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    • 1. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US5734047A
    • 1998-03-31
    • US761738
    • 1996-12-05
    • Choung U. KimMuzammil M. MansuriPeter F. MiscoJohn A. Wichtowski
    • Choung U. KimMuzammil M. MansuriPeter F. MiscoJohn A. Wichtowski
    • C07D501/00C07D501/36A61K31/545
    • C07D501/00
    • Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.
    • 由通式 + TR 表示的新型头孢烯衍生物,其中Ar是任选取代的亲脂性苯基,萘基,苯并噻唑基或吡啶基; R 1表示式(VIII)的基团,其中R 8和R 9各自独立地为氢,C 1 -C 6烷基或(C 1 -C 6)烷氧基羰基,所述C 1 -C 6烷基任选被1-5个羟基或C 1 -C 6 烷氧基 m为0或1; A是任选被1-5个羟基取代的C 2 -C 10烷基; 且R 2和R 3各自独立地为氢或C 1 -C 6烷基。 衍生物是革兰氏阳性抗菌剂,特别适用于治疗耐甲氧西林金黄色葡萄球菌引起的疾病。
    • 5. 发明授权
    • Vinyl ethers of nucleoside analogs
    • 核苷类似物的乙烯基醚
    • US5696265A
    • 1997-12-09
    • US488340
    • 1995-06-07
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/6512C07F9/6558C07F9/6561C07F9/6571C07H19/04C07H19/10C07H19/20A61K31/52C07D473/18C07D473/34C07D473/30
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/65121C07F9/65586C07F9/65616C07F9/657181C07H19/04C07H19/10C07H19/20
    • Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, and B is a purine or pyrimidine base. A compound of the formula (V) ##STR3## wherein B is cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil, 5-vinyluracil, hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, or 2-acetamido-6-diphenylcarbamoylpurine; and the pharmaceutically acceptable salts thereof.
    • 本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/嘧啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,羟基烷基或烷酰基,B为嘌呤或嘧啶碱基。 其中X和X'相同或不同且为氢或烷基,Y和Z相同或不同,为氢,羟基或烷基的4'-膦基甲氧基四氢呋喃基-1'-嘌呤嘧啶, Y + Z是烯基,环氧化物或环丙基,B是嘌呤或嘧啶碱基。 式(V)化合物其中B为胞嘧啶,5-乙基胞嘧啶,5-甲基胞嘧啶,胸腺嘧啶,尿嘧啶,5-氯尿嘧啶,5-溴尿嘧啶,5-乙基尿嘧啶,5-碘尿嘧啶,5-丙基尿嘧啶, 5-乙酰尿嘧啶,次黄嘌呤,黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-甲基鸟嘌呤,8-硫鸟嘌呤,3-脱氮鸟嘌呤,嘌呤,2-氨基嘌呤,2,6-二氨基嘌呤,腺嘌呤,3-脱氮腺嘌呤,8-氨基鸟嘌呤, 8-肼基鸟嘌呤,8-羟基鸟嘌呤或2-乙酰氨基-6-二苯基氨基甲酰基嘌呤; 及其药学上可接受的盐。
    • 8. 发明授权
    • Nucleoside analogs
    • 核苷类似物
    • US5837871A
    • 1998-11-17
    • US486991
    • 1995-06-07
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/6512C07F9/6558C07F9/6561C07F9/6571C07H19/04C07H19/10C07H19/20A61K31/675C07D473/18
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/65121C07F9/65586C07F9/65616C07F9/657181C07H19/04C07H19/10C07H19/20
    • Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms; and B is cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, any one of which is substituted at the 1-position; wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or are taken together to form an oxygen atom or a methylene group; or are taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.b is H or OH; wherein in the compound of formula (VIII), Y is halogen, phenylthio or phenylseleno; and the pharmaceutically acceptable salts thereof. B is a purine or pyrimidine base.
    • 本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/嘧啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,烷基或烷酰基,B为嘌呤或嘧啶碱基。 (II)或(VIII)化合物其中虚线是任选的键; X,R和X'相同或不同,为H或具有1至6个碳原子的烷基; B是胞嘧啶,5-乙基胞嘧啶,5-甲基胞嘧啶,胸腺嘧啶,尿嘧啶,5-氯尿嘧啶,5-溴尿嘧啶,5-乙基尿嘧啶,5-碘尿嘧啶,5-丙基尿嘧啶或5-乙烯基尿嘧啶,其中任何一个在1 -位置; 其中在式(II)化合物中,Y和Z相同或不同,为H; 哦; 具有1至6个碳原子的烷基; 被卤素,羟基,氨基或叠氮基取代的具有1至6个碳原子的烷基; 或者一起形成氧原子或亚甲基; 或与X'一起,以完成具有式(III)结构的环状膦酸酯,其中R b是H或OH; 其中在式(Ⅷ)化合物中,Y是卤素,苯硫基或苯基硒; 及其药学上可接受的盐。 B是嘌呤或嘧啶碱基。
    • 9. 发明授权
    • Nucleoside analogs
    • 核苷类似物
    • US5726174A
    • 1998-03-10
    • US488338
    • 1995-06-07
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/6512C07F9/6558C07F9/6561C07F9/6571C07H19/04C07H19/10C07H19/20A61K31/675
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/65121C07F9/65586C07F9/65616C07F9/657181C07H19/04C07H19/10C07H19/20
    • Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyridimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms; wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or Y and Z are taken together to form an oxygen atom or a methylene group; or Y is taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.b is H or OH; wherein in the compound of formula (VIII), Y is halogen, phenylthio or phenylseleno; wherein in the compound of formula (II), B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine or 3-deazaadenine, any one of which is substituted at the 9-position; and, wherein in the compound of formula (III) or (VIII), B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine or 8-hydroxyguanine, any one of which is substituted at the 9-position; and the pharmaceutically acceptable salts thereof.
