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1. 发明公开

EP1401451A2 QUINAZOLINE DERIVATIVES WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 有权
标题翻译： Chinazolines衍生促进PARATHYROIDMSHORMONEN的释放
公开(公告)号：EP1401451A2
公开(公告)日：2004-03-31
申请号：EP02758236.0
申请日：2002-06-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BEERLI, René , TOMMASI, Ruben, Alberto , WEILER, Sven , WIDLER, Leo
IPC分类号： A61K31/517 , A61P5/18 , A61P19/10 , C07D239/82
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 (a) is (b) or (c) 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.

2. 发明授权

EP1401451B1 QUINAZOLINE DERIVATIVES WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 有权
标题翻译：喹唑啉衍生物促进甲状旁腺激素的释放
公开(公告)号：EP1401451B1
公开(公告)日：2009-11-11
申请号：EP02758236.0
申请日：2002-06-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BEERLI, René , TOMMASI, Ruben, Alberto , WEILER, Sven , WIDLER, Leo
IPC分类号： A61K31/517 , A61P5/18 , A61P19/10 , C07D239/82
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 (a) is (b) or (c) 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：其中（a）是（b）或（c）且其中符号如上所定义的式（I）化合物或其药学上可接受的且可裂解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缺乏或再吸收增加相关的骨骼病症，或者其中需要刺激骨骼形成和骨骼中的钙固定。

3. 发明授权

EP1585521B8 DERIVATIVES OF ARYL-QUINAZOLINE/ARYL-2AMINO-PHENYL METHANONE WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 有权
标题翻译： DORIVATE VON ARYL-CHINAZOLIN / ARYL-2AMINO-PHENYL-METHANONZURFÖRDERUNGDER FREISETZUNG VON PARATHORMON
公开(公告)号：EP1585521B8
公开(公告)日：2009-03-25
申请号：EP03813593.5
申请日：2003-12-22
申请人： NOVARTIS AG , Novartis Pharma GmbH
发明人： ALTMANN, Eva , BEERLI, René , GERSPACHER, Marc , RENAUD, Johanne , WEILER, Sven , WIDLER, Leo
IPC分类号： A61K31/498 , C07D403/06 , C07D239/82 , C07D403/10 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , C07D413/06 , C07D401/12 , C07D239/78 , C07C49/84 , A61P5/18
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

4. 发明授权

EP1585521B1 DERIVATIVES OF ARYL-QUINAZOLINE/ARYL-2AMINO-PHENYL METHANONE WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 有权
标题翻译： EUROPE激素芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮ZURFÖRDERUNG释放衍生物
公开(公告)号：EP1585521B1
公开(公告)日：2008-06-18
申请号：EP03813593.5
申请日：2003-12-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALTMANN, Eva , BEERLI, René , GERSPACHER, Marc , RENAUD, Johanne , WEILER, Sven , WIDLER, Leo
IPC分类号： A61K31/498 , C07D403/06 , C07D239/82 , C07D403/10 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , C07D413/06 , C07D401/12 , C07D239/78 , C07C49/84 , A61P5/18
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.

5. 发明公开

EP1585521A2 DERIVATIVES OF ARYL-QUINAZOLINE/ARYL-2AMINO-PHENYL METHANONE WHICH PROMOTE THE RELEASE OF PARATHYROID HORMONE 有权
标题翻译： EUROPE激素芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮ZURFÖRDERUNG释放衍生物
公开(公告)号：EP1585521A2
公开(公告)日：2005-10-19
申请号：EP03813593.5
申请日：2003-12-22
申请人： Novartis AG , Novartis Pharma GmbH
发明人： ALTMANN, Eva , BEERLI, René , GERSPACHER, Marc , RENAUD, Johanne , WEILER, Sven , WIDLER, Leo
IPC分类号： A61K31/498 , C07D403/06 , C07D239/82 , C07D403/10 , C07D409/06 , C07D405/06 , C07D417/06 , C07D401/06 , C07D413/06 , C07D401/12 , C07D239/78 , C07C49/84 , A61P5/18
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.

6. 发明授权

EP2785713B1 NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE 有权
标题翻译：新三氟甲基恶二唑和它们在疾病治疗
公开(公告)号：EP2785713B1
公开(公告)日：2016-09-07
申请号：EP12805774.2
申请日：2012-11-26
申请人： Novartis AG
发明人： HEBACH, Christina , KALLEN, Joerg , NOZULAK, Joachim , TINTELNOT-BLOMLEY, Marina , WIDLER, Leo
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4245 , A61P25/28
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , C07D413/04

7. 发明公开

EP2382223A1 PHENYLALKYL-IMIDAZOLE-BISPHOSPHONATE COMPOUNDS 审中-公开
标题翻译：苯基 - 咪唑 - 二膦酸酯化合物
公开(公告)号：EP2382223A1
公开(公告)日：2011-11-02
申请号：EP09806020.5
申请日：2009-12-21
申请人： Novartis AG
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：（未取代的或取代的苯基） - 烷基取代的[（咪唑-1-基）-1-羟基-1-膦酰基乙基] - 膦酸，以及它们的制备方法或方法，它们在制备药物制剂中的用途，它们在治疗疾病中的用途，使用它们治疗疾病的方法，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度或不适当的骨吸收。所述化合物是式（I）的化合物，其中R 1和R 2中的一个如说明书中所定义，并且可以以游离形式，以酯和/或盐的形式存在。

8. 发明公开

EP2225252A1 C2-C5-ALKYL-IMIDAZOLE-BISPHOSPHONATES 有权
标题翻译： C2-C5烷基咪唑双膦酸盐
公开(公告)号：EP2225252A1
公开(公告)日：2010-09-08
申请号：EP08854485.3
申请日：2008-11-26
申请人： Novartis AG
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： C2-C5-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 R1 and R2 is hydrogen and the other is C2-C5-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，其在制备药物制剂中的用途，它们的用于治疗疾病，使用它们治疗疾病的方法，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度或不适当的骨吸收，并用于治疗由靶蛋白过度异戊二烯化引起的其他疾病，如Hutchinson-Gilford早衰综合征。所述化合物是式（I）的化合物，其中R 1和R 2中的一个是氢并且另一个是支链或非支链的C 2 -C 5 - 烷基，并且可以以酯的形式呈游离形式，和/或的盐。

9. 发明公开

EP2124893A1 PHARMACEUTICAL COMPOSITIONS COMPRISING A CALCILYTIC AGENT 审中-公开
标题翻译：与Active KALZILYTISCHEN药物组合物
公开(公告)号：EP2124893A1
公开(公告)日：2009-12-02
申请号：EP08717280.5
申请日：2008-02-29
申请人： Novartis AG
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.

10. 发明公开

EP2106400A2 BENZOQUINAZOLE DERIVATIVES 审中-公开
标题翻译：苯并喹唑衍生物
公开(公告)号：EP2106400A2
公开(公告)日：2009-10-07
申请号：EP08707148.6
申请日：2008-01-21
申请人： NOVARTIS AG
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 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 C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkoxy, amino; the further optional substituents being selected from cyano, halo, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 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的基团，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上的任选取代基是独立选自氧代，氰基，卤素或另外任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 1 -C 6烷氧基，氨基的一个或多个基团; 其他任选的取代基选自氰基，卤素，C 1 -C 6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缺乏或再吸收增加相关的骨骼病症，或者其中需要刺激骨骼形成和骨骼中的钙固定。

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