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51. 发明申请

US20100048711A1 Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states 失效
标题翻译：镁结合缺陷的拮抗剂作为治疗剂和治疗异常生理状态的方法
公开(公告)号：US20100048711A1
公开(公告)日：2010-02-25
申请号：US12589064
申请日：2009-10-16
申请人： Ibert Clifton Wells
发明人： Ibert Clifton Wells
IPC分类号： A61K31/17 , C07C275/18 , A61P3/10 , A61P9/12
CPC分类号： C07C237/20 , A61K31/16 , A61K31/165 , C07C237/12 , C07C237/22 , G01N2800/042 , G01N2800/321
摘要： This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans,trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
摘要翻译：本发明提供一类治疗化合物和治疗哺乳动物的方法，所述哺乳动物具有生理紊乱，例如经常发生的原发性高血压，其与镁与其细胞的质膜结合减少有关。这些方法包括对需要这种治疗的哺乳动物施用选自一系列二取代的反式，反式1,3-丁二烯，1,3-二取代的全氢丁二烯，1,2-二取代的反式亚乙基和1,2-二取代的乙烷的化合物和二取代的丙烷，它们各自共同体现了这些化合物的生物活性所必需的独特的结构特征。本发明还提供了使用这些新化合物的药物制剂。

52. 发明授权

US07645805B2 Gelling agents 有权
标题翻译：胶凝剂
公开(公告)号：US07645805B2
公开(公告)日：2010-01-12
申请号：US10515209
申请日：2003-05-22
申请人： Kjeld Jacobus Cornelis van Bommel , Johannes Henricus van Esch , Maaike de Loos , André Heeres , Bernard Lucas Feringa
发明人： Kjeld Jacobus Cornelis van Bommel , Johannes Henricus van Esch , Maaike de Loos , André Heeres , Bernard Lucas Feringa
IPC分类号： C08J3/075 , A61K9/10
CPC分类号： B01J20/291 , B01J20/22 , B01J20/281 , B01J2220/54 , C07C229/08 , C07C229/36 , C07C237/20 , C07C237/22 , C07C271/22
摘要： The invention relates to a novel class of gelling agents, to a process of preparing said agents, to the use of said agents to prepare gels, and to the gels thus obtained. A gelling agent or thickener according to the invention comprises a core which is functionalized with three amino acid derived groups by means of an amide or urea linkage. It may be used to gelate or thicken numerous solvents.
摘要翻译：本发明涉及一类新颖的胶凝剂，制备所述试剂的方法，所述试剂用于制备凝胶以及所得凝胶。根据本发明的胶凝剂或增稠剂包括通过酰胺或脲键与三个氨基酸衍生基团官能化的核心。它可用于使许多溶剂凝胶化或增稠。

53. 发明申请

US20090324540A1 COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS 失效
标题翻译：用于递送活性剂的化合物和组合物
公开(公告)号：US20090324540A1
公开(公告)日：2009-12-31
申请号：US12482320
申请日：2009-06-10
申请人： Donald J. Sarubbi , Eugene N. Barantsevitch
发明人： Donald J. Sarubbi , Eugene N. Barantsevitch
IPC分类号： A61K38/20 , A61K47/22 , A61K47/20 , A61K38/23 , A61K38/28 , A61K39/395 , A61K38/21 , A61K31/727 , A61K47/42 , A61K38/22 , A61K38/25 , A61K38/27 , A61K47/16 , A61K47/12 , C07C229/40 , C07C229/34 , C07D211/60 , C07C317/06 , C07D241/02 , C07F9/28 , C07D213/78 , C07D403/04 , C07D311/22 , C07D209/48 , C07D209/46 , C07D265/30 , C07D257/04
CPC分类号： C07D209/48 , A61K9/1617 , A61K31/195 , A61K31/445 , A61K31/4965 , A61K31/727 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K45/06 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K2300/00
摘要： Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要翻译：提供了可用于递送活性剂的载体化合物及其组合物。也提供给药和制备方法。

