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公开(公告)号:US5744600A
公开(公告)日:1998-04-28
申请号:US357561
申请日:1994-12-16
IPC分类号: C07F9/6512 , A61K31/675 , C07F9/6561 , C07D473/18 , C07D473/34
CPC分类号: C07F9/65121
摘要: A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino; R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; and B is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio; and the pharmaceutically acceptable acid addition, metal, and amine salts thereof. The compositions of the invention are useful for, among other things, antiviral agents.
摘要翻译: 式I或式II的化合物其中R 1和R 2独立地是氢,羟基,氯,氟,溴或具有1至5个碳原子并且选自具有烃的酰氧基的有机取代基 1至4个碳原子的烷氧基,烷硫基,氨基,烷基氨基和二烷基氨基; R3和R4独立地是氢,或具有1至12个碳原子并且选自烷基,烯基,芳基和芳烷基的有机膦酸酯取代基; 并且B是选自嘧啶,嘌呤,三嗪,脱氮嘌呤和三唑的杂环基,其通过环氮原子连接,任选被1-3个选自羟基,巯基,氨基,肼基的取代基取代 ,氟,氯,溴,碘,C 1至C 3烷基,C 2 -C 3烯基,C 2 -C 3卤代烯基,C 1 -C 3烷氧基和C 1 -C 3烷硫基; 及其药学上可接受的酸加成盐,金属盐和胺盐。 本发明的组合物尤其可用于抗病毒剂。
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公开(公告)号:US5559108A
公开(公告)日:1996-09-24
申请号:US445628
申请日:1995-05-22
申请人: Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco, Jr. , John A. Wichtowski , Joanne J. Bronson , Stanley V. D'Andrea , Thomas W. Hudyma
发明人: Choung U. Kim , Muzammil M. Mansuri , Peter F. Misco, Jr. , John A. Wichtowski , Joanne J. Bronson , Stanley V. D'Andrea , Thomas W. Hudyma
IPC分类号: C07D501/40 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/44 , C07D501/46 , C07D501/38
CPC分类号: C07D501/00
摘要: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## where Ar is a substituted phenyl or optionally substituted naphthyl or benzthiazolyl group and A is a substituted-pyridinium group are gram-positive antibiotics, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
摘要翻译: 由通式“IMAGE”表示的新型头孢烯衍生物,其中酰基取代基是式IMAMA的基团,其中Ar是取代的苯基或任选被取代的萘基或苯并噻唑基,A是取代的吡啶鎓基是革兰氏阳性 抗生素,特别适用于治疗由耐甲氧西林金黄色葡萄球菌引起的疾病。
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公开(公告)号:US5391817A
公开(公告)日:1995-02-21
申请号:US171038
申请日:1993-12-21
IPC分类号: A61K31/19 , A61K31/215 , A61K31/235 , A61P29/00 , C07C43/215 , C07C43/225 , C07C43/23 , C07C45/67 , C07C45/70 , C07C45/71 , C07C47/57 , C07C47/575 , C07C59/72 , C07C63/331 , C07C63/49 , C07C63/66 , C07C63/74 , C07C65/24 , C07C65/26 , C07C65/28 , C07C65/34 , C07C69/00 , C07C69/017 , C07C69/65 , C07C69/73 , C07C69/732 , C07C69/734 , C07C69/76 , C07C69/94 , C07C205/56 , C07C233/65 , C07C309/65 , C07C317/44 , C07F9/38 , C07C59/40
CPC分类号: C07C309/65 , C07C43/215 , C07C43/225 , C07C43/23 , C07C45/673 , C07C45/70 , C07C45/71 , C07C47/57 , C07C47/575 , C07C59/72 , C07C63/49 , C07C63/66 , C07C65/24 , C07C65/26 , C07C65/28 , C07C69/00 , C07C69/017 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2102/10 , C07C2103/00 , C07C2103/74
摘要: Certain novel biaryl compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.
摘要翻译: 某些新型联芳化合物是有效的磷脂酶A2(PLA2)抑制剂。
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公开(公告)号:US5218106A
公开(公告)日:1993-06-08
申请号:US857850
申请日:1992-03-26
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
摘要: There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.
