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    • 1. 发明授权
    • Prenylarene compound and use thereof
    • 普萘酰芳烃化合物及其用途
    • US09371301B2
    • 2016-06-21
    • US13696425
    • 2011-05-06
    • Motomasa KobayashiNaoyuki KotokuMasayoshi AraiTakashi Kawachi
    • Motomasa KobayashiNaoyuki KotokuMasayoshi AraiTakashi Kawachi
    • C07D307/36C07D333/06A61K31/341A61K31/381A61K45/06C07D333/08
    • C07D307/36A61K31/341A61K31/381A61K45/06C07D333/08A61K2300/00
    • A compound represented by the general formula (C): (wherein R101 represents a substituted or unsubstituted aromatic heterocyclic group, R102, R103, R104 and R105 may be the same or different, and each represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a haloalkyl group having 1 to 3 carbon atoms, and R106 represents a hydrogen atom, or a saturated or unsaturated hydrocarbon group which is a straight or branched chain having 1 to 12 carbon atoms, but excluded is the case where R101 is a 3-furyl group, R102, R103, R104 and R105 are all methyl groups, and R106 is a methyl group, a 4-methyl-3-pentenyl group or a 4,8-dimethyl-3,7-nonadienyl group); or a pharmaceutically acceptable salt thereof has selective inhibitory activity on hypoxic cell growth in a broad range of the concentration and therefore is useful as an active ingredient of a medicament for cancer prevention or treatment.
    • 由通式(C)表示的化合物:(其中R 101表示取代或未取代的芳族杂环基,R 102,R 103,R 104和R 105可以相同或不同,表示氢原子,卤素原子,烷基 具有1至3个碳原子的烷基或具有1至3个碳原子的卤代烷基,R 10 6表示氢原子,或具有1至12个碳原子的直链或支链的饱和或不饱和烃基,但不包括 R 101为3-呋喃基的情况,R102,R103,R104,R105均为甲基,R106为甲基,4-甲基-3-戊烯基或4,8-二甲基-3,7 - 壬二烯基); 或其药学上可接受的盐在宽范围的浓度下对缺氧细胞生长具有选择性抑制活性,因此可用作用于癌症预防或治疗的药物的活性成分。
    • 5. 发明申请
    • Novel macrolide derivatives havaing effect of potentiating antifungal activity
    • 新型大环内酯衍生物具有增强抗真菌活性的作用
    • US20050176655A1
    • 2005-08-11
    • US10472044
    • 2002-10-29
    • Satoshi OmuraHiroshi TomodaToshiaki SunazukaMasayoshi AraiTohru Nagamitsu
    • Satoshi OmuraHiroshi TomodaToshiaki SunazukaMasayoshi AraiTohru Nagamitsu
    • A01N43/04A61K31/7048A61P31/10C07H17/08
    • C07H17/08A61K31/7048
    • Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]: wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.
    • 大环内酯衍生物对唑类抗真菌剂的活性具有增强的作用,在低浓度和短时间内对真菌感染起作用,并降低抗性微生物出现的频率。 一种这样的物质是由式[I]表示的化合物:其中R1是Ac,R2和R3是Ac,R4是Me; 当R1为H时,R2和R3为Ac,R4为Me; 当R1为H时,R2和R3为Ac,R4为H时,当R1Bz1,R2和R3为Bz1,R4为Me时; 当R1为Ac时,R2和R3为Pr,R4为Me; 当R1为Ac时,R2和R3为Hex,R4为Me; 当R1为Ac时,R2和R3为Bz1,R4为Me; 当R1为H时,R2和R3为Pr,R4为Me; 当R1为H时,R2和R3为Hex,R4为Me; 当R1为H时,R2和R3为Bz1,R4为Me; 当R1为H时,R2为H,R3为Bz1,R4为Me; 当R1为H时,R2和R3为Hex,R4为H,或当R1为H时,R2和R3为Hex,R4为Et。
    • 7. 发明申请
    • NOVEL PRENYLARENE COMPOUND AND USE THEREOF
    • 新颖的苯乙烯化合物及其用途
    • US20130065937A1
    • 2013-03-14
    • US13696425
    • 2011-05-06
    • Motomasa KobayashiNaoyuki KotokuMasayoshi AraiTakashi Kawachi
    • Motomasa KobayashiNaoyuki KotokuMasayoshi AraiTakashi Kawachi
    • C07D333/08A61P35/00A61K31/341A61K31/381C07D307/36
    • C07D307/36A61K31/341A61K31/381A61K45/06C07D333/08A61K2300/00
    • A compound represented by the general formula (C): (wherein R101 represents a substituted or unsubstituted aromatic heterocyclic group, R102, R103, R104 and R105 may be the same or different, and each represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a haloalkyl group having 1 to 3 carbon atoms, and R106 represents a hydrogen atom, or a saturated or unsaturated hydrocarbon group which is a straight or branched chain having 1 to 12 carbon atoms, but excluded is the case where R101 is a 3-furyl group, R102, R103, R104 and R105 are all methyl groups, and R106 is a methyl group, a 4-methyl-3-pentenyl group or a 4,8-dimethyl-3,7-nonadienyl group); or a pharmaceutically acceptable salt thereof has selective inhibitory activity on hypoxic cell growth in a broad range of the concentration and therefore is useful as an active ingredient of a medicament for cancer prevention or treatment.
    • 由通式(C)表示的化合物:(其中R 101表示取代或未取代的芳族杂环基,R 102,R 103,R 104和R 105可以相同或不同,表示氢原子,卤素原子,烷基 具有1至3个碳原子的烷基或具有1至3个碳原子的卤代烷基,R 10 6表示氢原子,或具有1至12个碳原子的直链或支链的饱和或不饱和烃基,但不包括 R 101为3-呋喃基的情况,R102,R103,R104,R105均为甲基,R106为甲基,4-甲基-3-戊烯基或4,8-二甲基-3,7 - 壬二烯基); 或其药学上可接受的盐在宽范围的浓度下对缺氧细胞生长具有选择性抑制活性,因此可用作用于癌症预防或治疗的药物的活性成分。