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1. 发明申请

WO2007121484A3 6-O-SUBSTITUTED BENZOXAZOLE AND BENZOTHIAZOLE COMPOUNDS AND METHODS OF INHIBITING CSF-1R SIGNALING 审中-公开
标题翻译： 6-O-取代的苯并噻唑和苯并噻唑化合物和抑制CSF-1R信号的方法
公开(公告)号：WO2007121484A3
公开(公告)日：2008-02-07
申请号：PCT/US2007066898
申请日：2007-04-18
申请人： NOVARTIS AG , SUTTON JAMES C , WIESMANN MARION , WANG WEIBO , LINDVALL MIKA K , LAN JIONG , RAMURTHY SAVITHRI , SHARMA ANU , MIEULI ELIZABETH J , KLIVANSKY LIANA M , LENAHAN WILLIAM P , KAUFMAN SUSAN , YANG HONG , NG SIMON C , PFISTER KEITH , WAGMAN ALLAN , SUNG VICTORIA , SENDZIK MARTIN
发明人： SUTTON JAMES C , WIESMANN MARION , WANG WEIBO , LINDVALL MIKA K , LAN JIONG , RAMURTHY SAVITHRI , SHARMA ANU , MIEULI ELIZABETH J , KLIVANSKY LIANA M , LENAHAN WILLIAM P , KAUFMAN SUSAN , YANG HONG , NG SIMON C , PFISTER KEITH , WAGMAN ALLAN , SUNG VICTORIA , SENDZIK MARTIN
IPC分类号： C07D413/12 , A61K31/44 , A61P19/02 , A61P19/10 , A61P35/00 , C07D417/12
CPC分类号： C07D413/12 , C07D417/12
摘要： Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
摘要翻译：公开了苯并恶唑和苯并噻唑化合物及其立体异构体，互变异构体，溶剂合物，氧化物，酯和前药及其药学上可接受的盐。还公开了单独或与至少一种另外的治疗剂组合的化合物与药学上可接受的载体的组合，以及化合物单独或与至少一种其它治疗剂组合的用途。这些实施方案可用于抑制细胞增殖，抑制肿瘤的生长和/或复分解，治疗或预防癌症，治疗或预防退行性骨疾病如类风湿性关节炎和/或抑制分子如CSF-1R。

2. 发明申请

WO2004018419B1 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹啉酮及其用途
公开(公告)号：WO2004018419B1
公开(公告)日：2004-07-29
申请号：PCT/US0325990
申请日：2003-08-19
申请人： CHIRON CORP , BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
发明人： BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61P35/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04 , A61K31/435
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并具有本文所述的变量。这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。

3. 发明申请

WO2004018419A3 BENZIMIDAZOLE QUINOLINONES AND USES THEREOF 审中-公开
标题翻译：苯并咪唑喹诺酮及其用途
公开(公告)号：WO2004018419A3
公开(公告)日：2004-06-03
申请号：PCT/US0325990
申请日：2003-08-19
申请人： CHIRON CORP , BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
发明人： BARSANTI PAUL A , BUSSIERE DIRKSEN , HARRISON STEPHEN D , HEISE CARLA C , JANSEN JOHANNA M , JAZAN ELISA , MACHAJEWSKI TIMOTHY D , MCBRIDE CHRISTOPHER , MCCREA WILLIAM R , NG SIMON , NI ZHI-JIE , PECCHI SABINA , PFISTER KEITH , RAMURTHY SAVITHRI , RENHOWE PAUL A , SHAFER CYNTHIA M , SILVER JOEL B , WAGMAN ALLAN , WIESMANN MARION , WAYMAN KELLY
IPC分类号： A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , A61P35/00 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04 , A61K31/435
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或1B的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并且具有本文所述的变量。此类化合物可用于制备用于抑制各种酶的药物和用于治疗由这些酶介导的病症的药物。

