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1. 发明授权

US11905267B2 High triplet yield phenothiazine donor-acceptor complexes for photoredox catalysis 有权
公开(公告)号：US11905267B2
公开(公告)日：2024-02-20
申请号：US17789874
申请日：2021-01-08
申请人： The Regents of the University of Colorado , Colorado State University Research Foundation
发明人： Steven Sartor , Niels Damrauer , Garet Miyake , Cameron Chrisman , Ryan Pearson
IPC分类号： C07D279/30 , C07D279/24
CPC分类号： C07D279/30 , C07D279/24
摘要： Phenothiazine compounds of Formula (I) are described herein. These compounds are useful as highly reducing organic photoredox catalysts. Suitable substrates for use with the compounds of Formula (I) include acrylates, styrene, acrylamides, acrylonitrile, vinyl chloride, methylacrylonitrile, vinyl acetate, and acrylic acid.

2. 发明申请

US20070116757A1 Methylene Blue Derivatives 审中-公开
标题翻译：亚甲基蓝衍生物
公开(公告)号：US20070116757A1
公开(公告)日：2007-05-24
申请号：US11557889
申请日：2006-11-08
申请人： Roman Rariy , Jane Hirsh
发明人： Roman Rariy , Jane Hirsh
IPC分类号： A61K31/5415 , C07D279/24 , A61K9/64 , A61K9/20
CPC分类号： C07D279/18 , A61K9/1617 , A61K31/5415 , C07D265/38 , C07D279/20
摘要： Pharmaceutical compositions comprising a fatty acid salt, a dicarboxylic acid salt, an alkyl sulfate salt, an aryl sulfate salt or an alkyl aryl sulfonate salt of methylene blue or a derivative of methylene blue are described herein. The compositions are preferably administered orally and can be administered as tablets, soft or hard shell capsules (e.g. soft gelatin capsules), suspensions or solutions. The composition can also be formulated as a suppository or enema or rectal administration. The compositions further comprise a pharmaceutically acceptable carrier and optionally one or more pharmaceutically acceptable excipients. Suitable excipients include diluents, binders, plasticizers, lubricants, disintegrants, colorants, stabilizers, surfactants, and combinations thereof. The fatty acid salts, alkyl sulate salts, aryl sulfate salts or alkyl aryl sulfonate salts can be co-mixed or co-melted with one or more fatty acids to make more hydrophobic compositions, which may result in less staining formulations. The compositions can be formulated for immediate release, controlled release such as extended release, delayed release, and pulsatile release, or combinations thereof. In one embodiment, the derivative of methylene blue is methylene dodecylsulfate.
摘要翻译：本文描述了包含脂肪酸盐，二羧酸盐，烷基硫酸盐，芳基硫酸盐或亚甲基蓝或亚甲基衍生物的烷基芳基磺酸盐的药物组合物。组合物优选口服施用，并且可以片剂，软或硬壳胶囊（例如软明胶胶囊），悬浮液或溶液给药。组合物也可以配制成栓剂或灌肠剂或直肠给药。组合物还包含药学上可接受的载体和任选的一种或多种药学上可接受的赋形剂。合适的赋形剂包括稀释剂，粘合剂，增塑剂，润滑剂，崩解剂，着色剂，稳定剂，表面活性剂及其组合。脂肪酸盐，烷基磺酸盐，芳基硫酸盐或烷基芳基磺酸盐可以与一种或多种脂肪酸共混或共熔，以制备更疏水的组合物，这可能导致较少的染色制剂。组合物可以配制成立即释放，控制释放，例如延长释放，延迟释放和脉动释放，或其组合。在一个实施方案中，亚甲基蓝的衍生物是十二烷基硫酸亚甲酯。

3. 发明申请

US20050220888A1 Controlled release compositions and methods for using same 审中-公开
标题翻译：控制释放组合物及其使用方法
公开(公告)号：US20050220888A1
公开(公告)日：2005-10-06
申请号：US10499996
申请日：2003-01-31
申请人： Lakahmi Putcha , Joe McDonough , Edward Boland , Hong Dixon , Joseph Persyn , Niraj Vasishtha
发明人： Lakahmi Putcha , Joe McDonough , Edward Boland , Hong Dixon , Joseph Persyn , Niraj Vasishtha
IPC分类号： A61K9/00 , A61K9/16 , A61K9/22 , A61K9/50 , A61K31/54 , A61P1/08 , A61P37/00 , C07D279/24
CPC分类号： A61K9/0043 , A61K9/1617 , A61K9/5047 , A61K31/54 , C07D279/24
摘要： Pharmaceutical preparations adapted for mucosal delivery, preferably for nasal delivery, which can be easily and safely used over days to weeks with minimal side effects. The pharmaceutical preparations comprise microcapsules comprising at least one pharmaceutically active agent. The microcapsules provide controlled release of the pharmaceutically active agent. Cytotoxicity is avoided for cytotoxic pharmaceutically active agents and/or for cytotoxic dosages by one or more of the following: (a) manipulating the mucosal transport rate of the pharmaceutically active agent through the mucosal bodies to achieve a transport rate which is substantially the same as the controlled release rate, and/or (b) selecting only a most active and/or less cytotoxic enantiomer of the pharmaceutically active agent for use in the pharmaceutical preparation.
摘要翻译：适于粘膜递送的药物制剂，优选用于鼻腔输送，其可以在几天至数周内容易且安全地使用，具有最小的副作用。药物制剂包含含有至少一种药物活性剂的微胶囊。微胶囊提供药物活性剂的受控释放。通过一种或多种以下方法避免细胞毒性药物活性剂和/或细胞毒性剂量的细胞毒性：（a）操纵药物活性剂通过粘膜体的粘膜转运速率，以实现基本上相同于控制释放速率，和/或（b）仅选择用于药物制剂的药物活性剂的最有活性和/或更少的细胞毒性对映异构体。

