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1. 发明授权

US08580820B2 Tubulysin compounds with high cytotoxicity, pharmaceutical compositions thereof, and method of use thereof 失效
标题翻译：具有高细胞毒性的吐温素化合物，其药物组合物及其使用方法
公开(公告)号：US08580820B2
公开(公告)日：2013-11-12
申请号：US12841976
申请日：2010-07-22
申请人： Matteo Zanda , Monica Sani , Paolo Lazzari
发明人： Matteo Zanda , Monica Sani , Paolo Lazzari
IPC分类号： A01N43/40 , A61K31/445 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00 , C07D277/00
CPC分类号： C07K5/021 , C07K5/06139
摘要： Tubulysine compounds of formula (A) having a high cytotoxicity wherein: B is selected from CH2, CH2—CH2 or CH2—CH2—CH2, D is an aromatic linker, X1 is alkyl or alkenyl, X2 is selected from the X2a, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl, X2b: alkylene-O-alkyl, wherein alkylene is C2-C10, X2c: CH2—O-alkyl, X3 is selected from H, or together with X4 forms the group ═O, X4 is selected from H, halogen, OH, SH, alkyl, alkenyl, (OR5)n—OR6, OC(O)R7, NR6R7, or together with X4 forms the group ═O, R5 is an alkylene, n is zero or an integer from 1 to 10, R6 and R7, equal to or different from each other, have the following meanings: z1: H, alkyl, z2 substituted or non substituted: aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkyl-alkyl, X5 is z2, or has the meaning of z3-alkyl, alkenyl, X6 is selected from NR8R9, OR8, NH—NR8R9, SR8, R10, wherein R8 and R9, equal to or different from each other, have the same meanings of R6, R10 has the same meanings as R6 but excluding H, X7 is z3 or H, X8 is selected from z3, H, halogen, OH, SH, OCH3.
摘要翻译：具有高细胞毒性的式（A）的三烯酚化合物，其中：B选自CH 2，CH 2 -CH 2或CH 2 -CH 2 -CH 2，D是芳族连接基，X 1是烷基或烯基，X 2选自X 2a，取代或未取代的，选自：芳基，杂芳基，芳基烷基，环烷基烷基，杂环烷基烷基或杂芳基烷基，X2b：亚烷基-O-烷基，其中亚烷基是C2-C10，X2c：CH2-O-烷基，X3选自H或一起 X4形成基团= O，X4选自H，卤素，OH，SH，烷基，烯基，（OR5）n-OR6，OC（O）R7，NR6R7或与X4一起形成基团= O，R5 是亚烷基，n为0或1〜10的整数，R6和R7彼此相同或不同，具有以下含义：z1：H，烷基，z2取代或未取代：芳基，杂芳基，环烷基，杂环烷基，芳基烷基，杂芳基烷基，环烷基烷基，杂环烷基 - 烷基，X5是z2，或具有z3-烷基，烯基，X6选自NR8R9，OR8，NH-NR8R9，SR8，R10的含义，在R8和R9中相同或不同，具有与R6相同的含义，R 10具有与R 6相同的含义，不包括H，X 7为Z 3或H，X 8选自Z 3，H，卤素，OH，SH ，OCH 3。

