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41. 发明授权

US5001148A Mevinic acid derivatives 失效
标题翻译：乙酸衍生物
公开(公告)号：US5001148A
公开(公告)日：1991-03-19
申请号：US362899
申请日：1989-06-07
申请人： Jeffrey O. Saunders , Eric M. Gordon
发明人： Jeffrey O. Saunders , Eric M. Gordon
IPC分类号： A61K31/215 , A01N37/18 , A61K31/235 , A61P3/06 , A61P9/10 , A61P43/00 , C07C235/04 , C07C235/06 , C07C235/08 , C07C235/16 , C07C239/06 , C07D295/18 , C07D295/185 , C07D309/30 , C07F7/18
CPC分类号： C07D295/185 , C07C235/06 , C07C235/08 , C07C235/16 , C07D309/30 , C07F7/1856 , C07C2102/28
摘要： Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.n,(x) phenyl-S(O).sub.n,(xi) substituted phenyl-S(O).sub.n in which one or more substituents are X and Y, and(xii) oxo,(c) alkyl-S(O).sub.n,(d) cycloalkyl-S(O).sub.n,(e) phenyl-S(O).sub.n,(f) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y,(g) halogen,(h) hydroxy,(i) alkoxy,(j) alkoxycarbonyl,(k) acyloxy,(l) phenyl, and(m) substituted phenyl in which one or more substituents are X and Y,(7) phenyl,(8) substituted phenyl in which one or more substituents are X or Y,(9) amino,(10) alkylamino,(11) dialkylamino,(12) phenylamino,(13) substituted phenylamino in which one or more substituents are X or Y,(14) alkyl(substituted phenyl)amino in which one or more substituents are X and Y,(15) phenylalkylamino,(16) di(phenylalkyl)amino,(17) substituted phenylalkylamino in which one or more substituents are X or Y,(18) a member selected from(a) piperidinyl,(b) pyrrolidinyl,(c) piperazinyl,(d) morpholinyl,(e) thiomorpholino,(f) histaminyl,(g) 3-aminomethyl pyridinyl, and(19) hydroxy substituted alkylamino;X and Y are independently hydrogen, halogen, trifluoromethyl, alkyl, nitro, alkoxy, or cyano;n is 0, 1, or 2;R.sup.4 is ##STR2## M+ is hydrogen, ammonium, or an alkali metal.

42. 发明授权

US4970221A 3,5-dihydroxypentanoic acid derivatives useful as antihypercholesterolemic agents and method for preparing same 失效
标题翻译：可用作抗高血胆固醇药的3,5-二羟基戊酸衍生物及其制备方法
公开(公告)号：US4970221A
公开(公告)日：1990-11-13
申请号：US386162
申请日：1989-07-28
申请人： David R. Magnin , Eric M. Gordon
发明人： David R. Magnin , Eric M. Gordon
IPC分类号： C12N9/99 , A61K31/425 , A61K31/426 , A61P3/06 , A61P9/10 , A61P43/00 , C07D277/04 , C07D277/06 , C07D409/06 , C07D417/06
CPC分类号： C07D417/06 , C07D277/06
摘要： 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl;X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.

43. 发明授权

US4889874A Hydroxamic acid derivatives and method of using same 失效
标题翻译：羟肟酸衍生物及其使用方法
公开(公告)号：US4889874A
公开(公告)日：1989-12-26
申请号：US183406
申请日：1988-03-14
申请人： Martin F. Haslanger , Eric M. Gordon
发明人： Martin F. Haslanger , Eric M. Gordon
IPC分类号： A61K31/16
CPC分类号： A61K31/16
摘要： In accordance with the present invention, new hydroxamic acid derivatives useful as .DELTA..sup.5 -lipoxygenase inhibitors are provided. These new compounds have the general formula ##STR1## wherein ##STR2## are cycloalkyl groups which may be the same or different; R is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl or aralkyl; n is an integer from 3 to 12; and m is an integer from 3 to 12. Further in accordance with the present invention, a method for using the above compounds is provided.
摘要翻译：根据本发明，提供了用作DELTA5-脂肪氧合酶抑制剂的新的异羟肟酸衍生物。这些新化合物具有通式，其中是可以相同或不同的环烷基; R为氢，低级烷基，芳基，低级烯基，环烷基或芳烷基; n为3〜12的整数， m为3〜12的整数。此外，根据本发明，提供了使用上述化合物的方法。

