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11. 发明授权

US4057540A 4-Chloroazetidinone-1-(2',3'-dichloroisopropyl) acetates and process for preparing same 失效
标题翻译： 4-氯氮杂环丁酮-1-（2 {40,3 {40-二氯异丙基）乙酸酯及其制备方法
公开(公告)号：US4057540A
公开(公告)日：1977-11-08
申请号：US667825
申请日：1976-03-17
申请人： Ronald G. Micetich , Robert B. Morin , Kenneth E. Wilson
发明人： Ronald G. Micetich , Robert B. Morin , Kenneth E. Wilson
IPC分类号： C07D205/08 , C07D205/085 , C07D205/09 , C07D205/095 , C07D417/12 , C07D513/04
CPC分类号： C07D205/085 , C07D205/095
摘要： The invention relates to novel azetidinones of the general formula: ##STR1## wherein R stands for lower alkyl, phenyl, phenyloxyloweralkyl, phenylloweralkyl, 2-thiophenemethyl, 5-tetrazolylmethyl, R.sup.3 O--and R.sup.3 S--, wherein R.sup.3 stands for lower alkyl, phenyl or phenylloweralkyl; R.sup.1 is hydrogen or a cleavable radical selected from lower alkyl; loweralkoxymethyl, 2,2,2-trichloroethyl, benzyl, p-halobenzyl, p-nitrobenzyl and p-methoxybenzyl, benzhydryl and trimethylsilyl; R.sup.2 is hydrogen or methoxy; X is SCl, Sbr or --OH in which case the C.sub.3 -sidechain is better represented as the amide RCONH-- group; Y is chloro or bromo; and ##STR2## may also be taken as phthalimido. These novel compounds possess antibacterial activity and are useful intermediates for the synthesis of modified penicillins and the analogues of penicillins.
摘要翻译：本发明涉及以下通式的新型氮杂环丁酮：其中R代表低级烷基，苯基，苯氧基低级烷基，苯基低级烷基，2-噻吩甲基，5-四唑基甲基，R3O-和R3S-，其中R3代表低级烷基，苯基或苯基低级烷基; R1是氢或可以选自低级烷基的可裂解基; 低级烷氧基甲基，2,2,2-三氯乙基，苄基，对卤代苄基，对硝基苄基和对甲氧基苄基，二苯甲基和三甲基甲硅烷基; R2是氢或甲氧基; X是SCl，Sbr或-OH，在这种情况下，C3侧链更好地表示为酰胺RCONH-基团; Y是氯或溴; 也可以将作为邻苯二甲酰亚氨基。

12. 发明授权

US06232305B1 Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors 失效
标题翻译：取代的氨基双环β-内酰胺penam和cepham衍生物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US06232305B1
公开(公告)日：2001-05-15
申请号：US09010993
申请日：1998-01-22
申请人： Rajeshwar Singh , Nian Zhou , Deqi Guo , Ronald G. Micetich
发明人： Rajeshwar Singh , Nian Zhou , Deqi Guo , Ronald G. Micetich
IPC分类号： C07D49940
CPC分类号： C07D499/00 , C07D501/00
摘要： The present invention provides substituted amino bicyclic-&bgr;-lactam penam derivatives and substituted amino bicyclic-&bgr;-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis. muscular dystrophy, myocardial infarction, pulmonary emphysema, septic shock, cerebral ischemia, decreased memory function, Alzheimer, cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections and viral infections, wherein R is a peptidyl residue of a single natural &agr;-amino acid selected from a specific group of natural &agr;-amino acids or a peptidyl residue of a single non-natural amino acid selected from a specified group of non-natural amino acids, in which natural or non-natural peptidyl residue the terminal —NH2 group is unsubstituted or substituted once or twice with group R4, wherein R4 is selected from the group consisting of —COOR5, —COR5, —SO2R5, and —COR6, R6 is an amino group which is unsubstituted or substituted at least once with a C1-C6 alkyl group which is unsubstituted or substituted, R1 is selected from the group consisting of hydrogen, hydroxy, carboxy, —COOR6, —OR7, —CONHR7, and C1-C5 alkyl, in which the C1-C6 alkyl is unsubstituted or substituted, R2 and R3 are independently hydrogen or C1-C3 alkyl which is unsubstituted or substituted, n is 0, 1, or 2, and n1 is 0 or 1.
摘要翻译：本发明提供了取代的氨基双环β-内酰胺penam衍生物和取代的氨基双环-β-内酰胺头孢烯衍生物及其非对映异构体I，以及组合物，制备方法和使用方法，其表现出优异的半胱氨酸蛋白酶抑制活性，其可用于治疗诸如癌症（包括癌症转移），骨质疏松症，类风湿性关节炎等不同疾病。肌肉营养不良，心肌梗死，肺气肿，败血性休克，脑缺血，记忆功能下降，阿尔茨海默病，白内障，疟疾，肾小球基底膜降解，细菌感染，炎症性疾病，寄生虫感染和病毒感染，其中R是单一肽的肽基残基选自特定天然α-氨基酸组的天然α-氨基酸或选自特定非天然氨基酸组的单一非天然氨基酸的肽基残基，其中天然或非天然肽基残基末端-NH 2基团是未取代的或被基团R4取代一次或两次，其中R 4选自-COOR 5，-COR 5，-SO 2 R 5和-COR 6，R 6是未被取代或取代至少一次的氨基与未取代或取代的C1-C6烷基，R1选自氢，羟基，羧基，-COOR6，-OR7，-CONHR7和C1-C5烷基，其中 C 1 -C 6烷基是未取代或取代的，R 2和R 3独立地是氢或未被取代或取代的C 1 -C 3烷基，n是0,1或2，且n 1是0或1。

