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1. 发明申请

US20180044283A1 BIGUANIDE COMPOUND AND USE THEREOF 审中-公开
公开(公告)号：US20180044283A1
公开(公告)日：2018-02-15
申请号：US15527621
申请日：2015-11-20
申请人： ImmunoMet Therapeutics Inc.
发明人： Hong Woo KIM , Jae Kap JEONG , Ji Sun LEE , Hye Jin HEO , Hong Bum LEE , Ji Ae KOOK , Sung Wuk KIM
IPC分类号： C07C279/26 , C07D211/10
CPC分类号： C07C279/26 , A61K31/155 , A61P35/00 , C07D211/10 , C07D211/34
摘要： The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.

2. 发明授权

US09822135B2 STAT3 dimerization inhibitors 有权
公开(公告)号：US09822135B2
公开(公告)日：2017-11-21
申请号：US14435471
申请日：2013-10-30
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
发明人： Said M. Sebti , Nicholas James Lawrence , Harshani Rithma Lawrence
IPC分类号： A61K31/192 , C07F9/38 , C07F9/40 , C07C233/76 , C07C311/18 , C07D211/10 , C07D213/16
CPC分类号： C07F9/3834 , A61K31/192 , C07C233/76 , C07C311/18 , C07D211/10 , C07D213/16 , C07F9/3882 , C07F9/4021 , C07F9/4056
摘要： The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

3. 发明申请

US20160318866A1 SUBSTITUTED BIPIPERIDINYL DERIVATIVES 审中-公开
标题翻译：取代的双嘧哆醛衍生物
公开(公告)号：US20160318866A1
公开(公告)日：2016-11-03
申请号：US15106285
申请日：2014-12-16
申请人： Bayer Pharma Aktiengesellschaft
发明人： Eva Maria BECKER-PELSTER , Philipp BUCHGRABER , Anja BUCHMÜLLER , Karen ENGEL , Mark Jean GNOTH , Herbert HIMMEL , Raimund KAST , Joerg KELDENICH , Jürgen KLAR , Andreas KNORR , Dieter LANG , Niels LINDNER , Carsten SCHMECK , Rudolf SCHOHE-LOOP , Hanna TINEL , Hubert TRÜBEL , Frank WUNDER
IPC分类号： C07D211/10 , C07D211/42 , C07D211/22 , A61K45/06 , C07D401/14 , C07D413/14 , C07D405/14 , C07D211/60 , A61K31/4545
CPC分类号： C07D211/10 , A61K31/4545 , A61K45/06 , C07D211/16 , C07D211/22 , C07D211/42 , C07D211/60 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/14 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14
摘要： The invention relates to novel substituted bipiperidinyl derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardiac vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.
摘要翻译：本发明涉及新的取代的二哌啶基衍生物，其制备方法，其用于治疗和/或预防疾病及其用于制备用于治疗和/或预防疾病的药物的用途，特别是用于治疗和/ /或预防糖尿病性微血管病，四肢糖尿病溃疡，特别是用于促进糖尿病足溃疡的伤口愈合，糖尿病性心力衰竭，糖尿病性冠状动脉微血管性心脏病，外周和心脏血管疾病，血栓栓塞性疾病和局部缺血，外周循环障碍，雷诺现象，CREST综合征，微循环障碍，间歇性跛行，外周和自主神经病变。

