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1.发明授权Compositions and methods for the modulation of specific amidases for N-acylethanolamines for use in the therapy of inflammatory diseases 有权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.
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公开(公告)号：US08470373B2
公开(公告)日：2013-06-25
申请号：US13120408
申请日：2009-09-07
IPC分类号： A61K9/1694
CPC分类号： A61K9/14 , A61K9/0056 , A61K9/0095 , A61K9/2013 , A61K9/209 , A61K9/4858 , A61K31/05 , A61K31/16 , A61K31/164 , A61K31/352 , Y02A50/40 , A61K2300/00
摘要： The present invention relates to a composition for pharmaceutical or veterinary use, comprising palmitoylethanolamide. In particular, the present invention relates to a pharmaceutical composition for human or veterinary use, containing a therapeutically efficient amount of palmitoylethanolamide in the ultra-micronized form, wherein more than 90% by weight of palmitoylethanolamide has particle sizes lower than 6 microns, together with pharmaceutically acceptable excipients.
摘要翻译： 本发明涉及用于药物或兽医用途的组合物，其包含棕榈酰乙醇酰胺。 特别地，本发明涉及一种用于人或兽用药物的药物组合物，其含有超微粉化形式的治疗有效量的棕榈酰乙醇酰胺，其中超过90重量％的棕榈酰乙醇酰胺具有小于6微米的粒度，以及 药学上可接受的赋形剂。
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3.发明申请Pharmaceutical Composition for the Treatment of Pathologies Caused by the General Response of the Immune System 审中-公开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。
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4.发明授权Covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids functionally active on the CB2 cannabinoid receptor 有权单羧酸和二羧酸的链烷醇酰胺的共价衍生物在CB2大麻素受体上功能活性公开(公告)号：US06864285B1
公开(公告)日：2005-03-08
申请号：US10030061
申请日：1999-07-07
IPC分类号： A61P43/00 , C07C233/18 , C07C235/74 , C07C271/12 , C07C271/22 , C07D295/088 , C07D307/20 , A61K43/00 , C07C233/00
CPC分类号： C07D295/088 , C07C233/18 , C07C235/74 , C07C271/12 , C07C271/22 , C07D307/20
摘要： The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor
摘要翻译： 本发明涉及一元羧酸和二羧酸的链烷醇酰胺与通式（I）的氨基醇的新型共价衍生物，其可有效地用作CB2大麻素受体的激动剂，因此作为在病理状态下活性的药物，其可以通过刺激和 /或共刺激该受体
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公开(公告)号：US08288361B2
公开(公告)日：2012-10-16
申请号：US11406852
申请日：2006-04-19
IPC分类号： A01N43/04 , A61K31/715
CPC分类号： A61K31/047 , A61K31/164 , A61K31/194 , A61K2300/00
摘要： The present invention relates to a pharmaceutical composition, for human and veterinary use, that may be used to induce, potentiate and normalise the various phases of the tissue repair process triggered following ulceration and wounding—either involving the loss of matter or not—of neurogenic, vasogenic or traumatic origin, even in cases where the lesions are directly or indirectly associated with underlying systemic pathologies.Particularly, the present invention relates to a pharmaceutical composition comprising an N-acyl derivative of an amino alcohol belonging to the ALIAmides class of molecules, a polyhydroxy alcohol and trans-traumatic acid or a derivative thereof.
摘要翻译： 本发明涉及一种用于人类和兽医用途的药物组合物，其可用于诱导，增强和归一化溃疡和创伤后触发的组织修复过程的各个阶段 - 涉及物质的损失或非神经源性 ，血管性或创伤性起源，即使在病变与潜在的全身病理学直接或间接相关的情况下。 特别地，本发明涉及包含属于分子的ALIAmides类的氨基醇的N-酰基衍生物，多羟基醇和反式外伤性酸或其衍生物的药物组合物。
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公开(公告)号：US20110171313A1
公开(公告)日：2011-07-14
申请号：US13120408
申请日：2009-09-07
IPC分类号： A61K9/14 , A61K31/164 , A61P43/00
CPC分类号： A61K9/14 , A61K9/0056 , A61K9/0095 , A61K9/2013 , A61K9/209 , A61K9/4858 , A61K31/05 , A61K31/16 , A61K31/164 , A61K31/352 , Y02A50/40 , A61K2300/00
摘要： The present invention relates to a composition for pharmaceutical or veterinary use, comprising palmitoylethanolamide. In particular, the present invention relates to a pharmaceutical composition for human or veterinary use, containing a therapeutically efficient amount of palmitoylethanolamide in the ultra-micronized form, wherein more than 90% by weight of palmitoylethanolamide has particle sizes lower than 6 microns, together with pharmaceutically acceptable excipients.
