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1. 发明申请

WO2010076258A1 PHENYLALKYL-IMIDAZOLE-BISPHOSPHONATE COMPOUNDS 审中-公开
标题翻译：苯基 - 咪唑 - 二磷酸酯化合物
公开(公告)号：WO2010076258A1
公开(公告)日：2010-07-08
申请号：PCT/EP2009/067679
申请日：2009-12-21
申请人： NOVARTIS AG , COTESTA, Simona , JAHNKE, Wolfgang , RONDEAU, Jean-Michel , WEILER, Sven , WIDLER, Leo
发明人： COTESTA, Simona , JAHNKE, Wolfgang , RONDEAU, Jean-Michel , WEILER, Sven , WIDLER, Leo
IPC分类号： C07F9/6506 , A61K31/663
CPC分类号： C07F9/65061
摘要： (Unsubstituted or substituted phenyl)-alkyl-substituted [(imidazol-1-yl)-1-hydroxy-1- phosphono-ethyl]-phosρhonic, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are disclosed. The compounds are able to inhibit excessive or inappropriate bone resorption. The compounds are of the formula (I), wherein one of R 1 and R 2 are as defined in the specification, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译：（未取代或取代的苯基） - 烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 苯基，以及其制备方法或方法，它们在制备公开了其在治疗疾病中的用途，用于治疗疾病的方法，包含它们的药物制剂和/或用于治疗疾病的化合物。这些化合物能够抑制过量或不适当的骨吸收。化合物是式（I）的化合物，其中R 1和R 2之一如本说明书中所定义，并且可以为酯的形式的游离形式和/或盐。

2. 发明申请

WO2008089933A3 BENZOQUINAZOLE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：WO2008089933A3
公开(公告)日：2008-09-12
申请号：PCT/EP2008000415
申请日：2008-01-21
申请人： NOVARTIS AG , WIDLER LEO
发明人： WIDLER LEO
IPC分类号： C07D405/06 , A61K31/517 , A61P19/08 , A61P19/10 , C07D239/74 , C07D413/06
CPC分类号： C07D405/06
摘要： A compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein -R represents a group of two fused rings -A-B wherein A is optionally substituted heteroaryl or aryl and B is a saturated or unsaturated 4, 5, 6 or 7 membered ring optionally containing one or more heteroatoms selected from O, N and S; the optional substituents on R being one or more groups independently selected from oxo, cyano, halo or further optionally substituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 1 -C 6 alkoxy, amino; the further optional substituents being selected from cyano, halo, C 1 -C 6 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkoxy, amino; for promoting the release of parathyroid hormone; for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（I）化合物或其药学上可接受的盐：其中-R表示两个稠合环-AB，其中A是任选取代的杂芳基或芳基，B是饱和或不饱和的4,5,6或7元环任选地含有一个或多个选自O，N和S的杂原子; R上的任选的取代基是一个或多个独立地选自氧代，氰基，卤素或进一步任选取代的C 1 -C 6烷基，C 2 - C 1 -C 6亚烷基，C 1 -C 6烷氧基，氨基，另外任选的取代基选自氰基，卤素，C 1 -C 6烷基，C 1 -C 6亚烷基，C 1 -C 6 - >烯基，C 1 -C 6烷氧基，氨基; 用于促进甲状旁腺激素的释放; 用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

3. 发明申请

WO1997032879A1 7-ALKYL-PYRROLO[2,3-d]PYRIMIDINES 审中-公开
标题翻译： 7 - 烷基 - 吡咯并[2,3-D]嘧啶
公开(公告)号：WO1997032879A1
公开(公告)日：1997-09-12
申请号：PCT/EP1997000874
申请日：1997-02-24
申请人： NOVARTIS AG , ALTMANN, Eva , MISSBACH, Martin , WIDLER, Leo
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolo[2,3-d]pyrimidines of formula (I) in which R1, R2, R3 and R4 have the meanings given in the description, have valuable pharmaceutical properties and are particularly effective in inhibiting protein tyrosine kinases pp60 . They are produced in the prior-art manner.
摘要翻译：吡咯并[2,3-D]式（I）其中R1，R2，R3和R4具有说明书中给出的含义，具有有价值的药物性质，并且特别有用，因为蛋白酪氨酸激酶PP60的抑制剂<的嘧啶Ç -src>有效。它们以常规方式制备。

4. 发明申请

WO2008089933A2 BENZOQUINAZOLE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：WO2008089933A2
公开(公告)日：2008-07-31
申请号：PCT/EP2008/000415
申请日：2008-01-21
申请人： NOVARTIS AG , WIDLER, Leo
发明人： WIDLER, Leo
IPC分类号： C07D405/06 , C07D239/74 , C07D413/06 , A61K31/517 , A61P19/08 , A61P19/10
CPC分类号： C07D405/06
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein R is as defined in the specification.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药酯，其中R如说明书中所定义。