    • 本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/吡啶并吡啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,羟基烷基或烷酰基,B为嘌呤或嘧啶碱基。 (II)或(VIII)化合物其中虚线是任选的键; X,R和X'相同或不同,为H或具有1至6个碳原子的烷基; 其中在式(II)化合物中,Y和Z相同或不同,为H; 哦; 具有1至6个碳原子的烷基; 被卤素,羟基,氨基或叠氮基取代的具有1至6个碳原子的烷基; 或Y和Z一起形成氧原子或亚甲基; 或Y与X'一起形成具有式(III)结构的环状膦酸酯,其中R b是H或OH; 其中在式(Ⅷ)化合物中,Y是卤素,苯硫基或苯基硒; 其中在式(II)化合物中,B是次黄嘌呤,黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯胍,8-甲基鸟嘌呤,8-硫鸟嘌呤,3-脱氮鸟嘌呤,嘌呤,2-氨基嘌呤,2,6-二氨基嘌呤, 腺嘌呤或3-脱氮腺嘌呤,其中任何一个在9位被取代; 其中在式(III)或(VIII)的化合物中,B是次黄嘌呤,黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-甲基鸟嘌呤,8-硫鸟嘌呤,3-脱氮鸟嘌呤,嘌呤,2-氨基嘌呤, 6-二氨基嘌呤,腺嘌呤,3-脱氮腺嘌呤,8-氨基胍,8-肼基鸟嘌呤或8-羟基鸟嘌呤,其中任何一个在9位被取代; 及其药学上可接受的盐。
    • 10. 发明授权
    • Nucleoside analogs
    • 核苷类似物
    • US5686611A
    • 1997-11-11
    • US488339
    • 1995-06-07
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • Choung Un KimJohn C. MartinBing Uh LuhPeter F. Misco
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/6512C07F9/6558C07F9/6561C07F9/6571C07H19/04C07H19/10C07H19/20C07D473/18C07D473/34C07D473/24
    • C07D239/54C07D405/04C07D473/00C07D473/32C07D473/40C07F9/65121C07F9/65586C07F9/65616C07F9/657181C07H19/04C07H19/10C07H19/20
    • Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl and B is a purine or pyrimidine base. A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine. A compound of formula (VII) ##STR3## wherein B is guanine, 8-guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, or 5-methylcytosine.
    • 本发明提供下式的化合物:下式的膦酰甲氧基甲氧基甲氧基甲基嘌呤/嘧啶衍生物,其中X和X'相同或不同,为氢或烷基。 R和R'相同或不同,为氢,烷基,羟基烷基或烷酰基,B为嘌呤或嘧啶碱基。 式(VI)的化合物其中X是卤素,Y是S-苯基,Se-苯基或卤素,B是次黄嘌呤,黄嘌呤,鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-甲基鸟嘌呤, 8-硫鸟嘌呤,3-脱氮鸟嘌呤,嘌呤,2-氨基嘌呤,2,6-二氨基嘌呤,腺嘌呤,3-脱氮腺嘌呤,8-氨基胍,8-肼基鸟嘌呤,8-羟基鸟嘌呤,胞嘧啶,5-乙基胞嘧啶,5-甲基胞嘧啶,胸腺嘧啶, 尿嘧啶,5-氯尿嘧啶,5-溴尿嘧啶,5-乙基尿嘧啶,5-碘尿嘧啶,5-丙基尿嘧啶或5-乙烯基尿嘧啶,2-乙酰氨基-6-二苯基氨基甲酰基嘌呤,6-N-二甲基氨基 - 甲基腺嘌呤或6-N-新戊酰基腺嘌呤。 式(VII)化合物其中B是鸟嘌呤,8-鸟嘌呤,8-溴鸟嘌呤,8-氯鸟嘌呤,8-甲基鸟嘌呤,8-硫鸟嘌呤,3-脱氮鸟嘌呤,8-氨基胍,8-肼基鸟嘌呤, 5-羟基鸟嘌呤,胞嘧啶,5-乙基胞嘧啶或5-甲基胞嘧啶。