公开(公告)号：US10106555B2

公开(公告)日：2018-10-23

申请号：US15435003

申请日：2017-02-16

申请人： Massachusetts Institute of Technology

发明人： Angela N. Koehler ,  Eric Stefan ,  Francisco Caballero ,  Dylan Vijith Neel ,  Nicholas B. Struntz ,  Helen L. Evans ,  Andrew Chen

IPC分类号： C07D223/28 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10 ,  C07D233/28

摘要： The present disclosure provides compounds of Formula (I′), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.

公开(公告)号：US20130053387A1

公开(公告)日：2013-02-28

申请号：US13695376

申请日：2011-05-04

申请人： James W. Malecha

发明人： James W. Malecha

IPC分类号： A61K31/421 ,  C07D233/28 ,  A61K31/415 ,  C07D231/14 ,  C07D277/12 ,  A61P39/04 ,  C07D417/10 ,  A61K31/5377 ,  A61K31/496 ,  C07D249/10 ,  A61K31/4196 ,  C07D417/04 ,  C07D263/16 ,  A61K31/426

CPC分类号： C07D263/16 ,  C07D231/14 ,  C07D233/28 ,  C07D277/12 ,  C07D277/56

摘要： Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

摘要翻译： 本文公开了新型的脱氮铁硫代聚醚（DADFT-PE）类似物的化合物，以及包含它们的药物组合物及其作为用于治疗疾病的金属螯合剂的应用。 还提供了人或动物受试者中铁和其他金属的螯合方法用于治疗金属过载和毒性。

公开(公告)号：US07799929B2

公开(公告)日：2010-09-21

申请号：US12007118

申请日：2008-01-07

申请人： Masahiko Seki ,  Toshiaki Shimizu ,  Shin-ichi Yoshida ,  Masanori Hatsuda

发明人： Masahiko Seki ,  Toshiaki Shimizu ,  Shin-ichi Yoshida ,  Masanori Hatsuda

IPC分类号： C07D235/00 ,  C07D233/34 ,  C07D233/28

CPC分类号： C07F3/06 ,  C07D233/34 ,  C07D495/04 ,  C07F3/02

摘要： The present invention is to provide a process for preparing a synthetic intermediate of biotin which is industrially advantageous, and discloses a process for preparing a compound represented by the formula (I): 1 wherein R1 and R2 may be the same or different from each other, and each represents hydrogen atom, a benzyl group which may have a substituent(s) on the benzene ring, a benzhydryl group which may have a substituent(s) on the benzen ring, or a trityl group which may have a substituent(s) on the benzene ring, R3 represents cyano group, carboxyl group, an alkoxycarbonyl group, an alkylthiocarbonyl group, or a carbamoyl group which may have a substituent, or a salt thereof which comprises subjecting a compound represented by the formula (II-a): 2 wherein the symbols have the same meanings as defined above, or a salt thereof to ring transformation.

摘要翻译： 本发明提供一种制备在工业上有利的生物素的合成中间体的方法，并公开了制备由式（I）表示的化合物的方法：其中R1和R2可以相同或不同 ，各自表示氢原子，苯环上可具有取代基的苄基，可在苯环上具有取代基的二苯甲基或可具有取代基的三苯甲基（s ），R3表示氰基，羧基，烷氧基羰基，烷硫基羰基或可具有取代基的氨基甲酰基，或其盐，其包括使由式（II-a）表示的化合物 2，其中符号具有与上述相同的含义或其盐进行环转化。

公开(公告)号：US20100063050A1

公开(公告)日：2010-03-11

申请号：US11813546

申请日：2006-01-10

申请人： Alexandros Makriyannis ,  Rajesh Thotapally ,  Venkata Kiran Rao Vemuri ,  Teresa Olszewska

发明人： Alexandros Makriyannis ,  Rajesh Thotapally ,  Venkata Kiran Rao Vemuri ,  Teresa Olszewska

IPC分类号： A61K31/454 ,  C07D401/12 ,  C07D233/28 ,  C07D401/14 ,  C07D403/10 ,  C07D233/44 ,  C07D413/12 ,  C07D413/14 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4545 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/06 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  A61P25/02

CPC分类号： C07D233/90 ,  C07D401/10 ,  C07D403/10 ,  C07D417/10

摘要： Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.