54. 发明申请

US20090318432A1 Nitrate esters of aminoalcohols 审中-公开
标题翻译：氨基醇的硝酸酯
公开(公告)号：US20090318432A1
公开(公告)日：2009-12-24
申请号：US12310881
申请日：2007-09-11
申请人： Peter Herold , Robert Mah , Christiane Marti , Nathalie Jotterand
发明人： Peter Herold , Robert Mah , Christiane Marti , Nathalie Jotterand
IPC分类号： A61K31/538 , C07C229/02 , A61K31/195 , A61K31/445 , C07D211/60 , C07D265/36
CPC分类号： C07C237/20 , C07C2601/14 , C07D209/12 , C07D211/16 , C07D211/30 , C07D213/56 , C07D213/64 , C07D215/54 , C07D231/56 , C07D265/36 , C07D307/80 , C07D401/12 , C07D405/12 , C07D413/12
摘要： The application relates to novel nitrate ester derivatives of substituted aminoalcohols of the general formula (I), wherein R1, R2, R3, V, X, Y and Z0 have the meanings explained in more detail in the description, to a process for their preparation and to the use of these compounds as therapeutics in cardiovascular diseases, in particular in high blood pressure and vascular and organ damage age accompanying high blood pressure.
摘要翻译：本申请涉及通式（I）的取代氨基醇的新型硝酸酯衍生物，其中R1，R2，R3，V，X，Y和Z0具有在说明书中更详细解释的含义及其制备方法以及这些化合物在心血管疾病中的应用，特别是伴随高血压的高血压和血管和器官损伤年龄的使用。

55. 发明申请

US20090291945A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：US20090291945A1
公开(公告)日：2009-11-26
申请号：US12419722
申请日：2009-04-07
申请人： Gen Unoki , Takashi Hayamizu , Hiroshi Eguchi , Yumiko Muroga , Toshiyuki Kaneko , Naoki Yajima
发明人： Gen Unoki , Takashi Hayamizu , Hiroshi Eguchi , Yumiko Muroga , Toshiyuki Kaneko , Naoki Yajima
IPC分类号： A61K31/54 , A61K31/535 , A61K31/445 , A61K31/165 , C07D279/12 , C07D265/28 , C07D211/60 , C07C237/02
CPC分类号： C07C255/16 , C07C237/10 , C07C237/14 , C07C237/20 , C07C237/24 , C07C259/06 , C07C317/18 , C07C317/28 , C07C317/32 , C07C323/12 , C07C323/41 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/34 , C07D211/60 , C07D211/62 , C07D213/26 , C07D213/40 , C07D231/12 , C07D231/14 , C07D233/61 , C07D265/30 , C07D295/155 , C07D295/185 , C07D317/50 , C07D401/12
摘要： To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.
摘要翻译：提供具有优异的半胱氨酸蛋白酶抑制作用的化合物，提供治疗或预防选自骨质疏松症，骨关节炎，慢性类风湿性关节炎，骨关节炎，高钙血症，癌症骨转移的疾病的药物，和骨痛。由式（1）表示的化合物或其药学上可接受的盐，或其含有与有效成分相同的药物或药物组合物。

56. 发明授权

US07601708B2 Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration 失效
公开(公告)号：US07601708B2
公开(公告)日：2009-10-13
申请号：US11183911
申请日：2005-07-19
申请人： Kenneth C. Cundy , Mark A. Gallop , Cindy X. Zhou
发明人： Kenneth C. Cundy , Mark A. Gallop , Cindy X. Zhou
IPC分类号： A61K31/56 , C07J9/00
CPC分类号： C07K5/0205 , A61K31/56 , A61K38/00 , A61K47/54 , A61K47/554 , A61K47/64 , A61K47/65 , C07C237/12 , C07C237/20 , C07C323/60 , C07C2601/14 , C07D207/16 , C07D233/64
摘要： This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.

