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31. 发明申请

US20140206889A1 NOVEL MANGROMICIN COMPOUND AND PRODUCTION METHOD THEREFOR 有权
标题翻译：新型合成化合物及其生产方法
公开(公告)号：US20140206889A1
公开(公告)日：2014-07-24
申请号：US14342311
申请日：2012-08-31
申请人： Satoshi Omura , Yoko Takahashi , Takuji Nakashima , Kazuhiko Otoguro , Kazuro Shiomi , Masato Iwatsuki , Atsuko Matsumoto
发明人： Satoshi Omura , Yoko Takahashi , Takuji Nakashima , Kazuhiko Otoguro , Kazuro Shiomi , Masato Iwatsuki , Atsuko Matsumoto
IPC分类号： C07D493/16 , C12R1/01 , C12P17/18
CPC分类号： C07D493/16 , C07D493/18 , C12P17/181 , C12R1/01
摘要： [Problem]The present invention addresses the problem of providing an anti-trypanosomal drug having a novel skeleton, in order to solve issues that occur with conventional technologies.[Solution]The present invention is based on the discovery of a microbe that produces an anti-trypanosomal drug having a novel skeleton. Specifically, this invention provides: a compound indicated by formula (I) having a trypanosomal inhibitory activity; an analog thereof; a production method therefor; and a Lechevalieria sp. Kl0-0216 strain that produces said compound.
摘要翻译：本发明解决提供具有新骨架的抗锥虫毒素药物的问题，以解决常规技术中出现的问题。 [解决方案]本发明是基于产生具有新骨架的抗锥虫药物的微生物的发现。具体地，本发明提供：具有锥虫体抑制活性的式（I）表示的化合物; 其类似物; 一种生产方法; 和Lechevalieria sp。产生所述化合物的Kl0-0216菌株。

32. 发明申请

US20140005416A1 SYNTHETIC TRANSTAGANOLIDE AND BASILIOLIDE PRODUCTS, DERIVATIVES THEREOF, AND SYNTHESIS METHODS THEREOF 有权
标题翻译：合成三羟甲基氨丙菊酯和赖氨酸产品，其衍生物及其合成方法
公开(公告)号：US20140005416A1
公开(公告)日：2014-01-02
申请号：US13929425
申请日：2013-06-27
申请人： California Institute of Technology
发明人： Hosea Nelson , Kei Murakami , Scott C. Virgil , Brian M. Stoltz , Jonathan R. Gordon
IPC分类号： C07D493/16 , C07D493/08
CPC分类号： C07D311/00 , C07D493/08 , C07D493/16 , C07D493/18
摘要： Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.
摘要翻译：提供由式I表示的化合物，其包括合成的经斯曲肽内酯和巴利内酯产物。还提供了这些化合物的衍生物和合成方法。

33. 发明授权

US08530456B2 Sonic hedgehog modulators 有权
标题翻译：声波刺猬调制器
公开(公告)号：US08530456B2
公开(公告)日：2013-09-10
申请号：US12988755
申请日：2009-04-21
申请人： Lee F. Peng , Julia Lamenzo , Nicole Maloof , Kazuo Nakai , Benjamin Stanton , Sara Jean Buhrlage , Lawrence MacPherson , Michel Weiwer , Stuart L. Schreiber
发明人： Lee F. Peng , Julia Lamenzo , Nicole Maloof , Kazuo Nakai , Benjamin Stanton , Sara Jean Buhrlage , Lawrence MacPherson , Michel Weiwer , Stuart L. Schreiber
IPC分类号： C07D495/06 , C07D493/06 , C07D495/16 , C07D493/16 , A61K31/395 , A61P35/00
CPC分类号： C07D267/00 , C07D269/02 , C07D413/12
摘要： The present invention relates to macrocyclic small molecule inhibitors of the Sonic Hedgehog signaling pathway, syntheses thereof, and intermediates thereto. Such small molecule modulators of the Sonic Hedgehog signaling pathway are useful in the treatment of proliferative diseases (e.g., basal cell carcinoma, Gorlin syndrome, medulloblastoma, or pancreatic cancer), pulmonary diseases (e.g., interstitial pnuemonitis or interstitial pulmonary fibrosis), and developmental disorders (e.g., phocomelia or cyclopia). Novel non-natural macrocycles are provided that inhibit Sonic Hedgehog induced-protein transcription.
摘要翻译：本发明涉及Sonic Hedgehog信号通路的大环小分子抑制剂，其合成及其中间体。 Sonic Hedgehog信号通路的这种小分子调节剂可用于治疗增殖性疾病（例如基底细胞癌，Gorlin综合征，成神经管细胞瘤或胰腺癌），肺部疾病（例如间质性血管炎或间质性肺纤维化）和发育性疾病（例如，青光眼或环状）。提供新的非天然大环以抑制声刺猬诱导蛋白转录。

