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1. 发明申请

WO0232861A2 ORALLY ACTIVE SALTS WITH TYROSINE KINASE ACTIVITY 审中-公开
标题翻译： ORR活性盐与TYROSINE激酶活性
公开(公告)号：WO0232861A2
公开(公告)日：2002-04-25
申请号：PCT/US0132508
申请日：2001-10-17
申请人： MERCK & CO INC , FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
发明人： FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to orally active salts of compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
摘要翻译：本发明涉及化合物，其抑制，调节和/或调控酪氨酸激酶信号转导，含有这些化合物的组合物的口服活性的盐，以及使用它们来治疗酪氨酸激酶 - 依赖性疾病和病症，如血管生成，癌症的方法，肿瘤生长，动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病，炎性疾病等。

2. 发明申请

WO2004087651A3 FORMULATIONS FOR TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂的配方
公开(公告)号：WO2004087651A3
公开(公告)日：2004-12-16
申请号：PCT/US2004008828
申请日：2004-03-23
申请人： MERCK & CO INC , KARKI SHYAM B , DESHPANDE SAMEER R , THOMPSON KAREN C , PAYNE ANNE H , GANDEK THOMAS P
发明人： KARKI SHYAM B , DESHPANDE SAMEER R , THOMPSON KAREN C , PAYNE ANNE H , GANDEK THOMAS P
IPC分类号： A01N43/42 , A61K31/44 , C07D20060101
CPC分类号： A61K31/44 , A61K9/0095 , A61K9/10 , A61K9/1617 , A61K9/1623 , A61K9/1652 , A61K31/496
摘要： The present invention is related to a powder, powder blend or granulation formulation of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one, a tyrosine kinase inhibitor, which is adapted for reconstitution with a diluent. This invention is also related to a prepared aqueous suspension, or dispersion, formulation, particularly to a stable oral pharmaceutical formulation, comprising granules of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one mixed with a diluent. Additionally, the present invention is related to the method of preparing these formulations.
摘要翻译：本发明涉及3- [5-（4-甲磺酰基 - 哌嗪-1-基甲基）-1H-吲哚-2-基] -1H-喹啉-2-酮的粉末，粉末混合物或造粒制剂，酪氨酸激酶抑制剂，适用于用稀释剂重建。本发明还涉及制备的含水悬浮液或分散体制剂，特别涉及稳定的口服药物制剂，其包含3- [5-（4-甲磺酰基 - 哌嗪-1-基甲基）-1H-吲哚-2-基] 基] -1H-喹啉-2-酮与稀释剂混合。此外，本发明涉及制备这些制剂的方法。

3. 发明申请

WO0130804A3 SALT FORM OF A CONJUGATE USEFUL IN THE TREATMENT OF PROSTATE CANCER 审中-公开
标题翻译：联合用于治疗前列腺癌的盐形式
公开(公告)号：WO0130804A3
公开(公告)日：2002-01-10
申请号：PCT/US0029610
申请日：2000-10-27
申请人： MERCK & CO INC , KARKI SHYAM B , CAMERON MARK , LIEBERMAN DAVID R , LYNCH JOSEPH E , ROBBINS MICHAEL A , SHI YAO JUN , ALMARSSON ORN , KAUFMAN MICHAEL J , NERURKAR MANEESH J
发明人： KARKI SHYAM B , CAMERON MARK , LIEBERMAN DAVID R , LYNCH JOSEPH E , ROBBINS MICHAEL A , SHI YAO-JUN , ALMARSSON ORN , KAUFMAN MICHAEL J , NERURKAR MANEESH J
IPC分类号： A61K9/19 , A61K38/00 , A61K47/12 , A61K47/26 , A61K47/48 , A61P13/08 , A61P35/00 , C07K1/30 , C07K9/00 , C07K14/47
CPC分类号： A61K47/6425 , A61K47/65
摘要： The present invention is directed to the sodium salt of formula (5) which may be useful in the treatment of prostate cancer and benign prostatic hyperplasia. Also described are lyophilized formulations that comprise the sodium salt 5 or the corresponding free acid.
摘要翻译：本发明涉及可用于治疗前列腺癌和良性前列腺增生的式（5）的钠盐。还描述了包含钠盐5或相应的游离酸的冻干制剂。

4. 发明专利

CA2398828A1 A PHARMACEUTICAL COMPOSITION CONTAINING AN INDOLOPYRROLOCARBAZOLE DERIVATIVE 未知
公开(公告)号：CA2398828A1
公开(公告)日：2004-02-09
申请号：CA2398828
申请日：2002-08-20
申请人： BANYU PHARMA CO LTD , MERCK & CO INC
发明人： BRESLIN DAVID T , SATO YUICHI , KARKI SHYAM B
IPC分类号： A61K9/00 , A61K31/7056 , A61K47/02 , A61K47/10 , A61P35/00
摘要： The present invention is directed to a pharmaceutical composition comprising a compound of Formula I dissolved in propylene glycol and water. The present invention also relates to a pharmaceutical composition containing a compound of Formula I dissolved in propylene glycol and a buffer that has a pH betwee n about 3 and about 5

5. 发明专利

AU2687702A Orally active salts with tyrosine kinase activity 未知
公开(公告)号：AU2687702A
公开(公告)日：2002-04-29
申请号：AU2687702
申请日：2001-10-17
申请人： MERCK & CO INC
发明人： FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14
摘要： The present invention relates to orally active salts of compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

6. 发明专利

AU2004225949B2 Formulations for tyrosine kinase inhibitors 未知
公开(公告)号：AU2004225949B2
公开(公告)日：2006-11-02
申请号：AU2004225949
申请日：2004-03-23
申请人： MERCK & CO INC
发明人： PAYNE ANNE H , KARKI SHYAM B , GANDEK THOMAS P , THOMPSON KAREN C , DESHPANDE SAMEER R
IPC分类号： A01N43/42 , A61K31/44 , C07D20060101
摘要： The present invention is related to a powder, powder blend or granulation formulation of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one, a tyrosine kinase inhibitor, which is adapted for reconstitution with a diluent. This invention is also related to a prepared aqueous suspension, or dispersion, formulation, particularly to a stable oral pharmaceutical formulation, comprising granules of 3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1H-indol-2-yl]-1H-quinolin-2-one mixed with a diluent. Additionally, the present invention is related to the method of preparing these formulations.