4. 发明专利

MA30208B1 DERIVES DE PYRIMIDINE UTILISES EN TANT QU'INHIBITEURS DE KINASE PI -3 未知
公开(公告)号：MA30208B1
公开(公告)日：2009-02-02
申请号：MA31157
申请日：2008-08-06
申请人： MERITT HANNE , VOLIVA CHARLES , WIESMANN MARION , XIN XIAHUA
发明人： BURGER MATTHEW , NI ZHI-JIE , PECCHI SABINA , ATALLAH GORDANA , BARTULIS SARAH , FRAZIER KELLY , SMITH AARON , VERHAGEN JOELLE , ZHANG YANCHEN , WAGMAN ALLAN , NG SIMON , PFISTER KEITH , POON DANIEL , LOUIE ALICIA , PICK TERESA , BARSANTI PAUL , IWANOWICZ EDWIN , FANTL WENDY , HENDRICKSON THOMAS , KNAPP MARK , MERITT HANNE , VOLIVA CHARLES , WIESMANN MARION , XIN XIAHUA
IPC分类号： C07D401/04 , A61K31/506 , A61P35/00 , C07D401/14 , C07D405/12 , C07D405/14 , C07D417/12
摘要： La présente invention concerne des composés (I) inhibiteurs de phosphatidylinositol 3-kinase (PI), leurs sels pharmaceutiquement acceptables et des promédicaments de ceux-ci ; des compositions des nouveaux composés, soit seuls soit en association avec au moins un agent thérapeutique supplémentaire, avec un excipient pharmaceutiquement acceptable ; et des utilisations des nouveaux composés, soit seuls soit en association avec au moins un agent thérapeutique supplémentaire dans la prophylaxie ou le traitement de maladies prolifératives caractérisées par l'activité anormale de facteurs de croissance, de protéines sérine/thréonine kinases et des phospholipides kinases.

5. 发明专利

BRPI0710540B1 Compostos de benzoxazol e benzotiazol substituídos por 6-o, e composição farmacêutica 未知
公开(公告)号：BRPI0710540B1
公开(公告)日：2022-04-12
申请号：BRPI0710540
申请日：2007-04-18
申请人： NOVARTIS AG
发明人： WAGMAN ALLAN , SHARMA ANU , ELIZABETH J MIEULI , YANG HONG , JAMES C SUTTON , LAN JIONG , PFISTER KEITH , LIANA M KLIVANSKY , WIESMANN MARION , SENDZIK MARTIN , MIKA K LINDVALL , RAMURTHY SAVITHRI , SIMON C NG , KAUFMAN SUSAN , SUNG VICTORIA , WANG WEIBO , WILLIAM P LENAHAN
IPC分类号： A61K31/44 , A61P19/02 , A61P19/10 , A61P35/00 , C07D413/12 , C07D417/12
摘要： compostos de benzoxazol e benzotiazol substituídos por 6-o e métodos de inibir a sinalização de csf-1 r. compostas de benzoxazol e benzotiazol e os seus estereoisômeros, tautômeros, solvatos, óxidos, ésteres e prá-fármacos e sais farmaceuticamente aceitáveis destes são divulgados. as composições dos compostos, isoladamente ou em combinação com pelo menos um agente terapêutico adicional, com um veículo farmaceuticamente aceitável, e uso dos compostos, isoladamente ou em combinação com pelo menos um agente terapêutico adicional também são divulgadas. as modalidades são úteis para inibir a proliferação celular, inibir o desenvolvimento e/ou metástase de tumores, tratar ou prevenir o câncer, tratar ou prevenir as doenças ósseas de- generativas tais como artrire reumatóide, e/ou inibir as moléculas tais como csf-1r.