57. 发明授权

US07592373B2 Amide compounds with MCH antagonistic activity and medicaments comprising these compounds 有权
标题翻译：具有MCH拮抗活性的酰胺化合物和包含这些化合物的药物
公开(公告)号：US07592373B2
公开(公告)日：2009-09-22
申请号：US11021897
申请日：2004-12-23
申请人： Thorsten Lehmann-Lintz , Ralf R. H. Lotz , Philipp Lustenberger , Stephan Georg Mueller , Gerald Juergen Roth , Klaus Rudolf , Marcus Schindler , Dirk Stenkamp , Leo Thomas
发明人： Thorsten Lehmann-Lintz , Ralf R. H. Lotz , Philipp Lustenberger , Stephan Georg Mueller , Gerald Juergen Roth , Klaus Rudolf , Marcus Schindler , Dirk Stenkamp , Leo Thomas
IPC分类号： C07C233/29 , C07C235/24 , C07D209/18 , A61K31/40 , A61K31/167 , A61K31/404 , A61P3/04
CPC分类号： C07C255/24 , C07C233/29 , C07C233/44 , C07C233/55 , C07C237/20 , C07C311/08 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D211/14 , C07D211/22 , C07D211/44 , C07D211/58 , C07D213/36 , C07D213/56 , C07D221/20 , C07D231/12 , C07D233/60 , C07D249/08 , C07D263/56 , C07D295/155 , C07D309/14 , C07D401/12
摘要： Compounds of formula (I) wherein A, B, b, W, X, Y, Z, R1, R2, and R3 have the meanings given in claim 1, pharmaceutical compositions these compounds, and methods of preventing or treating metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes using these compounds.
摘要翻译：其中A，B，b，W，X，Y，Z，R 1，R 2和R 3具有权利要求1中给出的含义的式（I）化合物，这些化合物的药物组合物，以及预防或治疗代谢紊乱和/ 或进食障碍，特别是肥胖症，食欲过剩，厌食症，食欲过盛和糖尿病。

58. 发明授权

US07560482B2 Inhibitors of plasmepsins 有权
标题翻译：血浆素抑制剂
公开(公告)号：US07560482B2
公开(公告)日：2009-07-14
申请号：US10471655
申请日：2002-03-15
申请人： Ernesto Freire , Azin Nezami , Yoshiaki Kiso
发明人： Ernesto Freire , Azin Nezami , Yoshiaki Kiso
IPC分类号： A61K31/366 , A61K38/00
CPC分类号： C07C237/20 , A61K31/198 , A61K31/366 , A61K31/426 , A61K38/05 , A61K38/06 , Y02A50/411
摘要： Compounds and methods for the inhibition of anti-malarial target aspartyl protease plasmepsins (e.g. Plasmepsin I, Plasmepsin II, Plasmepsin IV and HAP) are provided. The compounds are based on allophenylnorstatine substituted at positions R1-R4, such that R1 is isoquinoline, carboxyl, naphtalene, phenyl, phenol, benzene, an amino acid, and derivatives thereof; R2 and R3 are aliphatic groups; and R4 is indan, naphthalene, benzylamine, phenyl, phenol, cyclopentane, tert-butylamine, or derivatives thereof. The compounds may be used to inhibit Plasmepsin II, to kill malarial parasites, and to treat malaria in a patient. Certain of the substituted allophenylnorstatine-based compounds also exhibit inhibitory activity against Cathepsin D.
摘要翻译：提供了用于抑制抗疟疾靶标天冬氨酰蛋白酶plasmepsin（例如Plasmepsin I，Plasmepsin II，Plasmepsin IV和HAP）的化合物和方法。这些化合物基于在R1-R4位置被取代的异氰酸酯基，其中R 1是异喹啉，羧基，萘，苯基，苯酚，苯，氨基酸及其衍生物; R2和R3是脂族基团; R4为茚满，萘，苄胺，苯基，苯酚，环戊烷，叔丁胺或其衍生物。该化合物可用于抑制Plasmepsin II，杀死疟疾寄生虫，并治疗患者的疟疾。某些取代的基于异氰酸酯基的化合物也表现出对组织蛋白酶D的抑制活性。

