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1. 发明申请

WO2014023643A1 MULTITARGET FAAH AND COX INHIBITORS AND THERAPEUTICAL USES THEREOF 审中-公开
标题翻译： MULTITARGET FAAH和COX抑制剂及其治疗用途
公开(公告)号：WO2014023643A1
公开(公告)日：2014-02-13
申请号：PCT/EP2013/066197
申请日：2013-08-01
申请人： FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , ALMA MATER STUDIORUM - UNIVERSITA' DI BOLOGNA
发明人： DE VIVO, Marco , SCARPELLI, Rita , CAVALLI, Andrea , MIGLIORE, Marco , PIOMELLI, Daniele , HABRANT, Damien , FAVIA, Angelo
IPC分类号： C07C271/28 , C07C271/42 , C07C271/44 , C07C271/56 , C07C271/58 , A61K31/325 , A61P35/00
CPC分类号： C07C271/56 , C07C271/28 , C07C271/44 , C07C271/58 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The invention provides novel multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. The invention concerns also with therapeutical application of the multitarget inhibitors in particular in the prevention and treatment of cancer.
摘要翻译：本发明提供了新的具有特定氨基甲酸酯部分的脂肪酸酰胺水解酶（FAAH），环氧合酶-1（COX-1）和/或环氧合酶-2（COX-2）的多靶点抑制剂取代的联苯核心的A环的间位或邻位，并且在联苯核心的B环的邻位具有卤素。本发明还涉及多靶点抑制剂在治疗癌症的预防和治疗中的应用。

2. 发明申请

WO2013149250A1 METHODS OF TREATMENT, DIAGNOSIS AND MONITORING FOR METHAMPHETAMINE TOXICITY WHICH TARGET CERAMIDE METABOLIC PATHWAYS AND CELLULAR SENESCENCE 审中-公开
标题翻译：治疗，诊断和监测甲磺平胺毒性的方法，其中目标氨基酸代谢途径和细胞敏感性
公开(公告)号：WO2013149250A1
公开(公告)日：2013-10-03
申请号：PCT/US2013/034834
申请日：2013-04-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA
发明人： PIOMELLI, Daniele , ASTARITA, Giuseppe , AVANESIAN, Agnesa , CAVALLI, Andrea
IPC分类号： A61K31/138
CPC分类号： A61K31/4152 , A61K31/095 , A61K31/137 , A61K31/195 , A61K31/201 , A61K31/42 , A61K31/4458 , A61K31/454
摘要： Methamphetamine is a highly addictive psychostimulant that causes profound damage to the brain and other body organs. Post mortem studies of human tissues have linked the use of this drug to diseases associated with aging, such as coronary atherosclerosis, but the molecular mechanism underlying these findings remains unknown. We report now that methamphetamine accelerates cellular senescence in vitro and activates transcription of genes involved in cell-cycle control and inflammation in vivo by stimulating production of the sphingolipid messenger ceramide. This pathogenic cascade is triggered by reactive oxygen species, generated through methamphetamine metabolism via cytochrome Pas0-2D6, which recruit nuclear factor (NF)-KB to induce expression of enzymes in the de novo pathway of ceramide biosynthesis. Inhibitors of ceramide formation prevent methamphetamine-induced senescence and attenuate systemic inflammation and health deterioration in rats self- administering the drug. The results support therapeutic approaches to reduce the adverse consequences of methamphetamine abuse and improve effectiveness of treatments.
摘要翻译：甲基苯丙胺是一种高度上瘾的精神兴奋剂，会对大脑和其他身体器官造成深刻的伤害。人类组织的死后研究已经将这种药物与衰老相关的疾病（如冠状动脉粥样硬化）联系在一起，但是这些发现的分子机制仍然是未知的。我们现在报告说，甲基苯丙胺在体外加速细胞衰老，并通过刺激神经鞘脂信使神经酰胺的产生来激活参与细胞周期控制和体内炎症的基因的转录。这种致病性级联由活性氧引发，通过细胞色素Pas0-2D6通过甲基苯丙胺代谢产生，其募集核因子（NF）-KB以诱导神经酰胺生物合成的从头途径中的酶的表达。神经酰胺形成抑制剂可以预防甲基苯丙胺诱导的衰老并减轻大鼠自身给药的全身炎症和健康恶化。结果支持减少甲基苯丙胺滥用的不良后果并提高治疗效果的治疗方法。