13. 发明授权

US5959123A 3,4-Disubstituted azetidin-2-one derivatives useful as cysteine proteinase regulators 失效
标题翻译：可用作半胱氨酸蛋白酶调节剂的3,4-二取代氮杂环丁-2-酮衍生物
公开(公告)号：US5959123A
公开(公告)日：1999-09-28
申请号：US935258
申请日：1997-09-22
申请人： Rajeshwar Singh , Nian E. Zhou , Deqi Guo , Ronald G. Micetich
发明人： Rajeshwar Singh , Nian E. Zhou , Deqi Guo , Ronald G. Micetich
IPC分类号： A61K38/00 , A61P3/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/00 , A61P27/12 , A61P29/00 , A61P31/12 , A61P33/00 , A61P33/06 , A61P35/04 , C07D205/085 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/08 , C07D205/00
CPC分类号： C07D401/12 , C07D205/085 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention is based on the discovery that certain 3,4-disubstituted-azetidin-2-one derivatives exhibit excellent cysteine proteinase inhibitory activity which can be used for treatment of different diseases such as muscular dystrophy, myocardial infarction, bone resorption, arthritis, cancer metastasis, pulmonary emphysema, septic shock, cerebral ischemia, memory function, Alzheimer and cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections, and viral infections. In accordance to the present invention, there is provided a 3,4-disubstituted-azetidin-2-one derivatives of formula I, wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or a pharmaceutically acceptable salt thereof. ##STR1##
摘要翻译：本发明基于以下发现：某些3,4-二取代 - 氮杂环丁-2-酮衍生物显示出优异的半胱氨酸蛋白酶抑制活性，其可用于治疗不同疾病如肌营养不良，心肌梗塞，骨吸收，关节炎，癌症转移，肺气肿，败血性休克，脑缺血，记忆功能，阿尔茨海默病和白内障，疟疾，肾小球基底膜降解，细菌感染，炎性疾病，寄生虫感染和病毒感染。根据本发明，提供式I的3,4-二取代 - 氮杂环丁-2-酮衍生物，其中R 1，R 2和R 3如本文所定义，或其药学上可接受的盐。

14. 发明授权

US5916887A 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives as cysteine proteinase regulators 失效
公开(公告)号：US5916887A
公开(公告)日：1999-06-29
申请号：US935259
申请日：1997-09-22
申请人： Rajeshwar Singh , Nian E. Zhou , Enrico O. Purisima , Ronald G. Micetich
发明人： Rajeshwar Singh , Nian E. Zhou , Enrico O. Purisima , Ronald G. Micetich
IPC分类号： A61K38/55 , A61K31/00 , A61K38/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/12 , A61P29/00 , A61P31/04 , A61P31/10 , A61P33/00 , A61P33/06 , A61P35/00 , A61P43/00 , C07K5/06 , C07K5/065 , A61K31/395 , C07D205/085 , C07D205/095
CPC分类号： C07K5/06078 , A61K31/00 , A61K38/00
摘要： In accordance with the present invention, there are provided 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives of the formula: ##STR1## wherein n is 1, 2 or 3; in which R.sub.1, R.sub.2 and R.sub.3 are as defined herein, and salts thereof, which exhibit excellent cysteine proteinase inhibitory activity and which can be used for treatment of different diseases such as muscular dystrophy, myocardial infarction, bone resorption, arthritis, cancer metastasis, pulmonary emphysema, septic shock, cerebral ischemia, memory function, Alzheimer and cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections, and viral infections.

