公开(公告)号：US08227496B2

公开(公告)日：2012-07-24

申请号：US12689878

申请日：2010-01-19

申请人： Hong-Suk Suh ,  Jin Soo Lee ,  Pan-Soo Kim ,  Yun-Ha Hwang ,  Jei Man Ryu ,  Yong-Ho Chung ,  Eun-Joo Kim ,  Do-Hui Kim ,  Yong-Youp Park

发明人： Hong-Suk Suh ,  Jin Soo Lee ,  Pan-Soo Kim ,  Yun-Ha Hwang ,  Jei Man Ryu ,  Yong-Ho Chung ,  Eun-Joo Kim ,  Do-Hui Kim ,  Yong-Youp Park

IPC分类号： A01N43/78 ,  A01N37/52 ,  A61K31/425 ,  A61K31/155 ,  C07D277/60 ,  C07D416/00 ,  C07C249/00 ,  C07C251/00 ,  C07C259/00 ,  C07C291/00

CPC分类号： A61K31/426 ,  Y10S514/878

摘要： A method of treating osteoporosis comprising administering to a subject a composition comprising a compound, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or a salt thereof, is described. A method of inhibiting osteoclast activity and stimulating osteoblast activity in a subject also is described.

摘要翻译： 一种治疗骨质疏松症的方法，包括向受试者施用包含化合物4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒或 其盐。 还描述了抑制破骨细胞活性并刺激受试者成骨细胞活性的方法。

公开(公告)号：US07884246B2

公开(公告)日：2011-02-08

申请号：US12092454

申请日：2006-11-01

申请人： Fabrice Gallou ,  Heewon Lee ,  Chris Hugh Senanayake ,  Jinhua J. Song ,  Zhulin Tan ,  Jinghua Xu ,  Nathan K. Yee

发明人： Fabrice Gallou ,  Heewon Lee ,  Chris Hugh Senanayake ,  Jinhua J. Song ,  Zhulin Tan ,  Jinghua Xu ,  Nathan K. Yee

IPC分类号： C07C259/00

CPC分类号： C07C213/02 ,  C07C249/08 ,  C07C251/44 ,  C07C2601/16 ,  C07C217/84

摘要： Disclosed is a process for preparing substituted anisidines of formula I starting from substituted cyclic hydroxy-ketones II via aromatization through a substituted oxime intermediate IV in which R is C1-C6 alkyl or halogen, and Alk is C1-C6 alkyl. The substituted anisidines of formula I have been found to be useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections.

摘要翻译： 公开了通过芳族化通过其中R是C 1 -C 6烷基或卤素的取代的肟中间体IV和Alk是C 1 -C 6烷基的取代的环状羟基酮II制备取代的茴香胺的方法。 已经发现式I的取代的茴香醚可用作制备用于治疗丙型肝炎病毒（HCV）感染的药剂的中间体。

公开(公告)号：US20100197676A1

公开(公告)日：2010-08-05

申请号：US12752396

申请日：2010-04-01

申请人： Yoshiaki Isshiki ,  Yasunori Kohchi ,  Eisaku Mizuguchi ,  Hitoshi Iikura ,  Yasuaki Matsubara ,  Shinji Tsujii ,  Nobuo Shimma ,  Masanori Miwa ,  Satoshi Aida ,  Masami Kohchi ,  Takeshi Murata ,  Kosuke Aso

发明人： Yoshiaki Isshiki ,  Yasunori Kohchi ,  Eisaku Mizuguchi ,  Hitoshi Iikura ,  Yasuaki Matsubara ,  Shinji Tsujii ,  Nobuo Shimma ,  Masanori Miwa ,  Satoshi Aida ,  Masami Kohchi ,  Takeshi Murata ,  Kosuke Aso

IPC分类号： A61K31/539 ,  A61P19/02 ,  A61K31/16 ,  C07C259/00 ,  C07D209/32 ,  A61K31/4035 ,  C07D265/02 ,  A61K31/535 ,  C07D273/01

CPC分类号： C07C259/10 ,  C07C317/18 ,  C07C323/12 ,  C07D207/27 ,  C07D211/76 ,  C07D239/10 ,  C07D261/04 ,  C07D263/22 ,  C07D265/02 ,  C07D265/32 ,  C07D273/00

摘要： An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases.The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

摘要翻译： 本发明的目的是提供具有强MEK抑制活性并且在体内稳定且可溶于水的化合物，其可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示：[其中R1，R2，R3，R4和X与本专利申请中定义相同]。

