公开(公告)号：US20240360115A1

公开(公告)日：2024-10-31

申请号：US18764292

申请日：2024-07-04

申请人： Ottawa Hospital Research Institute ,  University of Ottawa

发明人： Jean-Simon Diallo ,  Christopher Noyce Boddy ,  Mark Dornan ,  Ramya Krishnan ,  Rozanne Arulanandam ,  Fabrice Le Boeuf ,  Jeffrey Smith ,  Andrew Macklin

IPC分类号： C07D413/06 ,  A61K31/341 ,  A61K31/501 ,  A61K45/06 ,  A61P35/02 ,  C07D207/36 ,  C07D207/38 ,  C07D207/456 ,  C07D209/48 ,  C07D231/08 ,  C07D237/14 ,  C07D307/30 ,  C07D307/58 ,  C07D307/60 ,  C07D307/66 ,  C07D317/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D417/06 ,  C07D471/04 ,  C12N7/00

CPC分类号： C07D413/06 ,  A61K31/501 ,  A61K45/06 ,  A61P35/02 ,  C07D207/36 ,  C07D207/38 ,  C07D207/456 ,  C07D209/48 ,  C07D231/08 ,  C07D237/14 ,  C07D307/30 ,  C07D307/58 ,  C07D307/60 ,  C07D307/66 ,  C07D317/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D417/06 ,  C07D471/04 ,  C12N7/00 ,  A61K31/341 ,  A61K2300/00 ,  C12N2710/10334 ,  C12N2710/10351 ,  C12N2710/10352 ,  C12N2710/16651 ,  C12N2710/24151 ,  C12N2750/14151 ,  C12N2760/16134 ,  C12N2760/16151 ,  C12N2760/16152 ,  C12N2760/20234 ,  C12N2760/20251 ,  C12N2760/20252

摘要： Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

公开(公告)号：US20180230095A1

公开(公告)日：2018-08-16

申请号：US15950973

申请日：2018-04-11

申请人： Daiichi Sankyo Company, Limited

发明人： Masashi Watanabe ,  Hiroshi Nagasawa ,  Noritada Sato

IPC分类号： C07D207/34 ,  C07B57/00 ,  C07D207/456 ,  C12P17/10 ,  C12P41/00

CPC分类号： C07D207/34 ,  C07B57/00 ,  C07D207/456 ,  C12P17/10 ,  C12P41/005

摘要： The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.

公开(公告)号：US20180042948A1

公开(公告)日：2018-02-15

申请号：US15555721

申请日：2016-03-04

申请人： JAPAN SCIENCE AND TECHNOLOGY AGENCY

发明人： Motomu KANAI ,  Yohei SOMA ,  Yusuke SHIMIZU ,  Atsuhiko TANIGUCHI ,  Kounosuke OISAKI ,  Yoichiro KUNINOBU

IPC分类号： A61K31/69 ,  A61K31/4725 ,  C07F5/02 ,  C07D215/06 ,  C07D207/46 ,  C07D207/456 ,  A61K31/4025 ,  C07D401/14

CPC分类号： A61K31/69 ,  A61K31/4025 ,  A61K31/4725 ,  A61K41/00 ,  C07D207/44 ,  C07D207/456 ,  C07D207/46 ,  C07D215/06 ,  C07D401/14 ,  C07D455/04 ,  C07F5/02

摘要： Provided are a compound which is useful as an in vivo applicable, amyloid-oxygenating catalyst selective for amyloid and applicable not only to an Aβ peptide but also to other amyloids and a drug containing the compound for preventing and/or treating amyloid-related-diseases.Disclosed is a boron-dipyrrin complex represented by the following formula (1) wherein X1 and X2 are the same or different and each represent a halogenoalkyl group or a halogen atom; R1 represents a hydrogen atom, an alkyl group, or a group represented by formula (b); R2 and R6 are the same or different and each represent a hydrogen atom or a halogen atom; R3, R4, R5, and R7 are the same or different and each represent a hydrogen atom, a halogen atom, or an alkyl group; R8 represents a hydrogen atom or —(CH2)l—(Y)m—(CH2)n—Z wherein Y represents —CO—, —CONH—, or a triazole ring, Z represents a carboxyl group, a sulfonic acid group, or a —CO-peptide residue, l and n each represent an integer of 1 to 6, and m represents 0 or 1; R9 and R10 are the same or different and each represent a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; and R8 and R10 together optionally form an alkylene group.

公开(公告)号：US09296690B2

公开(公告)日：2016-03-29

申请号：US14293879

申请日：2014-06-02

申请人： Metacine, Inc.

发明人： Bae Keun Park ,  Sung-Hwa Yoon ,  Ju-Young Park ,  Sung Hoon Park

IPC分类号： A61K31/4015 ,  C07D207/448 ,  C07D207/452 ,  C07D207/38 ,  C07D207/444 ,  C07D409/04 ,  C07D207/20 ,  C07D207/408 ,  C07D207/456

CPC分类号： C07D207/448 ,  A61K31/4015 ,  C07D207/20 ,  C07D207/38 ,  C07D207/408 ,  C07D207/444 ,  C07D207/452 ,  C07D207/456 ,  C07D409/04

摘要： The present invention is for method of treating metabolic bone disease, new compounds and pharmaceutical compositions comprising the active ingredients having inhibition effects on osteoclast differentiation. The pharmaceutical composition comprising new compounds according to the present invention can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.

