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1. 发明申请

US20100022565A1 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：US20100022565A1
公开(公告)日：2010-01-28
申请号：US12529359
申请日：2008-02-29
申请人： Thomas Buhl , Elisabete Goncalves , Oskar Kalb , Lorenz Meinel , Sibylle Reidemeister , Agnes Taillardat , Leo Widler
发明人： Thomas Buhl , Elisabete Goncalves , Oskar Kalb , Lorenz Meinel , Sibylle Reidemeister , Agnes Taillardat , Leo Widler
IPC分类号： A61K31/517 , A61P5/18
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，当向受试者口服给药时，引起对钙化剂的快速和短暂吸收和/或甲状旁腺激素的快速和短暂释放。

2. 发明申请

US20100166765A1 BENZOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译：苯并噻唑衍生物
公开(公告)号：US20100166765A1
公开(公告)日：2010-07-01
申请号：US12063526
申请日：2006-08-14
申请人： Sandra Ammon , Rene Beerli , Leo Widler
发明人： Sandra Ammon , Rene Beerli , Leo Widler
IPC分类号： A61K31/517 , C07D239/72 , C07D403/12 , A61P19/08 , C07D237/30 , A61K31/502 , A61K33/06 , A61K38/23 , A61K31/56 , A61K39/395 , A61K31/59
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。

3. 发明申请

US20100063075A1 Aryl-quinazoline/aryl-2amino-phenyl methanone derivatives 失效
标题翻译：芳基 - 喹唑啉/芳基-2-氨基 - 苯基甲酮衍生物
公开(公告)号：US20100063075A1
公开(公告)日：2010-03-11
申请号：US12579735
申请日：2009-10-15
申请人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
发明人： Eva Altmann , Rene Beerli , Marc Gerspacher , Johanne Renaud , Sven Weiler , Leo Widler
IPC分类号： A61K31/517 , C07D239/72 , C07C211/00 , A61K31/135 , A61P19/00
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 (1): 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（1）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。

4. 发明申请

US20090143337A1 C2-C5-Alkyl-Imidazole-Bisphosphonates 有权
标题翻译： C2-C5-烷基 - 咪唑 - 二膦酸酯
公开(公告)号：US20090143337A1
公开(公告)日：2009-06-04
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean-Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/40 , A61P19/08
CPC分类号： C07F9/6506
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： C2-C5-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，它们在药物制剂的制备中的用途，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。该化合物具有式I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/或盐。

5. 发明授权

US5229405A Use of 2-iminothiazolidin-4-one derivatives as novel pharmaceutical active ingredients 失效
标题翻译： 2-IMINOTHIAZOLIDIN-4-ONE衍生物作为新药物活性成分的使用
公开(公告)号：US5229405A
公开(公告)日：1993-07-20
申请号：US866926
申请日：1992-04-10
申请人： Ulrich Feige , Irmgard Wiesenberg , Leo Widler , Pier G. Ferrini , Martin Missbach
发明人： Ulrich Feige , Irmgard Wiesenberg , Leo Widler , Pier G. Ferrini , Martin Missbach
IPC分类号： A61K31/425 , A61K31/426 , A61P29/00 , C07D277/20 , C07D277/38
CPC分类号： A61K31/425
摘要： Compounds of the formula I ##STR1## in which R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2-yn-1-yl or lower alkyl substituted in the 2,3-position by radicals which can be eliminated to give a double bond, R.sub.2 is hydrogen and R.sub.3 is methyl which is unsubstituted or substituted by radicals which can be eliminated together with hydrogen R.sub.2 to give a double bond or R.sub.2 and R.sub.3 are both hydrogen or lower alkyl or are together methylene and R.sub.4 is a group of the formula Ia, Ib or Ic ##STR2## in which R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl or lower alk-2-yn-1-yl and R.sub.6 is a group of the formula Id or Ie ##STR3## in which R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined, and their pharmaceutically acceptable salts can be used in a novel manner for the treatment of diseases of the rheumatoid type.
摘要翻译：其中R1是低级烷-2-烯-1-基，低级烯-3-烯-2-基，低级烷-2-炔-1-基或低级烷基的式I化合物（I）在2,3位上被可以被去除以产生双键的基团取代，R 2是氢，R 3是未被取代或被可以与氢R 2一起被除去的基团取代的甲基，得到双键或R 2和 R 3是氢或低级烷基或一起是亚甲基，R 4是式Ia，Ib或Ic的基团（Ia）其中R 5是氢，低级烷基（C 1 -C 6），低级烯-2-烯-1-基或低级烷-2-炔-1-基，R6是式Id或Ie（Ide）（Ie）的基团，其中R1，R2 ，R3和R5如上定义，并且其药学上可接受的盐可以以新颖的方式用于治疗类风湿病的疾病。

