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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.

    Method of neutralising organoboronates with acids
    2.
    发明申请
    Method of neutralising organoboronates with acids 审中-公开
    用酸中和有机硼酸盐的方法

    公开(公告)号：US20060172978A1

    公开(公告)日：2006-08-03

    申请号：US11292419

    申请日：2005-11-30

    申请人： Vincent Russell ,  Suresh Chahwala ,  Shouming Wang

    发明人： Vincent Russell ,  Suresh Chahwala ,  Shouming Wang

    IPC分类号： A61K31/66 ,  A61K31/202 ,  A61K31/185

    CPC分类号： A61K31/185 ,  A61K31/202 ,  A61K31/66

    摘要： The use of specified compounds for the manufacture of a medicament for therapeutically neutralising an organoboronate drug. The specified compounds are typically hydroxy fatty acids or hydroperoxy fatty acids, for example 9(S)-HODE, 8(S)-HETRE or 8(S)-HEPE, or their salts or prodrugs. The organoboronate drug may be TRI 50c or a salt or prodrug thereof. Also disclosed are intravenous formulations containing the specified compounds.

    摘要翻译： 使用指定的化合物来制造用于治疗中和有机硼酸盐药物的药物。 指定的化合物通常是羟基脂肪酸或氢过氧脂肪酸，例如9（S）-HODE，8（S）-HETRE或8（S）-HEPE，或其盐或前药。 有机硼酸盐药物可以是TRI 50c或其盐或前药。 还公开了含有特定化合物的静脉内制剂。

    METHOD OF NEUTRALISING ORGANOBORONATES WITH ACIDS
    3.
    发明申请
    METHOD OF NEUTRALISING ORGANOBORONATES WITH ACIDS 审中-公开
    将酸性有机酸与中性酸中和的方法

    公开(公告)号：US20100022646A1

    公开(公告)日：2010-01-28

    申请号：US12399289

    申请日：2009-03-06

    申请人： Vincent Patric Russel ,  Suresh Babubhai Chahwala ,  Shouming Wang

    发明人： Vincent Patric Russel ,  Suresh Babubhai Chahwala ,  Shouming Wang

    IPC分类号： A61K31/20

    CPC分类号： A61K31/185 ,  A61K31/202 ,  A61K31/66

    摘要： The use of specified compounds for the manufacture of a medicament for therapeutically neutralising an organoboronate drug. The specified compounds are typically hydroxy fatty acids or hydroperoxy fatty acids, for example 9(S)-HODE, 8(S)-HETRE or 8(S)-HEPE, or their salts or prodrugs. The organoboronate drug may be TRI 50c or a salt or prodrug thereof. Also disclosed are intravenous formulations containing the specified compounds.

    摘要翻译： 使用指定的化合物来制造用于治疗中和有机硼酸盐药物的药物。 指定的化合物通常是羟基脂肪酸或氢过氧脂肪酸，例如9（S）-HODE，8（S）-HETRE或8（S）-HEPE，或其盐或前药。 有机硼酸盐药物可以是TRI 50c或其盐或前药。 还公开了含有特定化合物的静脉内制剂。

    Boronic acid thrombin inhibitors
    6.
    发明申请
    Boronic acid thrombin inhibitors 审中-公开
    硼酸凝血酶抑制剂

    公开(公告)号：US20070185060A1

    公开(公告)日：2007-08-09

    申请号：US10591868

    申请日：2005-03-09

    申请人： Shouming Wang

    发明人： Shouming Wang

    IPC分类号： A61K31/69 ,  C07F5/02

    CPC分类号： C07F5/025 ,  Y02P20/55

    摘要： A thrombin inhibitor selected from boronic acids of formula (I), and salts, prodrugs and prodrug salts thereof: wherein X is H (to form NH2) or an amino-protecting group; aa1 is an amino acid residue having a side chain selected from formula (A) and (B)—(CO)a—(CH2)b-Dc-(CH2)d-E (A), —(CO)a—(CH2)b-Dc-Ce(E1)(E2)(E3) wherein E1, E2 and E3 are 5-6 membered saturated or unsaturated hydrocarbyl rings, or one of E1, E2 and E3 is hydrogen and the other two are a said hydrocarbyl ring, E, E1, E2 and E3 optionally being halogenated when saturated and mandatorily being halogenated when unsaturated, a particular halogen being fluorine; aa2 is a residue of an amino acid which binds to the thrombin S2 subsite; and R9 is a straight chain alkyl group interrupted by one or more ether linkages or R9 is —(CH2)mW and W is —OH or halogen.

    摘要翻译： 选自式（I）的硼酸的凝血酶抑制剂及其盐，前药和前药盐：其中X是H（以形成NH 2）或氨基保护基; aa <1>是具有选自式（A）和（B） - （CO）的侧链的氨基酸残基（CH 2/2） - （CH 2） - （CO） - （CO） - （CH 2） （CH 2 - ） - （CH 2） - - - - （C 2 -C 6） （E 2）（E 3）其中E 1，E 2，...，SUP >和E 3是5-6元饱和或不饱和烃基环，或者是E 1，E 2和E 3中的一个 其中H是氢，另外两个是烃基环，E，E 1，E 2和E 3任选被卤代 当饱和并且当不饱和时被强制卤化，特定的卤素是氟; α2是与凝血酶S2亚位点结合的氨基酸残基; R 9是被一个或多个醚键间隔的直链烷基，或者R 9是 - （CH 2）m W且W是-OH或卤素。

    Pharmaceutical compounds
    7.
    发明授权
    Pharmaceutical compounds 失效

    公开(公告)号：US07132419B2

    公开(公告)日：2006-11-07

    申请号：US11024759

    申请日：2004-12-30

    申请人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Alexander Denny

    发明人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Alexander Denny

    IPC分类号： C07D241/46 ,  A61K31/498

    CPC分类号： C07D403/12 ,  C07D241/46

    摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; R11 is C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1–C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

    Pharmaceutical compounds
    8.
    发明申请
    Pharmaceutical compounds 失效

    公开(公告)号：US20050143383A1

    公开(公告)日：2005-06-30

    申请号：US11024759

    申请日：2004-12-30

    申请人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Denny

    发明人： John Milton ,  Nigel Vicker ,  Adrian Folkes ,  Shouming Wang ,  William Denny

    IPC分类号： C07D241/46 ,  C07D403/12 ,  A61K31/498 ,  C07D241/36

    CPC分类号： C07D403/12 ,  C07D241/46

    摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R2)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (II) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; R11 is C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1-C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.