4. 发明授权

US5786141A Electrogenerated chemiluminescence labels for analysis and/or referencing 失效
标题翻译：电化学发光标记用于分析和/或参考
公开(公告)号：US5786141A
公开(公告)日：1998-07-28
申请号：US385864
申请日：1995-02-09
申请人： Allen J. Bard , Thomas Richards , Jonathan K. Leland
发明人： Allen J. Bard , Thomas Richards , Jonathan K. Leland
IPC分类号： G01N33/532 , C07D279/24 , C07H19/04 , C09K11/07 , C12N15/09 , C12Q1/00 , C12Q1/68 , C12Q1/70 , G01N21/76 , G01N21/78 , G01N27/00 , G01N33/483 , G01N33/53 , G01N33/543 , G01N33/58 , G01N37/00 , C12P19/34
CPC分类号： C12Q1/005 , C12Q1/6816 , C12Q1/6825 , C12Q1/6869 , G01N33/582
摘要： Biomolecule analysis using anodic oxidation of aqueous sodium 9, 10-diphenylanthracene-2-sulfonate (DPAS) and 1- and 2-thianthrenecarboxylic acid (1-THCOOH and 2-THCOOH) in the presence of tri-n-propylamine (TPrA) as a coreactant in aqueous solution produces electrogenerated chemiluminescence (ECL). In addition, the cathodic reduction of DPAS in the presence of peroxydisulfate (S.sub.2 O.sub.8.sup.2-) as a coreactant also produces ECL in an acetonitrile (MeCN)-water solution (1:1 by volume). The oxidation of chlorpromazine (CPZ) produces an ECL emission in the absence of an added coreactant following an unprecedented "self-annihilation" mechanism.
摘要翻译：在三正丙胺（TPrA）存在下，使用9,10-二苯基蒽-2-磺酸钠（DPAS）和1-和2-噻吩甲酸（1-THCOOH和2-THCOOH）的水溶液阳极氧化的生物分子分析水溶液中的共反应物产生电致化学发光（ECL）。此外，DPAS在作为共反应物的过氧化二硫酸酯（S2O82-）存在下的阴极还原还在乙腈（MeCN） - 水溶液（体积比1:1）中产生ECL。氯丙嗪（CPZ）的氧化在没有加入的共反应物的情况下，在空前的“自我消灭”机制之后产生ECL排放。

5. 发明授权

US4892878A Oleic acid esters and pharmaceutical compositions 失效
标题翻译：油酸酯和药物组合物
公开(公告)号：US4892878A
公开(公告)日：1990-01-09
申请号：US124819
申请日：1987-11-24
申请人： Klaus G. Jensen , Peter Bregnedal
发明人： Klaus G. Jensen , Peter Bregnedal
IPC分类号： C07D279/24 , A61K31/00 , A61K31/445 , A61K31/451 , A61P25/24 , A61P25/26 , A61P43/00 , C07D211/52 , C07D279/28 , C07D335/20 , C07D521/00
CPC分类号： C07D335/20 , C07D211/52 , C07D279/28
摘要： The present invention relates to pharmaceutical compositions of novel oleic acid esters of wellknown neuroleptics and tranquillizers of the phenothiazine, thioxanthene and butyrophenone type containing an aliphatic hydroxy group, and which may be represented by the following general formula: ##STR1## wherein R represents the residue of a hydroxy group containing neuroleptic selected from phenothiazines, thioxanthenes and butyrophenones, as well as pharmaceutically acceptable acid additions salts thereof, which compositions take the form of injectable solutions or suspensions in propylene glycol dioleate (TS-RD-9), methyl oleate or ethyl oleate.None of the esters of Formula I have been specifically described before but have only been broadly disclosed in the patent literature, and the esters as such, as well as a method of preparation of said esters, fall within the scope of the present invention.
摘要翻译：本发明涉及含有脂肪族羟基的吩噻嗪，噻吨酮和丁酰苯胺等众所周知的神经安定药和镇静剂的新型油酸酯的药物组合物，其可以由以下通式表示：其中R表示含有选自吩噻嗪，噻吨酮和丁酰苯的精氨酸的羟基的残基，以及其药学上可接受的酸加成盐，该组合物采用注射溶液或悬浮液形式的丙二醇二油酸酯（TS-RD-9），油酸甲酯或油酸乙酯。式I的酯都没有在前面被具体描述，但是在专利文献中仅被广泛地公开，并且酯本身以及所述酯的制备方法都在本发明的范围内。