4. 发明授权

US09206125B2 Use of compound binding to mSin3B that specifically binds to neuron restrictive silencer factor (NRSF) 有权
标题翻译：使用化合物结合到特异性结合神经元限制性消音因子（NRSF）的mSin3B
公开(公告)号：US09206125B2
公开(公告)日：2015-12-08
申请号：US13578230
申请日：2011-02-09
申请人： Yoshifumi Nishimura , Aritaka Nagadoi , Yuuka Hirao , Yoshio Goshima , Naoya Yamashita , Naoki Miyata , Takayoshi Suzuki , Ryuta Hiraishi , Hiroshi Ueda
发明人： Yoshifumi Nishimura , Aritaka Nagadoi , Yuuka Hirao , Yoshio Goshima , Naoya Yamashita , Naoki Miyata , Takayoshi Suzuki , Ryuta Hiraishi , Hiroshi Ueda
IPC分类号： C07D211/16 , C07D211/14 , C07D211/10 , C07C233/65 , A61K31/445 , C07D211/96 , C07D295/192 , C07C233/66 , C07D207/06 , C07D223/04 , C07D225/02 , C07D265/30
CPC分类号： C07D211/16 , A61K31/445 , C07C233/65 , C07C233/66 , C07C2601/14 , C07D207/06 , C07D211/10 , C07D211/14 , C07D211/96 , C07D223/04 , C07D225/02 , C07D265/30 , C07D295/192
摘要： The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain.The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g., a compound represented by the following formula (1), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof: wherein n represents 0 or 1; R1, R2, R3, R4 and R5 each independently represent a hydrogen atom, a hydrocarbon group or a functional group; Y represents a single bond, a carbonyl group, —CONH—, —NHCO— or a sulfonyl group; and Z represents a nitrogen-containing heterocyclic group which may have a substituent, an amino group which may have a hydrocarbon group or an aromatic hydrocarbon group, or a nitrogen and oxygen-containing heterocyclic group which may have a substituent.
摘要翻译：本发明鉴定了与特异性结合神经限制性沉默因子NRSF的mSin3B的PAH1结构域结合的化合物，并且将该化合物用作与神经限制性消音因子NRSF / REST的异常表达相关的疾病的预防和/或治疗或NRSF / REST靶向的基因异常表达，如亨廷顿氏病，成神经管细胞瘤和神经性疼痛。本发明提供了包含能够结合mSin3B的PAH1结构域的物质的药物组合物，例如下式（1）所示的化合物，其药理学上可接受的盐或其药理学上可接受的酯：其中n表示0 或1; R1，R2，R3，R4和R5各自独立地表示氢原子，烃基或官能团; Y表示单键，羰基，-CONH-，-NHCO-或磺酰基; Z表示可以具有取代基的含氮杂环基，可以具有烃基或芳香族烃基的氨基或可以具有取代基的含氮和含氧杂环基。

5. 发明申请

US20150259366A1 STAT3 DIMERIZATION INHIBITORS 有权
标题翻译： STAT3二维抑制剂
公开(公告)号：US20150259366A1
公开(公告)日：2015-09-17
申请号：US14435471
申请日：2013-10-30
申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
发明人： Said M. Sebti , Nicholas James Lawrence , Harshani Rithma Lawrence
IPC分类号： C07F9/38 , C07C233/76 , C07D213/16 , C07C311/18 , C07D211/10
CPC分类号： C07F9/3834 , A61K31/192 , C07C233/76 , C07C311/18 , C07D211/10 , C07D213/16 , C07F9/3882 , C07F9/4021 , C07F9/4056
摘要： The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.
摘要翻译：本文公开的主题涉及制备和使用组合物的组合物和方法。在另一方面，本文公开的主题涉及STAT3二聚化的抑制剂。还公开了制备这些组合物的方法以及包含这些组合物的组合物。还公开了通过给予有需要的个体和有效量的本文公开的化合物来治疗或预防某些癌症的方法。此外，本文公开的是通过使细胞与本文公开的化合物或组合物接触来抑制STAT3的方法。

6. 发明申请

US20140335079A1 SOLENOPSIN AND DERIVATIVES, THERAPEUTIC COMPOSITIONS, AND METHODS RELATED THERETO 审中-公开
标题翻译：联苯和衍生物，治疗组合物及其相关方法
公开(公告)号：US20140335079A1
公开(公告)日：2014-11-13
申请号：US14271682
申请日：2014-05-07
申请人： Jack L. Arbiser , J. Philip Bowen , E. Blake Watkins
发明人： Jack L. Arbiser , J. Philip Bowen , E. Blake Watkins
IPC分类号： C07D211/10 , A61K45/06 , C07D211/40 , A61K31/445
CPC分类号： A61K31/445 , A61K45/06 , C07D211/10 , C07D211/22 , C07D211/40 , A61K2300/00
摘要： This disclosure relates to solenopsin derivatives, pharmaceutical compositions, and therapeutic uses related thereto. In certain embodiments, the disclosure relates to compounds of the following formula: or salts, esters or prodrugs thereof as described herein.
摘要翻译：本公开内容涉及与其相关的依卡鲁汀衍生物，药物组合物和治疗用途。在某些实施方案中，本公开涉及如本文所述的下式的化合物或其盐，酯或前药。

