公开(公告)号：US07244767B2

公开(公告)日：2007-07-17

申请号：US10949322

申请日：2004-09-27

申请人： Tiziana Bisogno ,  Francesco Della Valle ,  Luciano De Petrocellis ,  Vincenzo Di Marzo ,  Gabriele Marcolongo ,  Dominique Melck

发明人： Tiziana Bisogno ,  Francesco Della Valle ,  Luciano De Petrocellis ,  Vincenzo Di Marzo ,  Gabriele Marcolongo ,  Dominique Melck

IPC分类号： A61K31/165 ,  A61K31/16

CPC分类号： A61K31/00

摘要： The present invention relates to the use of N-acylvanillinamide derivatives capable of activating the peripheral receptor CB1 of cannabinoids. In particular, the present invention relates to the use of compounds of general formula (I) in which the meanings of R, R1, R3 and Y are as defined in the description, for the preparation of a medicinal product which is capable of activating the peripheral receptor CB1 of cannabinoids.

摘要翻译： 本发明涉及能够激活大麻素的外周受体CB1的N-酰基万古霉素酰胺衍生物的用途。 特别地，本发明涉及通式（I）化合物的用途，其中R 1，R 1，R 3和Y的含义如 描述了用于制备能够激活大麻素的外周受体CB1的药用产品。

公开(公告)号：US20050065216A1

公开(公告)日：2005-03-24

申请号：US10949322

申请日：2004-09-27

申请人： Tiziana Bisogno ,  Francesco Della Valle ,  Luciano De Petrocellis ,  Vincenzo Di Marzo ,  Gabriele Marcolongo ,  Dominique Melck

发明人： Tiziana Bisogno ,  Francesco Della Valle ,  Luciano De Petrocellis ,  Vincenzo Di Marzo ,  Gabriele Marcolongo ,  Dominique Melck

IPC分类号： A61K31/00 ,  A61P29/00 ,  A61P31/00 ,  A61K31/165 ,  A61K31/16

CPC分类号： A61K31/00

摘要： The present invention relates to the use of N-acylvanillinamide derivatives capable of activating the peripheral receptor CB1 of cannabinoids. In particular, the present invention relates to the use of compounds of general formula (I) in which the meanings of R, R1, R3 and Y are as defined in the description, for the preparation of a medicinal product which is capable of activating the peripheral receptor CB1 of cannabinoids.

摘要翻译： 本发明涉及能够激活大麻素的外周受体CB1的N-酰基万古霉素酰胺衍生物的用途。 特别地，本发明涉及通式（I）化合物的用途，其中R，R 1，R 3和Y的含义如说明书中所定义，用于制备能够激活 大麻素的外周受体CB1。

公开(公告)号：US20120115808A1

公开(公告)日：2012-05-10

申请号：US13291294

申请日：2011-11-08

申请人： Francesco DELLA VALLE ,  Luciano De Petrocellis ,  Sabatino Maione ,  Vincenzo Di Marzo ,  Maria Federica Della Valle

发明人： Francesco DELLA VALLE ,  Luciano De Petrocellis ,  Sabatino Maione ,  Vincenzo Di Marzo ,  Maria Federica Della Valle

IPC分类号： A61K31/165 ,  A61K31/728 ,  A61P29/00 ,  A61K31/201

CPC分类号： A61K31/165 ,  A61K9/0014 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/0048 ,  A61K9/006 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/7038 ,  A61K31/07 ,  A61K31/194 ,  A61K31/728 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to topical preparations containing N-palmitoyl-vanillamide having hyperalgesic activity. In particular, the invention relates to N-palmitoyl-vanillamide for use in the treatment of pathologies selected from: post-herpetic neuralgia, neuralgia of trigeminus, occipital neuralgia, dental neuralgia, glottopharyngeal neuralgia, uremic neuralgia, diabetic neuralgia, headache of different origin, neuropathic itch, neurogenic itch, uremic itch, vulvodinia, vulvar vestibulitis, ano-rectal pain and itch, balano-preputial pain and itch, painful urogenital disorders of dogs and cats, psoriasis-associated pruritus and pain, itching skin diseases (e.g. atopic dermatitis) in the human and veterinary field, muscular pain, pain of the tendon, osteoarthritis associated pain in humans, dogs and cats; painful eye diseases in the human and veterinary field, inflammatory pathologies of the oral cavity in the human and veterinary field.