2. 发明申请

US20110200581A1 PHARMACEUTICAL COMPOSITIONS 失效
标题翻译：药物组合物
公开(公告)号：US20110200581A1
公开(公告)日：2011-08-18
申请号：US12841976
申请日：2010-07-22
申请人： Matteo ZANDA , Monica Sani , Paolo Lazzari
发明人： Matteo ZANDA , Monica Sani , Paolo Lazzari
IPC分类号： A61K39/395 , C07D401/12 , A61K31/454 , A61K38/00 , A61K38/22 , A61K31/715 , A61K31/724 , A61P35/00 , B82Y5/00
CPC分类号： C07K5/021 , C07K5/06139
摘要： Synthesis natural tubulisine derivatives of formula (A) having a high cytotoxicity wherein: B is selected from CH2, CH2—CH2 or CH2—CH2—CH2, D is an aromatic linker, X1 is alkyl or alkenyl, X2 is selected from the X2a, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl, X2b: alkylene-O-alkyl, wherein alkylene is C2-C10, X2c: CH2—O-alkyl, X3 is selected from H, or together with X4 forms the group ═O, X4 is selected from H, halogen, OH, SH, alkyl, alkenyl, (OR5)n—OR6, OC(O)R7, NR6R7, or together with X4 forms the group ═O, R5 is an alkylene, n is zero or an integer from 1 to 10, R6 and R7, equal to or different from each other, have the following meanings: z1: H, alkyl, z2 substituted or non substituted: aryl, heteroaryl, cycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, X5 is z2, or has the meaning of z3=alkyl, alkenyl, X6 is selected from NR8R9, OR8, NH—NR8R9, SR8, R10, wherein R8 and R9, equal to or different from each other, have the same meanings of R8, R10 has the same meanings as R6 but excluding H, X7 is z3 or H, X8 is selected from z3, H, halogen, OH, SH, OCH3.
摘要翻译：合成具有高细胞毒性的式（A）的天然水杨酸衍生物，其中：B选自CH 2，CH 2 -CH 2或CH 2 -CH 2 -CH 2，D是芳族连接基，X 1是烷基或烯基，X 2选自X 2a，取代或未取代的，选自：芳基，杂芳基，芳基烷基，环烷基烷基，杂环烷基烷基或杂芳基烷基，X2b：亚烷基-O-烷基，其中亚烷基是C2-C10，X2c：CH2-O-烷基，X3选自H，或与X 4一起形成基团≡O，X 4选自H，卤素，OH，SH，烷基，烯基，（OR 5）n -OR 6，OC（O）R 7，NR 6 R 7，或与X 4一起形成≡O R 5为亚烷基，n为0或1〜10的整数，R6和R7彼此相同或不同，具有以下含义：z1：H，烷基，z2取代或未取代：芳基，杂芳基，环烷基，杂环烷基，芳基烷基，杂芳基烷基，环烷基烷基，杂环烷基烷基，X5为z2，或具有z3 =烷基，烯基，X6选自NR8R 9，OR8，NH-NR8R9，SR8，R10，其中R8和R9彼此相同或不同，具有与R8相同的含义，R 10具有与R 6相同的含义，但不包括H，X 7为Z 3或H，X 8 选自z3，H，卤素，OH，SH，OCH3。

3. 发明授权

US07999101B2 Cationic lipids for the transfection of nucleic acids 失效
标题翻译：用于转染核酸的阳离子脂质
公开(公告)号：US07999101B2
公开(公告)日：2011-08-16
申请号：US11884354
申请日：2006-02-13
申请人： Matteo Zanda , Luca Bruche′ , Massimo Frigerio , Fiorenza Viani , Luca Chiamenti , Walter Panzeri , Nadia Zaffaroni , Marco Folini , Maria Angela Greco
发明人： Matteo Zanda , Luca Bruche′ , Massimo Frigerio , Fiorenza Viani , Luca Chiamenti , Walter Panzeri , Nadia Zaffaroni , Marco Folini , Maria Angela Greco
IPC分类号： C07D251/54 , C07D251/70 , A61K31/53 , A61K31/7105 , A61K31/711 , A61P43/00 , C12N15/00
CPC分类号： C07D251/44 , A61K48/0025 , C07D251/28 , C07D251/50 , C07D251/54 , Y10S977/773 , Y10S977/788 , Y10S977/792 , Y10S977/906 , Y10S977/915
摘要： The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; R1 and R2 are selected from H, —R7—NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R3 and R4 are selected from: H, —R8—SH, R8—NH—NH2/—R8—CO—R9 or —R8—NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.
摘要翻译：本发明涉及能够与核酸形成复合物的阳离子脂质及其用于转染真核细胞的用途。根据本发明的阳离子脂质具有通式（I）和（Ia）：（参见式（I）和（Ia）），其中E是杂芳基; R 1和R 2选自H，-R 7 -NH 2，烷基; R7选自烷基，烯基，芳基，（C1-C20）烷基 - 芳基 - （C0-C20）烷基; R3和R4选自：H，-R8-SH，R8-NH-NH2 / -R8-CO -R9或-R8-NH2; R8选自：烷基，烯基，芳基，（C1-C20）烷基 - 芳基 - （C0-C20）烷基; R9选自：H，烷基; R5和R6选自：H，烷基，链烯基，芳基，（C1-C20）烷基 - 芳基。

