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1. 发明申请

WO2005077945A3 PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 审中-公开
标题翻译：制备2-氨基噻唑-5-芳族羧酰胺作为激酶抑制剂的方法
公开(公告)号：WO2005077945A3
公开(公告)日：2006-05-18
申请号：PCT/US2005003728
申请日：2005-02-04
申请人： SQUIBB BRISTOL MYERS CO , CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
IPC分类号： C07C235/28 , C07C237/42 , C07D277/56 , C07D417/12 , C07D417/14 , A61P31/04 , A61P31/12 , C07D239 , C07D241 , C07D277
CPC分类号： C07D417/12 , C07C235/28 , C07C237/42
摘要： The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R 2 , R 3 , R 4 , and R 5 , are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
摘要翻译：本发明涉及制备具有式（I）的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R 2，R 3， R 4，R 4和R 5如本说明书中所定义，该化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶抑制剂和 p38激酶。

2. 发明申请

WO2007002308A9 PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN 审中-公开
标题翻译：制备三唑取代的阿拉伯糖氧基哌嗪衍生物和其中产生的新盐形式的方法
公开(公告)号：WO2007002308A9
公开(公告)日：2007-03-01
申请号：PCT/US2006024335
申请日：2006-06-21
申请人： SQUIBB BRISTOL MYERS CO , SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , KRONENTHAL DAVID R , SIRARD PIERRE , LAJEUNESSE JEAN , DROGHINI ROBERTO , CHIDAMBARAM RAMAKRISHNAN , QIAN XINHUA , NATALIE JR KENNETH J , PACK SHAWN K , REISING NATHAN , TANG ERQING , FAKES MICHAEL G , GAO QI , QIAN FENG , VAKKALAGADDA BLISSE J , LAI CHIAJEN , KUANG SHAN-MING
发明人： SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , KRONENTHAL DAVID R , SIRARD PIERRE , LAJEUNESSE JEAN , DROGHINI ROBERTO , CHIDAMBARAM RAMAKRISHNAN , QIAN XINHUA , NATALIE JR KENNETH J , PACK SHAWN K , REISING NATHAN , TANG ERQING , FAKES MICHAEL G , GAO QI , QIAN FENG , VAKKALAGADDA BLISSE J , LAI CHIAJEN , KUANG SHAN-MING
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoleoxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
摘要翻译：提供了制备三唑取代的氮杂吲哚氧乙酸哌嗪衍生物的方法。还提供了在上述方法中产生的新中间体以及1,2,3-三唑取代的氮杂吲哚氧乙酸哌嗪衍生物的新型N-1和无定形形式以及制备这种新型形式的方法。

3. 发明申请

WO2007002308A3 PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN 审中-公开
标题翻译：制备三唑取代的氮杂双环氧哌嗪衍生物及其生产的新型盐形式的方法
公开(公告)号：WO2007002308A3
公开(公告)日：2007-07-12
申请号：PCT/US2006024335
申请日：2006-06-21
申请人： SQUIBB BRISTOL MYERS CO , SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , KRONENTHAL DAVID R , SIRARD PIERRE , LAJEUNESSE JEAN , DROGHINI ROBERTO , CHIDAMBARAM RAMAKRISHNAN , QIAN XINHUA , NATALIE JR KENNETH J , PACK SHAWN K , REISING NATHAN , TANG ERQING , FAKES MICHAEL G , GAO QI , QIAN FENG , VAKKALAGADDA BLISSE J , LAI CHIAJEN , KUANG SHAN-MING
发明人： SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , KRONENTHAL DAVID R , SIRARD PIERRE , LAJEUNESSE JEAN , DROGHINI ROBERTO , CHIDAMBARAM RAMAKRISHNAN , QIAN XINHUA , NATALIE JR KENNETH J , PACK SHAWN K , REISING NATHAN , TANG ERQING , FAKES MICHAEL G , GAO QI , QIAN FENG , VAKKALAGADDA BLISSE J , LAI CHIAJEN , KUANG SHAN-MING
IPC分类号： C07D471/04 , A61K31/4745 , A61P31/12
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoleoxoacetic piperazine derivatives and processes for producing such novel forms are also provided.
摘要翻译：提供了制备三唑取代的氮杂糊精乙酸哌嗪衍生物的方法。还提供了在上述方法中制备的新型中间体和新的N-1和无定形形式的1,2,3-三唑取代的氮杂糊精乙酸哌嗪衍生物和制备这种新型的方法。

