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    Antibacterial agents
    1.
    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

    申请人： 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

    发明人： 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分类号： C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/517 ,  A61K31/536

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： 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.

    Cytokine production and tyrosine kinase inhibitors
    3.
    发明授权
    Cytokine production and tyrosine kinase inhibitors 失效
    细胞因子生成和酪氨酸激酶抑制剂

    公开(公告)号：US06518316B1

    公开(公告)日：2003-02-11

    申请号：US09743284

    申请日：2001-03-27

    申请人： Roya Mansour Sadeghi Guilani ,  Stephen Keith Wrigley ,  Sangeeta Bahl ,  Steven Michael Martin ,  David Andrew Kau ,  Jenny Seugkin Tang ,  Michael Moore ,  David James Hardick

    发明人： Roya Mansour Sadeghi Guilani ,  Stephen Keith Wrigley ,  Sangeeta Bahl ,  Steven Michael Martin ,  David Andrew Kau ,  Jenny Seugkin Tang ,  Michael Moore ,  David James Hardick

    IPC分类号： A61K3112

    CPC分类号： C12R1/645 ,  C07C43/196 ,  C07C49/753 ,  C07C217/52 ,  C07C251/44 ,  C07C2603/90 ,  C07D303/32 ,  C12P15/00

    摘要： A compound of formula (I), wherein &agr;X is ═O, ═N—OR6, &bgr;NHR or &bgr;OH wherein R6 is H or C1-C6 alkyl, bond a is oriented &ggr; or &dgr; and R is H, C1-C6 alkyl which is unsubstituted or substituted by C6-C10 aryl, or C3-C6 cycloalkyl; &egr; is a bond when &zgr; and &eegr; are not bonds or, when X is ═O, &zgr; and &eegr; are both bonds and &egr; is not a bond; R1 and R2, which are the same or different, are H or a halogen; R3 and R4, which are the same or different, are H, C1-C6 alkyl, C3-C6 cycloalkyl, a heterocyclic group or an aromatic group; bond e is oriented &ggr; or &dgr;; and R5 is C1-C6 alkyl; or formula (Ib), or formula (II), or formula (III), has activity as a cytokine production inhibitor and an inhibitor and an inhibitor of tyrosine kinase. A process for producing some of the compounds from a fungal strain, processes for producing synthetic analogues from these compounds and the use of the compounds in treating immunoinflammatory and cancerous conditions are also described.

    摘要翻译： 式（I）化合物，其中αX为= O，= N-OR6，βNHR或βOH，其中R6为H或C1-C6烷基，键a为取向的γ或δ，R为H，C 1 -C 6烷基为 未取代或被C 6 -C 10芳基或C 3 -C 6环烷基取代; 当zeta和eta不是键时，epsi是一个键，或当X = O时，zeta和eta都是键，而epsi不是键; R 1和R 2相同或不同，为H或卤素; R 3和R 4相同或不同，为H，C 1 -C 6烷基，C 3 -C 6环烷基，杂环基或芳基; 键e是取向的γ或δ; R5是C1-C6烷基; 或式（Ib）或式（II）或式（III））具有作为细胞因子产生抑制剂和抑制剂和酪氨酸激酶抑制剂的活性。 还描述了从真菌菌株产生一些化合物的方法，从这些化合物制备合成类似物的方法以及该化合物在治疗免疫炎症和癌症病症中的用途。