摘要翻译： 本发明是治疗代谢性骨病的方法，新化合物和药物组合物，其含有对破骨细胞分化具有抑制作用的活性成分。 包含根据本发明的新化合物的药物组合物可用作治疗代谢性骨疾病如骨转移癌，固体癌骨转移，通过固体癌骨转移的肌肉骨骼并发症，恶性肿瘤的高钙血症，多发性骨髓瘤，原发骨 肿瘤，骨质疏松症，类风湿关节炎，骨关节炎，牙周病，牙槽骨炎症吸收，骨吸收性炎症和佩吉特氏病。

公开(公告)号：US20150306069A1

公开(公告)日：2015-10-29

申请号：US14648115

申请日：2013-11-27

申请人： The University of Chicago

发明人： Philip P. Connell ,  Brian Budke ,  Jay H. Kalin ,  Michal Pawlowski ,  Alan P. Kozikowski

IPC分类号： A61K31/402 ,  A61K31/496 ,  A61K31/5377

CPC分类号： A61K31/402 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/456

摘要： The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have particular applications for cancer patients. In some embodiments of the invention, the RAD51 inhibitor is a small molecule that directly affects RAD51 activity, such as its ability to promote filament formation.

摘要翻译： 本发明涉及涉及抑制剂和参与同源重组的蛋白质RAD51的方法和组合物。 在一些实施方案中，存在使细胞对DNA损伤剂的作用敏感的方法，其可以具有癌症患者的特殊应用。 在本发明的一些实施方案中，RAD51抑制剂是直接影响RAD51活性的小分子，例如其促进丝状细胞形成的能力。

公开(公告)号：US20120253053A1

公开(公告)日：2012-10-04

申请号：US13431590

申请日：2012-03-27

申请人： Matsuo Satoshi ,  Yuji Yamamoto ,  Chika Itoh

发明人： Matsuo Satoshi ,  Yuji Yamamoto ,  Chika Itoh

IPC分类号： C07C233/05 ,  C07D207/404

CPC分类号： C07D207/456 ,  C07C269/04 ,  C07C271/16 ,  C07D207/452

摘要： Provided are a thiol-reactive polyoxyalkylene-modified lipid which can be used to chemically modify bioactive substances and which can be used for drug delivery systems such as liposomes and a method for producing the same. The polyoxyalkylene-modified lipid is represented by the following formula (1): (wherein, R1 and R2 are hydrocarbon groups which are the same as or different from each other and which contain 4 to 24 carbon atoms, R3 is a divalent hydrocarbon group containing 1 to 6 carbon atoms, OA is oxyalkylene groups containing 2 to 4 carbon atoms, n is the average addition mole number of the oxyalkylene groups and is 5 to 1,000, and Z is a group containing either maleimide or iodoacetamide.)

摘要翻译： 提供了可用于化学修饰生物活性物质并且可用于药物递送系统如脂质体的硫醇反应性聚氧化烯修饰的脂质及其制备方法。 聚氧化烯修饰的脂质由下式（1）表示：（其中，R 1和R 2为彼此相同或不同且含有4〜24个碳原子的烃基，R 3为含有 1〜6个碳原子，OA为含有2〜4个碳原子的氧化烯基，n为氧化烯基的平均加成摩尔数，为5〜1000，Z为含有马来酰亚胺或碘乙酰胺的基团。

公开(公告)号：US07812113B2

公开(公告)日：2010-10-12

申请号：US11995329

申请日：2006-07-04

申请人： Geert Deroover ,  Wojciech Jaunky ,  Lambertus Groenendaal ,  Johan Loccufier

发明人： Geert Deroover ,  Wojciech Jaunky ,  Lambertus Groenendaal ,  Johan Loccufier

IPC分类号： C08G73/00 ,  C07C251/00 ,  C07C241/00 ,  C07C257/00 ,  C07C243/10 ,  C07C291/00 ,  C07C249/00 ,  C08L39/00 ,  C08F2/22 ,  C08F2/20 ,  C08K3/00 ,  C09D11/00

CPC分类号： C07D207/452 ,  C07C251/76 ,  C07D207/456 ,  C07D233/70 ,  C07D235/26 ,  C09B29/337 ,  C09B31/11 ,  C09B69/106 ,  C09D11/101 ,  C09D11/326

摘要： A monomer with a chromophore group represented by Formula (I): wherein AR1 represents a substituted or unsubstituted aromatic group; AR2 represents a substituted or unsubstituted aromatic group or a substituted or unsubstituted alkyl group; and R represents a substituted or unsubstituted alkyl group, with the proviso that one of R, AR1, and AR2 has a substituent with a polymerizable functional group. The monomer can be advantageously used to prepare polymeric dispersants for pigment dispersion, especially inkjet inks.