7. 发明申请

US20110288296A1 PRODUCTION AND USE OF ZINC AMIDES 有权
标题翻译：锌的生产和使用
公开(公告)号：US20110288296A1
公开(公告)日：2011-11-24
申请号：US13147339
申请日：2010-02-11
申请人： Paul Knochel , Marc Mosrin
发明人： Paul Knochel , Marc Mosrin
IPC分类号： C07D473/12 , C07D237/06 , C07D239/24 , C07D333/56 , C07D241/10 , C07C211/52 , C07D213/61 , C07D307/71 , C07F3/06 , C07D405/06
CPC分类号： C07F3/06 , C07D211/10 , C07D237/12 , C07D239/30 , C07D241/16 , C07D405/06 , C07F3/003
摘要： The application relates to a reagent of the general formula R1R2N—ZnY LiY (I) wherein R1, R2 are, independently, selected from H, substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or silyl derivatives thereof; and R1 and R2 together can be part of a cyclic or polymeric structure; and wherein at least one of R1 and R2 is other than H; Y is selected from the group consisting of F; Cl; Br; I; CN; SCN; NCO; Halon, wherein n=3 or 4 and Hal is selected from Cl, Br and I; NO3; BF4; PF6; H; a carboxylate of the general formula RXCO2; an alcoholate of the general formula ORX; a thiolate of the general formula SRX; RXP(O)O2; or SCORX; or SCSRX; OnSRx; wherein n=2 or 3; or NOn, wherein n=2 or 3; and a derivative thereof; wherein Rx is a substituted or unsubstituted aryl or heteroaryl containing one or more heteroatoms, linear, branched or cyclic, substituted or unsubstituted alkyl, alkenyl, alkynyl, or derivatives thereof, or H; or as adduct with a solvent; as well as to the preparation and use thereof.34
摘要翻译：本申请涉及通式为R 1 R 2 N-ZnY LiY（I）的试剂，其中R 1，R 2独立地选自H，具有直链，支链或环状的取代或未取代的一个或多个杂原子的取代或未取代的芳基或杂芳基烷基，烯基，炔基或甲硅烷基衍生物; R1和R2一起可以是环状或聚合物结构的一部分; 并且其中R 1和R 2中的至少一个不是H; Y选自F; Cl; Br; 一世; CN; SCN; NCO; Halon，其中n = 3或4，Hal选自Cl，Br和I; NO3; BF4; PF6; H; 通式为RXCO2的羧酸酯; 通式ORX的醇化物; 通式SRX的硫醇盐; RXP（O）O2; 或SCORX; 或SCSRX; OnSRx; 其中n = 2或3; 或NO n，其中n = 2或3; 及其衍生物; 其中Rx是取代或未取代的芳基或含有一个或多个杂原子的直链，支链或环状取代或未取代的烷基，烯基，炔基或衍生物，或H; 或作为与溶剂的加合物; 以及其制备和使用。 34

8. 发明授权

US5196412A Gallium compounds 失效
标题翻译： GALLIUM化合物
公开(公告)号：US5196412A
公开(公告)日：1993-03-23
申请号：US665233
申请日：1991-03-06
申请人： Fontaine C. Bradley , Chris M. Giandomenico , Michael J. Abrams , Danielle T. Frost , Jean F. Vollano
发明人： Fontaine C. Bradley , Chris M. Giandomenico , Michael J. Abrams , Danielle T. Frost , Jean F. Vollano
IPC分类号： A61K31/16 , A61K31/28 , A61K31/555 , A61P3/00 , A61P35/00 , C07C259/06 , C07D211/10 , C07D211/76 , C07D211/94 , C07D223/10 , C07F5/00
CPC分类号： C07D223/10 , C07C259/06 , C07D211/10 , C07D211/94
摘要： The present invention relates to compounds of gallium (III) which can be given orally to achieve high serum levels of gallium (III) for the treatment of hypercalcemia of malignancy and related disorders of bone metabolism. Complexes of gallium (III) of the formula (I) ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.8 n-alkyl and R.sub.2 is H or C.sub.1 -C.sub.2 alkyl, or R.sub.1 and R.sub.2 together form tetra- or penta-methylene and wherein said complex is useful in increasing calcium content of bone tissue and decreasing bone resorption, are used in an amount sufficient to cause an increase in calcium content of said bone and to cause decreased bone resorption.