摘要翻译: 公开了新的2',3'-二脱氧-2'-氟核苷和2'-3'-二脱氧-2',3'-二脱氢-2'-氟核苷及其制备方法。 如此制备的化合物显示出治疗上有用的抗病毒,更具体地,抗HIV作用。
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公开(公告)号:US5733920A
公开(公告)日:1998-03-31
申请号:US551031
申请日:1995-10-31
IPC分类号: C07D311/30 , C07D405/04 , C07D405/14 , A61K31/44 , C07D405/02
CPC分类号: C07D405/04 , C07D311/30 , C07D405/14
摘要: The invention provides novel inhibitors of cyclin-dependent kinases, in particular inhibitors of the CDK/cyclin complexes such as CDK4/cyclin D1. The novel compounds are analogs of chromones. These compounds can be used for inhibiting excessive or abnormal cell proliferation. Thus, the novel compounds are useful for treating a subject with a disorder associated with excessive cell proliferation, such as cancer.
摘要翻译: 本发明提供细胞周期蛋白依赖性激酶的新型抑制剂,特别是CDK /细胞周期蛋白复合物例如CDK4 /细胞周期蛋白D1的抑制剂。 新化合物是色酮的类似物。 这些化合物可用于抑制细胞增殖过多或异常。 因此,新化合物可用于治疗与过度细胞增殖相关的疾病如癌症的受试者。
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公开(公告)号:US5436369A
公开(公告)日:1995-07-25
申请号:US200798
申请日:1994-02-23
申请人: Joanne J. Bronson , Katharine M. Greene , Muzammil M. Mansuri , Stanley V. D'Andrea , F. Ivy Carroll , Anita Lewin
发明人: Joanne J. Bronson , Katharine M. Greene , Muzammil M. Mansuri , Stanley V. D'Andrea , F. Ivy Carroll , Anita Lewin
IPC分类号: C07C69/612 , A61K31/19 , A61P29/00 , C07C63/66 , C07C67/30 , C07C69/00 , C07C69/618 , C07C69/65 , C07C69/734 , C07C69/76 , C07C69/94 , C07C63/64
CPC分类号: C07C63/66 , C07C69/618 , C07C69/65 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2103/74
摘要: Certain novel alicyclic compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.
摘要翻译: 某些新型脂环化合物是有效的磷脂酶A2(PLA2)抑制剂。
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公开(公告)号:US4904770A
公开(公告)日:1990-02-27
申请号:US173473
申请日:1988-03-24
申请人: John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
发明人: John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
IPC分类号: C07D405/04 , C07H19/04 , C07H19/073
CPC分类号: C07D405/04 , C07H19/04
摘要: There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).
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公开(公告)号:US5648385A
公开(公告)日:1997-07-15
申请号:US464186
申请日:1995-06-05
申请人: John E. Starrett, Jr. , Kuo-Long Yu , Muzammil M. Mansuri , David R. Tortolani , Peter R. Reczek
发明人: John E. Starrett, Jr. , Kuo-Long Yu , Muzammil M. Mansuri , David R. Tortolani , Peter R. Reczek
IPC分类号: A61K31/695 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/24 , A61K31/245 , A61K31/255 , A61P17/00 , A61P35/00 , A61P43/00 , C07C17/16 , C07C45/41 , C07C45/45 , C07C45/59 , C07C45/63 , C07C45/64 , C07C45/67 , C07C47/548 , C07C49/67 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/798 , C07C51/09 , C07C63/331 , C07C63/49 , C07C63/66 , C07C63/74 , C07C65/26 , C07C65/28 , C07C65/36 , C07C67/14 , C07C67/317 , C07C67/333 , C07C67/343 , C07C69/00 , C07C69/618 , C07C69/76 , C07C69/773 , C07C69/78 , C07C69/82 , C07C69/83 , C07C69/90 , C07C69/92 , C07C69/94 , C07C205/06 , C07C205/45 , C07C205/58 , C07C227/18 , C07C229/38 , C07C229/60 , C07C231/02 , C07C231/12 , C07C233/15 , C07C233/54 , C07C233/65 , C07C233/66 , C07C233/76 , C07C233/81 , C07C233/87 , C07C309/71 , C07C309/75 , C07C319/14 , C07C323/56 , C07C323/62 , C07C327/26 , C07C327/28 , C07C327/32 , C07C327/48 , C07F7/10 , A61K31/215
