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公开(公告)号：US10239839B2
公开(公告)日：2019-03-26
申请号：US15333766
申请日：2016-10-25
申请人： Solenne BV
IPC分类号： C07D221/02 , C07D221/18 , C07D471/06 , A61K8/49 , A61Q19/00
摘要： The present invention relates to compositions and methods of using free radical scavengers with reduced 1O2 generation. In certain embodiments, these compositions and methods of use relate to fullerene-derived ketolactams and fullerene-derived ketolactam derivatives, fullerene derivatives, and/or fullerenes. In yet other embodiments, the invention relates to cosmetic or dermatological compositions comprising said free radical scavengers with reduced 1O2 generation.
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2.发明申请公开(公告)号：US20180338965A1
公开(公告)日：2018-11-29
申请号：US15769789
申请日：2016-10-21
发明人： Pengfei Wang , Jiasheng Wu , Weimin Liu , Ying Gu , Jiechao Ge , Xiuli Zheng , Hongyan Zhang
IPC分类号： A61K31/473 , C07D221/02 , C07C225/32 , A61K31/122 , A61K31/135 , C07C50/36
摘要： The invention discloses a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, and a preparation method and application thereof. The amphiphilic hypocrellin derivative substituted by a group containing PEG, a quaternary ammonium salt or the like prepared according to the invention has an obvious red shift in its absorption spectrum and a significantly enhanced molar extinction coefficient, compared with the parent hypocrellin, can efficiently produce singlet state oxygen and other reactive oxygen species under photosensitive conditions; has different amphiphilicities and increased biocompatibility with cells or tissues by regulating its hydrophilicity and hydrophobicity; can meet the requirements of different clinical drugs, and solves the requirements of different drug delivery methods for different drug hydrophilicity and lipophilicity. Under identical conditions, the amphiphilic hypocrellin derivative photosensitizer according to the invention has higher ability to photodynamically inactivate tumor cells than the first and second generation commercial photosensitizers.
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公开(公告)号：USRE46695E1
公开(公告)日：2018-02-06
申请号：US14881790
申请日：2015-10-13
申请人： WILD Flavors, Inc.
发明人： Shaowen Wu , Chad Ford , Gregory Horn
CPC分类号： A23L5/48
摘要： A method of preparing colored products from edible materials comprises processing Genipa americana fruit juice, which contains genipin, genipin derivatives, or pre-genipin compounds, with other edible juices or extracts which contain nitrogenous compounds such as amino acids, polypeptides, or proteins. The generated natural colored products have excellent stability and can be used in a broad range of applications including beverages, foodstuffs, drugs, dietary supplements, cosmetics, personal care stuffs, and animal feeds.
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公开(公告)号：US09512119B2
公开(公告)日：2016-12-06
申请号：US14417488
申请日：2013-07-26
发明人： Keita Nagai , Motoaki Baba , Shinichi Fujioka , Koh Nagasawa , Hirobumi Takahashi , Eri Kondoh , Sachie Sogo , Kenichi Tanaka , Yoshiki Itoh
IPC分类号： C07D221/02 , C07D471/04 , C07D401/14 , C07D231/56 , C07D401/06 , C07D403/06 , C07D409/06 , C07D209/08 , C07D413/06
CPC分类号： C07D471/04 , C07D209/08 , C07D231/56 , C07D401/06 , C07D401/14 , C07D403/06 , C07D409/06 , C07D413/06
摘要： The present invention relates to a compound having an URAT1 inhibitory activity, and to an URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition containing the compound.More specifically, the present invention relates to a compound represented by the formula (I): wherein R1 is -Q1-A1 or the like; R2 is a hydrogen atom, a halogen atom, a lower alkyl group or the like; W1, W2, W3 and W4 are each independently a nitrogen atom or a methine group optionally having substituents, or the like; X and Y are each a single bond, an oxygen atom or the like; Z is a hydroxyl group or COOR3 or the like.
