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1. 发明申请

US20120115808A1 PHARMACOLOGICAL PREPARATION FOR TOPICAL USE CONTAINING N-PALMITOYL-VANILLAMIDE 有权
标题翻译：含有N-棕榈酰 - 丹宁的局部使用药理学准备
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。

2. 发明授权

US08546352B2 Pharmacological preparation for topical use containing N-palmitoyl-vanillamide 有权
标题翻译：含有N-棕榈酰 - 香草酰胺的局部用药物制剂
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。

3. 发明申请

US20110288037A1 Pharmaceutical Composition for the Treatment of Pathologies Caused by the General Response of the Immune System 审中-公开
标题翻译：用于治疗由免疫系统的一般反应引起的病理学的药物组合物
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。

4. 发明授权

US09512091B2 Compositions and methods for the modulation of specific amidases for N-acylethanolamines for use in the therapy of inflammatory diseases 有权
标题翻译：用于调节用于治疗炎性疾病的N-乙酰乙醇胺的特异性酰胺酶的组合物和方法
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.

5. 发明申请

US20150057269A1 COMPOSITIONS AND METHODS FOR THE MODULATION OF SPECIFIC AMIDASES FOR N-ACYLETHANOLAMINES FOR USE IN THE THERAPY OF INFLAMMATORY DISEASES 有权
标题翻译：用于调节用于治疗炎性疾病的N-乙酰氨基酚的特异性氨基甲酸酯的组合物和方法
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）

6. 发明授权

US07244767B2 N-acylvanillinamide derivatives capable of activating peripheral cannabinoid receptors 有权
标题翻译：能够激活外周大麻素受体的N-酰基万古林酰胺衍生物
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。

7. 发明申请

US20050065216A1 N-acylvanillinamide derivatives capable of activating peripheral cannabinoid receptors 有权
标题翻译：能够激活外周大麻素受体的N-酰基万古林酰胺衍生物
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。

8. 发明申请

US20100249223A1 NEW USE FOR CANNABINOID-CONTAINING PLANT EXTRACTS 审中-公开
标题翻译：用于含CANNABINOID的植物提取物的新用途
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。

9. 发明申请

US20070105940A1 Method for treating pain 审中-公开
标题翻译：治疗疼痛的方法
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。

10. 发明申请

US20070259945A1 METHOD FOR TREATING PAIN 审中-公开
标题翻译：治疗疼痛的方法
公开(公告)号：US20070259945A1
公开(公告)日：2007-11-08
申请号：US11549334
申请日：2006-10-13
申请人： Luciano De Petrocellis , Sabatino Malone , Vito De Novellis , Vincenzo Di Marzo
发明人： Luciano De Petrocellis , Sabatino Malone , Vito De Novellis , Vincenzo Di Marzo
IPC分类号： A61K31/40 , A61P25/02 , C07D209/00
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 X may be Y may be wherein R is H or (CH2)mH, alternatively the bond between X and Y may be a double or triple bond, e.g. X═Y or X≡Y; 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X可以是Y，其中R是H或（CH 2）或者X和Y之间的键可以是双键或三键，例如 X-Y或X≡Y; 其中n为1至10的整数，m为1至4的整数，链烯基酰胺链中的总碳原子数为约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。

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