGDGIQRH-BFIDDRIFSA-N 0.000 description 1
- 108020000948 Antisense Oligonucleotides Proteins 0.000 description 1
- 206010059512 Apoptosis Diseases 0.000 description 1
- 229960003563 Calcium Carbonate Drugs 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N D-sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- NEFBYIFKOOEVPA-UHFFFAOYSA-K Dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
- 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
- 210000001650 Focal Adhesions Anatomy 0.000 description 1
- 239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 1
- 229960001375 Lactose Drugs 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 229920000272 Oligonucleotide Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- CZMRCDWAGMRECN-GDQSFJPYSA-N Sucrose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)[C@@]1(CO)[C@H](O)[C@@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-GDQSFJPYSA-N 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K Trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 239000000074 antisense oligonucleotide Substances 0.000 description 1
- 230000006907 apoptotic process Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000034196 cell chemotaxis Effects 0.000 description 1
- 230000035605 chemotaxis Effects 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000014509 gene expression Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000003446 ligand Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 230000001404 mediated Effects 0.000 description 1
- 230000003000 nontoxic Effects 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000002018 overexpression Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 230000000865 phosphorylative Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 102000027656 receptor tyrosine kinases Human genes 0.000 description 1
- 108091007921 receptor tyrosine kinases Proteins 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 150000004760 silicates Chemical class 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- 229960001790 sodium citrate Drugs 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000007885 tablet disintegrant Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 239000011778 trisodium citrate Substances 0.000 description 1
- 210000004881 tumor cells Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0115393.1A GB0115393D0 (en) | 2001-06-23 | 2001-06-23 | Chemical compounds |
| US30167801P | 2001-06-28 | 2001-06-28 | |
| PCT/GB2002/002835 WO2003000695A1 (fr) | 2001-06-23 | 2002-06-21 | Pyrrolopyrimidines utilisees en tant qu'inhibiteurs des proteines kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005508300A JP2005508300A (ja) | 2005-03-31 |
| JP2005508300A5 true JP2005508300A5 (fr) | 2006-01-05 |
| JP4344607B2 JP4344607B2 (ja) | 2009-10-14 |
Family
ID=9917225
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003507098A Expired - Fee Related JP4344607B2 (ja) | 2001-06-23 | 2002-06-21 | 蛋白キナーゼ阻害剤としてのピロロピリミジン |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP1404676A1 (fr) |
| JP (1) | JP4344607B2 (fr) |
| CN (1) | CN1294135C (fr) |
| AU (1) | AU2002314325B8 (fr) |
| BR (1) | BR0210652A (fr) |
| CA (1) | CA2451932C (fr) |
| CZ (1) | CZ20033443A3 (fr) |
| EA (1) | EA007415B1 (fr) |
| EC (1) | ECSP034922A (fr) |
| EE (1) | EE05432B1 (fr) |
| GB (1) | GB0115393D0 (fr) |
| HU (1) | HUP0400300A3 (fr) |
| ME (1) | MEP19308A (fr) |
| NZ (1) | NZ529766A (fr) |
| OA (1) | OA12632A (fr) |
| PL (1) | PL374096A1 (fr) |
| RS (1) | RS51698B (fr) |
| SK (1) | SK15882003A3 (fr) |
| TN (1) | TNSN03144A1 (fr) |
| TR (1) | TR200302242T2 (fr) |
| UA (1) | UA76760C2 (fr) |
| WO (1) | WO2003000695A1 (fr) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0202679D0 (en) * | 2002-02-05 | 2002-03-20 | Glaxo Group Ltd | Novel compounds |
| EP1534286B1 (fr) | 2002-07-29 | 2009-12-09 | Rigel Pharmaceuticals, Inc. | Procede de traitement ou de prevention de maladies auto-immunes au moyen de composes de 2,4-pyrimidinediamine |
| CA2546192C (fr) | 2003-11-17 | 2010-04-06 | Pfizer Products Inc. | Composes de pyrrolopyrimidine utiles dans le traitement du cancer |