摘要翻译： 本发明涉及具有过敏反应活性的N-棕榈酰 - 香草酰胺的局部制剂。 特别地，本发明涉及用于治疗选自以下的病理学的N-棕榈酰基 - 香草酰胺：疱疹后神经痛，三叉神经痛神经痛，枕骨神经痛，牙齿神经痛，咽喉神经痛，尿毒症神经痛，糖尿病性神经痛，不同来源的头痛 ，神经性瘙痒，神经源性瘙痒，尿毒症瘙痒，外阴阴道炎，外阴前庭炎，直肠疼痛和瘙痒，巴拉阴性疼痛和瘙痒，狗和猫的疼痛性泌尿生殖器疾病，牛皮癣相关性瘙痒和疼痛，瘙痒性皮肤病 人类和兽医领域的肌肉炎，肌肉疼痛，肌腱疼痛，人类，狗和猫中的骨关节炎相关疼痛; 人类和兽医领域的痛苦的眼睛疾病，人类和兽医领域的口腔炎症病理。

公开(公告)号：US08546352B2

公开(公告)日：2013-10-01

申请号：US13291294

申请日：2011-11-08

申请人： Francesco Della Valle ,  Luciano De Petrocellis ,  Sabatino Maione ,  Vincenzo Di Marzo ,  Maria Federica Della Valle

发明人： Francesco Della Valle ,  Luciano De Petrocellis ,  Sabatino Maione ,  Vincenzo Di Marzo ,  Maria Federica Della Valle

IPC分类号： A61K31/165

CPC分类号： A61K31/165 ,  A61K9/0014 ,  A61K9/0031 ,  A61K9/0034 ,  A61K9/0048 ,  A61K9/006 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/7038 ,  A61K31/07 ,  A61K31/194 ,  A61K31/728 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to topical preparations containing N-palmitoyl-vanillamide having hyperalgesic activity. In particular, the invention relates to N-palmitoyl-vanillamide for use in the treatment of pathologies selected from: post-herpetic neuralgia, neuralgia of trigeminus, occipital neuralgia, dental neuralgia, glottopharyngeal neuralgia, uremic neuralgia, diabetic neuralgia, headache of different origin, neuropathic itch, neurogenic itch, uremic itch, vulvodinia, vulvar vestibulitis, ano-rectal pain and itch, balano-preputial pain and itch, painful urogenital disorders of dogs and cats, psoriasis-associated pruritus and pain, itching skin diseases (e.g. atopic dermatitis) in the human and veterinary field, muscular pain, pain of the tendon, osteoarthritis associated pain in humans, dogs and cats; painful eye diseases in the human and veterinary field, inflammatory pathologies of the oral cavity in the human and veterinary field.

摘要翻译： 本发明涉及具有过敏反应活性的N-棕榈酰 - 香草酰胺的局部制剂。 特别地，本发明涉及用于治疗选自以下的病理学的N-棕榈酰基 - 香草酰胺：疱疹后神经痛，三叉神经痛神经痛，枕骨神经痛，牙齿神经痛，咽喉神经痛，尿毒症神经痛，糖尿病性神经痛，不同来源的头痛 ，神经性瘙痒，神经源性瘙痒，尿毒症瘙痒，外阴阴道炎，外阴前庭炎，直肠疼痛和瘙痒，巴拉阴性疼痛和瘙痒，狗和猫的疼痛性泌尿生殖器疾病，牛皮癣相关性瘙痒和疼痛，瘙痒性皮肤病 人类和兽医领域的肌肉炎，肌肉疼痛，肌腱疼痛，人类，狗和猫中的骨关节炎相关疼痛; 人类和兽医领域的痛苦的眼睛疾病，人类和兽医领域的口腔炎症病理。

公开(公告)号：US09512091B2

公开(公告)日：2016-12-06

申请号：US14378185

申请日：2012-02-17

申请人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Vincenzo Di Marzo ,  Salvatore Cuzzocrea

发明人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Vincenzo Di Marzo ,  Salvatore Cuzzocrea

IPC分类号： C07D263/12 ,  C07D277/10 ,  C07D265/06 ,  A61K31/421 ,  C07D263/10 ,  C07D263/14 ,  A61K45/06 ,  A61K31/164 ,  A61K31/426 ,  A61K31/535 ,  C07D263/32

CPC分类号： C07D263/12 ,  A61K31/164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/535 ,  A61K45/06 ,  C07D263/10 ,  C07D263/14 ,  C07D263/32 ,  C07D265/06 ,  C07D277/10 ,  A61K2300/00

摘要： The present invention regards compositions and methods for the modulation of amidases capable of hydrolyzing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH═CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.