3. 发明申请

WO2005115370A2 COMPOUNDS AND METHODS FOR TREATING NON-INFLAMMATORY PAIN USING PPARALPHA AGONISTS 审中-公开
标题翻译：使用PPARALPHA激动剂治疗非炎性疼痛的化合物和方法
公开(公告)号：WO2005115370A2
公开(公告)日：2005-12-08
申请号：PCT/US2005/013858
申请日：2005-04-22
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , LOVERME, Jesse
发明人： PIOMELLI, Daniele , LOVERME, Jesse
IPC分类号： A61K31/192
CPC分类号： A61K31/192
摘要： Compositions and methods for treating noninflammatory pain, including but not limited to, neuropathic pain by using peroxisome proliferator activated receptor a (PPARa) agonists to treat a subject having such pain are described. The agonists may be used with additional therapeutic agents such as an inhibitor of fatty acid amide hydrolase or a cannabinoid CB1 or CB2 cannabinoid receptor agonist.
摘要翻译：描述了通过使用过氧化物酶体增殖物激活受体a（PPARα）激动剂治疗非炎性疼痛的组合物和方法，包括但不限于神经性疼痛，以治疗患有这种疼痛的受试者。激动剂可以与其它治疗剂一起使用，例如脂肪酸酰胺水解酶抑制剂或大麻素CB1或CB2大麻素受体激动剂。

4. 发明申请

WO2005046580A2 DIETARY AND OTHER COMPOSITIONS, COMPOUNDS, AND METHODS FOR REDUCING BODY FAT, CONTROLLING APPETITE, AND MODULATING FATTY ACID METABOLISM 审中-公开
标题翻译：膳食和其他组合物，化合物和减少身体脂肪的方法，控制适应症和调节脂肪酸代谢
公开(公告)号：WO2005046580A2
公开(公告)日：2005-05-26
申请号：PCT/US2004/034609
申请日：2004-10-18
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
发明人： PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
IPC分类号： A61K
CPC分类号： A61K31/164 , A23L33/12 , A23V2002/00 , A61K31/16 , A23V2250/188 , A23V2200/332 , A23V2250/186 , A23V2250/1872 , A23V2250/1874
摘要： Methods, pharmaceutical, dietary supplement, and nutraceutical compositions, and compounds for reducing body weight, modulating body lipid metabolism, and reducing food intake in mammals are provided. The compounds of the invention include fatty acid ethanolamide compounds, homologues and analogs of which the prototype is the endogenous fatty acid ethanolamide, oleoylethanolamide.
摘要翻译：提供了方法，药物，膳食补充剂和营养保健组合物，以及用于减少体重，调节体内脂质代谢和减少哺乳动物食物摄入的化合物。本发明的化合物包括脂肪酸乙醇酰胺化合物，其原型是内源性脂肪酸乙醇酰胺的同系物和类似物，油基乙醇酰胺。

5. 发明申请

WO2015173168A1 BENZOXAZOLONE DERIVATIVES AS ACID CERAMIDASE INHIBITORS, AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：作为酸性陶瓷抑制剂的苯并吖唑酮衍生物及其作为药物使用
公开(公告)号：WO2015173168A1
公开(公告)日：2015-11-19
申请号：PCT/EP2015/060291
申请日：2015-05-11
申请人： FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： PIOMELLI, Daniele , PAGLIUCA, Chiara , PIZZIRANI, Daniela , BACH, Anders , REALINI, Natalia , DE VIVO, Marco
IPC分类号： C07D413/12 , A61K31/423 , A61K31/4439 , C07D263/58 , A61P35/00 , A61P29/00 , A61P11/00
CPC分类号： A61K31/423 , A61K31/4439 , A61K45/06 , C07D263/58 , C07D413/12
摘要： The present invention relates to benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides benzoxazolone derivatives for use as a medicament in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.
摘要翻译：本发明涉及作为酸性神经酰胺酶抑制剂的苯并恶唑酮衍生物，含有这些抑制剂的药物组合物和抑制酸性神经酰胺酶用于治疗神经酰胺水平调节临床相关的疾病的方法。本发明还提供了用作治疗癌症，炎症，疼痛，炎性疼痛或肺部疾病的药物的苯并恶唑酮衍生物。