6. 发明授权

US5177091A Use of carbazones as novel active ingredients in medicaments 失效
标题翻译：使用CARBAZONES作为药物中的新型活性成分
公开(公告)号：US5177091A
公开(公告)日：1993-01-05
申请号：US795210
申请日：1991-11-20
申请人： Ulrich Feige , Irmgard Wiesenberg , Leo Widler , Pier G. Ferrini , Martin Missbach
发明人： Ulrich Feige , Irmgard Wiesenberg , Leo Widler , Pier G. Ferrini , Martin Missbach
IPC分类号： A61K31/425 , A61K31/426 , A61P29/00 , C07D277/20 , C07D277/38
CPC分类号： A61K31/425
摘要： Compounds of formula I ##STR1## wherein X and Y are each independently of the other thio or sulfynyl, R.sub.1 is lower alk-2-en-1-yl, lower alk-3-en-2-yl, lower alk-2--yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, R.sub.2 is hydrogen and R.sub.3 is unsubstituted methyl or methyl substituted by a radical that can be eliminated together with hydrogen Rhd 2 to form a double bond, or R.sub.2 and R.sub.3 are each hydrogen or lower alkyl or together are methylene, R.sub.4 is free or protected hydroxy, or hydrogen, and R.sub.5 is hydrogen, lower alkyl, lower alk-2-en-1-yl, lower alk-2-yn-1-yl, or lower alkyl that is substituted in the 2,3-position by radicals that can be eliminated to form a double bond, and their pharmaceutically acceptable salts may be used in a novel manner for the treatment of disorders of the rheumatoid type.
摘要翻译：式I的化合物其中X和Y各自独立地为其它硫代或亚硫炔基，R 1为低级烷-2-烯-1-基，低级烯-3-烯-2-基，低级烷基 -2-yn-1-基或在2,3位被可以被去除以形成双键的基团取代的低级烷基，R 2是氢，R 3是未被取代的甲基或被以下基团取代的甲基：可以与氢Rhd 2一起消除以形成双键，或者R 2和R 3各自为氢或低级烷基或一起为亚甲基，R 4为游离或被保护的羟基或氢，R 5为氢，低级烷基，低级烷基， 2-烯-1-基，低级烷-2-炔-1-基或在2,3位被可以被去除以形成双键的自由基取代的低级烷基，及其药学上可接受的盐可以以新颖的方式用于治疗类风湿病的病症。

7. 发明授权

US09670193B2 Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease 有权
公开(公告)号：US09670193B2
公开(公告)日：2017-06-06
申请号：US14360013
申请日：2012-11-26
申请人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
发明人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
IPC分类号： A61K31/4245 , C07D413/04 , C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , C07D413/04
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.

8. 发明申请

US20140329825A1 NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE 有权
标题翻译：新型三氟甲基 - 氧杂唑衍生物及其在治疗疾病中的应用
公开(公告)号：US20140329825A1
公开(公告)日：2014-11-06
申请号：US14360013
申请日：2012-11-26
申请人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
发明人： Christina Hebach , Joerg Kallen , Joachim Nozulak , Marina Tintelnot-Blomley , Leo Widler
IPC分类号： C07D413/14 , C07D413/04 , A61K31/444 , A61K31/4439 , A61K31/497 , A61K31/506
CPC分类号： C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/506 , C07D413/04
摘要： The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
摘要翻译：本发明涉及式（I）的新型三唑 - 恶二唑衍生物及其药学上可接受的盐，其中所有变量如说明书，其药物组合物，其药物组合，及其作为药物的用途，特别是通过抑制HDAC4治疗神经变性，肌肉萎缩或糖尿病/代谢综合征。

9. 发明授权

US4939130A Substituted alkanediphosphonic acids and pharmaceutical use 失效
标题翻译：取代的烷二膦酸和药用
公开(公告)号：US4939130A
公开(公告)日：1990-07-03
申请号：US315962
申请日：1989-02-27
申请人： Knut A. Jaeggi , Leo Widler
发明人： Knut A. Jaeggi , Leo Widler
IPC分类号： C07F9/38 , A61K31/66 , A61K31/665 , A61K31/67 , A61K31/675 , A61P3/00 , A61P3/02 , A61P3/14 , A61P9/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07F9/547 , C07F9/645 , C07F9/6503 , C07F9/6506 , C07F9/6518 , C07F9/653 , C07F9/6539
CPC分类号： C07F9/65061 , C07F9/65032 , C07F9/65033 , C07F9/65062 , C07F9/65181 , C07F9/65182 , C07F9/6539
摘要： Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.1 is a functionally modified phosphono group and X.sub.2 is a free or functionally modified phosphono group, X.sub.1 and, if appropriate X.sub.2, into the free phosphono group.
摘要翻译：烷基膦酸，特别是式（I）的杂芳烷基亚烷基二酸，其中R 1是可与苯或环己烯核稠合的5元杂芳基，并且其含有2至4个N原子或1或4个N原子 2个N原子以及1个O-或S-原子，并且是被低级烷基，苯基或被低级烷基，低级烷氧基和/或卤素取代的苯基未被取代或C取代，或被低级烷氧基，羟基，二低级烷基氨基，低级烷硫基和/或卤素，和/或在能够被低级烷基，低级烷氧基和/或卤素取代的N-原子上被N-取代，并且R 2是氢，羟基，氨基，低级烷硫基或卤素及其盐具有对钙代谢的调节作用，可用作治疗与钙代谢损伤有关的疾病的药物。化合物例如通过在其中X 1是官能改性的膦酰基并且X 2是游离或官能改性的膦酰基的式（II）化合物中转化为X1，并且如果合适的话，X2转化成游离膦酰基组。

10. 发明授权

US07977323B2 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：US07977323B2
公开(公告)日：2011-07-12
申请号：US12323696
申请日：2008-11-26
申请人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
发明人： Sven Weiler , Leo Widler , Jean Michel Rondeau , Simona Cotesta , Wolfgang Jahnke
IPC分类号： A61K31/675 , C07F9/02
CPC分类号： C07F9/6506
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： C2-C5-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，它们在药物制剂的制备中的用途，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。该化合物具有式I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/或盐。

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