摘要翻译： 公开了能够与CB1和/或CB2大麻素受体相互作用的生物活性杂吡咯类似物，例如咪唑，噻唑，恶唑和吡唑。 一方面公开了作为CB1和/或CB2受体拮抗剂的杂吡咯类似物。 另一方面公开了对CB1或CB2大麻素受体具有选择性的异构吡咯类似物。 还公开了采用公开的类似物的药物制剂和施用治疗有效量的所公开的类似物以提供生理作用的方法。

公开(公告)号：US20080015208A1

公开(公告)日：2008-01-17

申请号：US11820681

申请日：2007-06-20

申请人： Ralph New Harris ,  James Kress ,  David Repke ,  Russell Stabler

发明人： Ralph New Harris ,  James Kress ,  David Repke ,  Russell Stabler

IPC分类号： A61K31/18 ,  A61K31/4168 ,  A61K31/505 ,  A61P25/28 ,  C07C311/21 ,  C07D233/28 ,  C07D239/12

CPC分类号： C07C311/21 ,  C07C311/37 ,  C07C2602/10 ,  C07D233/48 ,  C07D233/88 ,  C07D239/14

摘要： Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein Ar, X, m, R1, R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of 5-HT6-mediated diseases.

摘要翻译： 式I化合物或其药学上可接受的盐，其中Ar，X，m，R 1，R 2，如本文所定义。 还提供了制备方法，组合物和使用式I化合物治疗5-HT6介导的疾病的方法。

公开(公告)号：US07304164B1

公开(公告)日：2007-12-04

申请号：US11549146

申请日：2006-10-13

申请人： Reddy Damavarapu ,  C. Rao Surapaneni ,  Nathaniel Gelber ,  Raja G. Duddu ,  MaoXi Zhang ,  Paritosh R. Dave

发明人： Reddy Damavarapu ,  C. Rao Surapaneni ,  Nathaniel Gelber ,  Raja G. Duddu ,  MaoXi Zhang ,  Paritosh R. Dave

IPC分类号： C07D233/28

CPC分类号： C07D233/92

摘要： 1-Methyl-2,4,5-Trinitroimidazole is synthesized starting from 4-nitroimidazole using stepwise nitration method and further methylation using Dimethylsulphate. It is relatively insensitive to impact and its thermal stability is excellent. The calculated detonation properties indicate that its performance is about 30% better than TATB. It can be prepared easily, with reasonable yield, starting from commercially available Imidazole. Results from impact sensitivity, friction sensitivity, time-to-explosion temperature and vacuum stability tests indicate that it is less sensitive than both RDX and HMX. The good oxygen balance and measured heat of formation data of this material indicate that its propellant performance should be good.

摘要翻译： 使用逐步硝化方法从4-硝基咪唑开始合成1-甲基-2,4,5-三硝基咪唑，并使用二甲基硫酸盐进一步甲基化。 对冲击相对不敏感，其热稳定性优异。 计算的爆轰特性表明其性能比TATB好约30％。 从市售的咪唑开始，可以容易地制备出合理的产率。 冲击敏感性，摩擦灵敏度，时间 - 爆炸温度和真空稳定性测试结果表明，它比RDX和HMX都敏感。 该材料的良好的氧气平衡和测量的热量数据表明其推进剂性能应良好。

公开(公告)号：US06878735B2

公开(公告)日：2005-04-12

申请号：US10347323

申请日：2003-01-17

申请人： Jetze J. Tepe ,  Satyamaheshwar Peddibhotla

发明人： Jetze J. Tepe ,  Satyamaheshwar Peddibhotla

IPC分类号： C07D233/22 ,  C07D233/28 ,  C07D401/04 ,  C07D403/06 ,  A61K31/4164 ,  C07D233/26

CPC分类号： C07D401/04 ,  C07D233/22 ,  C07D233/28 ,  C07D403/06

摘要： A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 μm/mL.

摘要翻译： 描述了一类新的具有非常有效的抗炎和抗微生物活性的4-位酸或酯的咪唑啉。 这些咪唑啉的合成包括适用于组合合成方法的多组分反应。 这两个关键特征的组合在治疗脓毒性休克以及许多其他炎症（关节炎和哮喘）和感染性疾病方面提供了有效的治疗药物。 描述了使用这种新型的非甾体试剂作为抗炎剂（用于治疗哮喘等），抗菌剂和防腐剂。 这些化合物也可用于治疗肿瘤（如癌症）。 咪唑啉是转录因子NF-κB的有效抑制剂，以及对具有50mum / mL范围的MIC值的革兰氏阴性细菌（B. subtilis）和蜡状芽胞杆菌（B. cereus）的有效活性。

