公开(公告)号：US20070197580A1

公开(公告)日：2007-08-23

申请号：US11551562

申请日：2006-10-20

申请人： Xiaoming Zhang ,  Jurg Pfister ,  Cyrus Becker ,  Pascal Druzgala

发明人： Xiaoming Zhang ,  Jurg Pfister ,  Cyrus Becker ,  Pascal Druzgala

IPC分类号： A61K31/4745 ,  A61K31/4178 ,  C07D403/02 ,  C07D471/02

CPC分类号： C07D403/06 ,  C07D451/14 ,  C07D471/04

摘要： The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.

摘要翻译： 本发明提供有用的和新颖的5-HT 3拮抗剂。 本发明还提供了合成本发明化合物的方法。 本发明还提供了治疗肠易激综合征和其他此类病症的方法。

公开(公告)号：US20060116418A1

公开(公告)日：2006-06-01

申请号：US11220364

申请日：2005-09-06

申请人： Pascal Druzgala ,  Xiaoming Zhang ,  Jurg Pfister

发明人： Pascal Druzgala ,  Xiaoming Zhang ,  Jurg Pfister

IPC分类号： A61K31/405 ,  C07D209/18

CPC分类号： C07D239/42 ,  A61K31/405 ,  A61K31/47 ,  A61K31/505 ,  C07C69/675 ,  C07C69/708 ,  C07C69/732 ,  C07C2602/28 ,  C07D207/34 ,  C07D209/12 ,  C07D209/24 ,  C07D213/55 ,  C07D215/14 ,  C07D307/80 ,  C07D311/72

摘要： The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can be advantageously used to treat patients suffering hypercholesterolemia.

摘要翻译： 本发明提供新的HMG-CoA还原酶抑制剂。 在优选的实施方案中，本发明的HMG-CoA还原酶抑制剂可以通过水解酶而失活至初级无活性代谢物。 本发明的化合物可有利地用于治疗患有高胆固醇血症的患者。

公开(公告)号：US20050107365A1

公开(公告)日：2005-05-19

申请号：US10971522

申请日：2004-10-22

申请人： Cyrus Becker ,  Joan Caroon ,  Chris Melville ,  Fernando Padilla ,  Jurg Pfister ,  Xiaoming Zhang

发明人： Cyrus Becker ,  Joan Caroon ,  Chris Melville ,  Fernando Padilla ,  Jurg Pfister ,  Xiaoming Zhang

IPC分类号： A61K31/517 ,  A61K31/519 ,  A61K31/549 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

CPC分类号： C07D417/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

摘要： This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X-Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

公开(公告)号：US20050075379A1

公开(公告)日：2005-04-07

申请号：US10759617

申请日：2004-01-16

申请人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

发明人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

IPC分类号： C07D261/12 ,  C07D277/20 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  A61K31/426

CPC分类号： C07D277/20 ,  C07D261/12 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  Y10S514/824 ,  Y10S514/866

摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

摘要翻译： 本发明提供了可用于治疗II型糖尿病的药物化合物。 这些化合物是有利的，因为它们容易被代谢药物解毒体系代谢。 特别地，提供了被设计为在化合物的结构内包含酯的噻唑烷二酮类似物。 本发明还涉及治疗疾病如糖尿病的方法，其包括施用包含化合物的治疗有效组合物，所述化合物被设计为由血清或细胞内水解酶和酯酶代谢。 还教导了含酯的噻唑烷二酮类似物的药物组合物。

公开(公告)号：US5082847A

公开(公告)日：1992-01-21

申请号：US555201

申请日：1990-07-18

申请人： Jean-Claude Pascal ,  Leslie Patmore ,  Jurg Pfister ,  Dominique Blondet ,  John M. Armstrong

发明人： Jean-Claude Pascal ,  Leslie Patmore ,  Jurg Pfister ,  Dominique Blondet ,  John M. Armstrong

IPC分类号： A61K31/47 ,  A61P9/00 ,  A61P9/10 ,  C07D401/12

CPC分类号： C07D401/12

摘要： Carbostyril derivatives of Formula I: ##STR1## wherein: m is 0, 1, or 2;n is 0, 1, or 2;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, aralkoxy, or acyloxy;R.sup.3 is hydrogen, halogen, lower alkyl, or lower alkoxy;R.sup.4 is hydrogen, hydroxy, lower alkyl, acyloxy, provided that when R.sup.4 is hydroxy or acyloxy, m and n are both 1;R.sup.5 is hydrogen or lower alkyl; andR.sup.6 is alkyl, hydroxyalkyl, alkoxyalkyl, or (dialkylamino)alkyl;and the pharmaceutically acceptable acid addition salts and N-oxides (at the carbostyril nitrogen) thereof, and compositions containing them, are useful in treating cardiovascular diseases, particularly arrhythmias. Methods of preparing intermediates, the compounds, their formulations and methods of treatment therewith are also disclosed.

