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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. 发明授权

US08329187B2 Compositions of spores of non pathogenic bacteria 失效
标题翻译：非病原菌孢子的组成
公开(公告)号：US08329187B2
公开(公告)日：2012-12-11
申请号：US12712647
申请日：2010-02-25
申请人： Paolo Lazzari , Paolo Fadda , Luca Pani
发明人： Paolo Lazzari , Paolo Fadda , Luca Pani
IPC分类号： A61K39/00 , A61K39/02 , A61K39/07 , A61K39/08
CPC分类号： A61K35/742 , A23K10/18 , A23L29/10 , A23L33/135 , A61K9/1075 , A61K9/1274
摘要： Liquid-based phamaceutical and/or veterinary and/or nutraceutical compositions comprising non pathogenic sporogenic bacteria, component SP), and the following components: O) from 0.001 to 95% by weight of one or more oils selected from esters of C4-C32 acids, C4-C32, S) from 0 to 90% by weight of one or more amphiphilic compounds, selected from surfactants, polymers forming organized structures such as aggregates, micelles, liquid crystals, vesicles, in the liquid in which they are solubilized, AD) from 0 to 60% by weight of one or more additive compounds selected from modifiers of the water and/or oil polarity, modifiers of the film curvature of component S), co-surfactants, PA) from 0.001 to 70% of one or more compounds selected from food supplements and pharmaceutical and/or veterinary active principles, W) from 0.1 to 99.9% by weight of water or saline aqueous solution, optionally buffered, the sum of the percentages by weight of the components, excluding SP), is 100%.
摘要翻译：液体制药和/或兽医和/或营养保健组合物，包含非致病性致孢杆菌，组分SP）和以下组分：O）0.001至95重量％的一种或多种选自C 4 -C 32酸的酯的油，C 4 -C 32，S）0至90重量％的一种或多种两亲化合物，其选自表面活性剂，形成有组织结构的聚合物，例如聚集体，胶束，液晶，囊泡，在它们被溶解的液体中，AD ）0至60重量％的一种或多种选自水和/或油极性改性剂的添加剂化合物，组分S的膜曲率的改性剂），助表面活性剂，PA），0.001至70％的一种或多种更多选自食品添加剂和药物和/或兽用活性成分的化合物，W）0.1至99.9重量％的水或盐水溶液（任选缓冲的）除组分重量除外的百分比之和除外）是 100％。

3. 发明授权

US08227620B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US08227620B2
公开(公告)日：2012-07-24
申请号：US12645415
申请日：2009-12-22
申请人： Paolo Lazzari , Stefania Ruiu , Gerard Aime Pinna , Gabriele Murineddu
发明人： Paolo Lazzari , Stefania Ruiu , Gerard Aime Pinna , Gabriele Murineddu
IPC分类号： A61K31/4155 , A61K31/454
CPC分类号： C07D409/04
摘要： Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R″ wherein v is equal to 1 or 2; R″ is as defined in the present application; a ketone group of formula —C(O)—Z′, wherein Z′ is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z′, being as defined in the present application; an amide substituent of formula —C(O)—NH-T′, T′ being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.
摘要翻译：具有对大麻素能CB1和/或CB2受体的亲和力的下式（I）的吡唑衍生物：其中：R是选自C1-C10烷基的基团; 未被取代或具有1-4个取代基的芳基，芳基烷基或芳基烯基，彼此相等或不同; A是选自以下的基团：式 - （CH 2）-O-（CH 2）v -R“的醚基，其中v等于1或2; R“如本申请中所定义; 式-C（O）-Z'的酮基，其中Z'如本申请中所定义; 具有式-CH（OH）-Z'羟基官能团的取代基，如本申请中所定义; 式-C（O）-NH-T'，T'的酰胺取代基如本申请中所定义; B是本申请中定义的组; D是任选取代的杂芳基。

