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1. 发明授权

US5736554A Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties 失效
标题翻译：具有抗高血压，心脏保护作用，抗缺血性和抗脂解性的化合物
公开(公告)号：US5736554A
公开(公告)日：1998-04-07
申请号：US455361
申请日：1995-05-31
申请人： Alfred P. Spada , Cynthia A. Fink , Michael R. Myers
发明人： Alfred P. Spada , Cynthia A. Fink , Michael R. Myers
IPC分类号： C07D473/34 , A61K31/435 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P3/06 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , C07D471/04 , C07D473/00 , C07H19/04 , C07H19/052 , C07H19/16 , A61K31/44
CPC分类号： C07D473/00 , C07D471/04 , C07H19/052 , C07H19/16
摘要： Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.b are independently H, OH, alkyl, hydroxyalkyl, alkyl mercaptyl, thioalkyl, alkoxy, alkyoxyalkyl, amino, alkyl amino, carboxyl, acyl, halogen, carbamoyl, alkyl carbamoyl, aryl or heterocyclyl; and R' and R" are independently hydrogen, alkyl, aralkyl, carbamoyl, alkyl carbamoyl, dialkylcarbamoyl, acyl, alkoxycarbonyl, aralkoxycarbonyl, aryloxycarbonyl, or R' and R" together may form ##STR4## where R.sub.c is hydrogen or alkyl, ##STR5## where R.sub.d and R.sub.e are independently hydrogen, alkyl, or together with the carbon atom to which they are attached may form a 1,1-cycloalkyl group; provided that when X is straight chain alkylene and Q is oxygen, then Z represents a heterocyclyl including at least two heteroatoms, which are adenosine agonists useful as antihypertensive, cardioprotective, antiischemic, and antilipolytic agents, pharmaceutical compositions including such compounds, and their use in treating hypertension, myocardial ischemia, ameliorating ischemic injury and myocardial infarct size consequent to myocardial ischemia, hyperlipidemia and hypercholesterolemia are claimed.
摘要翻译：式的化合物其中：K为N或N-> O; Q是CH 2或O; T为或R3O-CH2; X是直链或支链亚烷基，亚环烷基或环亚烯基，其各自任选被至少一个CH 3，CH 3 CH 2，Cl，F，CF 3或CH 3 O取代; Y为NR4，O或S; a = 0或1; Z为式（Ⅰ）Z1为N，CR5，（CH）m-CR5或（CH）m-N，m为1或2; Z2为N，NR6，O或S，n为0或1; R1，R2，R3，R4，R5和R6独立地为H，烷基，芳基或杂环基; R a和R b独立地是H，OH，烷基，羟基烷基，烷基硫醇基，硫代烷基，烷氧基，烷氧基烷基，氨基，烷基氨基，羧基，酰基，卤素，氨基甲酰基，烷基氨基甲酰基，芳基或杂环基。并且R'和R“独立地为氢，烷基，芳烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基或R'和R”一起可以形成E>，其中Rd和Re独立地为氢，烷基或与它们所连接的碳原子一起可以形成1,1-环烷基; 条件是当X是直链亚烷基并且Q是氧时，Z代表包括至少两个杂原子的杂环基，它们是可用作抗高血压，心脏保护，抗缺血和抗脂肪分解剂的腺苷激动剂，包括这些化合物的药物组合物，以及它们在要求治疗高血压，心肌缺血，改善缺血性损伤和心肌缺血，高脂血症和高胆固醇血症引起的心肌梗死面积。

2. 发明授权

US5731315A Substituted sulfonic acid n-�(aminoiminomethyl)phenylalkyl!-azaheterocyclamide compounds 失效
标题翻译：取代的磺酸n - [（氨基亚氨基甲基）苯基烷基] - 杂环酰胺化合物
公开(公告)号：US5731315A
公开(公告)日：1998-03-24
申请号：US761414
申请日：1996-12-06
申请人： William R. Ewing , Michael R. Becker , Yong Mi Choi-Sledeski , Heinz W. Pauls , Daniel G. McGarry , Roderick S. Davis , Alfred P. Spada
发明人： William R. Ewing , Michael R. Becker , Yong Mi Choi-Sledeski , Heinz W. Pauls , Daniel G. McGarry , Roderick S. Davis , Alfred P. Spada
IPC分类号： C07D223/10 , A61K31/00 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/401 , A61K31/4015 , A61K31/4025 , A61K31/415 , A61K31/42 , A61K31/422 , A61K31/435 , A61K31/4353 , A61K31/4365 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/445 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/4725 , A61K31/505 , A61K31/506 , A61K31/55 , A61P7/00 , A61P7/02 , A61P9/00 , A61P43/00 , C07D205/085 , C07D207/14 , C07D207/26 , C07D207/273 , C07D207/40 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D495/04 , C07D401/02
CPC分类号： C07D207/273 , C07D205/085 , C07D207/14 , C07D207/416 , C07D211/76 , C07D223/12 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14
摘要： The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
摘要翻译：式I的化合物显示出有用的药理活性，因此并入药物组合物中并用于治疗患有某些医学病症的患者。更具体地说，它们是因子Xa活性的抑制剂。本发明涉及式I化合物，其含有式I化合物的组合物及其用途，其用于治疗患有或经受生理条件的患者，其可通过施用活性抑制剂而改善因子Xa。