公开(公告)号：US20070129429A1

公开(公告)日：2007-06-07

申请号：US11551302

申请日：2006-10-20

申请人： Pascal Druzgala ,  Xiaoming Zhang ,  Jurg Pfister

发明人： Pascal Druzgala ,  Xiaoming Zhang ,  Jurg Pfister

IPC分类号： A61K31/366 ,  C07D405/02

CPC分类号： A61K31/366 ,  A61K31/37 ,  C07D311/56

摘要： This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

摘要翻译： 本发明涉及更容易被代谢药物解毒系统代谢的化合物。 特别地，教导了被设计成在化合物的结构内包含酯的华法林类似物。 本发明教导了在药物合成期间降低包括将酯基引入药物的药物的毒性的方法。 本发明还涉及治疗凝血障碍的方法，其包括施用被设计为由血清或细胞内水解酶和酯酶代谢的化合物。 还教导了含有华法林酯类药物组合物。

公开(公告)号：USRE42412E1

公开(公告)日：2011-05-31

申请号：US11962592

申请日：2007-12-21

申请人： Pascal Druzgala ,  Peter G. Milner ,  Jurg Pfister ,  Cyrus Becker

发明人： Pascal Druzgala ,  Peter G. Milner ,  Jurg Pfister ,  Cyrus Becker

IPC分类号： A61K31/445 ,  C07D211/56

CPC分类号： C07D211/58 ,  A61K31/4468 ,  C07D211/46

摘要： The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions of the subject invention comprise esterified cisapride derivatives. These compositions possess potent activity in treating gastroesophageal reflux disease and substantially reduce adverse effects associated with the administration of cisapride. These adverse effects include, but are not limited to, diarrhea, abdominal cramping and elevations of blood pressure and heart rate.

摘要翻译： 本发明提供了用于安全有效地治疗胃食管反流和相关病症的新型化合物和组合物。 在优选的实施方案中，本发明的组合物包含酯化的西沙必利衍生物。 这些组合物在治疗胃食管反流疾病中具有有效的活性，并且显着减少与西沙必利施用相关的不良反应。 这些不良影响包括但不限于腹泻，腹部绞痛和血压升高和心率升高。

公开(公告)号：US20050037997A9

公开(公告)日：2005-02-17

申请号：US10251522

申请日：2002-09-20

申请人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

发明人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

IPC分类号： A61P3/10 ,  C07D261/12 ,  C07D277/20 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  C07J1/00 ,  A61K31/58 ,  A61K31/69 ,  C07J17/00 ,  C07J43/00

CPC分类号： C07D277/20 ,  C07D261/12 ,  C07D277/34 ,  C07D311/70 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07J3/00 ,  Y10S514/866

摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

公开(公告)号：US4598938A

公开(公告)日：1986-07-08

申请号：US717229

申请日：1985-03-18

申请人： Hans Boss ,  Jurg Pfister, deceased ,  by Lisa Pfister, administrator

发明人： Hans Boss ,  Jurg Pfister, deceased ,  by Lisa Pfister, administrator

IPC分类号： B21D39/04 ,  F16L20060101 ,  F16L13/14 ,  F16L21/04

CPC分类号： F16L13/146 ,  B21D39/04 ,  Y10T29/49913 ,  Y10T29/49934

摘要： In this pipe connection, the pipe end part (5) is pressed, as a result of cold-forming in zones, by means of a press ring (4) to be displaced axially, to form a positive leak-proof connection with a connection piece (1) inserted into the pipe end part and belonging to a pipe fitting (2). A sleeve (3) to be pushed onto the pipe end part is provided with an annular outer bead (7) and, when the press ring is pressed on, is deformed in such a way that the sleeve material is displaced radially inwards in the bead zone (8), the pipe end part and connection piece acquiring an annular recess (9). Moreover, the press ring (4) has at its rear end an annular inner bead (10) which at the same time displaces the sleeve material radially inwards at the rear sleeve end, as a result of which further pressing takes place at the end (12) of the connection piece (1). The gap between the pipe and connection piece is thus closed, so that no crevice corrosion can occur.

摘要翻译： PCT No.PCT / CH84 / 00114 Sec。 371日期1985年3月18日 102（e）1985年3月18日PCT提交1984年7月12日PCT公布。 出版物WO85 / 00646 日期为1985年2月14日。在该管道连接中，由于在区域中冷成型，管端部（5）通过压环（4）被轴向移动，以形成正的 与插入管端部并属于管接头（2）的连接件（1）的防漏连接。 被推入管端部的套筒（3）设置有环形外胎圈（7），并且当按压环时，其变形使得套筒材料在胎圈中径向向内位移 （8），管端部和连接件获取环形凹部（9）。 此外，压环（4）在其后端处具有环形内胎圈（10），其同时在后套筒端部沿径向向内移动套筒材料，由此在末端进一步压紧（ 12）。 因此，管和连接件之间的间隙被封闭，从而不会发生缝隙腐蚀。

公开(公告)号：US20060047000A1

公开(公告)日：2006-03-02

申请号：US11167925

申请日：2005-06-27

申请人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

发明人： Pascal Druzgala ,  Peter Milner ,  Jurg Pfister

IPC分类号： A61K31/426 ,  A61K31/42 ,  A61K31/198 ,  A61K31/192

CPC分类号： C07D417/06 ,  C07D401/04 ,  C07D413/04 ,  C07J3/005 ,  C07J9/00

摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.