15. 发明授权

US5527920A Economical manufacturing process for 1,2,3-triazoles 失效
标题翻译： 1,2,3-三唑的经济制造工艺
公开(公告)号：US5527920A
公开(公告)日：1996-06-18
申请号：US344586
申请日：1994-11-18
申请人： Inder P. Singh , Paul Spevak , Bhupinder Palak , Samuel Amedjo , Ronald G. Micetich
发明人： Inder P. Singh , Paul Spevak , Bhupinder Palak , Samuel Amedjo , Ronald G. Micetich
IPC分类号： C07D249/04 , C07D249/06
CPC分类号： C07D249/06
摘要： A high quality 1,2,3-triazole is obtained in a one pot two step reaction between appropriately substituted hydrazide derivatives, dihaloethanediol and NH.sub.3 in methanol. Synthesis of various N.sub.1 -alkyl, N.sub.1 -aryl, and N.sub.1 -heterocyclic-1,2,3-triazoles is also accomplished following the same general procedure.
摘要翻译：在适当取代的酰肼衍生物，二卤代乙二醇和NH 3在甲醇中的一锅二步反应中获得高质量的1,2,3-三唑。各种N1-烷基，N1-芳基和N1-杂环-1,2,3-三唑的合成也按照相同的一般方法进行。

16. 发明授权

US5342846A 7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid compounds and 7-(substituted triazolyl pyrrolidin-1-yl) 4-oxoquinoline-3-carboxylic acid derivatives useful as antibacterial agents 失效
标题翻译： 7-取代-6-氟-1,4-二氢-4-氧代 - 喹啉-3-羧酸化合物和可用作抗菌剂的7-（取代三唑基吡咯烷-1-基）-4-氧代喹啉-3-羧酸衍生物
公开(公告)号：US5342846A
公开(公告)日：1994-08-30
申请号：US913505
申请日：1992-07-14
申请人： Rajeshwar Singh , Rakhshandeh Fathi-Afshar , Inder P. Singh , George Thomas , Thomas R. Doerksen , Maya P. Singh , Ronald G. Micetich
发明人： Rajeshwar Singh , Rakhshandeh Fathi-Afshar , Inder P. Singh , George Thomas , Thomas R. Doerksen , Maya P. Singh , Ronald G. Micetich
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/4427 , A61K31/445 , A61K31/4545 , A61K31/4709 , A61K31/5383 , A61P31/04 , C07D401/14 , C07D403/04 , C07D471/04 , C07D498/06 , C07D521/00 , A61K31/47
CPC分类号： C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04
摘要： Substituted quinoline compounds and intermediates thereto, processes for producing those compounds and intermediates, pharmaceutical compositions using those compounds, methods for treating bacterial infections using those compounds, and methods for disinfecting using those compounds.
摘要翻译：取代的喹啉化合物及其中间体，制备这些化合物和中间体的方法，使用这些化合物的药物组合物，使用这些化合物治疗细菌感染的方法，以及使用这些化合物进行消毒的方法。

17. 发明授权

US5051515A Novel generation of heteroaryl thio, sulfoxy, or sulfonyl alkyl azoles 失效
标题翻译：杂芳基硫代，亚磺酰基或磺酰基烷基唑的新一代
公开(公告)号：US5051515A
公开(公告)日：1991-09-24
申请号：US329040
申请日：1989-03-27
申请人： Mohsen Daneshtalab , Ronald G. Micetich , Dai Q. Nguyen , Chan M. Ha , Hiep T. Luu
发明人： Mohsen Daneshtalab , Ronald G. Micetich , Dai Q. Nguyen , Chan M. Ha , Hiep T. Luu
IPC分类号： C07D233/64 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/426 , A61P31/12 , C07D231/12 , C07D231/16 , C07D261/08 , C07D275/02 , C07D277/22 , C07D277/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07D231/16 , C07D233/56 , C07D249/08 , C07D261/08 , C07D275/02 , C07D277/22 , C07D277/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： There are provided compounds having the general formulae ##STR1## wherein R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a substituted, fused or non-fused azole moiety.These compounds have been demonstrated as having antipicornavirus activity.