公开(公告)号：US20030236438A1

公开(公告)日：2003-12-25

申请号：US10394758

申请日：2003-03-21

发明人： David W.C. MacMillan ,  Nick A. Paras

IPC分类号： C07C045/68 ,  C07D233/28

CPC分类号： C07D207/333 ,  C07B2200/07 ,  C07C45/69 ,  C07C327/22 ,  C07D209/12 ,  C07D209/18 ,  C07D209/22 ,  C07D209/24 ,  C07D233/32 ,  C07D261/02 ,  C07D295/155 ,  C07D307/58 ,  C07D311/20 ,  C07D333/32 ,  C07D487/04 ,  C07C47/453 ,  C07C47/445

摘要： Nonmetallic, chiral organic catalysts are used to catalyze the 1,4-addition of an aromatic nucleophile to an null,null-unsaturated aldehyde. The aromatic nucleophile may be an N,N-disubstituted aniline compound, or an analog thereof. The reaction is efficient and enantioselective, and proceeds with a variety of substituted and unsubstituted aromatic nucleophiles and aldehydes. The invention also provides a method for the deamination of aromatic N,N-disubstituted amines such as those resulting from the 1,4-addition of an aromatic nucleophile to an null,null-unsaturated aldehyde.

摘要翻译： 非金属手性有机催化剂用于催化芳族亲核试剂向α，β-不饱和醛的1,4-加成。 芳族亲核试剂可以是N，N-二取代的苯胺化合物或其类似物。 该反应是有效的和对映选择性的，并且进行各种取代和未取代的芳族亲核试剂和醛。 本发明还提供了芳族N，N-二取代的胺脱氨基的方法，例如由芳香族亲核试剂1,4-加成到α，β-不饱和醛中的那些。

公开(公告)号：US20030195363A1

公开(公告)日：2003-10-16

申请号：US10366356

申请日：2003-02-14

发明人： Tsutomu Aoki ,  Toshiro Konoike

IPC分类号： C07D233/28 ,  C07C323/00

CPC分类号： C07D401/06 ,  C07C313/08 ,  C07C319/14 ,  C07C323/09 ,  C07D233/84

摘要： A process for producing a compound of the formula (II): 1 wherein Hal1 represents halogen and R1 and R2 each independently represents halogen, alkyl, alkoxy, nitro or cyano, which comprises allowing a halogenating agent to react with a compound of the formula (I): 2 wherein Alk represents branched alkyl and R1 and R2 are as defined above.

摘要翻译： 一种制备式（II）化合物的方法：其中Hal 1>代表卤素，R 1>和R 2各自独立地表示卤素，烷基，烷氧基，硝基或氰基，其中 包括允许卤化剂与式（I）的化合物反应：其中Alk表示支链烷基，R <上标>>和R 2>如上所定义。

公开(公告)号：US20030073047A1

公开(公告)日：2003-04-17

申请号：US10106373

申请日：2002-03-27

发明人： Kiyoshi Takeuchi ,  Shigeki Uehira ,  Mario Aoki ,  Jun Ogasawara ,  Yasuhiro Shimada ,  Seiji Ichijima ,  Yasuaki Deguchi ,  Naoto Matsuda ,  Akira Ikeda ,  Hisashi Mikoshiba ,  Masahara Sugai ,  Taiji Katsumata

IPC分类号： G03C007/36 ,  C07D233/28

CPC分类号： G03C1/08 ,  C07D239/90 ,  C07D285/18 ,  C07D285/24 ,  C07D403/06 ,  C07D417/06 ,  C07D417/12 ,  C07D513/04 ,  C09B55/002 ,  C09B55/003 ,  G03C7/30535 ,  G03C7/36

摘要： A dye-forming coupler of formula (I), a silver halide photographic light-sensitive material containing the coupler, and an azomethine dye that can be derived from the dye-forming coupler: 1 wherein Q is a group nullC(nullR11)nullC(nullR12)nullSO2null; R11 and R12 bond with each other to form, together with the nullCnullCnull moiety, a 5- to 7-membered ring, or they each represent a hydrogen atom or a substituent; R1, R3 and R4 each represent a substituent; m is an integer of 0 to 4; and X represents a hydrogen atom or a group that splits off upon a coupling reaction with an oxidized product of a developing agent; with the proviso that the following compound (I-A) is excluded from the dye-forming coupler of formula (I). 2

摘要翻译： 式（I）的染料形成成色剂，含有偶合剂的卤化银照相感光材料和可衍生自染料形成成色剂的偶氮甲碱染料：其中Q为基团-C（-R 11）= C（ - R 12）-SO 2 - ; R 11和R 12彼此键合，与-C = C-部分一起形成5-至7-元环，或它们各自表示氢原子或取代基; R1，R3和R4各自表示取代基; m为0〜4的整数。 X表示氢原子或与显影剂的氧化物偶合反应时分裂的基团; 条件是从式（I）的染料形成成色剂除去下列化合物（I-A）。