6. 发明申请

WO2015007615A1 PHENYL CARBAMATES AND THEIR USE AS INHIBITORS OF THE FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME AND MODULATORS OF THE D3 DOPAMINE RECEPTOR (D3DR) 审中-公开
标题翻译：苯甲酸酯及其作为D3多巴胺受体（D3DR）的脂肪酸酰胺水解酶（FAAH）酶和调节剂的抑制剂
公开(公告)号：WO2015007615A1
公开(公告)日：2015-01-22
申请号：PCT/EP2014/064853
申请日：2014-07-10
申请人： FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： BOTTEGONI, Giovanni , DE SIMONE, Alessio , RUDA, Gian Filippo , CAVALLI, Andrea , BANDIERA, Tiziano , PIOMELLI, Daniele
IPC分类号： C07D209/88 , C07D211/38 , C07D213/30 , C07D295/125 , C07D295/13 , A61K31/495 , A61K31/496 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30
CPC分类号： C07D295/13 , C07D209/88 , C07D211/14 , C07D211/38 , C07D213/30 , C07D295/125
摘要： The invention provides compounds of Formula (I) or pharmaceutically acceptable salts thereof wherein Ar', R 1 , R 2 , R 3 , R 4 , X, Y are as defined in the description of invention, as multi-target directed ligands (MTDLs) that are at the same time inhibitors of the fatty acid amide hydrolase (FAAH) enzyme and modulators of the D3 dopamine receptor (D3DR), their methods of preparation, formulations and therapeutic applications thereof.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中Ar'，R 1，R 2，R 3，R 4，X，Y如发明描述中所定义，为多靶向配体（MTDL）同时抑制脂肪酸酰胺水解酶（FAAH）酶和D3多巴胺受体（D3DR）的调节剂，其制备方法，制剂及其治疗应用。

7. 发明申请

WO2012167133A2 INHIBITORS OF ANANDAMIDE TRANSPORT AND THEIR THERAPEUTIC USES 审中-公开
标题翻译： ANANDAMIDE运输的抑制剂及其治疗用途
公开(公告)号：WO2012167133A2
公开(公告)日：2012-12-06
申请号：PCT/US2012/040531
申请日：2012-06-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , IIT - ISTITUTO ITALIANO DI TECNOLOGIA , PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
发明人： PIOMELLI, Daniele , FU, Jin , BOTTEGONI, Giovanni , CAVALLI, Andrea , BANDIERA, Tiziano
IPC分类号： A61K31/502 , A61K31/495 , A61P29/00 , A61P25/00
CPC分类号： C07D237/34 , A61K31/495 , A61K31/502 , C07K14/435 , C12N15/11 , G01N33/5008
摘要： Nucleic acid and polypeptide sequences corresponding to FLAT, a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1), are provided. FLAT lacks amidase activity but binds the endocannibinoid anandamide and facilitates its transport into cells. A chemical scaffold for the inhibition of anandamide transport is identified. Compositions of the invention prevent anandamide internalization in vitro, interrupt anandamide deactivation in vivo, and cause profound CB1 cannabinoid receptor-mediated analgesia in a mouse model of inflammatory pain. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the modulation of anandamide transport would be of benefit.
摘要翻译：提供了对应于FLAT，细胞内anandamide降解酶的部分胞质变体，脂肪酸酰胺水解酶-1（FAAH-1）的核酸和多肽序列。 FLAT没有酰胺酶活性，但是结合内源性抗生素Aandamide并促进其转运到细胞中。鉴定了用于抑制anandamide转运的化学支架。本发明的组合物在体外阻止氨酰胺内化，在体内中断anandamide失活，并在炎症性疼痛的小鼠模型中引起严重的CB1大麻素受体介导的镇痛。因此，本发明还提供了用于治疗其中调节anandamide转运有益的病症的方法和药物组合物。