44. 发明授权

US4711900A Certain arylalkyl or pyridylalkyl hydroxamates useful for treating allergies and asthma 失效
标题翻译：某些用于治疗过敏和哮喘的芳基烷基或吡啶基烷基异羟肟酸盐
公开(公告)号：US4711900A
公开(公告)日：1987-12-08
申请号：US888616
申请日：1986-07-23
申请人： Ravi K. Varma , Eric M. Gordon
发明人： Ravi K. Varma , Eric M. Gordon
IPC分类号： C07C69/76 , C07D213/56 , C07C83/10 , A61K31/235 , A61K31/44 , C07D213/64
CPC分类号： C07D213/56 , C07C69/76
摘要： Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; and ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
摘要翻译：提供了具有结构的芳基羟基化合物，其中R 1是氢，低级烷基，芳基，低级烯基，环烷基或芳烷基; R2是氢，低级烷基，芳基，环烷基，烷酰基或芳酰基; m为2〜8; 和其中R 3是OH，COOH的化合物这些化合物可用作DELTA5-脂肪氧合酶的抑制剂，因此可用作抗过敏剂。

45. 发明授权

US4681937A 3-acylamino-2-oxo-1-azetidinyl esters of phosphonic acids, phosphoric acid and phosphoric acid esters 失效
标题翻译：膦酸，磷酸和磷酸酯的3-酰基氨基-2-氧代-1-氮杂环丁烷基酯
公开(公告)号：US4681937A
公开(公告)日：1987-07-21
申请号：US424132
申请日：1982-09-27
申请人： William A. Slusarchyk , Tamara Dejneka , William H. Koster , Eric M. Gordon
发明人： William A. Slusarchyk , Tamara Dejneka , William H. Koster , Eric M. Gordon
IPC分类号： C07D205/08 , A61K31/675 , A61P31/04 , C07D205/085 , C07F9/568 , C07F9/6561 , C07F9/65
CPC分类号： C07D205/085 , C07F9/5683
摘要： Antimicrobial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position, or a pharmaceutically acceptable salt thereof; wherein Y is oxygen or sulfur and R.sub.5 is hydroxyl, alkyl, substituted alkyl, phenyl, substituted phenyl, alkoxy, alkylthio, (substituted alkyl)oxy, (substituted alkyl)thio, phenyloxy, phenylthio, (substituted phenyl)oxy or (substituted phenyl)thio.
摘要翻译：抗体活性由1位具有取代基和3位酰基氨基取代基的β-内酰胺或其药学上可接受的盐显示出来; 其中Y是氧或硫，R5是羟基，烷基，取代的烷基，苯基，取代的苯基，烷氧基，烷硫基，（取代的烷基）氧基，（取代的烷基）硫代，苯氧基，苯硫基，（取代的苯基）氧基或（取代的苯基）硫代。

46. 发明授权

US4672075A 7-Oxabicyclo(2.2.1)heptane hydroxamic acid derivatives useful as antiinflammatory, antiasthma and antipsoriatic agents 失效
标题翻译：可用作抗炎，抗哮喘和抗牛皮癣药的7-氧杂双环（2.2.1）庚烷异羟肟酸衍生物
公开(公告)号：US4672075A
公开(公告)日：1987-06-09
申请号：US900565
申请日：1986-08-26
申请人： Eric M. Gordon , Ravi K. Varma
发明人： Eric M. Gordon , Ravi K. Varma
IPC分类号： A61K31/34 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicyclo(2.2.1)heptane hydroxamic acid derivatives are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or alkenyl; R.sub.2 is hydrogen, lower alkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; and n is an integer from 0 to 9, with the proviso that when A is a single bond, n is an integer from 1 to 9; and including all stereoisomers and pharmaceutically acceptable salts thereof.These new compounds have been found to simultaneously inhibit the arachidonic acid enzymes cyclooxygenase and 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
摘要翻译：公开了具有通式“IMAGE”的7-氧杂二环（2.2.1）庚烷异羟肟酸衍生物，其中R 1是氢，低级烷基，芳基，芳烷基或烯基; R2是氢，低级烷基，烷酰基或芳酰基; R3是低级烷基，烯基或炔基; A是-CH 2 -CH = CH-或单键; 且n为0至9的整数，条件是当A为单键时，n为1至9的整数; 并且包括其所有立体异构体及其药学上可接受的盐。已经发现这些新化合物同时抑制花生四烯酸酶环加氧酶和5-脂氧合酶，因此可用作抗炎，抗哮喘和抗牛皮癣药。

47. 发明授权

US4642315A Carboxy and substituted carboxy alkanoyl and cycloalkanoyl peptides 失效
标题翻译：羧基和取代的羧基烷酰基和环烷酰基肽
公开(公告)号：US4642315A
公开(公告)日：1987-02-10
申请号：US663723
申请日：1984-10-22
申请人： Eric M. Gordon , Harold N. Weller, III
发明人： Eric M. Gordon , Harold N. Weller, III
IPC分类号： A61K38/00 , C07C61/39 , C07D217/26 , C07D263/42 , C07D311/00 , C07K5/072 , C07K5/078 , A61K31/475 , A61K31/47 , C07D217/16
CPC分类号： C07D311/00 , C07C61/39 , C07D217/26 , C07D263/42 , C07K5/06095 , C07K5/06156 , A61K38/00
摘要： Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.
摘要翻译：其中X是各种氨基或亚氨基酸或酯的式“IMAGE”的肽可用作降压剂。