8. 发明专利

ES2381895T3 Inhibidores de PI 3-quinasa y métodos para su uso 未知
公开(公告)号：ES2381895T3
公开(公告)日：2012-06-01
申请号：ES08729174
申请日：2008-02-06
申请人： NOVARTIS AG
发明人： PECCHI SABINA , NI ZHI-JIE , BURGER MATTHEW , WAGMAN ALLAN , ATALLAH GORDANA , BARTULIS SARAH , NG SIMON , PFISTER KEITH , SMITH AARON , ZHANG YANCHEN , MERRITT HANNE , VOLIVA CHARLES
IPC分类号： C07D401/04 , A61K31/5377 , A61P35/00 , C07D401/14 , C07D405/14 , C07D413/14
摘要： Un compuesto de Fórmula I, o un estereoisómero, tautómero o sal farmacéuticamente aceptables de los mismos, en donde, **Fórmula** X es N y Y es CR5, o Y es N y X es CR5; Z es N o CR6; R1 se selecciona del grupo consistente de hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, alcoxi, alcoxi sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilo, cicloalquilo, cicloalquilo sustituido, heterociclilo sustituido, ariloxi, ariloxi sustituido, heteroariloxi, heteroariloxi sustituido, heterocicliloxi, heterocicliloxi sustituido, cicloalquiloxi, cicloalquiloxi sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminocarbonilo, aminotiocarbonilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxi, aminosulfonilo, aminosulfoniloxi, aminosulfonilamino, amidino, carboxilo, carboxil éster, (carboxil éster)amino, (carboxil éster)oxi, ciano, halo, hidroxi, nitro, SO3H, sulfonilo, sulfonilo sustituido, sulfóxido, sulfóxido sustituido, sulfonilamino, sulfonilamino sustituido, sulfoniloxi, sulfoniloxi susituido, tioacilo, tiol, alquiltio, y alquiltio sustituido, con la condición de que cuando X es N, R1 no es morfolino; R2 y R4, son seleccionados cada uno independientemente del grupo consistente hidrógeno, alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, alcoxi, alcoxi sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilo, cicloalquilo, cicloalquilo sustituido, heterociclilo sustituido, ariloxi, ariloxi sustituido, heteroariloxi, heteroariloxi sustituido, heterocicliloxi, heterocicliloxi sustituido, cicloalquiloxi, cicloalquiloxi sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminocarbonilo, aminotiocarbonilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxi, aminosulfonilo, aminosulfoniloxi, aminosulfonilamino, amidino, carboxilo, carboxil éster, (carboxil éster)amino, (carboxil éster)oxi, ciano, halo, hidroxi, nitro, SO3H, sulfonilo, sulfonilo sustituido, sulfoniloxi, tioacilo, tiol, alquiltio, y alquiltio sustituido; R3 se selecciona del grupo consistente de hidrógeno, alquilo, -CO-R3a, alquilo sustituido, un cicloalquilo de tres a siete miembros o un anillo cicloalquilo sustituido de tres a siete miembros, y un heterociclilo de cuatro a siete miembros o un anillo heterociclilo sustituido de cuatro a siete miembros; y R3a se selecciona del grupo consistente de alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, amino, amino sustituido, y alquilamino; y R5 se selecciona del grupo consistente de hidrógeno, ciano, nitro, halógeno, hidroxi, amino, amino sustituido, alquilo, alquilo sustituido, -COR5a, y NR5aCOR5b, en donde R5a, y R5b se seleccionan independientemente del grupo consistente de hidrógeno, y alquilo sustituido o no sustituido; y R6 se selecciona del grupo consistente de hidrógeno, C1-3 alquilo, alquilo C1-C3 sustituido, metoxi, trifluorometilo, cicloalquilo, alquilo sustituido, acilo, acilamino, aciloxi, amino, amino sustituido, aminocarbonilo, aminosulfonilo, carboxilo, carboxil éster, ciano, halo, hidroxi, nitro, SO3H, sulfonilo, sulfonilo sustituido, sulfóxido, sulfóxido sustituido, sulfoniloxi, tioacilo, tiol y metiltio donde alquil donde se menciona tiene 1 a 10 átomos de carbono y donde alquenilo y alquinilo donde se menciona tiene 2 a 6 átomos de carbono.

9. 发明专利

ECSP12011638A DERIVADOS DE PIRIDINA Y PIRAZINA COMO MODULADORES DE CINASA DE PROTEÍNA 未知
公开(公告)号：ECSP12011638A
公开(公告)日：2012-02-29
申请号：ECSP12011638
申请日：2012-01-30
申请人： NOVARTIS AG
发明人： BARSANTI PAUL A , LIN XIAODONG , PFISTER KEITH , SENDZIK MARTIN , JIN JEFF , HU CHENG , KEYES ROBERT , KUCEJKO ROBERT , PAN YUE , SUTTON JAMES , WAN LIFENG
IPC分类号： C07D213/74 , A61K31/506 , A61P29/00 , A61P35/00 , C07D401/04 , C07D401/12
摘要： La presente invención proporciona un compuesto de la fórmula (I): (I)y las sales farmacéuticamente aceptables, enantiómeros, estereoisómeros, rotámeros, tautómeros, diaestereómeros, o racematos del mismo. También se proporciona un método para el tratamiento de una enfermedad o condición mediada por CDK9.

10. 发明专利

BRPI0710540A2 未知
公开(公告)号：BRPI0710540A2
公开(公告)日：2012-01-31
申请号：BRPI0710540
申请日：2007-04-18
申请人： NOVARTIS AG
发明人： SUTTON JAMES C , WIESMANN MARION , WANG WEIBO , LINDVALL MIKA K , LAN JIONG , RAMURTHY SAVITHRI , SHARMA ANU , MIEULI ELIZABETH J , KLIVANSKY LIANA M , LENAHAN WILLIAM P , KAUFMAN SUSAN , YANG HONG , NG SIMON C , PFISTER KEITH , WAGMAN ALLAN , SUNG VICTORIA , SENDZIK MARTIN
IPC分类号： C07D413/12 , A61K31/44 , A61P19/02 , A61P19/10 , A61P35/00 , C07D417/12
摘要： Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.

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