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1. 发明授权

US07485730B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US07485730B2
公开(公告)日：2009-02-03
申请号：US11134502
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： A61K31/4162 , C07D495/14
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′, a substituent having an hydroxyl function of formula —CH(OH)-Z′; and 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，具有羟基的取代基式-CH（OH）-Z'的功能; 和式-C（O）-NH-T'的酰胺取代基。

2. 发明授权

US08609659B2 Substituted 3,8-diazabicyclo[3.2.1]octane compounds 失效
标题翻译：取代的3,8-二氮杂双环[3.2.1]辛烷化合物
公开(公告)号：US08609659B2
公开(公告)日：2013-12-17
申请号：US12966371
申请日：2010-12-13
申请人： Paolo Lazzari , Giovanni Loriga , Stefania Ruiu , Gabriele Murineddu , Luca Pani , Gerard Aime Pinna
发明人： Paolo Lazzari , Giovanni Loriga , Stefania Ruiu , Gabriele Murineddu , Luca Pani , Gerard Aime Pinna
IPC分类号： A61K31/495
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。

3. 发明授权

US08106218B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US08106218B2
公开(公告)日：2012-01-31
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
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'如所定义下面; 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。

4. 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。

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. 发明授权

US08399457B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US08399457B2
公开(公告)日：2013-03-19
申请号：US12512818
申请日：2009-07-30
申请人： Paolo Lazzari , Giovanni Loriga , Stefania Ruiu , Ilaria Manca , Luca Pani , Gerard Aime Pinna
发明人： Paolo Lazzari , Giovanni Loriga , Stefania Ruiu , Ilaria Manca , Luca Pani , Gerard Aime Pinna
IPC分类号： A61P21/02 , A61K31/551 , C07D487/08
CPC分类号： C07D487/08
摘要： Nonane and decane diazabicyclic derivatives having homopiperazine as main ring, having affinity for the opioidergic μ and/or δ and/or k receptors and/or for all their receptorial subclasses, with central and/or peripheral activity, having formula (I), the isomeric forms and their mixtures included, wherein one or more atoms are in the corresponding isotopic forms: wherein: n is an integer equal to 1 or 2; one of the substituents R and R1 of the nitrogen atoms of the diazabicyclic ring is a —C(O)—RB group, wherein RB is a C1-C10 alkyl group, linear or branched when possible, the other remained substituent of R and R1 has the meanings reported in the description.
摘要翻译：具有高哌嗪作为主环的壬烷和癸烷二氮杂双环衍生物，对具有式（I）的具有中枢和/或外周活性的对阿片样物质的μ和/或δ和/或k受体和/或所有其接受的亚类具有亲和力，异构体及其混合物，其中一个或多个原子为相应的同位素形式：其中：n为等于1或2的整数; 二氮杂双环的氮原子的取代基R和R中的一个是-C（O）-RB基团，其中R b是C 1 -C 10烷基，如果可能的话是直链或支链的，另一个保留R和R 1的取代基具有说明书中报道的含义。

7. 发明申请

US20100105896A1 PHARMACEUTICAL COMPOUNDS 失效
标题翻译：药物化合物
公开(公告)号：US20100105896A1
公开(公告)日：2010-04-29
申请号：US12645415
申请日：2009-12-22
申请人： Paolo Lazzari , Stefania Rulu , Gerard Aime Pinna , Gabriele Murineddu
发明人： Paolo Lazzari , Stefania Rulu , Gerard Aime Pinna , Gabriele Murineddu
IPC分类号： C07D403/14 , C07D231/10 , C07D401/14
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′, 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。

8. 发明申请

US20050261281A1 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US20050261281A1
公开(公告)日：2005-11-24
申请号：US11134627
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： A61K31/4155 , A61K31/4453 , A61K31/55 , A61K47/20 , A61P1/08 , A61P1/16 , A61P3/00 , A61P7/06 , A61P9/00 , A61P11/00 , A61P13/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D409/04 , A61K31/53 , A61K31/416 , A61K31/454 , C07D49/02
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; Description of the industrial invention in the name of: NEUROSCIENZE S.c. a r.l., of Italian nationality, with head office in Cagliari, via Palabanda 9.
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是选自以下的基团：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）2 - 的醚基团 - （CH 2 CH 2）v -R “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; 工业发明的描述，名称为：NEUROSCIENZE S. 一个意大利国籍的r.l.，总部设在卡利亚里，通过Palabanda 9。

9. 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。

10. 发明授权

US6013747A Polymerization process in suspension 失效
标题翻译：悬浮液中的聚合过程
公开(公告)号：US6013747A
公开(公告)日：2000-01-11
申请号：US888690
申请日：1997-07-07
申请人： Julio A. Abusleme , Paolo Lazzari
发明人： Julio A. Abusleme , Paolo Lazzari
IPC分类号： C08G65/28 , C08F2/00 , C08F2/20 , C08F14/18 , C08G65/00
CPC分类号： C08G65/007 , C08F14/18
摘要： Use of surfactants in the suspension polymerization of fluorinated monomers for preparing fluoropolymers containing hydrogen, said surfacants having the general formula:R.sub.f --[L--(OCHR.sub.1 --CHR.sub.2).sub.m --OZ)].sub.iwherein:i is equal to 1 or 2;m is an integer comprised between 4 and 60;L can be chosen between: --(CFY--CO--O).sub.p R'-- and --(CFY--CO--NH).sub.p R'--wherein p is an integer equal to 0 or to 1;Y=F, CF.sub.3 ; R'=alkylic radical C.sub.1 -C.sub.5, linear or branched when possible;R.sub.1, R.sub.2 can be both H or the former H and the latter CH.sub.3 ;Z can be H, alkyl radical C.sub.1 -C.sub.3, linear or branched when possible; or (CH.sub.2).sub.n OH with n an integer from 1 to 6;R.sub.f 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：Rf- [L-（OCHR1-CHR2）m-OZ）]其中i等于1或2; m是4和60之间的整数; L可以选自： - （CFY-CO-O）pR'-和 - （CFY-CO-NH）pR'，其中p是等于0或1的整数; Y = F，CF3; R'=烷基C1-C5，尽可能直链或支链; R1，R2可以是H或前者H，后者可以是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; Rf是全氟烷基或全氟聚醚基，其数均分子量在250和1500之间。

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