48. 发明授权

US4636522A Acylaminoalkanoyl urethanes or thiourethanes 失效
标题翻译：酰氨基烷酰基氨基甲酸酯或硫代氨基甲酸酯
公开(公告)号：US4636522A
公开(公告)日：1987-01-13
申请号：US715217
申请日：1985-03-22
申请人： Eric M. Gordon
发明人： Eric M. Gordon
IPC分类号： C07D205/04 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/27 , A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/472 , A61K38/55 , A61P9/12 , A61P25/04 , A61P43/00 , C07C67/00 , C07C239/00 , C07C271/08 , C07C313/00 , C07C323/59 , C07C325/00 , C07C333/04 , C07D207/16 , C07D207/22 , C07D209/02 , C07D209/42 , C07D213/53 , C07D213/81 , C07D217/26 , C07D231/06 , C07D233/64 , C07D277/06 , C07D333/00 , C07D333/22 , C07D339/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D487/04 , C07D495/10 , C12N9/99 , C07D207/04 , A61K31/34 , A61K31/38
CPC分类号： C07D213/53 , C07D207/16 , C07D209/42 , C07D213/81 , C07D217/26 , C07D231/06 , C07D277/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D495/10
摘要： Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
摘要翻译：公开了其中Z是氧或硫的式“IMAGE”的化合物。这些化合物由于其血管紧张素转换酶抑制活性而可用作降压剂，并且取决于X的定义，由于其脑啡肽酶抑制活性也可用作镇痛药。

49. 发明授权

US4552866A Use of diamino alcohols as analgesic agents 失效
标题翻译：二氨基醇用作止痛剂
公开(公告)号：US4552866A
公开(公告)日：1985-11-12
申请号：US628004
申请日：1984-07-05
申请人： Norma G. Delaney , Eric M. Gordon
发明人： Norma G. Delaney , Eric M. Gordon
IPC分类号： A61K38/00 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/083 , A61K37/00
CPC分类号： C07K5/0808 , C07K5/06026 , C07K5/06043 , C07K5/06078 , A61K38/00
摘要： An enkephalin-degrading aminopeptidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.5 each is independently glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, or prolyl, norleucyl, or norvalyl; andn.sub.1, n.sub.2, n.sub.3, n.sub.4 and n.sub.5 each is independently 0 or 1.
摘要翻译：脑啡肽降解氨基肽酶被具有式（IMA）> TR（A1）n1（A2）n2（A3）n3（A4）n4（A5）n5R3的化合物及其药学上可接受的盐抑制，其中R1和R2是烷基，羧基烷基，卤素取代的烷基，羟基烷基，氨基烷基，巯基烷基，烷硫基烷基，（环烷基）烷基，（杂芳基）烷基，芳基烷基，氨基甲酰基烷基，胍基烷基或杂芳基; R3是羟基，烷氧基，（取代的烷基）氧基，芳基烷氧基，（杂芳基）烷氧基或-NY1Y2，其中Y1和Y2各自独立地是氢，烷基，芳基或芳烷基或Y1是氢，Y2是取代的烷基或（杂芳基）烷基; A1是甘氨酰基，丙氨酰基，亮氨酰基，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺基，赖氨酰，谷氨酰，组氨酸，色氨酸，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰，脯氨酰，其中n6为2至15的整数; A2，A3，A4和A5各自独立地是甘氨酰，丙氨酰，亮氨酰，苯丙氨酰，精氨酰，肌氨酰，丝氨酰，天冬酰胺酰基，赖氨酰，谷氨酰，组氨酸，色氨酰，半胱氨酰，甲硫氨酰，苏氨酰，酪氨酰，亮氨酰，缬氨酰，天冬氨酰或脯氨酰，正亮酰基或诺瓦尔基; n1，n2，n3，n4和n5各自独立地为0或1。

50. 发明授权

US4533660A Antibacterial O-sulfated .beta.-lactam hydroxamic acids 失效
标题翻译：抗菌O-硫酸化β-内酰胺异羟肟酸
公开(公告)号：US4533660A
公开(公告)日：1985-08-06
申请号：US320407
申请日：1981-11-12
申请人： Eric M. Gordon , Miguel A. Ondetti
发明人： Eric M. Gordon , Miguel A. Ondetti
IPC分类号： C07D205/085 , C07D205/08 , A61K31/395
CPC分类号： C07D205/085
摘要： Antibacterial activity is exhibited by .beta.-lactams having a sulfate substituent in the 1-position and an acylamino substituent in the 3-position.
摘要翻译：在1-位具有硫酸酯取代基和3-位酰基氨基取代基的β-内酰胺显示出抗菌活性。

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