7. 发明专利

CA2387901A1 SALT FORM OF A CONJUGATE USEFUL IN THE TREATMENT OF PROSTATECANCER 未知
公开(公告)号：CA2387901A1
公开(公告)日：2001-05-03
申请号：CA2387901
申请日：2000-10-27
申请人： MERCK & CO INC
发明人： KAUFMAN MICHAEL J , ALMARSSON ORN , NERURKAR MANEESH J , LYNCH JOSEPH E , LIEBERMAN DAVID R , KARKI SHYAM B , CAMERON MARK , SHI YAO-JUN , ROBBINS MICHAEL A
IPC分类号： A61K9/19 , A61K38/00 , A61K47/12 , A61K47/26 , A61K47/48 , A61P13/08 , A61P35/00 , C07K1/30 , C07K9/00 , C07K14/47
摘要： The present invention is directed to the sodium salt of formula (5) which ma y be useful in the treatment of prostate cancer and benign prostatic hyperplasia. Also described are lyophilized formulations that comprise the sodium salt 5 or the corresponding free acid.

8. 发明公开

EP1496982A4 SOLID FORMS OF SALTS WITH TYROSINE KINASE ACTIVITY 审中-公开
标题翻译：具有酪氨酸激酶-EFFECT盐的固体形式
公开(公告)号：EP1496982A4
公开(公告)日：2006-07-19
申请号：EP03746960
申请日：2003-04-11
申请人： MERCK & CO INC , BANYU PHARMA CO LTD
发明人： KARKI SHYAM B , PAYACK JOSEPH , TREEMANEEKARN VARAPORN , WANG YALING , SATO YUICHI
IPC分类号： C07D401/04 , A61K31/138 , A61K31/337 , A61K31/4465 , A61K31/4535 , A61K31/454 , A61K31/496 , A61K38/00 , A61K38/21 , A61K39/395 , A61K45/00 , A61P1/04 , A61P1/18 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/04 , A61P13/00 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/08 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/08 , A61P43/00
CPC分类号： C07D401/04

9. 发明公开

EP1328519A4 ORALLY ACTIVE SALTS WITH TYROSINE KINASE ACTIVITY 有权
标题翻译：光学活性的盐具有酪氨酸激酶活性
公开(公告)号：EP1328519A4
公开(公告)日：2004-12-15
申请号：EP01987742
申请日：2001-10-17
申请人： MERCK & CO INC
发明人： FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D241/04 , A61K31/4704 , C07D243/06
CPC分类号： C07D401/04 , C07D401/14

10. 发明专利

ES2247187T3 SALES ORALMENTE ACTIVAS CONACTIVIDAD TIROSINA QUINASA. 未知
公开(公告)号：ES2247187T3
公开(公告)日：2006-03-01
申请号：ES01987742
申请日：2001-10-17
申请人： MERCK & CO INC
发明人： FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D241/04 , C07D243/06 , A61K31/4704
摘要： Se ilustra una realización de la invención por una sal mesilato de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)-1H-indol- 2-il]-1H-quinolin-2-ona. Otra realización es una sal cloruro de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)-1H-indol-2-il]-1H-quinolin-2-ona. También está incluida dentro del alcance de la invención la sal mesilato de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)- 1H-indol-2-il]-1H-quinolin-2-ona conforme a una forma cristalina caracterizada por un patrón de difracción de rayos X de polvo de que tiene ángulos de difracción de: 7, 39, 8, 20, 9, 03, 9, 90, 10, 94, 15, 45, 17, 12, 17, 84, 18, 29, 18, 64, 19, 24, 19, 77, 20, 28, 21, 73, 22, 49, 23, 27, 24, 15, 24, 73, 25, 40, 26, 79 y 27, 50. Otra realización es la sal mesilato de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)-1H-indol-2-il]-1H-quinolin-2-ona en forma cristalina caracterizada por un patrón de difracción de rayos X de polvo que tiene ángulos de difracción de: 6, 94, 8, 01, 9, 74, 10, 47, 10, 77, 11, 75, 12, 61, 14,02, 15, 28, 15, 86, 16, 93, 17, 61, 18, 69, 19, 04, 19, 47, 20, 11, 21, 56, 21, 94, 22, 53, 23, 85 y 27, 22. Otra realización es la sal cloruro de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)-1H-indol-2-il]-1H-quinolin-2-ona en forma cristalina caracterizada por un patrón de difracción de rayos X de polvo que tiene ángulos de difracción de: 7, 08, 7, 86, 8, 99, 14, 54, 15, 40, 16, 14, 16, 81, 18, 06, 19, 91, 20, 72, 22, 72, 24, 11, 26, 09, 28, 67 y 29, 89. Y otra realización más es la sal cloruro de 3-[5-(4-metanosulfonil-piperazin-1-ilmetil)-1H-indol-2-il]-1H-quino-lin- 2-ona en forma cristalina caracterizada por un patrón de difracción de rayos X de polvo que tiene varios picos de difracción entre 5º y 30º 2-theta y una endotermia de fusión de 284, 08ºC a una velocidad de 10ºC por minuto.

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