公开(公告)号：US07642280B2

公开(公告)日：2010-01-05

申请号：US10474138

申请日：2002-04-08

申请人： Robert C. Fahey ,  Gerald L. Newton ,  Carole A. Bewley ,  Gillian Nicholas

发明人： Robert C. Fahey ,  Gerald L. Newton ,  Carole A. Bewley ,  Gillian Nicholas

IPC分类号： A61K31/415 ,  A61K31/15 ,  C07D223/00 ,  C07C259/00

CPC分类号： C07D213/06 ,  C07C225/06 ,  C07C279/12 ,  C07D213/36 ,  C07D233/88 ,  C07D413/12 ,  C07D413/14 ,  C07H15/12

摘要： The present invention provides compounds with activity as inhibitors of acyl glucosaminylinositol amidases with amidase activity against S-conjugate amides, particularly mycothiol-derived S-conjugate amides. Certain of the invention compounds are naturally occurring compounds obtained from marine sponges and other organisms. The invention further provides methods for using the compounds to inhibit virulence and reduce antibiotic resistance of mycothiol-producing bacteria.

摘要翻译： 本发明提供了作为具有针对S-缀合物酰胺的酰胺酶活性的酰基葡糖胺基肌氨酸酰胺酶抑制剂的活性的化合物，特别是由咪唑硫醇衍生的S-缀合物酰胺。 某些本发明化合物是从海洋海绵和其他生物得到的天然存在的化合物。 本发明进一步提供了使用该化合物来抑制产毒霉菌产生菌的毒力并减少抗生素抗性的方法。

公开(公告)号：US20090297417A1

公开(公告)日：2009-12-03

申请号：US12472508

申请日：2009-05-27

申请人： William H. Sun ,  John M. Boyle ,  Ronald A. Lau

发明人： William H. Sun ,  John M. Boyle ,  Ronald A. Lau

IPC分类号： B01D53/56 ,  C07C259/00 ,  C01C1/00 ,  B01J7/00

CPC分类号： B01B1/005 ,  B01D53/90 ,  B01D2251/2067 ,  B01D2257/404 ,  C01C1/086 ,  F01N3/2066 ,  F01N2240/20 ,  F01N2240/40 ,  F01N2610/02

摘要： Disclosed are methods and apparatus enabling the efficient utilization of urea for purposes such as selective catalytic reduction (SCR) of NOx, which enable feeding urea to a chamber designed to efficiently and completely gasify the urea to enable ammonia feed. Preferably, aqueous urea is fed to a gasification chamber, which is also fed with heated gases. An injector means, capable of distributing the aqueous urea as fine droplets, is positioned centrally of a gas distribution plate in the chamber. An arrangement of spaced holes in the gas distribution plate provides higher gas velocity in the vicinity of the injector means than near the walls of the chamber. Uniform gas distribution without equipment fouling is achieved.

摘要翻译： 公开了能够有效利用尿素的方法和装置，例如NOx的选择性催化还原（SCR），其使得能够将尿素输送到设计成有效地和完全气化尿素以使氨进料的室。 优选地，将水性尿素供给到气化室，其也被加热气体。 能够将尿素作为细小液滴分配的喷射器装置位于腔室中的气体分配板的中心。 在气体分配板中的间隔开的孔的布置在喷射器装置附近提供比在腔的壁附近更高的气体速度。 实现无设备污染的均匀气体分配。

公开(公告)号：US20080200525A1

公开(公告)日：2008-08-21

申请号：US12098594

申请日：2008-04-07

申请人： Werner Zambach ,  Roger Graham Hall ,  Peter Renold ,  Stephan Trah

发明人： Werner Zambach ,  Roger Graham Hall ,  Peter Renold ,  Stephan Trah

IPC分类号： A01N43/40 ,  C07C233/02 ,  C07C259/00 ,  A01N37/18 ,  A01N33/24 ,  A01N43/80 ,  C07D261/02 ,  A01P17/00 ,  C07D211/82

CPC分类号： C07D333/58 ,  A01N33/24 ,  A01N35/10 ,  A01N37/52 ,  A01N41/06 ,  A01N43/10 ,  A01N43/40 ,  A01N43/78 ,  A01N43/80 ,  C07C49/753 ,  C07C49/755 ,  C07C49/84 ,  C07C235/84 ,  C07C251/44 ,  C07C251/48 ,  C07C251/54 ,  C07C251/58 ,  C07C311/04 ,  C07C311/05 ,  C07C311/09 ,  C07C323/47 ,  C07D213/50 ,  C07D213/53 ,  C07D213/61 ,  C07D213/64 ,  C07D261/08 ,  C07D277/24 ,  C07D277/28 ,  C07D307/52 ,  C07D307/81 ,  C07D333/22

摘要： Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(═O)—O— or —O—C(═O)—; T is, for example, a bond, O, S, SO, SO2, —C(═O)—O— or —O—C(═O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkylcarbonyl or formyl; k is 0, 1, 2, 3 or 4; m is 1 or 2; and q is 0, 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds and their use, pesticidal compositions in which the active ingredient has been selected from those compounds and agrochemically acceptable salts thereof, and a process for the preparation of those compositions and their use, to plant propagation material treated with those compositions, and a method of controlling pests.