CPC分类号: C07C69/00 , C07C17/16 , C07C205/06 , C07C205/45 , C07C205/58 , C07C229/38 , C07C229/60 , C07C233/65 , C07C233/76 , C07C233/81 , C07C323/56 , C07C323/62 , C07C327/26 , C07C327/28 , C07C327/32 , C07C327/48 , C07C45/41 , C07C45/45 , C07C45/59 , C07C45/63 , C07C45/64 , C07C45/673 , C07C47/548 , C07C49/67 , C07C49/683 , C07C49/697 , C07C49/747 , C07C49/798 , C07C63/49 , C07C63/66 , C07C63/74 , C07C65/26 , C07C65/36 , C07C69/618 , C07C69/76 , C07C69/82 , C07C69/90 , C07C69/92 , C07C2102/08 , C07C2102/10 , C07C2103/00 , C07C2103/24 , Y10S514/825
摘要: The present invention relates to a compound of formula ##STR1## or a nontoxic pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof, in whichX is --O--CO--, --NH--CO--, --CS--NH--, --CO--O--, --CO--NH--, --COS--, --SCO--, --SCH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --C.tbd.C--, --CH.sub.2 --NH--, --COCH.sub.2 --, --NHCS--, --CH.sub.2 S--, --CH.sub.2 O--, --OCH.sub.2 --, --NHCH.sub.2 -- or --CR.sup.5 .dbd.CR.sup.6 --;R.sup.m and R.sup.k are independently hydrogen, halogen, C.sub.1-6 alkyl, hydroxy, C.sub.1-6 alkyloxy or nitro;n is zero or one;R.sup.4 is --(CH.sub.2).sub.t --Y, C.sub.1-6 alkyl, or C.sub.3-6 cycloalkyl;R.sup.1 is --CO.sub.2 Z, C.sub.1-6 alkyl, CH.sub.2 OH, --CONHR.sup.y, or CHO;R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1-6 alkyl;R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl; but when n is one, R.sup.a and R.sup.b together can form a radical of the formula ##STR2## Y is naphthyl or phenyl, both radicals can be optionally substituted with one to three same or different C.sub.1-6 alkyl or halogen;Z is hydrogen or C.sub.1-6 alkyl;R.sup.5, R.sup.6 and R.sup.y are independently hydrogen or C.sub.1-6 alkyl; andt is zero to six.
摘要翻译: 本发明涉及式I的化合物或其无毒的药学上可接受的盐,生理上可水解的酯或其溶剂合物,其中X是-O-CO-,-NH-CO-,-CS-NH-, CO-O-,-CO-NH-,-COS-,-SCO-,-SCH 2 - , - CH 2 -CH 2 - , - C 3BOND C - , - CH 2 -NH-,-COCH 2 - , - NHCS-, CH2S-,-CH2O-,-OCH2-,-NHCH2-或-CR5 = CR6-; R m和R k独立地是氢,卤素,C 1-6烷基,羟基,C 1-6烷氧基或硝基; n为零或一; R4是 - (CH2)t-Y,C1-6烷基或C3-6环烷基; R1是-CO2Z,C1-6烷基,CH2OH,-CONHRy或CHO; R2和R3独立地是氢或C1-6烷基; R a和R b独立地是氢或C 1-6烷基; 但是当n为1时,R a和R b可以一起形成下式的基团:Y是萘基或苯基,两个基团可任选地被一至三个相同或不同的C 1-6烷基或卤素取代; Z是氢或C 1-6烷基; R5,R6和Ry独立地是氢或C1-6烷基; t为0〜6。
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9.
公开(公告)号:US5567698A
公开(公告)日:1996-10-22
申请号:US454058
申请日:1995-05-30
申请人: Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
发明人: Choung U. Kim , Peter F. Misco, Jr. , John A. Wichtowski , Yasutsugu Ueda , Thomas W. Hudyma , John D. Matiskella , Stanley V. D'Andrea , Shelley E. Hoeft , Raymond F. Miller , Muzammil M. Mansuri , Joanne J. Bronson
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36 , A61K31/43 , C07D501/60
CPC分类号: C07D501/00
摘要: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R.sup.1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译: 由通式
表示的新型头孢烯衍生物,其中酰基取代基是式IMA的组,其中Ar是亲脂性任选取代的苯基,萘基,吡啶基或苯并噻唑基; R1选自某些任选取代的脂族,芳族,芳基脂族或糖部分,R2和R3各自独立地为氢,烷基或氨基烷基羰基氨基为革兰氏阳性抗菌剂,特别可用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病( MRSA)。 -
公开(公告)号:US4908440A
公开(公告)日:1990-03-13
申请号:US120051
申请日:1987-11-12
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61P31/12 , C07H19/04 , C07H19/056 , C07H19/06 , C07H19/16 , C07H19/19
摘要: There are disclosed novel 2',3'-dideoxy-2'-fluoronucleosides and 2'-3'-dideoxy-2',3'-didehydro-2'-fluoronucleosides and processes for their preparation. The compounds so produced exhibit therapeutically useful antiviral and, more particularly, anti-HIV effects.
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