6. 发明授权

US3147255A Phenothiazine derivatives 失效
标题翻译：吩噻嗪衍生物
公开(公告)号：US3147255A
公开(公告)日：1964-09-01
申请号：US78532559
申请日：1959-01-07
申请人： GRACE W R & CO
发明人： BERNARD RUDNER , PRAPAS ARISTOTLE G
IPC分类号： C07D279/24
CPC分类号： C07D279/24

7. 发明授权

US3055890A Phenthiazine derivatives 失效
标题翻译：苯噻嗪衍生物
公开(公告)号：US3055890A
公开(公告)日：1962-09-25
申请号：US78667159
申请日：1959-01-14
申请人： RHONE POULENC SA
发明人： MICHEL JACOB ROBERT , JACQUES HORCLOIS RAYMOND
IPC分类号： C07D279/24
CPC分类号： C07D279/24

8. 发明申请

US20190031639A1 ZUCLOPENTHIXOL HYDROCHLORIDE DERIVATIVES AND EBSELEN DERIVATIVES AS ERBB2 INHIBITORS 审中-公开
公开(公告)号：US20190031639A1
公开(公告)日：2019-01-31
申请号：US16069049
申请日：2017-01-11
申请人： Centre National De La Recherche Scientifique (CNRS) , Institut National de la Sante et de la Recherche Medicale (INSERM) , Universite Paris Descartes
发明人： Sandrine Bourdoulous , Camille Faure
IPC分类号： C07D335/20 , C07D409/06 , C07D405/06 , C07D279/24 , C07D293/12 , C07D275/04 , A61P35/00
CPC分类号： C07D335/20 , A61K31/41 , A61K31/497 , A61P35/00 , C07D275/04 , C07D279/24 , C07D293/12 , C07D405/06 , C07D409/06
摘要： The present invention relates to compounds of the following general formula (I) or (II): or a pharmaceutically acceptable salt and/or solvate thereof, for use in the treatment and/or in the prevention of ErbB2 dependent cancers, and pharmaceutical compositions containing such compounds.

9. 发明申请

US20090176745A1 TRIARYLMETHANE ANALOGS AND THEIR USE IN TREATING CANCERS 审中-公开
标题翻译：三叉戟类似物及其在治疗癌症中的应用
公开(公告)号：US20090176745A1
公开(公告)日：2009-07-09
申请号：US12345652
申请日：2008-12-29
申请人： Jack L. Arbiser
发明人： Jack L. Arbiser
IPC分类号： A61K31/662 , C07D223/28 , A61K31/55 , C07F9/40 , A61K31/47 , C07D215/26 , C07D279/24 , A61K31/54 , A61K31/553 , C07D413/04 , A61P35/00
CPC分类号： A61K31/55 , A61K9/127 , A61K31/136 , A61K31/14 , A61K31/353 , A61K31/404 , A61K31/422 , A61K31/428 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/54 , A61K31/553 , A61K31/662 , C07D215/26 , C07D215/46 , C07D223/26 , C07D223/28 , C07D263/32 , C07D275/06 , C07D279/28 , C07D311/36 , C07F9/4056 , C07F9/4059 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415
摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.
摘要翻译：公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。化合物是三苯甲烷类似物。化合物和组合物可用于治疗和/或预防多种癌症，包括耐药性癌症，炎性，退行性和血管性疾病，包括各种眼部疾病和寄生虫感染。代表性的三苯甲烷类似物包括各种染料，激素，糖，肽，寡核苷酸，氨基酸，核苷酸，核苷和多元醇的三苯基甲烷类似物。据信这些化合物通过抑制tNOX表达，ROS的作用和/或HIF2的产生起作用。因此，这些化合物是用于各种癌症和其它疾病的新型治疗剂。

10. 发明申请

US20070282100A1 Boronic ester and acid compounds, synthesis and uses 审中-公开
标题翻译：硼酸酯和酸化合物，合成和用途
公开(公告)号：US20070282100A1
公开(公告)日：2007-12-06
申请号：US11642372
申请日：2006-12-20
申请人： Julian Adams , Yu-Ting Ma , Ross Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
发明人： Julian Adams , Yu-Ting Ma , Ross Stein , Matthew Baevsky , Louis Grenier , Louis Plamondon
IPC分类号： C07D279/24 , C07D265/34 , C07D473/02 , C07D475/02
CPC分类号： C07K5/0808 , A61K38/00 , C07F5/025 , C07F5/04 , C07K5/06 , C07K5/06043 , C07K5/06139 , C07K5/06191 , C07K5/0827
摘要： Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
摘要翻译：本文公开了一种降低动物中蛋白质降解速率的方法，包括使动物细胞与某些硼酸酯和酸化合物接触。本文还公开了新的硼酸酯和酸化合物，它们的合成和用途。

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