3. 发明授权

US5721237A Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties 失效
标题翻译：具有HER-2自身磷酸化特性选择性抑制的蛋白酪氨酸激酶芳基和杂芳基喹唑啉化合物
公开(公告)号：US5721237A
公开(公告)日：1998-02-24
申请号：US469147
申请日：1995-06-06
申请人： Michael R. Myers , Alfred P. Spada , Martin P. Maguire , Paul E. Persons
发明人： Michael R. Myers , Alfred P. Spada , Martin P. Maguire , Paul E. Persons
IPC分类号： C07D239/42 , A61K31/495 , A61K31/505 , A61K31/517 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07C43/205 , C07C43/225 , C07C43/23 , C07D213/30 , C07D213/64 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/50 , C07D239/74 , C07D239/88 , C07D239/91 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/52 , C07D265/22 , C07D277/64 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04 , C07D235/02
CPC分类号： C07C43/2055 , A61K31/517 , A61K31/5377 , C07C43/225 , C07C43/23 , C07D213/30 , C07D213/64 , C07D215/14 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/50 , C07D239/74 , C07D239/88 , C07D239/91 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/52 , C07D265/22 , C07D277/64 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D471/04
摘要： This invention relates to a method for the selective treatment of cell growth and differentiation characterized by activity of the human epidermal growth factor receptor type 2 (HER2). More specifically, this invention relates to the use of substituted or unsubstituted mono- or bi-cyclic aryl, heteroaryl, cycloalkyl or heterocycloalkyl compounds in selectively regulating cell growth. Pharmaceutical compositions useful for the selective treatment of cell growth and differentiation are also described.
摘要翻译：本发明涉及一种选择性处理细胞生长和分化的方法，其特征在于人表皮生长因子受体2型（HER2）的活性。更具体地，本发明涉及取代或未取代的单环或双环芳基，杂芳基，环烷基或杂环烷基化合物在选择性调节细胞生长中的用途。还描述了可用于选择性处理细胞生长和分化的药物组合物。

4. 发明授权

US5674482A Polymers with alkyl- or heteroalkyl -aryl backbone and pharmaceutical compositions incorporating same 失效
标题翻译：具有烷基 - 或杂烷基 - 芳基骨架的聚合物和包含其的药物组合物
公开(公告)号：US5674482A
公开(公告)日：1997-10-07
申请号：US742794
申请日：1991-08-09
申请人： John R. Regan , Michael N. Chang , Jack Newman , Schmuel Ben-Sasson
发明人： John R. Regan , Michael N. Chang , Jack Newman , Schmuel Ben-Sasson
IPC分类号： A61K31/775 , C08G8/04
CPC分类号： A61K31/775
摘要： A biologically active polymeric compound comprising an alkylaryl or heteroalkylaryl backbone having about 5 to about 50 repeating aromatic ring-containing units and which, according to the computer program marketed as SYBYL.RTM. version 5.2 running on a DEC VAX.RTM. 11/750 computer, is capable of forming a linear backbone having a helical secondary structure, and wherein the maximum diameter of the helical structure, as measured by the alkylaryl or heteroalkylaryl backbone, is less than 3 times greater than the maximum diameter of the aryl group of the alkylaryl or heteroalkylaryl backbone.
摘要翻译：包含具有约5至约50个重复含芳环单元的烷基芳基或杂烷基芳基主链的生物活性聚合物，并且根据在DEC VAX TM 11/750计算机上运行的以SYBYL TM 5.2版为基础的计算机程序，其能够形成具有螺旋二级结构的线性主链，并且其中通过烷基芳基或杂烷基芳基主链测量的螺旋结构的最大直径小于烷基芳基或杂烷基芳基骨架的芳基的最大直径的3倍。