| MXPA06005882A (es) * | 2003-11-25 | 2006-06-27 | Pfizer Prod Inc | Metodo de tratamiento de la aterosclerosis. |
| WO2005105788A1 (fr) * | 2004-04-23 | 2005-11-10 | Takeda San Diego, Inc. | Derives d'indole et leur utilisation en tant qu'inhibiteurs de kinases |
| FR2876103B1 (fr) | 2004-10-01 | 2008-02-22 | Aventis Pharma Sa | Nouveaux derives bis-azaindoles, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| JP2008516973A (ja) | 2004-10-15 | 2008-05-22 | タケダ サン ディエゴ インコーポレイテッド | キナーゼ阻害剤 |
| FR2878849B1 (fr) | 2004-12-06 | 2008-09-12 | Aventis Pharma Sa | Indoles substitues, compositions les contenant, procede de fabrication et utilisation |
| JP2008543855A (ja) | 2005-06-13 | 2008-12-04 | ライジェル ファーマシューティカルズ， インコーポレイテッド | 変形性骨疾患を処置するための方法および組成物 |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| ES2611588T3 (es) | 2005-12-13 | 2017-05-09 | Incyte Holdings Corporation | Pirrolo[2,3-b]piridinas y pirrolo[2,3-b]pirimidinas sustituidas con heteroarilo como inhibidores de quinasas Janus |
| US20100120717A1 (en) | 2006-10-09 | 2010-05-13 | Brown Jason W | Kinase inhibitors |
| LT3070090T (lt) | 2007-06-13 | 2019-06-25 | Incyte Holdings Corporation | Janus kinazės inhibitoriaus (r)-3-(4-(7h-pirol[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrilo druskų panaudojimas |
| EP2247596A2 (fr) | 2008-01-11 | 2010-11-10 | Natco Pharma Limited | Nouveaux derives de pyrazolo [3,4 -d] pyrimidine en tant qu'agents anticancereux |
| CN104592231A (zh) | 2008-06-10 | 2015-05-06 | Abbvie公司 | 新的三环化合物 |
| EA020494B1 (ru) | 2009-05-22 | 2014-11-28 | Инсайт Корпорейшн | 3-[4-(7H-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1H-ПИРАЗОЛ-1-ИЛ]ОКТАН- ИЛИ ГЕПТАННИТРИЛ КАК JAK-ИНГИБИТОРЫ |
| EA025520B1 (ru) | 2009-05-22 | 2017-01-30 | Инсайт Холдингс Корпорейшн | N-(ГЕТЕРО)АРИЛПИРРОЛИДИНОВЫЕ ПРОИЗВОДНЫЕ ПИРАЗОЛ-4-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ И ПИРРОЛ-3-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ |
| WO2011018894A1 (fr) * | 2009-08-10 | 2011-02-17 | Raqualia Pharma Inc. | Dérivés de pyrrolopyrimidine comme modulateurs des canaux potassium |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2485589A4 (fr) | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | Inhibiteurs hétéroaryles de btk |
| DK2506716T3 (en) | 2009-12-01 | 2017-09-04 | Abbvie Inc | HIS UNKNOWN TRICYCLIC RELATIONS |
| NZ602313A (en) | 2010-03-10 | 2014-08-29 | Incyte Corp | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| ME02445B (fr) | 2010-05-21 | 2016-09-20 | Incyte Holdings Corp | Formulation topique pour inhibiteur de jak |
| WO2012068440A1 (fr) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Pyrrolopyridines et pyrrolopyrimidines à substitution hétérocyclique utilisées en tant qu'inhibiteurs des jak |
| CA2818542A1 (fr) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Derives pyrrolopyridine et pyrrolopyrimidine a substitution cyclobutyle utilises comme inhibiteurs des jak |
| CN103476776B (zh) * | 2011-01-07 | 2016-09-28 | 北京赛林泰医药技术有限公司 | 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物 |
| CN102093364B (zh) | 2011-01-07 | 2015-01-28 | 北京赛林泰医药技术有限公司 | 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物 |
| WO2012177606A1 (fr) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Dérivés d'azétidinyl-phényl-, de pyridyl- ou de pyrazinyl-carboxamide en tant qu'inhibiteurs des jak |
| 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 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| EP2838898B1 (fr) | 2012-04-20 | 2017-01-18 | Advinus Therapeutics Limited | Composés hétéro-bicycliques substitués, compositions et leurs applications médicinales |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| PT2877467T (pt) | 2012-07-26 | 2017-01-02 | Glaxo Group Ltd | 2-(azaindol-2-il)benzimidazóis como inibidores de pad4 |
| CN104981247A (zh) * | 2012-09-06 | 2015-10-14 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
| LT2919766T (lt) | 2012-11-15 | 2021-09-27 | Incyte Holdings Corporation | Ruksolitinibo pailginto atpalaidavimo vaisto formos |
| SG10201707259PA (en) | 2013-03-06 | 2017-10-30 | Incyte Corp | Processes and intermediates for making a jak inhibitor |