18. 发明授权

US5026848A Novel generation of heteroaryloxyalkyl heterocycles with antipicornaviruses activities 失效
标题翻译：新一代具有反义核糖核酸活性的杂芳基烷基杂环
公开(公告)号：US5026848A
公开(公告)日：1991-06-25
申请号：US329147
申请日：1989-03-27
申请人： Mohsen Daneshtalab , Dai Q. Nguyen , Chan M. Ha , Hiep T. Luu , Laurence M. Tempest , Ronald G. Micetich
发明人： Mohsen Daneshtalab , Dai Q. Nguyen , Chan M. Ha , Hiep T. Luu , Laurence M. Tempest , Ronald G. Micetich
IPC分类号： C07D233/64 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/426 , A61P31/12 , C07D231/12 , C07D231/16 , C07D261/08 , C07D275/02 , C07D277/22 , C07D277/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07D231/16 , C07D233/56 , C07D249/08 , C07D261/08 , C07D275/02 , C07D277/22 , C07D277/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： A heteroaryloxyalkylheterocyclic derivative of the Formula I:R--(CH.sub.2).sub.n --O--R.sup.1 Iis provided wherein:R is a non-fused azole moiety;n is 5, 6, 7 or 8; andR.sup.1 is a non-fused or fused substituted azole, azine, furyl or polycyclic hydrocarbon.

19. 发明授权

US4496484A Penicillin derivatives 失效
标题翻译：青霉素衍生物
公开(公告)号：US4496484A
公开(公告)日：1985-01-29
申请号：US487557
申请日：1983-04-22
申请人： Ronald G. Micetich , Shigeru Yamabe , Shoji Hirata , Naobumi Ishida
发明人： Ronald G. Micetich , Shigeru Yamabe , Shoji Hirata , Naobumi Ishida
IPC分类号： C07D499/00 , A61K31/425
CPC分类号： C07D499/00
摘要： This invention provides a penicillin derivative of the formula and a salt thereof ##STR1## wherein X represents chlorine atom or bromine atom and R represents hydrogen atom or penicillin carboxy-protecting radical, and a process for preparing the derivative of the formula (I) and a salt thereof by reacting a compound of the formula ##STR2## wherein R is as defined above with a chlorinating reagent or brominating reagent and, when required, forming a salt thereof.
摘要翻译：本发明提供一种下式的青霉素衍生物及其盐，其中X表示氯原子或溴原子，R表示氢原子或青霉素羧基保护基，以及制备式（I）的衍生物的方法 I）化合物及其盐，其中R为如上定义的式的化合物与氯化试剂或溴化试剂反应，并且当需要时，形成其盐。

20. 发明授权

US6133485A Asymmetric synthesis of 2-(2,4-difluorophenyl)-1-heterocycl-1-yl butan-2,3-diols 失效
标题翻译： 2-（2,4-二氟苯基）-1-杂环-1-丁基-2,3-二醇的不对称合成
公开(公告)号：US6133485A
公开(公告)日：2000-10-17
申请号：US60138
申请日：1998-04-15
申请人： Inder Pal Singh , Inderjit Sidhu , Bhupinder Palak , Ronald G. Micetich
发明人： Inder Pal Singh , Inderjit Sidhu , Bhupinder Palak , Ronald G. Micetich
IPC分类号： C07B53/00 , C07B61/00 , C07C29/10 , C07C33/48 , C07C41/18 , C07C43/166 , C07D249/08 , C07D301/00 , C07D301/19 , C07D303/14 , C07D303/16 , C07D303/18 , C07D309/12 , C07D521/00 , C07C27/10
CPC分类号： C07D231/12 , C07C29/106 , C07C33/483 , C07D233/56 , C07D249/08 , C07D303/14 , C07D303/16 , C07D309/12 , C07B2200/07
摘要： The asymmetric production of pure diastereomeric (2R,3R), (2R,3S), (2S,3R) and (2S,3S)-2-aryl-1-substituted butan-2,3-diols from the derivatives of lactic acid.
摘要翻译：来自乳酸衍生物的纯非对映体（2R，3R），（2R，3S），（2S，3R）和（2S，3S）-2-芳基-1-取代的丁-2,3-二醇的不对称生产。

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