公开(公告)号：US20010015267A1

公开(公告)日：2001-08-23

申请号：US09742865

申请日：2000-12-20

申请人： Penford Corporation

发明人： Edward P. Pauley ,  Katherine Sue Neighbor

IPC分类号： B32B029/06 ,  C07C259/00

CPC分类号： D06M15/285 ,  C07C41/50 ,  C07C41/56 ,  C07C43/303 ,  C08B15/00 ,  C08B31/00 ,  D06M13/137 ,  D06M15/11 ,  D06M15/59 ,  D21H17/06 ,  D21H17/29 ,  D21H17/375 ,  D21H17/55 ,  D21H21/16 ,  Y10T442/2402

摘要： Improved water resistant acetal sizing agents including 1,1-octadecoxyoctadecane are provided along with methods for their synthesis including methods in which C8 to C30 alkyl bromides are reacted with a polyol under basic conditions and those in which a C8 to C30 primary alcohol is reacted with an organic base in the presence of a suitable oxidizing agent under basic conditions.

摘要翻译： 提供包括1,1-十八烷氧基十八烷在内的改进的防水缩醛施胶剂及其合成方法，包括在碱性条件下使C8〜C30烷基溴与多元醇反应的方法，以及其中C8〜C30伯醇与 在碱性条件下在合适的氧化剂存在下的有机碱。

公开(公告)号：US6031130A

公开(公告)日：2000-02-29

申请号：US81943

申请日：1998-05-21

申请人： Masuji Motoki ,  Tadahisa Sato

发明人： Masuji Motoki ,  Tadahisa Sato

IPC分类号： C07D295/22 ,  B01J23/36 ,  C07B61/00 ,  C07C239/08 ,  C07C239/10 ,  C07C239/12 ,  C07C253/30 ,  C07C255/64 ,  C07D207/46 ,  C07D209/08 ,  C07D217/08 ,  C07C239/00 ,  C07C259/00

CPC分类号： C07C253/30 ,  C07C239/10 ,  C07C239/12

摘要： A method for preparing N,N-disubstituted hydroxylamine compounds represented by the formula (II): HO--N(R.sup.1)(R.sup.2) wherein R.sup.1 and R.sup.2 may be the same or different, and independently represent a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, which comprises the step of adding a rhenium catalyst and aqueous hydrogen peroxide to a mixture containing a secondary amine compound represented by the formula (I): HN(R.sup.1)(R.sup.2) wherein R.sup.1 and R.sup.2 have the same meanings as those defined above and a dehydrating agent.

摘要翻译： 制备由式（II）表示的N，N-二取代羟胺化合物的方法：HO-N（R1）（R2）其中R1和R2可以相同或不同，并且独立地表示取代或未取代的烷基， 取代或未取代的芳基或取代或未取代的芳族杂环基，其包括将铼催化剂和过氧化氢水溶液加入到由式（I）表示的仲胺化合物的混合物中：HN（R1）（R2 ）其中R1和R2具有与上述相同的含义和脱水剂。

公开(公告)号：US20230270894A1

公开(公告)日：2023-08-31

申请号：US18049609

申请日：2022-10-25

申请人： REGENERON PHARMACEUTICALS, INC.

发明人： Marcus Kelly ,  Dangshe Ma ,  William Olson ,  Gavin Thurston ,  Richard Tavare

IPC分类号： A61K51/10 ,  C07K16/28 ,  A61K39/00 ,  C07C259/00

CPC分类号： A61K51/1027 ,  C07K16/2803 ,  A61K51/1039 ,  A61K39/00 ,  C07C259/00 ,  C07K2317/21

摘要： Radiolabeled anti-LAG3 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of LAG3 proteins in a patient or sample.

公开(公告)号：US20210138096A1

公开(公告)日：2021-05-13

申请号：US17127618

申请日：2020-12-18

申请人： REGENERON PHARMACEUTICALS, INC.

发明人： Marcus Kelly ,  Dangshe Ma ,  William Olson ,  Gavin Thurston ,  Richard Tavare

IPC分类号： A61K51/10 ,  C07K16/28 ,  A61K39/00 ,  C07C259/00

摘要： Radiolabeled anti-LAG3 antibodies and their use in immuno-PET imaging are provided herein. Included are methods of detecting the presence of LAG3 proteins in a patient or sample.