4. 发明申请

US20080146518A1 Cationic Lipids for the Transfection of Nucleic Acids 失效
标题翻译：阳离子脂质用于转染核酸
公开(公告)号：US20080146518A1
公开(公告)日：2008-06-19
申请号：US11884354
申请日：2006-02-13
申请人： Matteo Zanda , Luca Bruche , Massimo Fricerio , Fiorenza Viani , Luca Chiamenti , Walter Panzeri , Nadia Zaffaroni , Marco Folini , Maria Angela Greco
发明人： Matteo Zanda , Luca Bruche , Massimo Fricerio , Fiorenza Viani , Luca Chiamenti , Walter Panzeri , Nadia Zaffaroni , Marco Folini , Maria Angela Greco
IPC分类号： A61K48/00 , C07D251/54 , C12N15/00 , C12N15/63 , C12P1/00 , A61P43/00
CPC分类号： C07D251/44 , A61K48/0025 , C07D251/28 , C07D251/50 , C07D251/54 , Y10S977/773 , Y10S977/788 , Y10S977/792 , Y10S977/906 , Y10S977/915
摘要： The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; R1 and R2 are selected from H, —R7-NH2, aklyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R3 and R4 are selected from: H, —R8-SH, R8-NH—NH2/—R8-CO—R9 or —R8-NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl-(C0-C20) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.
摘要翻译：本发明涉及能够与核酸形成复合物的阳离子脂质及其用于转染真核细胞的用途。根据本发明的阳离子脂质具有通式（I）和（Ia）：（参见式（I）和（Ia）），其中E是杂芳基; R 1和R 2选自H，-R 7 -NH- R 2选自烷基，烯基，芳基，（C 1 -C 20 -C 20）烷基 - 芳基 - （C 0 -C 20烷基） C 1 -C 20烷基; R 3和R 4选自：H，-R 8 -SH，R 8 -NH-NH 2 - 或-R 8 -NH 2; R 8选自：烷基，烯基，芳基，（C 1 -C 20 -C 20）烷基 - 芳基 - （C 0 -C 20）烷基; R 9选自：H，烷基; R 5和R 6选自：H，烷基，烯基，芳基，（C 1 -C 20） C 1 -C 20烷基 - 芳基。

5. 发明授权

US07361668B2 Quinuclidine derivatives processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors 失效
标题翻译：奎宁环衍生物的制备方法及其作为m2和/或m3毒蕈碱受体抑制剂的用途
公开(公告)号：US07361668B2
公开(公告)日：2008-04-22
申请号：US10490436
申请日：2002-09-23
申请人： Michel Guyaux , Chimmanamada U. Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Matteo Zanda
发明人： Michel Guyaux , Chimmanamada U. Dinesh , Charles Mioskowski , Luc Quere , Jean-Philippe Starck , Patrice Talaga , Alain Wagner , Matteo Zanda
IPC分类号： A61K31/45 , A61K43/96 , A61K43/40 , C07D453/02
CPC分类号： C07D453/02
摘要： The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.
摘要翻译：本发明涉及式I或II的奎宁环衍生物，其中取代基如说明书中所定义，以及它们作为药物的用途。本发明化合物对于m 3和/或m 2毒蕈碱受体显示出高亲和力，特别适用于治疗尿失禁。

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