5. 发明授权

US5656655A Styryl-substituted heteroaryl compounds which inhibit EGF receptor tyrosine kinase 失效
标题翻译：抑制EGF受体酪氨酸激酶的苯乙烯基取代的杂芳基化合物
公开(公告)号：US5656655A
公开(公告)日：1997-08-12
申请号：US444696
申请日：1995-05-19
申请人： Alfred P. Spada , Paul E. Persons , Alexander Levitzki , Chaim Gilon , Aviv Gazit
发明人： Alfred P. Spada , Paul E. Persons , Alexander Levitzki , Chaim Gilon , Aviv Gazit
IPC分类号： A61K31/404 , A61K31/4406 , C07D209/18 , C07D213/57 , C07D209/04 , A61K31/40
CPC分类号： C07D213/57 , A61K31/404 , A61K31/4406 , C07D209/18
摘要： A method of inhibiting cell proliferation in a patient suffering from such disorder comprising the administration to the patient of a pharmaceutically effective amount of a pharmaceutical composition containing, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, of the formula ##STR1## wherein the radicals are defined in the specification.
摘要翻译：一种抑制患有这种病症的患者的细胞增殖的方法，包括向患者施用药学有效量的药物组合物，其包含与药学上可接受的载体，化合物或其药学上可接受的盐的混合物式其中基团在说明书中定义。

6. 发明授权

US5652366A DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof 失效
标题翻译： DI（1R） - （ - ）樟脑磺酸）盐，其制备及其用途
公开(公告)号：US5652366A
公开(公告)日：1997-07-29
申请号：US484811
申请日：1995-06-07
申请人： Alfred P. Spada , Cynthia A. Fink , Michael R. Myers , Laurence W. Reilly , Benoit J. Vanasse
发明人： Alfred P. Spada , Cynthia A. Fink , Michael R. Myers , Laurence W. Reilly , Benoit J. Vanasse
IPC分类号： C07D471/04 , C07D473/00 , C07H19/052 , C07H19/16
CPC分类号： C07D471/04 , C07D473/00 , C07H19/052 , C07H19/16
摘要： This invention relates to di[(1 R)-(-)-camphosulfonic acid) salt of [1S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl)-1-ethylethyl]amino]3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide, and a process for preparing the compound, comprising reacting a reaction mixture of (-)-1.beta.-N-ethyl-2.alpha.,3.alpha.-isopropylidenedioxy-4.beta.-[3-amino-4-[2-(5-chloro-2-thienyl)-(1R)-1-ethylethyl]amino-2-pyridyl]aminocyclopentanecarboxamide and formamidine acetate, and then treating the reaction mixture with (1 R)-(-)-10-camphorsulfonic acid.The salt is useful in purifying [1 S-[1.alpha.,2.beta.,3.beta.,4.alpha.,(S*)]]-4-[7-[[2-(3-chloro-2-thienyl)-1-ethylethyl]amino]-3 H-imidazo[4,5-b]pyridin-3-yl]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide which possesses adenosine agonist activity and is useful as an anti-hypertensive, cardioprotective, anti-ischemic, and antilipolytic agent.
摘要翻译：本发明涉及[1S- [1α，2β，3β，4α，（S *）]] - 4- [7 - [[ 2-（3-氯-2-噻吩基）-1-乙基乙基]氨基] 3 H-咪唑并[4,5-b]吡啶-3-基] -N-乙基-2,3-二羟基环戊烷甲酰胺，以及制备该化合物，包括使（ - ） - 1β-N-乙基-2α，αα-异亚丙基二氧基-4β-[3-氨基-4- [2-（5-氯-2-噻吩基）） - （1R）-1-乙基乙基]氨基-2-吡啶基]氨基环戊烷甲酰胺和甲脒乙酸盐，然后用（1R） - （ - ） - 10-樟脑磺酸处理反应混合物。该盐可用于纯化[1 S- [1α，2β，3β，4α，（S *）]] -4- [7 - [[2-（3-氯-2-噻吩基） - 乙基]氨基] -3H-咪唑并[4,5-b]吡啶-3-基] -N-乙基-2,3-二羟基环戊烷甲酰胺，其具有腺苷激动剂活性，可用作抗高血压，心脏保护，抗 - 抗血清剂和抗脂肪分解剂。