34. 发明申请

US20130190497A1 FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS 审中-公开
标题翻译：单色运输机荧光底物作为光学神经递质
公开(公告)号：US20130190497A1
公开(公告)日：2013-07-25
申请号：US13718832
申请日：2012-12-18
申请人： The Trustees of Columbia University in the City of New York
发明人： Niko Gert GUBERNATOR , Dalibor SAMES , David SULZER , Paul VADOLA
IPC分类号： C07D493/16 , C07D311/16 , C07D219/06 , C07D309/30
CPC分类号： C07D493/16 , C07D219/06 , C07D309/30 , C07D311/16 , C07D491/16
摘要： The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
摘要翻译：本发明涉及通式结构的化合物：其中Y是O，X是O，不存在α键，存在键β，或Y是H，X是CH，存在α键，键β不存在; 原子Z是碳并键合i，δ和γ存在，或是氮和键i，δ和γ不存在; R1是-H，-OH，-O-R7，-N（H）-R8，-N（H） - （CH2）n-NH2，-N（R9）（R10）或哌嗪阳离子; R 2与R 9共价结合或为-H，或与R3共价结合，形成取代或未取代的吡咯，或者R2与R 8或R 8或R 7共价键合; 或R 1和R 2共价连接形成芳香环; R3与R2共价结合形成吡咯，或者尤其是-H，-OH，烷基，或Z为氮时，R3为= O; R4尤其是-H，-OH或-R11NH2; R5尤其是-H，-OH或-R12NH2，R6与R10共价结合或为-H，或R6与R10或R8或R7共价键合。本发明还提供了制备该化合物的方法以及通过使用该化合物来监测单胺转运蛋白的活性或治疗单胺转运蛋白相关疾病的方法。

35. 发明申请

US20120083527A1 Anticancer Agents 有权
标题翻译：抗癌剂
公开(公告)号：US20120083527A1
公开(公告)日：2012-04-05
申请号：US13263141
申请日：2010-04-16
申请人： Michael D. Burkart , James J. La Clair , Minjin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
发明人： Michael D. Burkart , James J. La Clair , Minjin Kang , Brian D. Jones , Alexander L. Mandel , Wei-Luen Yu , Justin C. Hammons
IPC分类号： A61K31/365 , C12P17/18 , C12N9/96 , G01N33/53 , C07D493/16 , A61P35/00
CPC分类号： C07D493/18
摘要： The present disclosure relates generally to compositions and methods for treating cancer. In some aspects, novel spirohexenolides and methods of using and producing them are described.
摘要翻译：本公开一般涉及用于治疗癌症的组合物和方法。在一些方面，描述了新颖的螺烯烯内酯及其使用和制备方法。

36. 发明申请

US20110077193A1 Artemisinin Derivatives with Natural Amino Acids, Peptides, and Amino Sugars for the Treatment of Infection and Topical Condition in Mammals 失效
标题翻译：具有天然氨基酸，肽和氨基糖的青蒿素衍生物用于治疗哺乳动物的感染和局部状况
公开(公告)号：US20110077193A1
公开(公告)日：2011-03-31
申请号：US12957598
申请日：2010-12-01
申请人： Shyam K. Gupta
发明人： Shyam K. Gupta
IPC分类号： A61K38/02 , C07D493/16 , C07K2/00 , C07H5/06 , C07D491/153 , A61K31/357 , A61K31/7008 , A61P33/00 , A61P35/00 , A61P3/10 , A61P17/06 , A61P17/04 , A61P29/00 , A61P17/00 , A61P17/10 , A61P17/12 , A61Q19/08 , A61Q19/00 , A61P31/04 , A61P31/10 , A61P33/02
CPC分类号： A61Q19/02 , A61K8/49 , A61K8/498 , A61K31/205 , A61K31/357 , A61K31/60 , A61K31/7008 , A61K31/728 , A61K2800/28 , A61Q5/006 , A61Q19/008 , A61K2300/00
摘要： The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars, and isomers and salts thereof (formula I). The compounds of the present invention possess wide-spectrum antibacterial and antifungal biological activity suitable for topical or oral application for the treatment of infections and topical ailments in mammals, including acne, rosacea, topical wounds, infections, dandruff, skin disfigurements caused by infection, skin discoloration, age spots, wrinkles, excess facial oil, and veterinary problems including canine infections;
摘要翻译：本发明公开了青蒿素的某些衍生物和含有氨基酸，肽和氨基糖的艾蒿提取物及其异构体和盐（式I）中的活性成分。本发明的化合物具有广泛的抗菌和抗真菌生物活性，适用于局部或口服施用以治疗哺乳动物感染和局部疾病，包括痤疮，酒渣鼻，局部创伤，感染，头皮屑，由感染引起的皮肤损伤，皮肤变色，老年斑，皱纹，多余面部油脂和兽医问题，包括犬类感染;