| CN105189481A (zh) | 2013-03-13 | 2015-12-23 | 艾伯维公司 | 吡啶cdk9激酶抑制剂 |
| US8969375B2 (en) | 2013-03-13 | 2015-03-03 | Abbvie, Inc. | CDK9 kinase inhibitors |
| CA2903538A1 (fr) | 2013-03-14 | 2014-10-02 | Abbvie Inc. | Inhibiteurs de pyrrolopyrimidine cdk9 kinase |
| UY35419A (es) | 2013-03-14 | 2014-10-31 | Abbvie Inc | Inhibidores de cdk9 quinasa de pirrolo (2,3- b) piridina |
| US9796708B2 (en) | 2013-03-14 | 2017-10-24 | Abbvie Inc. | Pyrrolo [2,3-B] pyridine CDK9 kinase inhibitors |
| ES2792549T3 (es) | 2013-08-07 | 2020-11-11 | Incyte Corp | Formas de dosificación de liberación sostenida para un inhibidor de JAK1 |
| CN104804001B9 (zh) * | 2014-01-24 | 2022-02-08 | 江苏柯菲平医药股份有限公司 | 4-取代吡咯并[2,3-d]嘧啶化合物及其用途 |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| US20170129902A1 (en) | 2015-10-16 | 2017-05-11 | Abbvie Inc. | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-alpha]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
| US10550126B2 (en) | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11365198B2 (en) | 2015-10-16 | 2022-06-21 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11512092B2 (en) | 2015-10-16 | 2022-11-29 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11524964B2 (en) | 2015-10-16 | 2022-12-13 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| US11780848B2 (en) | 2015-10-16 | 2023-10-10 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof |
| TW201840318A (zh) | 2017-03-09 | 2018-11-16 | 美商艾伯維有限公司 | 治療克羅恩氏病和潰瘍性結腸炎之方法 |
| US11564922B2 (en) | 2017-03-09 | 2023-01-31 | Abbvie Inc. | Methods of treating crohn's disease and ulcerative colitis |
| WO2019113487A1 (fr) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Polythérapie à faible dose pour le traitement de néoplasmes myéloprolifératifs |
| AR114810A1 (es) | 2018-01-30 | 2020-10-21 | Incyte Corp | Procesos e intermedios para elaborar un inhibidor de jak |
| AU2019245420A1 (en) | 2018-03-30 | 2020-11-12 | Incyte Corporation | Treatment of hidradenitis suppurativa using JAK inhibitors |
| RS65335B1 (sr) | 2018-10-05 | 2024-04-30 | Annapurna Bio Inc | Jedinjenja i kompozicije za lečenje stanja povezanih sa aktivnošću receptora apj |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1441497A (en) * | 1996-01-23 | 1997-08-20 | Novartis Ag | Pyrrolopyrimidines and processes for their preparation |
| EP0946554A1 (fr) * | 1996-11-27 | 1999-10-06 | Pfizer Inc. | Derives de pyrimidines bicycliques fusionnes |
| PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| CN1128800C (zh) * | 1998-06-19 | 2003-11-26 | 辉瑞产品公司 | 吡咯并[2,3－d]嘧啶化合物及其组合物和用途 |
| CA2344262A1 (fr) * | 1998-09-18 | 2000-03-30 | Basf Aktiengesellschaft | 4-aminopyrrolopyrimidines utilisees comme inhibiteurs de kinases |
| TR200400105T4 (tr) * | 1999-12-10 | 2004-02-23 | Prizer Products Inc. | Pirrolo [2,3-d] pirimidin bileşikleri |
-
2001
- 2001-06-23 GB GBGB0115393.1A patent/GB0115393D0/en not_active Ceased
-
2002
- 2002-06-21 ME MEP-193/08A patent/MEP19308A/xx unknown
- 2002-06-21 EA EA200400073A patent/EA007415B1/ru not_active IP Right Cessation
- 2002-06-21 EP EP02740895A patent/EP1404676A1/fr not_active Withdrawn
- 2002-06-21 RS YU99203A patent/RS51698B/en unknown
- 2002-06-21 HU HU0400300A patent/HUP0400300A3/hu unknown
- 2002-06-21 BR BR0210652-3A patent/BR0210652A/pt not_active Application Discontinuation
- 2002-06-21 NZ NZ529766A patent/NZ529766A/en not_active IP Right Cessation
- 2002-06-21 CZ CZ20033443A patent/CZ20033443A3/cs unknown
- 2002-06-21 JP JP2003507098A patent/JP4344607B2/ja not_active Expired - Fee Related
- 2002-06-21 OA OA1200300335A patent/OA12632A/en unknown
- 2002-06-21 SK SK1588-2003A patent/SK15882003A3/sk not_active Application Discontinuation
- 2002-06-21 TN TNPCT/GB2002/002835A patent/TNSN03144A1/en unknown
- 2002-06-21 UA UA2004010502A patent/UA76760C2/uk unknown
- 2002-06-21 AU AU2002314325A patent/AU2002314325B8/en not_active Ceased
- 2002-06-21 TR TR2003/02242T patent/TR200302242T2/xx unknown
- 2002-06-21 WO PCT/GB2002/002835 patent/WO2003000695A1/fr active Application Filing
- 2002-06-21 CN CNB028119320A patent/CN1294135C/zh not_active Expired - Fee Related
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