4. 发明申请

US20110152238A1 PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物
公开(公告)号：US20110152238A1
公开(公告)日：2011-06-23
申请号：US12966371
申请日：2010-12-13
申请人： Paolo LAZZARI , Giovanni Loriga , Stefania Ruiu , Gabrieie Murineddu , Luca Pani , Gerard Aime Pinna
发明人： Paolo LAZZARI , Giovanni Loriga , Stefania Ruiu , Gabrieie Murineddu , Luca Pani , Gerard Aime Pinna
IPC分类号： A61K31/4995 , C07D487/18 , C07D471/08 , C07D487/08 , A61K31/55 , A61K31/439 , A61K31/551 , A61K31/4748 , A61P29/00 , A61P25/04 , A61P25/30 , A61P25/32 , A61P1/10 , A61P1/12 , A61P1/00 , A61P1/08 , A61P17/00 , A61P3/04 , A61P25/22 , A61P25/24 , A61P25/34 , A61P15/00 , A61P27/02 , A61P27/06 , A61P35/00 , A61P19/02 , A61P17/06 , A61P11/06 , A61P9/00 , A61P13/00 , A61P25/16 , A61P25/28 , A61P3/10 , A61P9/10 , A61P5/00 , A61P37/00 , A61P37/06
CPC分类号： C07D471/08 , C07D487/08
摘要： Diazapolycyclic compounds having affinity for the opioidergic receptors, preferably for the delta opioidergic receptors, with central and/or peripheral activity, having formula: A1-D1-T1 (I) wherein: A1 is a group of formula (II): wherein: R1 is phenyl wherein one of the ring hydrogen atoms is substituted with a group selected from C(O)R′, C(O)OR′, C(O)NHR′ or C(O)NR3R4, R′, R3 and R4, being as defined in the application; R2 is phenyl, optionally substituted D1 is a diazapolycyclic group T1 is a group selected from H, alkyl, alkenyl, alkynyl and from the following optionally substituted groups: cycloalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkylalkyl, heterocycloalkylalkyl, arylalkyl or heteroarylalkyl, and their hydrates and solvates and pharmaceutically acceptable salts.
摘要翻译： A1-D1-T1（Ⅰ）其中：A1是式（Ⅱ）的基团：其中：R1（ⅰ），其中R1为具有中性和/或外周活性的阿片样物质受体的阿片样物质受体，是其中一个环状氢原子被选自C（O）R'，C（O）OR'，C（O）NHR'或C（O）NR 3 R 4，R'，R 3和R 4的基团取代的苯基，正如申请中所定义的; R2是苯基，任意取代的D1是一个二氮杂多环基团，T1是选自H，烷基，烯基，炔基和下列任选取代的基团：环烷基，杂环烷基，芳基，杂芳基，环烷基烷基，杂环烷基烷基，芳基烷基或杂芳基烷基，水合物和溶剂化物和药学上可接受的盐。

5. 发明授权

US07659407B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07659407B2
公开(公告)日：2010-02-09
申请号：US11134627
申请日：2005-05-23
申请人： Paolo Lazzari , Stefania Ruiu , Gerard Aime Pinna , Gabriele Murineddu
发明人： Paolo Lazzari , Stefania Ruiu , Gerard Aime Pinna , Gabriele Murineddu
IPC分类号： A61K31/4155 , A61K31/454 , C07D409/04 , C07D409/14
CPC分类号： C07D409/04
摘要： Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: R is a group selected from: C1-C10 alkyl; aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; A is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R″ wherein v is equal to 1 or 2; R″ is as defined in the present application; a ketone group of formula —C(O)—Z′, wherein Z′ is as defined in the present application; a substituent having an hydroxyl function of formula —CH(OH)—Z′, Z′ being as defined in the present application; an amide substituent of formula —C(O)—NH—T′, T′ being as defined in the present application; B is a group as defined in the present application; D is an heteroaryl optionally substituted.
摘要翻译：具有对大麻素能CB1和/或CB2受体的亲和力的下式（I）的吡唑衍生物：其中：R是选自：C 1 -C 10烷基; 未被取代或具有1-4个取代基的芳基，芳基烷基或芳基烯基，彼此相等或不同; A是选自以下的基团：式 - （CH 2）-O-（CH 2）v -R'的醚基，其中v等于1或2; R“如本申请中所定义; 式-C（O）-Z'的酮基，其中Z'如本申请中所定义; 具有式-CH（OH）-Z'，Z'的羟基官能团的取代基如本申请中所定义; 式-C（O）-NH-T'，T'的酰胺取代基如本申请中所定义; B是本申请中定义的组; D是任选取代的杂芳基。