37. 发明申请

US20100266570A1 DIMERIC DERIVATIVES OF ARTEMISININ AND APPLICATION IN ANTICANCER THERAPY 有权
标题翻译：阿司匹林的二元衍生物和应用于抗生素治疗
公开(公告)号：US20100266570A1
公开(公告)日：2010-10-21
申请号：US12808828
申请日：2008-12-22
申请人： Jean-Pierre Begue , Danièle Bonnet-Delpon , Benoît Crousse , Fabienne Grellepois , Constance Chollet , Jacques Fahy , Céline Mordant
发明人： Jean-Pierre Begue , Danièle Bonnet-Delpon , Benoît Crousse , Fabienne Grellepois , Constance Chollet , Jacques Fahy , Céline Mordant
IPC分类号： A61K38/46 , C07D493/16 , A61K31/357 , C07D405/14 , A61K31/4433 , C07D409/14 , A61K31/381 , A61K31/4192 , A61K31/497 , A61K31/7076 , A61K31/7064 , A61K31/519 , A61K31/4745 , A61K31/662 , A61K33/24 , A61P35/00
CPC分类号： C07D519/00 , C07F9/6561
摘要： The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C═O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.
摘要翻译：本发明涉及式（I）的10-三氟甲基化青蒿素的二聚衍生物或其药学上可接受的盐，其中B1和B2选自C = O，CHOH和CH2，以及它们在治疗癌症中的用途及其用途制备方法。

38. 发明授权

US4677103A Labdane compounds, pharmaceutical compositions and use 失效
公开(公告)号：US4677103A
公开(公告)日：1987-06-30
申请号：US921647
申请日：1986-10-20
申请人： Raymond W. Kosley, Jr. , Robert J. Cherill
发明人： Raymond W. Kosley, Jr. , Robert J. Cherill
IPC分类号： C07D311/92 , C07D407/12 , C07D493/04 , C07D493/10 , C07D493/20 , C07F7/18 , C07F9/655 , A61K31/39 , A61K31/535 , C07D493/16 , C07D497/16
CPC分类号： C07D407/12 , C07D311/92 , C07D493/04 , C07D493/10 , C07F7/1856 , C07F9/65502
摘要： Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.

39. 发明授权

US11700769B2 Organic electroluminescent element, compound, and light emitting device, display device and lighting system, using said element 有权
公开(公告)号：US11700769B2
公开(公告)日：2023-07-11
申请号：US16423251
申请日：2019-05-28
申请人： UDC IRELAND LIMITED
发明人： Toshihiro Ise , Saki Takada
IPC分类号： H10K85/60 , C09B57/00 , C07D495/06 , C07D209/94 , C07C13/62 , C09K11/06 , H05B33/10 , C07D307/93 , C07D487/06 , C07D493/06 , C07D493/16 , C07D493/22 , C07D495/16 , C07D495/22 , C07D307/77 , C07F7/08 , H10K50/11
CPC分类号： H10K85/6576 , C07C13/62 , C07D209/94 , C07D307/77 , C07D307/93 , C07D487/06 , C07D493/06 , C07D493/16 , C07D493/22 , C07D495/06 , C07D495/16 , C07D495/22 , C07F7/0812 , C09B57/001 , C09K11/06 , H05B33/10 , H10K50/11 , H10K85/624 , H10K85/657 , H10K85/6572 , C07C2603/54 , C09K2211/1011 , C09K2211/1088 , C09K2211/1092 , C09K2211/1096
摘要： An organic electroluminescent element including a substrate, a pair of electrodes including an anode and a cathode, disposed on the substrate, and at least one organic layer including a light emitting layer, disposed between the electrodes, in which at least one kind of compound represented by the following general formula is contained in any layer of the at least one organic layer, is an organic electroluminescent element, in which the generation of dark spots during driving is inhibited:

40. 发明申请

US20210300938A1 METHODS FOR CRYSTALLIZATION OF DRUGS 有权
公开(公告)号：US20210300938A1
公开(公告)日：2021-09-30
申请号：US17200434
申请日：2021-03-12
申请人： BOSTON SCIENTIFIC SCIMED, INC.
发明人： HONGXIA ZENG , JONATHAN PASCAL CHAKY , YEN-LANE CHEN
IPC分类号： C07D493/16
摘要： Methods are disclosed including methods for crystallizing a material such as a drug. An example method may include combining a nucleation initiator, a surfactant solution, and an amorphous form of a drug to form a drug precursor dispersion/suspension. The method may also include incubating the drug precursor dispersion/suspension to allow the drug to convert from the amorphous form to a crystalline form.

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