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公开(公告)号：US09505758B2
公开(公告)日：2016-11-29
申请号：US14920000
申请日：2015-10-22
发明人： Andrea Wolkerstorfer , Oliver Szolar , Norbert Handler , Helmut Buschmann , Stephen Cusack , Mark Smith , Sung-Sau So , Ronald Charles Hawley , Achyutharao Sidduri
IPC分类号： C07D471/04 , C07D221/02 , A61K31/4375 , A61K31/4985 , A61K45/06
CPC分类号： A61K31/519 , A61K31/4375 , A61K31/4985 , A61K31/513 , A61K45/06 , C07D401/04 , C07D471/02 , C07D471/04
摘要： The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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6.发明授权Antibiotic and anti-parasitic agents that modulate class II fructose 1,6-bisphosphate aldolase 有权调节二级果糖1,6-二磷酸醛缩酶的抗生素和抗寄生虫药物公开(公告)号：US09394254B2
公开(公告)日：2016-07-19
申请号：US14273411
申请日：2014-05-08
IPC分类号： C07D221/02 , C07D215/48 , A01N43/42 , C07D401/04 , C07D413/04 , C07D417/04 , C12Q1/527
CPC分类号： C07D215/48 , A01N43/42 , C07D401/04 , C07D413/04 , C07D417/04 , C12Q1/527 , G01N2333/988 , G01N2500/04
摘要： This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
摘要翻译： 本发明提供一种抑制II型果糖1,6-二磷酸醛缩酶（FBA）的化合物家族，其涉及广泛的细菌和寄生虫的致病活性。 通过实验检验鉴定出化合物，为进一步的8-羟基喹啉-2-羧酸衍生化和优化提供依据。 晶体结构显示这些化合物不直接与酶的催化位点结合，因此不被简单地定义为底物类似物。 相反，他们通过诱导拟合创建口袋，从而对FBA活动产生强大而具体的抑制作用。
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7.发明授权Indolizinone based derivatives as potential phosphodiesterase 3 (PDE3) inhibitors and a process for the preparation thereof 有权基于Indolizinone的衍生物作为潜在的磷酸二酯酶3（PDE3）抑制剂及其制备方法公开(公告)号：US09249139B2
公开(公告)日：2016-02-02
申请号：US14168370
申请日：2014-01-30
发明人： Budde Mahendar , Saidulu Mattapally , Mettu Ravinder , Sanjay Kumar Banerjee , Vaidya Jayathirtha Rao
IPC分类号： C07D221/02 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
摘要翻译： 本发明提供可用作潜在磷酸二酯酶3（PDE3）抑制剂的通式A的化合物及其制备方法。 式A的衍生物可用作人和兽医学中的治疗剂，其可用于例如治疗和预防以下疾病：心力衰竭，扩张型心肌病，血小板抑制剂，癌症和阻塞性肺疾病。
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8.发明授权Intermediate compounds and processes for the preparation of quinoline derivatives such as laquinimod sodium 有权用于制备喹啉衍生物如拉喹莫德钠的中间体化合物和方法公开(公告)号：US09102592B2
公开(公告)日：2015-08-11
申请号：US14471951
申请日：2014-08-28
申请人： MAPI PHARMA LTD.
发明人： Ehud Marom , Michael Mizhiritskii , Shai Rubnov
IPC分类号： C07D215/00 , C07D215/22 , C07C233/55 , C07C63/70 , C07C233/11 , C07D221/02 , C07C235/78 , C07C229/56
CPC分类号： C07C235/78 , C07C63/70 , C07C229/56 , C07C233/11 , C07C233/55 , C07D215/00 , C07D215/22
摘要： The present invention relates to processes for the preparation of quinoline-3-carboxamide derivatives, such as sodium 5-chloro-3-(ethylphenylcarbamoyl)-1-methyl-2-oxo-1,2-dihydroquinolin-4-olate (Laquinimod sodium). The present invention further relates to intermediates formed in such processes.
摘要翻译： 本发明涉及制备喹啉-3-甲酰胺衍生物的方法，例如5-氯-3-（乙基苯基氨基甲酰基）-1-甲基-2-氧代-1,2-二氢喹啉-4-醇酸钠（Laquinimod钠 ）。 本发明还涉及在这些方法中形成的中间体。
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公开(公告)号：US09090612B2
公开(公告)日：2015-07-28
申请号：US14267759
申请日：2014-05-01
申请人： CalciMedica, Inc.
发明人： Jeffrey P. Whitten , Yazhong Pei , Jianguo Cao , Zhijun Wang , Evan Rogers , Brian Dyck , Jonathan Grey
IPC分类号： C07D221/02 , C07D471/04 , C07C233/75 , C07C233/80 , C07C255/60 , C07D231/16 , C07D231/12 , C07D231/14 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07C233/92 , C07D213/81 , C07D231/18 , C07D231/56 , C07D263/57 , C07D277/34 , C07D277/56 , C07D317/62 , C07D333/38
CPC分类号： C07D417/12 , C07C233/75 , C07C233/80 , C07C233/92 , C07C255/60 , C07C2601/02 , C07D213/81 , C07D231/12 , C07D231/14 , C07D231/16 , C07D231/18 , C07D231/56 , C07D263/57 , C07D277/34 , C07D277/56 , C07D317/62 , C07D333/38 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
摘要翻译： 本文描述了含有这种化合物的化合物和药物组合物，其调节储存操作的钙（SOC）通道的活性。 本文还描述了使用这种SOC通道调节剂单独和与其它化合物组合用于治疗将受益于SOC通道活性抑制的疾病或病症的方法。
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公开(公告)号：US08912210B2
公开(公告)日：2014-12-16
申请号：US13293177
申请日：2011-11-10
申请人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
发明人： Ian M. Bell , Mark E. Fraley , Steven N. Gallicchio , Anthony Ginnetti , Helen J. Mitchell , Daniel V. Paone , Donnette D. Staas , Cheng Wang , C. Blair Zartman
IPC分类号： A01N43/42 , A61K31/44 , C07D221/02
CPC分类号： A61K31/4545 , A61K31/435 , A61K31/438 , C07D471/10 , C07D471/20
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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