4. 发明专利

HRP20100166T4 POSTUPAK ZA PRIPREMU 2-AMINOTIAZOL-5-AROMATIÄŚNIH KARBOKSAMIDA KAO INHIBITORA KINAZE 未知
公开(公告)号：HRP20100166T4
公开(公告)日：2013-09-30
申请号：HRP20100166
申请日：2010-03-22
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
IPC分类号： C07D277/56 , A61P31/04 , A61P31/12 , C07C235/28 , C07C237/42 , C07D417/12 , C07D417/14

5. 发明专利

GEP20094804B PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 未知
公开(公告)号：GEP20094804B
公开(公告)日：2009-10-26
申请号：GEAP2005009607
申请日：2005-02-04
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHIDAMBARAM RAMAKRISHNAN , GALELLA MICHAEL , DIMARCO JOHN D , LAJEUNESSE JEAN , DROGHINI ROBERTO , CHEN BANG-CHI
IPC分类号： A61K31/425 , C07C235/28 , C07C237/42 , C07D277/42 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds having the formula (I) and processes for preparing crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein. Said compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

6. 发明专利

PE20070122A1 PROCESO PARA PREPARAR DERIVADOS DE PIPERAZINA AZINDOLOXOACETICA SUSTITUIDA CON TRIAZOL Y NUEVAS FORMAS DE SAL PRODUCIDAS DE LOS MISMOS 未知
公开(公告)号：PE20070122A1
公开(公告)日：2007-03-11
申请号：PE2006000714
申请日：2006-06-22
申请人： SQUIBB BRISTOL MYERS CO
发明人： SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , SIRARD PIERRE , DROGHINI ROBERTO , QIAN XINHUA , PACK SHAWN K , FAKES MICHAEL G , QIAN FENG , KUANG SHAN-MING , LAI CHIAJEN , VAKKALAGADDA BLISSE J , GAO QI , TANG ERQUING , NATALIE , CHIDAMBARAM RAMAKRISHNAN , LAJEUNESSE JEAN , KRONENTHAL DAVID R
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D471/02
摘要： SE REFIERE A UN COMPUESTO DE FORMULA A, B, C, D ENTRE OTROS DONDE R18 ES H, ALQUILO; R1, R2 Y R3 SON CADA UNO H, HALOGENO, CIANO, NITRO, ENTRE OTROS. UN COMPUESTO PREFERIDO ES II. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A PROCEDIMIENTOS DE PREPRACION DE LOS COMPUESTOS MENCIONADOS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DEL SIDA

7. 发明专利

PE01222007A1 PROCESO PARA PREPARAR DERIVADOS DE PIPERAZINA AZINDOLOXOACETICA SUSTITUIDA CON TRIAZOL Y NUEVAS FORMAS DE SAL PRODUCIDAS DE LOS MISMOS 未知
公开(公告)号：PE01222007A1
公开(公告)日：2007-03-11
申请号：PE0007142006
申请日：2006-06-22
申请人： SQUIBB BRISTOL MYERS CO
发明人： SOUNDARARAJAN NACHIMUTHU , QIU YUPING , HU WENHAO , SIRARD PIERRE , DROGHINI ROBERTO , QIAN XINHUA , PACK SHAWN K , FAKES MICHAEL G , QIAN FENG , KUANG SHAN-MING , LAI CHIAJEN , VAKKALAGADDA BLISSE J , GAO QI , TANG ERQUING , NATALIE , CHIDAMBARAM RAMAKRISHNAN , LAJEUNESSE JEAN , KRONENTHAL DAVID R
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/5377 , A61K31/55 , C07D471/02
CPC分类号： C07D471/04 , C07C311/49 , C07D213/26
摘要： SE REFIERE A UN COMPUESTO DE FORMULA A, B, C, D ENTRE OTROS DONDE R18 ES H, ALQUILO; R1, R2 Y R3 SON CADA UNO H, HALOGENO, CIANO, NITRO, ENTRE OTROS. UN COMPUESTO PREFERIDO ES II. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A PROCEDIMIENTOS DE PREPRACION DE LOS COMPUESTOS MENCIONADOS. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DEL SIDA

