公开(公告)号：US07964648B2

公开(公告)日：2011-06-21

申请号：US12688038

申请日：2010-01-15

申请人： Matthew W. Davis

发明人： Matthew W. Davis

IPC分类号： A01N37/18 ,  A01N43/50 ,  A61K31/16 ,  A61K31/497 ,  A61K31/415 ,  C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  C07C239/00 ,  C07C211/00 ,  C07C205/00 ,  C07C207/00

CPC分类号： A61K31/165 ,  A61K31/496 ,  G06F19/00 ,  G06Q50/22 ,  A61K2300/00

摘要： Methods for concomitant administration of colchicine together with one or more second active agents, e.g., ketoconazole and ritonavir, are disclosed. Such methods reduce the dangers commonly associated with such concomitant administration and provide additional benefits. Methods of notifying health care practitioners and patients regarding appropriate dosing for concomitant administration of colchicine together with second active agents are also provided.

公开(公告)号：US07718145B2

公开(公告)日：2010-05-18

申请号：US11597756

申请日：2006-03-17

申请人： Masaaki Sasaki ,  Hirofumi Takahashi ,  Kouji Maeba ,  Takao Naito ,  Kouichirou Terada ,  Takashi Yamaguchi ,  Takuya Saeki

发明人： Masaaki Sasaki ,  Hirofumi Takahashi ,  Kouji Maeba ,  Takao Naito ,  Kouichirou Terada ,  Takashi Yamaguchi ,  Takuya Saeki

IPC分类号： B01J8/00 ,  B01J10/00 ,  C07C205/00 ,  C07C207/00

CPC分类号： C01B7/0725 ,  B01D53/18 ,  B01D53/68 ,  B01D2251/304 ,  B01D2251/306 ,  B01D2257/2045 ,  C01B7/04 ,  C07C263/10 ,  C07C265/14

摘要： A polyisocyanate production system is provided that can stably produce chlorine from hydrogen chloride produced secondarily while reacting stably between carbonyl chloride and polyamine and can perform an effective treatment of the hydrochloric gas produced secondarily. A hydrochloric gas control unit 32 controls a flow-rate control valve 23 to keep constant an amount of hydrogen chloride supplied from a hydrogen chloride purifying tank 4 to a hydrogen chloride oxidation reactor 6 via a second hydrochloric-gas connection line 11 to be constant, and also controls a pressure control valve 22 based on an inner pressure of the hydrogen chloride purifying tank 4 input from a pressure sensor 25 to discharge the hydrochloric gas from the hydrogen chloride purifying tank 4 to the hydrogen chloride absorbing column 5 via a first hydrochloric-gas connection line 10, so as to keep an inner pressure of the hydrogen chloride purifying tank 4 to be constant.

摘要翻译： 提供了一种多异氰酸酯生产系统，其能够在氯化碳和多胺之间稳定反应的同时使氯化氢稳定地产生氯，同时可以对二次生成的盐酸进行有效的处理。 盐酸气体控制单元32控制流量控制阀23，使得从氯化氢净化槽4经由第二盐酸气体连接管线11将氯化氢供给到氯化氢氧化反应器6的量恒定， 并且还基于从压力传感器25输入的氯化氢净化槽4的内部压力来控制压力控制阀22，以通过第一盐酸盐排出氯化氢净化槽4的氯化氢气体到氯化氢吸收塔5。 气体连接管线10，以使氯化氢净化槽4的内部压力保持恒定。

公开(公告)号：US07696373B2

公开(公告)日：2010-04-13

申请号：US12293374

申请日：2007-04-13

申请人： S. Bruce King

发明人： S. Bruce King

IPC分类号： C07C69/76 ,  C07C207/00 ,  A61K31/235 ,  A61K31/04

CPC分类号： C07C207/04 ,  C07C2601/14

摘要： Active compounds of Formula (I) are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.

摘要翻译： 描述了式（I）的活性化合物：其中：R 1和R 2各自独立地为C 1 -C 4烷基; 或R 1和R 2一起形成C 2 -C 7亚烷基链; Z是非甾体抗炎药（NSAID）; 以及其药学上可接受的盐和前药，及其使用方法。

公开(公告)号：US07696247B2

公开(公告)日：2010-04-13

申请号：US10885055

申请日：2004-07-06

申请人： Robert A. Herrmann ,  Wendy Naimark

发明人： Robert A. Herrmann ,  Wendy Naimark

IPC分类号： A61K31/20 ,  A01N33/26 ,  C07C205/00 ,  C07C207/00 ,  C07C241/00 ,  C07C243/00

CPC分类号： A61L29/16 ,  A61K45/06 ,  A61L15/44 ,  A61L31/16 ,  A61L2300/114 ,  A61L2300/416 ,  C07C243/42 ,  C07J41/0055 ,  Y10T436/104165

摘要： Novel nitric-oxide releasing lipid molecules are provided which comprise a lipid molecule selected from (a) phosphoglycerides, (b) lipids having a sphingosine base as a backbone, (c) monoacylglyerols, (d) diacylglycerols, (e) glycosylacylglycerols, and (f) sterol compounds of the formula: where R is a branched aliphatic chain of eight or more carbon atoms, wherein the lipid molecule is provided with a nitric-oxide containing group which comprises (a) a —S—N═O moiety, (b) a —O—N═O moiety, or (c) a a moiety. Also provided are methods of forming such nitric oxide releasing lipid molecules. Various pharmaceutical compositions, topical liquids and drug delivery systems comprising the nitric-oxide releasing lipid molecules are also described. Further provided are methods for therapeutically administering nitric oxide to patients, methods of treating or preventing various conditions, methods for promoting wound healing and methods of reducing the cells present in an atherosclerotic lesion, which methods utilize the nitric-oxide releasing lipid molecules.