公开(公告)号：US20070270496A1

公开(公告)日：2007-11-22

申请号：US11724501

申请日：2007-03-14

申请人： Francesco Della Valle ,  Maria Della Valle ,  Gabriele Marcolongo ,  Gianpiero Ravagnan ,  Vincenzo Di Marzo

发明人： Francesco Della Valle ,  Maria Della Valle ,  Gabriele Marcolongo ,  Gianpiero Ravagnan ,  Vincenzo Di Marzo

IPC分类号： A61K31/195 ,  A61P37/00

CPC分类号： A61K31/7032 ,  A61K31/05 ,  A61K31/16 ,  A61K31/194 ,  A61K2300/00

摘要： The present invention relates to a pharmaceutical composition consisting of amides of mono- and di-carboxylic acids and hydroxystilbenes, and may be used for the treatment of pathologies caused, sustained and/or characterised by an abnormal general response of the immune system, in both humans and animals.

摘要翻译： 本发明涉及由单羧酸和二羧酸和羟基茋的酰胺组成的药物组合物，可用于治疗由免疫系统的异常一般反应引起，持续和/或表征的病理学 人类和动物。

公开(公告)号：US20110288037A1

公开(公告)日：2011-11-24

申请号：US13196964

申请日：2011-08-03

申请人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Gianpiero Ravagnan ,  Vincenzo Di Marzo

发明人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Gianpiero Ravagnan ,  Vincenzo Di Marzo

IPC分类号： A61K31/16 ,  A61P37/00 ,  A61P37/08 ,  A61P17/00 ,  A61P27/02 ,  A61P25/00 ,  A61P17/06 ,  A61P29/00 ,  A61P19/04 ,  A61P13/08 ,  A61P9/10 ,  A61P25/02 ,  A61P15/00 ,  A61P31/12 ,  A61P1/00 ,  A61P1/04 ,  A61K31/7034

CPC分类号： A61K31/7032 ,  A61K31/05 ,  A61K31/16 ,  A61K31/194 ,  A61K2300/00

摘要： The present invention relates to a pharmaceutical composition consisting of amides of mono- and di-carboxylic acids and hydroxystilbenes, and may be used for the treatment of pathologies caused, sustained and/or characterised by an abnormal general response of the immune system, in both humans and animals.

摘要翻译： 本发明涉及由单羧酸和二羧酸和羟基茋的酰胺组成的药物组合物，可用于治疗由免疫系统的异常一般反应引起，持续和/或表征的病理学 人类和动物。

公开(公告)号：US20150057269A1

公开(公告)日：2015-02-26

申请号：US14378185

申请日：2012-02-17

申请人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Vincenzo Di Marzo ,  Salvatore Cuzzocrea

发明人： Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo ,  Vincenzo Di Marzo ,  Salvatore Cuzzocrea

IPC分类号： C07D263/12 ,  A61K31/164 ,  C07D263/14 ,  C07D263/32 ,  A61K31/535 ,  C07D277/10 ,  A61K31/426 ,  A61K31/421 ,  C07D265/06

CPC分类号： C07D263/12 ,  A61K31/164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/535 ,  A61K45/06 ,  C07D263/10 ,  C07D263/14 ,  C07D263/32 ,  C07D265/06 ,  C07D277/10 ,  A61K2300/00

摘要： The present invention regards compositions and methods for the modulation of amidases capable of hydrolysing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH═CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.