8. 发明申请

WO2012015704A3 PERIPHERALLY RESTRICTED FAAH INHIBITORS 审中-公开
公开(公告)号：WO2012015704A3
公开(公告)日：2012-02-02
申请号：PCT/US2011/045114
申请日：2011-07-22
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , UNIVERSITA DEGLI STUDI DI URBINO "CARLO BO" , UNIVERSITA DEGLI STUDI DI PARMA , PIOMELLI, Daniele , CLAPPER, Jason, R. , MORENO-SANZ, Guillermo , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio
发明人： PIOMELLI, Daniele , CLAPPER, Jason, R. , MORENO-SANZ, Guillermo , DURANTI, Andrea , TONTINI, Andrea , MOR, Marco , TARZIA, Giorgio
IPC分类号： C07C271/56 , A61K31/27 , A61P29/00 , A61P37/00
摘要： Peripherally restricted inhibitors of fatty acid amide hydrolase (FAAH) are provided. The compounds can suppress FAAH activity and increases anandamide levels outside the central nervous system (CNS). Despite their relative inability to access brain and spinal cord, the compounds attenuate behavioral responses indicative of persistent pain in rodent models of inflammation and peripheral nerve injury, and suppresses noxious stimulus-evoked neuronal activation in spinal cord regions implicated in nociceptive processing. CBi receptor blockade prevents these effects. Accordingly, the invention also provides methods, and pharmaceutical compositions for treating conditions in which the inhibition of peripheral FAAH would be of benefit. The compounds of the invention are according to the formula (I): in which R 1 is a polar group. In some embodiments, R 1 is selected from the group consisting of hydroxy and the physiologically hydro lysable esters thereof. R 2 and R 3 are independently selected from the group consisting of hydrogen and substituted or unsubstituted hydrocarbyl; each R 4 is independently selected from the group consisting of halogen and substituted or unsubstituted hydrocarbyl and n is an integer from 0 to 4; each R 5 is independently selected from the group consisting of halo and substituted or unsubstituted hydrocarbyl and m is an integer from 0 to 3; and R 6 is substituted or unsubstituted cyclohexyl; and the pharmaceutically acceptable salts thereof.

9. 发明申请

WO2002080860A3 METHODS, COMPOUNDS, AND COMPOSITIONS FOR REDUCING BODY FAT AND MODULATING FATTY ACID METABOLISM 审中-公开
公开(公告)号：WO2002080860A3
公开(公告)日：2002-10-17
申请号：PCT/US2002/009773
申请日：2002-03-27
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
发明人： PIOMELLI, Daniele , DE FONSECA, Fernando, Rodriguez
IPC分类号： A61K31/16
摘要： Methods, pharmaceutical compositions, and compounds for reducing body weight (figure 5), modulating body lipid metabolism, and reducing food intake in mammals are provided. The compounds of the invention include fatty acid ethanolamide compounds, homologues and analogs of which the prototype is the endogenous fatty acid ethanolamide, oleoylethanolamide.

10. 发明申请

WO2015173169A1 SUBSTITUTED BENZOXAZOLONE DERIVATIVES AS ACID CERAMIDASE INHIBITORS, AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：作为酸性陶瓷酶抑制剂的替代苄基苯甲酮衍生物及其作为药物使用
公开(公告)号：WO2015173169A1
公开(公告)日：2015-11-19
申请号：PCT/EP2015/060292
申请日：2015-05-11
申请人： FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA , THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , UNIVERSITA' DEGLI STUDI DI PARMA
发明人： PIOMELLI, Daniele , PIZZIRANI, Daniela , BACH, Anders , SCARPELLI, Rita , MELZIG, Laurin , MOR, Marco
IPC分类号： C07D263/58 , A61K31/423 , A61P35/00
CPC分类号： A61K31/421 , C07D263/58
摘要： The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.
摘要翻译：本发明涉及取代的苯并恶唑酮衍生物作为酸性神经酰胺酶抑制剂，含有这些抑制剂的药物组合物和抑制酸性神经酰胺酶用于治疗神经酰胺水平调节临床相关的疾病的方法。本发明还提供了用于治疗癌症，炎症，疼痛，炎性疼痛或肺部疾病的取代的苯并恶唑酮衍生物。

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