8. 发明专利

AR047533A1 PROCESO PARA PREPARAR CARBOXAMIDAS 2-AMINOTIAZOL-5-AROMATICAS COMO INHIBIDORES DE LA QUINASA 未知
公开(公告)号：AR047533A1
公开(公告)日：2006-01-25
申请号：ARP050100427
申请日：2005-02-04
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DI MARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM
IPC分类号： C07C235/28 , C07C237/42 , C07D277/56 , C07D417/12 , C07D417/14
摘要： Reivindicacion 1: U proceso para preparar un compuesto que tiene la formula (1), en donde L, Ar, R2, R3, R4, R5, y m son como se definen abajo, caracterizado porque comprende hacer reaccionar un compuesto que tiene la formula (2), en donde Q es el grupo -O-P*, en donde P* se selecciona de manera que, cuando se considera junto con el átomo de O al cual P* se enlaza, Q es un grupo saliente, y Ar, L, R2, R3, y m son como se definen a continuacion, con un reactiva halogenante seguido por un compuesto de tiourea que tiene la formula (3), en donde, R4 y R5 son como se definen a continuacion, para proporcionar el compuesto de formula (1), en donde, Ar es el mismo en las formulas (1) y (2) y es arilo o heteroarilo; L es el mismo en las formulas (19 y (2) y es alquileno opcionalmente sustituido; R2 es el mismo en las formulas (1) y (2), y se selecciona de H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, heteroarilo, cicloalquilo, y heterociclo; R3 es el mismo en las formulas (1) y (2), y se selecciona de H, halogeno, ciano, haloalquilo, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, arilo, heteroarilo, cicloalquilo, y heterociclo; R4 es (i) el mismo en cada una de las formulas (1) y (3), y (ii) es independientemente seleccionado de H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, heteroarilo, cicloalquilo, y heterociclo, o alternativamente, R4 se toma junto con R5 para formar heteroarilo o heterociclo; R5 es (i) el mismo en cada una de las formulas (1) y (3), y (ii) es independientemente seleccionado de H, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, arilo, heteroarilo, cicloalquilo, y heterociclo, o alternativamente, R5 se toma junto con R4 para formar heteroarilo o heterociclo; y m es 0 o 1.

9. 发明专利

NZ548613A Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors 未知
公开(公告)号：NZ548613A
公开(公告)日：2010-05-28
申请号：NZ54861305
申请日：2005-02-04
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHEN BANG-CHI , DROGHINI ROBERTO , LAJEUNESSE JEAN , DIMARCO JOHN D , GALELLA MICHAEL , CHIDAMBARAM RAMAKRISHNAN
IPC分类号： C07D417/14 , A61K31/496 , A61K31/506 , A61P31/04 , A61P31/12 , A61P35/00 , C07C235/28 , C07C237/42 , C07D239/48 , C07D277/56 , C07D417/12
摘要： Disclosed is a crystalline solvate of a 2-aminothiazole-5-aromatic carboxamides with formula (IV) which is characterized by its x-ray powder diffraction pattern, wherein the solvate is monohydrate, butanol or ethanol. Also disclosed is the pharmaceutical use of the compound for the treatment of cancer in particular chronic myelogenous leukemia (CML), gastrointestinal stromal tumor (GIST), small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), ovarian cancer, melanoma, mastocytosis, germ cell tumors, acute myelogenous leukemia (AML), pediatric sarcomas, breast cancer, colorectal cancer, pancreatic cancer, and prostate cancer. The process for preparing the crystalline solvate is also disclosed.

10. 发明专利

ZA200606242B PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS 未知
公开(公告)号：ZA200606242B
公开(公告)日：2008-01-08
申请号：ZA200606242
申请日：2006-07-27
申请人： SQUIBB BRISTOL MYERS CO
发明人： CHIDAMBARAM RAMAKRISHNAN , DIMARCO JOHN D , DROGHINI ROBERTO , GALELLA MICHAEL , LAJEUNESSE JEAN , CHEN BANG CHI
IPC分类号： C07C235/28 , C07C237/42 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R 2 , R 3 , R 4 , and R 5 , are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

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