9. 发明授权

US4333932A Organic diamine therapeutic compositions and methods 失效
标题翻译：有机二胺治疗组合物和方法
公开(公告)号：US4333932A
公开(公告)日：1982-06-08
申请号：US123063
申请日：1980-02-20
申请人： John L. Belletire
发明人： John L. Belletire
IPC分类号： C07D209/44 , C07D211/10 , C07D213/38 , C07D213/53 , C07D213/82 , C07D295/02 , C07D295/073 , C07D295/096 , C07D295/135 , C07D295/155 , C07D307/52 , C07D307/68 , A61K31/535
CPC分类号： C07D213/53 , C07D209/44 , C07D211/10 , C07D213/38 , C07D213/82 , C07D295/02 , C07D295/073 , C07D295/096 , C07D295/135 , C07D295/155 , C07D307/52 , C07D307/68 , Y10S514/866
摘要： A series of organic diamine base compounds derived from either an aromatic, alicyclic or heterocyclic ring and possessing, for the most part, an intervening methylene group between the ring and the aforesaid basic moiety have been prepared, including their pharmaceutically acceptable acid addition salts as well as oral pharmaceutical compositions containing same. These particular compounds are found to be useful in therapy as oral hypoglycemic agents. Preferred member compounds include 1,1'-[1,2-phenylenebis(methylene)]bispiperidine, 2,3-dihydro-2-[2-(1-piperidinomethyl)phenylmethyl]-1H-isoindole and 2,3-dihydro-2-[2-(4-morpholinomethyl)phenylmethyl]-1H-isoindole. Alternate methods of preparation are provided and the two principal synthetic routes leading to these compounds are described in some detail.
摘要翻译：已经制备了一系列衍生自芳族，脂环族或杂环的有机二胺基化合物，并且大部分在环和前述碱性部分之间具有中间的亚甲基，包括其药学上可接受的酸加成盐作为含有其的口服药物组合物。发现这些特定化合物可用于作为口服降血糖药的治疗。优选的成员化合物包括1,1' - [1,2-亚苯基双（亚甲基）]双哌啶，2,3-二氢-2- [2-（1-哌啶基甲基）苯甲基] -1H-异吲哚和2,3-二氢 - 2- [2-（4-吗啉代甲基）苯基甲基] -1H-异吲哚。提供了替代的制备方法，并且进一步描述了导致这些化合物的两种主要合成途径。

10. 发明申请

US20180282295A1 MATERIALS FOR ORGANIC ELECTTROLUMINESCENT DEVICES 审中-公开
公开(公告)号：US20180282295A1
公开(公告)日：2018-10-04
申请号：US15524389
申请日：2015-10-13
申请人： Merck Patent GmbH
发明人： Amir Hossain Parham , Philipp Stoessel , Thomas Eberle , Anja Jatsch , Jonas Valentin Kroeber , Christof Pflumm
IPC分类号： C07D401/04 , C07D405/14 , C07D409/14 , C07D401/14 , C07D401/10 , C07D413/10 , C07D417/10 , C07D471/04 , H01L51/00 , H01L51/50
CPC分类号： C07D401/04 , C07D211/10 , C07D401/10 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/10 , C07D417/10 , C07D471/04 , C07D487/06 , C07D491/107 , C09K11/06 , H01L51/0059 , H01L51/006 , H01L51/0061 , H01L51/0067 , H01L51/0072 , H01L51/0073 , H01L51/0074 , H01L51/0085 , H01L51/0087 , H01L51/5016 , H01L51/5056 , H01L51/5096 , Y02E10/549
摘要： The invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.

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