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    ANTIBACTERIAL 1-(4-MONO- AND DI-HALOMETHYLSULPHONYLPHENYL)-2-ACYLAMINO-3-FLUOROPROPONALS AND PREPARATION THEREOF
    4.
    发明申请
    ANTIBACTERIAL 1-(4-MONO- AND DI-HALOMETHYLSULPHONYLPHENYL)-2-ACYLAMINO-3-FLUOROPROPONALS AND PREPARATION THEREOF 失效
    抗真菌剂1-（4-单 - 和对 - 二甲基磺酰基苯基）-2-亚氨基-3-氟代丙烯酸酯及其制备方法

    公开(公告)号：US20080146527A1

    公开(公告)日：2008-06-19

    申请号：US12038105

    申请日：2008-02-27

    Applicant: Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    Inventor： Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    IPC: A61K31/165 ,  C07F9/09 ,  A61K31/661 ,  A61P31/04

    CPC classification number: C07F9/094 ,  A61K31/165 ,  A61K31/661 ,  C07C317/32 ,  C07F9/091 ,  Y02A50/475

    Abstract: Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

    Abstract translation: 具有化学结构的新型氟苯尼考化合物：或其药学上可接受的盐或其溶剂化物或其前药，其中R 1是CHCl 2，CHClF，CHF CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 3 CH （R 2）NH 2或CH X 1 X 2 2; 其中R 2是H，CH 3或CH 2 OH，X 1和X 2 是独立选择的卤素; 和R 3是CH 2 CH 2，CH 2 F，CHF 2，CHCl 2， SUB或CH 2 OH。 该化合物可用于治疗和/或预防广泛范围的患者中的细菌感染，例如但不限于鸟类，鱼类，贝类和哺乳动物。

    Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors
    7.
    发明授权
    Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors 失效
    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

    Applicant: Rajeshwar Singh ,  Nian Zhou ,  Deqi Guo ,  Ronald G. Micetich

    Inventor： Rajeshwar Singh ,  Nian Zhou ,  Deqi Guo ,  Ronald G. Micetich

    IPC: C07D49940

    CPC classification number: C07D499/00 ,  C07D501/00

    Abstract: 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.

    Abstract translation: 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。

    Antibacterial agents
    8.
    发明授权
    Antibacterial agents 失效

    公开(公告)号：US6057315A

    公开(公告)日：2000-05-02

    申请号：US269492

    申请日：1999-03-29

    Applicant: John Michael Domagala ,  Edmund Lee Ellsworth ,  Michael Andrew Stier ,  Liren Huang ,  Ronald George Micetich ,  Rajeshwar Singh ,  Stephen Keith Wrigley ,  Shouming Wang ,  Michael Roe ,  David Michael Thornton

    Inventor： John Michael Domagala ,  Edmund Lee Ellsworth ,  Michael Andrew Stier ,  Liren Huang ,  Ronald George Micetich ,  Rajeshwar Singh ,  Stephen Keith Wrigley ,  Shouming Wang ,  Michael Roe ,  David Michael Thornton

    IPC: C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/517 ,  A61K31/536

    CPC classification number: C07D487/04 ,  C07D513/04

    Abstract: Described are antibacterial agents of formula (I): X is O, S or N--R.sub.8 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, R heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, CO.sub.2 R, COR, CON(R).sub.2, CON(R").sub.2, SR, SON, SCO.sub.2 R or SCON(R).sub.2 ; R.sub.4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, NO.sub.2, N(R).sub.2, NRCOR, NRCOR", COR, CO.sub.2 R, CON(R).sub.2, CON(R").sub.2, NRCON(R).sub.2, NRCO.sub.2 R; R.sub.5 is 1-6 straight or branched alkyl, a cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, OR, N(R).sub.2, NRCOR, NRCOR", COR, CON(R).sub.2, CON(R").sub.2, SR or SO.sub.2 R; R.sub.6, R.sub.7 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, COR, COR", SO.sub.2 NR.sub.2, CONR.sub.2 and these may be optionally substituted by any of the groups listed for R.sub.5 ; R is H, straight or branched alkyl of 1-6 carbon atoms, cycloalkyl of from 3-6 carbon atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or pheny, all of which may be optionally substituted by halogen, OR', NR'.sub.2, NR'COR', CN, CO.sub.2 R', CONR'.sub.2, R' is H, alkyl of from 1-3 carbon atoms or Ph; R" is part of a naturally occurring amino acid connected via an amide or acyl bond as determined by the formula; halogen is any one of fluoro, chloro, bromo or iodo; or a pharmaceutically acceptable salt.

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