5. 发明申请

WO2002102782A2 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO2002102782A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006606
申请日：2002-06-14
申请人： NOVARTIS AG , NOVARTIS-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H. , BEERLI, René , TOMMASI, Ruben, Alberto , WEILER, Sven , WIDLER, Leo
发明人： BEERLI, René , TOMMASI, Ruben, Alberto , WEILER, Sven , WIDLER, Leo
IPC分类号： C07D239/00
CPC分类号： C07D401/06 , C07D213/88 , C07D239/74 , C07D239/78 , C07D239/82 , C07D239/84 , C07D265/36 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/12 , C07D417/06
摘要： Use of compound of formula (I), wherein, is, or, and wherein the symbols are as defined, or a pharmaceutically-acceptable and-cleavable ester, or acid addition salt thereof, for the preparation of a medicament for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：使用式（I）化合物，其中（a）为（b）或（c），其中符号如上所定义，或其药学上可接受的和可切割的酯或其酸加成盐，用于制备用于促进甲状旁腺激素释放的药物，例如用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

6. 发明申请

WO1997049706A1 SUBSTITUTED 7-AMINO-PYRROLO[3,2-d]PYRIMIDINES AND THE USE THEREOF 审中-公开
标题翻译：取代的7-氨基吡咯并[3,2-d]吡啶并及其用途
公开(公告)号：WO1997049706A1
公开(公告)日：1997-12-31
申请号：PCT/EP1997003115
申请日：1997-06-16
申请人： NOVARTIS AG , ALTMANN, Eva , MISSBACH, Martin , WIDLER, Leo , MAIBAUM, Jürgen, Klaus
发明人： NOVARTIS AG
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolo[3,2-d]pyrimidines of formula (I) wherein R1, R2 and R3, are as defined in the description, are described. The compounds have valuable pharmaceutical properties and are effective especially as tyrosine protein kinase inhibitors. They can be used in warm-blooded animals in the treatment of bone diseases and other diseases that are favourably influenced by the inhibition of tyrosine protein kinase.
摘要翻译：描述了式（I）的吡咯并[3,2-d]嘧啶，其中R1，R2和R3如说明书中所定义。这些化合物具有有价值的药物性质，特别是作为酪氨酸蛋白激酶抑制剂是有效的。它们可用于温血动物治疗骨骼疾病和其他有利于抑制酪氨酸蛋白激酶影响的疾病。

7. 发明申请

WO2009068567A1 C2-C5-ALKYL-IMIDAZOLE-BISPHOSPHONATES 审中-公开
标题翻译： C2-C5烷基咪唑双膦酸盐
公开(公告)号：WO2009068567A1
公开(公告)日：2009-06-04
申请号：PCT/EP2008/066245
申请日：2008-11-26
申请人： NOVARTIS AG , WEILER, Sven , WIDLER, Leo , RONDEAU, Jean-Michel , COTESTA, Simona , JAHNKE, Wolfgang
发明人： WEILER, Sven , WIDLER, Leo , RONDEAU, Jean-Michel , COTESTA, Simona , JAHNKE, Wolfgang
IPC分类号： C07F9/6506 , A61K31/663 , A61P19/00
CPC分类号： C07F9/65061
摘要： C 2 -C 5 -Alkyl-substituted [(imidazol-1 -yl)-1-hydroxy-1-phosphono-ethyl]-phosphonic acids, as well as methods or processes for their manufacture, their use in the manufacture of pharmaceutical formulations, their use in the treatment of diseases, methods of using them in the treatment of diseases, pharmaceutical formulations encompassing them and/or the compounds for use in the treatment of diseases, are described. The compounds are able to inhibit excessive or inappropriate bone resorption and for the treatment of other diseases which are caused by excessive prenylation of target proteins, such as Hutchinson-Gilford progeria syndrome. The compounds are of the formula (I), wherein one of R 1 and R 2 is hydrogen and the other is C 2 -C 5 -alkyl that is branched or unbranched, and can be in free form, in the form of an ester, and/or of a salt.
摘要翻译： C 2 -C 5烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基 - 乙基] - 膦酸，以及其制备方法或方法，它们在制备药物制剂中的用途，它们描述了用于治疗疾病，用于治疗疾病的方法，包括它们的药物制剂和/或用于治疗疾病的化合物。该化合物能够抑制过度或不适当的骨吸收和用于治疗由靶向蛋白过度异戊二烯化引起的其他疾病，例如Hutchinson-Gilford progeria综合征。化合物是式（I）的化合物，其中R 1和R 2之一是氢，另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以是酯的游离形式，和/或的盐。

