JP2014521725A5 - - Google Patents
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- JP2014521725A5 JP2014521725A5 JP2014525162A JP2014525162A JP2014521725A5 JP 2014521725 A5 JP2014521725 A5 JP 2014521725A5 JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014525162 A JP2014525162 A JP 2014525162A JP 2014521725 A5 JP2014521725 A5 JP 2014521725A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- pharmaceutically acceptable
- acceptable salt
- methyl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 239000000203 mixture Substances 0.000 claims 17
- 238000009472 formulation Methods 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 9
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims 9
- 239000002552 dosage form Substances 0.000 claims 8
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 8
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 5
- 208000003476 primary myelofibrosis Diseases 0.000 claims 5
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 206010028537 myelofibrosis Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 208000037244 polycythemia vera Diseases 0.000 claims 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 239000002207 metabolite Substances 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- -1 (3R) -3-cyclopentyl-3- [4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl] propanenitrile phosphorus Chemical compound 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 208000033755 Neutrophilic Chronic Leukemia Diseases 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 208000021668 chronic eosinophilic leukemia Diseases 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 230000002071 myeloproliferative effect Effects 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161522001P | 2011-08-10 | 2011-08-10 | |
| US61/522,001 | 2011-08-10 | ||
| PCT/US2012/050252 WO2013023119A1 (en) | 2011-08-10 | 2012-08-10 | JAK P13K/mTOR COMBINATION THERAPY |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014521725A JP2014521725A (ja) | 2014-08-28 |
| JP2014521725A5 true JP2014521725A5 (enExample) | 2015-09-17 |
Family
ID=46690743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014525162A Pending JP2014521725A (ja) | 2011-08-10 | 2012-08-10 | ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9358229B2 (enExample) |
| EP (1) | EP2741747A1 (enExample) |
| JP (1) | JP2014521725A (enExample) |
| CA (1) | CA2844507A1 (enExample) |
| HK (1) | HK1198579A1 (enExample) |
| WO (1) | WO2013023119A1 (enExample) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214484B (zh) | 2005-12-13 | 2016-07-06 | 因塞特控股公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶 |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| HUE029236T2 (en) | 2007-06-13 | 2017-02-28 | Incyte Holdings Corp | (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor |
| PE20211639A1 (es) | 2009-01-15 | 2021-08-24 | Incyte Holdings Corp | Procesos para preparar inhibidores de jak y compuestos intermediarios relacionado |
| EP2432472B1 (en) | 2009-05-22 | 2019-10-02 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| MY156727A (en) * | 2009-05-22 | 2016-03-15 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| 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 |
| EP3354652B1 (en) | 2010-03-10 | 2020-05-06 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| AR084691A1 (es) | 2010-05-21 | 2013-06-05 | Incyte Corp | Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| CA2844507A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | Jak pi3k/mtor combination therapy |
| 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 |
| WO2013072392A1 (en) * | 2011-11-15 | 2013-05-23 | Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute For Biomedical Research | Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the janus kinase 2-signal transducer and activator of transcription 5 pathway |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| JP6359546B2 (ja) | 2012-11-01 | 2018-07-18 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害薬としての三環式縮合チオフェン誘導体 |
| TWI761825B (zh) | 2012-11-15 | 2022-04-21 | 美商英塞特控股公司 | 盧梭利替尼之緩釋性劑型 |
| MX384910B (es) | 2013-03-06 | 2025-03-14 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak. |
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| SG11201600815WA (en) | 2013-08-07 | 2016-03-30 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| CN104744302A (zh) * | 2013-12-31 | 2015-07-01 | 上海药谷药业有限公司 | 一种2-(4-氨基苯基)-2-甲基丙腈化合物的制备方法 |
| CN106413716B (zh) | 2014-04-08 | 2020-03-27 | 因赛特公司 | 通过jak和pi3k抑制剂组合治疗b细胞恶性肿瘤 |
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| CN113768934A (zh) | 2018-03-30 | 2021-12-10 | 因赛特公司 | 使用jak抑制剂治疗化脓性汗腺炎 |
| JP7565798B2 (ja) | 2018-03-30 | 2024-10-11 | インサイト・コーポレイション | 炎症性皮膚疾患のバイオマーカー |
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| CN118978535A (zh) | 2018-05-01 | 2024-11-19 | 锐新医药公司 | 作为mTOR抑制剂的C40-、C28-及C-32连接的雷帕霉素类似物 |
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| WO2026020084A1 (en) * | 2024-07-18 | 2026-01-22 | The Trustees Of The University Of Pennsylvania | Combination of topical kinase inhibitors to achieve synergistic clearance of skin cancers and related lesions |
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2012
- 2012-08-10 CA CA2844507A patent/CA2844507A1/en not_active Abandoned
- 2012-08-10 JP JP2014525162A patent/JP2014521725A/ja active Pending
- 2012-08-10 HK HK14112079.3A patent/HK1198579A1/xx unknown
- 2012-08-10 EP EP12748346.9A patent/EP2741747A1/en not_active Withdrawn
- 2012-08-10 US US13/571,525 patent/US9358229B2/en active Active
- 2012-08-10 WO PCT/US2012/050252 patent/WO2013023119A1/en not_active Ceased