59. 发明授权

US07553872B2 Compounds and compositions for delivering active agents 有权
公开(公告)号：US07553872B2
公开(公告)日：2009-06-30
申请号：US11354045
申请日：2006-02-13
申请人： Donald J. Sarubbi , Evgueni Barantsevitch
发明人： Donald J. Sarubbi , Evgueni Barantsevitch
IPC分类号： A61K31/195 , A61K38/14
CPC分类号： C07D209/48 , A61K9/1617 , A61K31/195 , A61K31/445 , A61K31/4965 , A61K31/727 , A61K38/21 , A61K38/23 , A61K38/27 , A61K38/28 , A61K38/29 , A61K45/06 , C07C229/42 , C07C233/51 , C07C233/54 , C07C233/69 , C07C233/81 , C07C233/83 , C07C235/12 , C07C235/24 , C07C235/34 , C07C235/38 , C07C235/52 , C07C235/56 , C07C235/60 , C07C235/64 , C07C235/66 , C07C235/74 , C07C237/12 , C07C237/20 , C07C237/36 , C07C237/40 , C07C237/42 , C07C243/38 , C07C259/06 , C07C271/28 , C07C271/54 , C07D211/62 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24 , C07D257/04 , C07D295/192 , C07D311/12 , C07D311/24 , C07D311/30 , A61K2300/00
摘要： Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

60. 发明申请

US20090156465A1 DERIVATIVES OF BETA-AMINO ACID AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译：作为DIPEPTIDYLPEPDDASE-IV抑制剂的β-氨基酸的衍生物
公开(公告)号：US20090156465A1
公开(公告)日：2009-06-18
申请号：US12159562
申请日：2006-12-12
申请人： Jitendra A. Sattigeri , Shahadat Ahmed , Murugaiah M.S. Andappan , Sachin Sethi , Lalima Sharma , Chanchal Kumar Pal , Sachin Ramesh Kandalkar , Dipak C. Mahajan , Kaushal Kishore , Sumati Bhatia , Anil G. Gadhave , Vinay S. Bansal , Joseph Alexanand Davis
发明人： Jitendra A. Sattigeri , Shahadat Ahmed , Murugaiah M.S. Andappan , Sachin Sethi , Lalima Sharma , Chanchal Kumar Pal , Sachin Ramesh Kandalkar , Dipak C. Mahajan , Kaushal Kishore , Sumati Bhatia , Anil G. Gadhave , Vinay S. Bansal , Joseph Alexanand Davis
IPC分类号： A61K38/28 , C07D413/02 , A61K31/5377 , C07D241/36 , A61K31/4995 , A61K31/702 , A61K31/397 , A61P3/00 , A61P3/10 , A61P37/00 , A61P35/00 , A61P1/00 , A61P15/08
CPC分类号： C07D409/12 , C07C237/20 , C07C2603/74 , C07D209/44 , C07D209/52 , C07D211/58 , C07D401/12 , C07D405/12 , C07D487/08
摘要： The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.
摘要翻译：本发明涉及作为二肽基肽酶-IV抑制剂的β-氨基酸衍生物及其合成方法。本发明还涉及含有本发明化合物的药物组合物，以及治疗糖尿病，特别是2型糖尿病以及糖尿病前期，糖尿病性血脂异常，代谢性酸中毒，酮症，饱腹感和肥胖症的方法。这些抑制剂也可用于治疗由各种代谢，神经，抗炎和自身免疫性疾病如炎症性疾病，多发性硬化，类风湿性关节炎所表现的病症; 病毒，癌症和胃肠道疾病。本发明的化合物也可用于治疗由于多囊卵巢综合征引起的不育症。

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