6. 发明申请

US20090081123A1 PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物
公开(公告)号：US20090081123A1
公开(公告)日：2009-03-26
申请号：US12330434
申请日：2008-12-08
申请人： Paolo LAZZARI , Stefania RUIU , Gerard Aime PINNA , Gabriele MURINEDDU
发明人： Paolo LAZZARI , Stefania RUIU , Gerard Aime PINNA , Gabriele MURINEDDU
IPC分类号： A61K31/4162 , C07D495/04 , A61K31/454 , A61P37/00 , A61K51/04 , A61P25/00 , A61P29/00 , A61K31/55
CPC分类号： C07D495/04
摘要： Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R′ is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R″, a ketonic group of formula —C(O)-Z′, wherein Z′ is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z′; an amide substituent of formula —C(O)—NH-T′.
摘要翻译：具有对大麻素能CB1和/或CB2受体具有亲和力的下式（I）的三环吡唑衍生物：其中：A表示选自以下之一的基团：（CH 2）t - ， - （CH 2）-S（O） Z - 或-S（O）z - （CH 2） - ，B是任选取代的杂芳基; R是选自以下的基团：未被取代或具有1-4个取代基的烷基，芳基，芳基烷基或芳基烯基，彼此相等或不同; R'是选自以下的基团：式 - （CH 2）-O-（CH 2）v -R'的醚基团，式-C（O）-Z'的酮基，其中Z'为定义如下具有式-CH（OH）-Z'的羟基官能团的取代基; 式-C（O）-NH-T'的酰胺取代基。

7. 发明申请

US20050282798A1 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US20050282798A1
公开(公告)日：2005-12-22
申请号：US11134502
申请日：2005-05-23
申请人： Paolo Lazzari , Stefania Ruiu , Gerard Pinna , Gabriele Murineddu
发明人： Paolo Lazzari , Stefania Ruiu , Gerard Pinna , Gabriele Murineddu
IPC分类号： A61K31/4162 , A61K31/454 , A61K51/00 , A61P1/08 , A61P3/04 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/12 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/36 , A61P27/02 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D231/54 , C07D495/04 , A61K31/55 , C07D498/02
CPC分类号： C07D495/04
摘要： Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R′ is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R″, a ketonic group of formula —C(O)-Z′, wherein Z′ is as defined below; a substituent having an hydroxyl function of formula —CH(OH)-Z′; an amide substituent of formula —C(O)—NH-T′.
摘要翻译：具有对大麻素能CB1和/或CB2受体具有亲和性的下式（I）的三环吡唑衍生物：其中：A表示选自以下之一的基团：（CH 2）2 - （CH 2 - ） - S（O）z - ，或-S（O）z - （CH B是任选取代的杂芳基; R是选自以下的基团：未被取代或具有1-4个取代基的烷基，芳基，芳基烷基或芳基烯基，彼此相等或不同; R'是选自以下的基团：式 - （CH 2 CH 2）-O-（CH 2）2 - 的醚基 - R“，式-C（O）-Z'的酮基，其中Z'如下所定义; 具有式-CH（OH）-Z'的羟基官能团的取代基; 式-C（O）-NH-T'的酰胺取代基。

8. 发明授权

US06417390B1 Polymerization process in suspension 失效
标题翻译：悬浮聚合工艺
公开(公告)号：US06417390B1
公开(公告)日：2002-07-09
申请号：US09435778
申请日：1999-11-08
申请人： Julio A. Abusleme , Paolo Lazzari
发明人： Julio A. Abusleme , Paolo Lazzari
IPC分类号： C07C6966
CPC分类号： C08G65/007 , C08F14/18 , C08F2/16
摘要： Use of surfactants in the suspension polymerization of fluorinated monomers for preparing fluoropolymers containing hydrogen, said surfacants having the general formula: Rf—[L—(OCHR1—CHR2)m—OZ)]i wherein: i is equal to 1 or 2; m is an integer comprised between 4 and 60; L can be chosen between: —(CFY—CO—O)pR′— and —(CFY—CO—NH)pR′— wherein is an integer equal to 0 or to 1; Y═F, CF3; R′=alkylic radical C1-C5, linear or branched when possible; R1, R2 can be both H or the former H and the latter CH3; Z can be H, alkyl radical C1-C3, linear or branched when possible; or (CH2)nOH with n an integer from 1 to 6; Rf is a perfluoroalkylic radical or a perfluoropolyether radical, having a number average molecular weight comprised between 250 and 1500.
摘要翻译：在氟化单体的悬浮聚合中使用表面活性剂来制备含氢的含氟聚合物，所述表面活性剂具有以下通式：其中：i等于1或2; m是4至60之间的整数; L可以选自：（CFY-CO-O）pR'-和 - （CFY-CO-NH）pR'，其中等于0或1的整数; Y = F，CF 3; R'=烷基C1-C5，如果可能，则为直链或支链; R1，R2可以是H或前者H和后者CH3; Z可以是H，烷基C1-C3，尽可能直链或支链; 或（C 1）n OH，n为1至6的整数; R f为全氟烷基或全氟聚醚基，其数均分子量为250至1500。