摘要翻译： 本发明涉及用于药物或兽医用途的组合物，其包含棕榈酰乙醇酰胺。 特别地，本发明涉及一种用于人或兽用药物的药物组合物，其含有超微粉化形式的治疗有效量的棕榈酰乙醇酰胺，其中超过90重量％的棕榈酰乙醇酰胺具有小于6微米的粒度，以及 药学上可接受的赋形剂。
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7.发明授权Pharmaceutical compositions containing N-palmitoylethanolamide and use thereof in the veterinary field 有权含有N-棕榈酰乙醇酰胺的药物组合物及其在兽医领域中的应用公开(公告)号：US06548550B1
公开(公告)日：2003-04-15
申请号：US10030060
申请日：2002-01-04
IPC分类号： A61K3116
CPC分类号： A61K31/16
摘要： The present invention relates to a method for treating eosinophilic granuloma in a Feline comprising administering a pharmaceutical composition, the composition comprising N-palmitoylethanolamide. The present invention also relates to said pharmaceutical composition and the process for the preparation thereof.
摘要翻译： 本发明涉及一种用于治疗猫科动物嗜酸粒细胞肉芽肿的方法，其包括施用药物组合物，所述组合物包含N-棕榈酰乙醇酰胺。 本发明还涉及所述药物组合物及其制备方法。
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8.发明申请COMPOSITIONS AND METHODS FOR THE MODULATION OF SPECIFIC AMIDASES FOR N-ACYLETHANOLAMINES FOR USE IN THE THERAPY OF INFLAMMATORY DISEASES 有权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）
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9.发明授权Pharmacological preparation for topical use containing N-palmitoyl-vanillamide 有权含有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。
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10.发明申请USE OF AMIDES OF MONO- AND DICARBOXYLIC ACIDS IN THE TREATMENT OF RENAL DISEASES 审中-公开单一和二羧酸用于治疗肾病的用途公开(公告)号：US20120083533A1
公开(公告)日：2012-04-05
申请号：US13251871
申请日：2011-10-03
IPC分类号： A61K31/164 , A61P19/04 , A61P13/12 , C07C235/08 , C07C233/20
CPC分类号： A61K31/164 , A61K31/198
摘要： A therapy for renal diseases, in particular renal diseases which develop in diabetic patients or patients who have been subjected to a treatment with an antitumor chemotherapy such as a platinum derivative and more generally cytotoxic drugs at renal level for treating of neoplastic diseases. More particularly, the present invention relates to palmitoylethanolamide and diethanolamide of fumaric acid for use in the treatment of renal diseases, in particular those caused by dysmetabolic diseases or by toxic or chemotherapy agents, such as platinum derivatives. Palmitoylethanolamide is used preferably in micronized or ultra-micronized form. Diethanolamide of fumaric acid is used preferably in aqueous solution.
摘要翻译： 一种治疗肾脏疾病，特别是在糖尿病患者中发展的肾脏疾病或已经用抗肿瘤化学疗法例如铂衍生物治疗的患者，以及更常见的用于肾脏水平的细胞毒性药物治疗肿瘤性疾病的患者。 更具体地说，本发明涉及富马酸的棕榈酰乙醇酰胺和二乙醇酰胺，用于治疗肾脏疾病，特别是由代谢异常疾病引起的或通过有毒或化学药剂如铂衍生物。 棕榈酰乙醇酰胺优选以微粉化或超微粉化形式使用。 富马酸的二乙醇酰胺优选在水溶液中使用。
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