7. 发明授权

US5614496A Use of fibroblast growth factors to stimulate bone growth 失效
标题翻译：使用成纤维细胞生长因子刺激骨骼生长
公开(公告)号：US5614496A
公开(公告)日：1997-03-25
申请号：US458634
申请日：1995-06-02
申请人： Colin R. Dunstan , Elzbieta Izbicka , Gregory R. Mundy , Wilson Burgess , Michael C. Jaye
发明人： Colin R. Dunstan , Elzbieta Izbicka , Gregory R. Mundy , Wilson Burgess , Michael C. Jaye
IPC分类号： G01B21/20 , A61K38/00 , A61K38/18 , A61K38/22 , A61K45/00 , A61P1/02 , A61P5/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07K14/50 , C12P21/02 , G01N21/35 , G01N21/85 , G01N33/10 , A61K38/16 , C07K14/475
CPC分类号： C07K14/501 , A61K38/1825 , C07K14/50 , G01N21/85 , G01N33/10 , Y10S530/84
摘要： The present invention provides therapeutic compositions for the prevention and treatment of pathological conditions involving bone and dental tissue. The present invention also provides a method to promote bone repair and/or growth for the treatment of pathological conditions involving bone tissue, for example, osteoporosis, Paget's disease, osteopetrosis, and periodontal disease and fracture repair, and healing of bone defects by administering FGF-1 to an animal or human in need of treatment.
摘要翻译：本发明提供了用于预防和治疗涉及骨和牙齿组织的病理状况的治疗组合物。本发明还提供一种促进骨修复和/或生长的方法，用于治疗涉及骨组织的病理状况，例如骨质疏松症，佩吉特氏病，骨硬化症，牙周病和骨折修复，以及通过施用FGF来治疗骨缺损 -1给需要治疗的动物或人类。

8. 发明授权

US5571790A Recombinant human endothelial cell growth factor 失效
公开(公告)号：US5571790A
公开(公告)日：1996-11-05
申请号：US472964
申请日：1995-06-07
申请人： Michael Jaye , Wilson Burgess , Thomas Maciag , William N. Drohan
发明人： Michael Jaye , Wilson Burgess , Thomas Maciag , William N. Drohan
IPC分类号： A61K38/00 , C07K14/50 , A61K38/27
CPC分类号： C07K14/501 , A61K38/00 , Y10S930/12
摘要： Endothelial cell growth factor is achieved through the application of recombinant DNA technology to prepare cloning vehicles encoding the ECGF protein and procedures are disclosed for recovering ECGF protein essentially free of other proteins of human origin. The product is useful for, among other purposes, diagnostic applications and as potential in the treatment of damaged blood vessels or other endothelial cell-lined structures.

9. 发明授权

US5571506A Aromatic oligomeric compounds useful as mimics of bioactive macromolecules 失效
标题翻译：用作生物活性大分子模拟物的芳族寡聚化合物
公开(公告)号：US5571506A
公开(公告)日：1996-11-05
申请号：US119456
申请日：1993-09-10
申请人： John R. Regan , Daniel G. McGarry , Michael N. Chang , Jeffrey N. Barton , Jack Newman , Schmuel Ben-Sasson
发明人： John R. Regan , Daniel G. McGarry , Michael N. Chang , Jeffrey N. Barton , Jack Newman , Schmuel Ben-Sasson
IPC分类号： A61K31/74 , A61K31/765 , A61K31/785 , A61K31/795 , C08G8/04 , C08G8/08 , C08G8/18 , C08G8/20 , A61K31/775
CPC分类号： C08G8/18 , A61K31/74 , A61K31/765 , A61K31/785 , A61K31/795 , C08G8/04 , C08G8/08 , C08G8/20 , Y10S514/822 , Y10S514/824
摘要： This invention relates to aromatic oligomeric compounds useful in the treatment of cardiovascular, bone metabolic, hypolipidaemic, neuronal, gastrointestinal and elastase-mediated connective tissue degradation disorders and disorders which may be treated by agents effective in binding DNA, to processes for preparation of such oligomeric compounds, to pharmaceutical compositions including such oligomeric compounds, and to their use in the treatment of such disorders.
摘要翻译：本发明涉及可用于治疗心血管，骨代谢，降血脂症，神经元，胃肠和弹性蛋白酶介导的结缔组织降解障碍和可由有效结合DNA的试剂治疗的病症的芳族低聚物，制备这种低聚物的方法化合物，包括这种低聚化合物的药物组合物，以及它们在治疗这些疾病中的用途。

10. 发明授权

US5563128A Phosphonate derivatives of lipophilic amines 失效
公开(公告)号：US5563128A
公开(公告)日：1996-10-08
申请号：US435020
申请日：1995-05-04
申请人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
发明人： Henry W. Pauls , Yong-Mi Choi , Dilip V. Amin
IPC分类号： C07F9/38 , C07F9/40 , C07F9/653 , C07F9/6558 , A61K31/675 , A61K31/66
CPC分类号： C07F9/65583 , C07F9/3808 , C07F9/3873 , C07F9/4006 , C07F9/404 , C07F9/405 , C07F9/65324
摘要： This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

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