9. 发明授权

US06025307A Fluorinated greases 失效
标题翻译：氟化润滑脂
公开(公告)号：US06025307A
公开(公告)日：2000-02-15
申请号：US44180
申请日：1998-03-19
申请人： Alba Chittofrati , Paolo Lazzari , Luca Caluso
发明人： Alba Chittofrati , Paolo Lazzari , Luca Caluso
IPC分类号： C10M119/22 , C08L27/18 , C08L29/10 , C10M169/00 , C10N50/10
CPC分类号： C10M169/00 , C10M2211/044 , C10M2211/06 , C10M2213/00 , C10M2213/02 , C10M2213/023 , C10M2213/04 , C10M2213/043 , C10M2213/06 , C10M2213/0606 , C10M2213/062 , C10M2213/0623 , C10M2215/042 , C10M2215/08 , C10M2215/082 , C10M2215/182 , C10M2215/28 , C10M2217/041 , C10M2219/044 , C10M2223/04 , C10M2223/041 , C10M2223/042
摘要： Fluorinated greases comprising (by weight):15%-50% polytetrafluoroethylene or tetrafluoroethylene copolymers with other ethylenically unsaturated monomers;30%-84.5% perfluoropolyether oil having a viscosity comprised between 20 and 4000 cSt at 20.degree. C.;0.5%-10% surfactant or dispersant having perfluoropolyether or perfluoroalkylic chain;0%-10% of an anticorrosion and/or antiwear additive, such that the (per)fluoropolymer particles based on TFE or their aggregates have average sizes lower than the micron and show improved diameter WEAR values.
摘要翻译：包含（重量）的氟化润滑脂：15％-50％的聚四氟乙烯或与其它烯属不饱和单体的四氟乙烯共聚物; 30％-84.5％的全氟聚醚油，其在20℃下的粘度为20至4000cSt; 具有全氟聚醚或全氟烷基链的0.5％-10％表面活性剂或分散剂; 0％-10％的抗腐蚀和/或抗磨添加剂，使得基于TFE或它们的聚集体的（per）含氟聚合物颗粒具有低于微米的平均尺寸并且显示改善的直径WEAR值。

10. 发明授权

US6013712A Perfluoropolymer dispersions 失效
标题翻译：全氟聚合物分散体
公开(公告)号：US6013712A
公开(公告)日：2000-01-11
申请号：US124966
申请日：1998-07-30
申请人： Alba Chittofrati , Paolo Lazzari , Daria Lenti
发明人： Alba Chittofrati , Paolo Lazzari , Daria Lenti
IPC分类号： C08J3/02 , C08J3/09 , C08L27/18 , C09D7/12 , C09D127/18 , C09G1/00 , C11D1/00 , C11D3/24 , C11D3/37 , C11D3/43 , C08K5/06
CPC分类号： C08J3/09 , C09D127/18 , C09D7/125 , C09G1/00 , C11D1/004 , C11D3/245 , C11D3/3749 , C11D3/43 , C08J2327/18 , C08L27/18
摘要： Dispersions comprising at least:0.1-30% by weight of a polytetrafluoroethylene or tetrafluoroethylene copolymers with other ethylenically unsaturated monomers;50-99% by weight of fluorinated liquid;polar solvent (water and/or alcohol) complement to 100;0.01-5% by weight of surfactant selected from:(a) nonionic hydrogenated or(b) fluorinated, having a perfluoropolyether or perfluoroalkylic chain, both of ionic and non ionic type, selected from the following classes:A') mono and dicarboxylic acid salts;B') sulphonic acid salts;C') phosphoric mono and diesters and their mixtures, as such or salified, optionally containing amounts of triesters lower than 15% by moles;D') nonionic surfactants formed by fluorinated and polyoxyalkylenic chains with a number of oxyalkylenic repeating units higher than 6;E') cationic surfactants having one or more fluorinated hydrophobic chains.
摘要翻译：包含至少0.1-30重量％的聚四氟乙烯或四氟乙烯与其它烯属不饱和单体的共聚物的分散体; 50-99重量％的氟化液体; 极性溶剂（水和/或醇）互补100; 0.01-5重量％的表面活性剂，选自：（a）非离子氢化或（b）氟化的，具有全氟聚醚或全氟烷基链，离子型和非离子型，选自以下类别：A'）单和二羧酸盐 B'）磺酸盐; C'）磷酸单酯和二酯及其混合物，如此或成盐，任选地含有低于15摩尔％的三酯的量; D'）非离子表面活性剂，其通过具有高于6的多个氧化烯重复单元的氟化和聚氧化亚烷基链形成; E'）具有一个或多个氟化疏水链的阳离子表面活性剂。

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