摘要翻译： 本发明涉及调节能够水解可用于治疗炎性疾病的N-酰基乙醇胺的酰胺酶的组合物和方法。 特别地，本发明涉及通式（I）的化合物：对映异构体，非对映异构体，总状体和混合物，多晶型物，盐，溶剂合物，其中：（a）R是具有13至19个碳原子的直链烷基或链烯基 具有13至19个具有双键的碳原子的基团; （b）X为0或S; （c）Y是2或3个碳原子的亚烷基，任选地被一个或两个彼此相同或不同的基团取代，并且选自：-CH 3，-CH 2 OH，-COOCH 3，-COOH。 Y可优选为：-CH 2 -CH 2 - ， - CH 2 -CH 2 -CH 2 - ，CH（CH 3）-CH 2 - ， - CH 2 -CH（CH 3） - ， - CH 2 -C（CH 3）2 - ， - CH 2 -CH （CH 2 OH） - ， - CH 2 -C（（CH 2 OH）2） - ， - CH = CH - ， - CH 2 -CH（COOCH 3） - ， - CH 2 -CH（COOH）

公开(公告)号：US20100249223A1

公开(公告)日：2010-09-30

申请号：US12596500

申请日：2008-04-17

申请人： Vincenzo Di Marzo ,  Luciano De Petrocellis ,  Aniello Schiano Moriello

发明人： Vincenzo Di Marzo ,  Luciano De Petrocellis ,  Aniello Schiano Moriello

IPC分类号： A61K31/352 ,  A61K31/05 ,  A61P25/00 ,  A61P29/00

CPC分类号： A61K36/185 ,  A61P35/00

摘要： The present invention relates to the use of cannabinoid-containing plant extracts in the prevention or treatment of diseases or conditions that are alleviated by blockade of one or more types of TRP channel. Preferably the subset of TRP channel that is blockaded is the TRPA channel. More preferably the TRPA channel is the TRPA1 channel. Preferably the diseases or conditions to be prevented or treated include: neuropathic pain, inflammation or vasoconstriction. Alternatively the TRP channel that is blockaded is the TRPM channel. More preferably the TRPM channel is the TRPM8 channel. Preferably the diseases or conditions to be prevented or treated are cancer. More preferably the cancers to be treated include: cancer of the prostate, cancer of the breast, cancer of the colon, cancer of the lung or cancer of the skin. Alternatively the TRP channel that is blockaded is the TRPV channel. More preferably the TRPV channel is the TRPV1 channel. Preferably the diseases or conditions to be prevented or treated include neuropathic pain, inflammation or vasoconstriction.

摘要翻译： 本发明涉及含有大麻素的植物提取物在预防或治疗通过封锁一种或多种TRP通道而减轻的疾病或病症中的用途。 优选地，阻塞的TRP信道的子集是TRPA信道。 更优选地，TRPA信道是TRPA1信道。 优选地，要预防或治疗的疾病或病症包括：神经性疼痛，炎症或血管收缩。 或者，阻塞的TRP信道是TRPM信道。 更优选地，TRPM信道是TRPM8信道。 优选地，预防或治疗的疾病或病症是癌症。 更优选地，待治疗的癌症包括：前列腺癌，乳腺癌，结肠癌，肺癌或皮肤癌。 或者，阻塞的TRP信道是TRPV信道。 更优选地，TRPV信道是TRPV1信道。 优选地，要预防或治疗的疾病或病症包括神经性疼痛，炎症或血管收缩。

公开(公告)号：US20070105940A1

公开(公告)日：2007-05-10

申请号：US11549289

申请日：2006-10-13

申请人： Vincenzo Di Marzo ,  Luciano De Petrocellis ,  Sabatino Malone ,  Vito De Novellis

发明人： Vincenzo Di Marzo ,  Luciano De Petrocellis ,  Sabatino Malone ,  Vito De Novellis

IPC分类号： A61K31/405

CPC分类号： A61K31/4045

摘要： The present invention provides pharmaceutical compositions useful in a method for treating neuropathic pain, said method comprising administration of a pain-ameliorating effective amount of the compound according to formula I wherein n is an integer of from 1 to 10, m is an integer of from 1 to 4 and the total carbon atoms in the alkenyl amide chain is from about 11 to about 20 as an active ingredient together with one or more pharmaceutically-acceptable additives, excipients or diluents.

摘要翻译： 本发明提供了可用于治疗神经性疼痛的方法的药物组合物，所述方法包括施用改善疼痛的有效量的式I化合物，其中n为1至10的整数，m为 1至4，并且链烯基酰胺链中的总碳原子为约11至约20作为活性成分以及一种或多种药学上可接受的添加剂，赋形剂或稀释剂。