摘要翻译： 具有由式（I）表示的发色团的单体：其中AR1表示取代或未取代的芳基; AR2表示取代或未取代的芳基或取代或未取代的烷基; 并且R表示取代或未取代的烷基，条件是R，AR1和AR2中的一个具有可聚合官能团的取代基。 该单体可有利地用于制备用于颜料分散的聚合物分散剂，特别是喷墨油墨。

公开(公告)号：US07432288B2

公开(公告)日：2008-10-07

申请号：US10564235

申请日：2004-07-08

申请人： Jonas Boström ,  Kay Brickmann ,  Patrik Holm ,  Pernilla Sandberg ,  Marianne Swanson ,  Christer Westerlund

发明人： Jonas Boström ,  Kay Brickmann ,  Patrik Holm ,  Pernilla Sandberg ,  Marianne Swanson ,  Christer Westerlund

IPC分类号： A61K31/4439 ,  C07D401/04

CPC分类号： C07D405/06 ,  C07D207/456 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06

摘要： The present invention relates to certain novel compounds of the Formula I to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR)α(NR1H3) and/or β(NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

摘要翻译： 本发明涉及一些式I化合物的制备方法，用于调节核激素受体肝X受体（LXR）α（NR1H3）和/或β（NR1H2）以及在治疗和 /或预防包括心血管疾病如动脉粥样硬化的临床病症; 炎性疾病，阿尔茨海默病，与胰岛素抵抗相关的脂质紊乱（血脂异常），2型糖尿病和代谢综合征的其他表现，其治疗用途的方法和含有它们的药物组合物。

公开(公告)号：US20080171741A1

公开(公告)日：2008-07-17

申请号：US11923760

申请日：2007-10-25

申请人： Stephen T. Wrobleski ,  Jagabandhu Das ,  T.G. Murali Dhar ,  Alaric J. Dyckman ,  John Hynes ,  Katerina Leftheris ,  James Lin ,  Shuqun Lin

发明人： Stephen T. Wrobleski ,  Jagabandhu Das ,  T.G. Murali Dhar ,  Alaric J. Dyckman ,  John Hynes ,  Katerina Leftheris ,  James Lin ,  Shuqun Lin

IPC分类号： A61K31/5377 ,  C07D261/06 ,  C07D271/10 ,  C07D271/06 ,  C07D211/86 ,  C07D253/06 ,  C07D333/06 ,  C07D413/10 ,  A61P29/00 ,  C07D413/06 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/4412 ,  A61K31/53 ,  A61K31/381

CPC分类号： C07D261/18 ,  C07C237/42 ,  C07C2601/02 ,  C07D207/456 ,  C07D209/08 ,  C07D209/42 ,  C07D211/62 ,  C07D213/81 ,  C07D213/82 ,  C07D231/56 ,  C07D233/90 ,  C07D235/06 ,  C07D249/06 ,  C07D271/06 ,  C07D271/10 ,  C07D275/03 ,  C07D295/192 ,  C07D307/68 ,  C07D333/38 ,  C07D409/04 ,  C07D487/04 ,  C07D513/04

摘要： A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.

摘要翻译： 式I化合物及其对映异构体，非对映异构体和药学上可接受的盐。 还公开了含有式I化合物的药物组合物，以及治疗与p38激酶活性相关的病症的方法。

公开(公告)号：US20080033012A1

公开(公告)日：2008-02-07

申请号：US11788755

申请日：2007-04-20

申请人： Ana Gil ,  Ana Morera ,  Maria Perez ,  Mercedes Cascon ,  Isabel Diaz ,  Francisco Moreno Munoz ,  Francisco Jurado

发明人： Ana Gil ,  Ana Morera ,  Maria Perez ,  Mercedes Cascon ,  Isabel Diaz ,  Francisco Moreno Munoz ,  Francisco Jurado

IPC分类号： A61K31/433 ,  A61K31/4436 ,  A61K31/4535 ,  A61P17/06 ,  A61P25/28 ,  A61P35/00 ,  C07D285/08 ,  C07D417/04

CPC分类号： C07D207/456 ,  C07C49/395 ,  C07C49/597 ,  C07D209/48 ,  C07D249/12 ,  C07D277/36 ,  C07D285/08 ,  C07D417/12

摘要： Compounds of general formula (I): where A, E, G, X, Y and the bond - - - take various meanings are of use in the preparation of a pharmaceutical formulation, for example in the treatment of a disease in which GSK-3 is involved, including Alzheimer's disease or the non-dependent insulin diabetes mellitus, or hyperproliferative disease such as cancer, displasias or metaplasias of tissue, psoriasis, arteriosclerosis or restenosis.

摘要翻译： 通式（I）的化合物：其中A，E，G，X，Y和键 - 具有各种含义，可用于制备药物制剂，例如用于治疗GSK- 3涉及阿尔茨海默病或非依赖性胰岛素糖尿病，或过度增生性疾病如癌症，组织移位或化生，银屑病，动脉硬化或再狭窄。