8. 发明申请

WO2008107390A1 PHARMACEUTICAL COMPOSITIONS COMPRISING A CALCILYTIC AGENT 审中-公开
标题翻译：包含计算机代理的药物组合物
公开(公告)号：WO2008107390A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052500
申请日：2008-02-29
申请人： NOVARTIS AG , BUHL, Thomas , GONCALVES, Elisabete , KALB, Oscar , MEINEL, Lorenz , REIDEMEISTER, Sibylle , TAILLARDAT, Agnes , WIDLER, Leo
发明人： BUHL, Thomas , GONCALVES, Elisabete , KALB, Oscar , MEINEL, Lorenz , REIDEMEISTER, Sibylle , TAILLARDAT, Agnes , WIDLER, Leo
IPC分类号： A61K9/107 , A61K9/14 , A61K47/44 , A61K31/517 , A61K31/4184
CPC分类号： A61K9/1075 , A61K9/146
摘要： Provided is a pharmaceutical composition comprising a calcilytic agent which, when administered orally to a subject induces a rapid and short-lasting absorption of the calcilytic agent and/ or a rapid and short-lasting release of the parathyroid hormone.
摘要翻译：本发明提供一种药物组合物，其包含溶解剂，其当向受试者口服给药时，诱导所述钙化剂的快速和短暂的吸收和/或甲状旁腺激素的快速和短暂的释放。

9. 发明申请

WO2007020046A1 BENZOQUINAZOLINE DERIVATIVES AND THEIR USE IN TREATING BONE DISORDERS 审中-公开
标题翻译：苯并噻唑啉衍生物及其在治疗骨质疏松症中的应用
公开(公告)号：WO2007020046A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/008036
申请日：2006-08-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AMMON, Sandra , BEERLI, René , WIDLER, Leo
发明人： AMMON, Sandra , BEERLI, René , WIDLER, Leo
IPC分类号： C07D217/12 , C07D217/26 , C07D239/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D417/06 , C07D417/12 , A61K31/395 , A61K31/435
CPC分类号： C07D409/06 , C07D217/12 , C07D217/26 , C07D239/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R2, R3, R4, Q, X and Y are as defined in the specification, is useful in the treatment of bone conditions related to increased calcium depletion or resorption.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药酯，其中基团R 2，R 3，R 4，Q，X和Y如说明书中所定义，可用于治疗与增加的钙相关的骨条件耗尽或吸收。

10. 发明申请

WO2004056365A3 DERIVATIVES OF ARYL-QUINAZOLINE/ARYL-2AMINO-PHENYL METHANONE WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 审中-公开
标题翻译：芳基喹唑啉衍生物/芳基-2-氨基苯甲醇的衍生物，其促进PARAMYROID HORMONE的释放
公开(公告)号：WO2004056365A3
公开(公告)日：2004-08-19
申请号：PCT/EP0314741
申请日：2003-12-22
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , ALTMANN EVA , BEERLI RENE , GERSPACHER MARC , RENAUD JOHANNE , WEILER SVEN , WIDLER LEO
发明人： ALTMANN EVA , BEERLI RENE , GERSPACHER MARC , RENAUD JOHANNE , WEILER SVEN , WIDLER LEO
IPC分类号： A61P5/18 , C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , A61K31/498 , C07C49/84 , C07D239/78
CPC分类号： C07C17/12 , C07C45/30 , C07C205/37 , C07C205/44 , C07C205/45 , C07C225/22 , C07C229/18 , C07C255/24 , C07C255/25 , C07C317/18 , C07C317/32 , C07C323/25 , C07C2601/02 , C07D213/64 , C07D239/82 , C07D239/93 , C07D317/58 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07C25/18 , C07C47/277
摘要： A compound of formula (I): wherein R1, R2, R3 and Y are as defined herein, or a pharmaceutically-acceptable and -cleavable ester, or acid addition salt thereof, useful for promoting the release of parathyroid hormone, e.g. for preventing or treating bone conditions which are associated with increased calcium depletion or resorption or in which stimulation of bone formation and calcium fixation in the bone is desirable.
摘要翻译：式（I）的化合物：其中R 1，R 2，R 3和Y如本文所定义，或其药学上可接受的可裂解的酯或其酸加成盐，其可用于促进甲状旁腺激素的释放，例如，用于预防或治疗与钙耗竭或再吸收增加相关的骨质状况或其中期望刺激骨形成和骨固定的刺激。

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