摘要翻译： 提供新的一氧化氮释放脂质分子，其包含选自（a）磷酸甘油酯，（b）具有鞘氨醇碱作为主链的脂质的脂质分子，（c）单酰基甘醇，（d）二酰基甘油，（e）糖基酰基甘油和（ f）下式的甾醇化合物：其中R是具有8个或更多个碳原子的支链脂族链，其中所述脂质分子具有含一氧化氮的基团，其包含（a）-S-N = O部分，（ b）-O-N = O部分，或（c）aa部分。 还提供了形成这种一氧化氮释放脂质分子的方法。 还描述了包含释放一氧化氮的脂质分子的各种药物组合物，局部液体和药物递送系统。 还提供了向患者治疗性给予一氧化氮的方法，治疗或预防各种病症的方法，促进伤口愈合的方法以及减少存在于动脉粥样硬化病变中的细胞的方法，该方法利用释放一氧化氮的脂质分子。

公开(公告)号：US20050203295A1

公开(公告)日：2005-09-15

申请号：US11052777

申请日：2005-02-09

申请人： Jonathan Stamler ,  Eric Toone

发明人： Jonathan Stamler ,  Eric Toone

IPC分类号： A61K31/00 ,  A61K31/194 ,  A61K31/195 ,  A61K31/222 ,  A61K31/553 ,  A61K31/635 ,  A61K38/00 ,  A61L27/00 ,  A61L31/00 ,  A61P7/02 ,  A61P9/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  C07C207/00 ,  C07C291/08 ,  C07D231/12 ,  C07D267/04 ,  C07D279/02 ,  C07D267/02

CPC分类号： C07C207/00 ,  A61K31/00 ,  A61K31/195 ,  A61K2300/00

摘要： A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to about 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. The compound is preferably water-soluble and preferably contains a carbon alpha to the nitrosylated carbon which is part of a ketone group. In one embodiment, the C-nitroso compound is obtained by nitrosylation of a conventional drug or such drug modified to modify the carbon acid pKa thereof When such drug is a nonsteroidal anti-inflammatory drug, the resulting C-nitroso compound functions as a COX-1 and COX-2 inhibitor without the deleterious effects associated with COX-1 inhibition but with the advantageous effects associated with COX-1 and COX-2 inhibition. One such C-nitroso compound is a nitrosoketoibuprofen. A specific example of this kind of compound is isolated as dimeric 2-[4′-(α-nitroso)isobutyrylphenyl]propionic acid. In another case, the C-nitroso compound contains the moiety where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.

摘要翻译： 单体基团的分子量范围为约225至约1,000（约225至约600）的C-亚硝基化合物，其中亚硝基连接到叔碳上，其通过碳的亚硝基化获得 pKa小于约25的酸可用作NO供体。 当化合物从pKa小于约10的碳酸获得时，当以微摩尔浓度使用时，其提供血管松弛效果，并且该活性由以纳摩尔浓度获得的谷胱甘肽加强。 当化合物由pKa为约15至约20的碳酸获得时，在没有谷胱甘肽的纳摩尔浓度下获得血管松弛效果。 该化合物优选是水溶性的并且优选地含有作为酮基的一部分的亚硝基化碳的碳α。 在一个实施方案中，C-亚硝基化合物通过常规药物的亚硝基化或经修饰以改变其碳酸pKα的药物而获得。当这种药物是非甾体抗炎药物时，所得的C-亚硝基化合物起COX- 1和COX-2抑制剂，没有与COX-1抑制相关的有害作用，但具有与COX-1和COX-2抑制相关的有利效果。 一种这样的C-亚硝基化合物是亚硝基基布洛芬。 这种化合物的具体实例被分离为二聚2- [4' - （α-亚硝基）异丁酰苯基]丙酸。 在另一种情况下，C-亚硝基化合物包含其中X是S，O或NR的部分。 一个实施方案涉及其中叔碳原子和/或氧原子和/或硫原子被亚硝酰化的COX-2抑制剂。

公开(公告)号：US06887994B2

公开(公告)日：2005-05-03

申请号：US10346146

申请日：2003-01-17

申请人： Jonathan S. Stamler ,  Eric J. Toone

发明人： Jonathan S. Stamler ,  Eric J. Toone

IPC分类号： A61K31/00 ,  A61K31/194 ,  A61K31/195 ,  A61K31/222 ,  A61K31/553 ,  A61K31/635 ,  A61K38/00 ,  A61L27/00 ,  A61L31/00 ,  A61P7/02 ,  A61P9/10 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  C07C207/00 ,  C07C291/08 ,  C07D231/12 ,  C07D267/04 ,  C07D231/04 ,  C07D237/04 ,  C07D261/02 ,  C07D295/24

CPC分类号： C07C207/00 ,  A61K31/00 ,  A61K31/195 ,  A61K2300/00

摘要： A C-nitroso compound having a molecular weight ranging from about 225 to about 1,000 (from about 225 to about 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. In another case, the C-nitroso compound contains the moiety —C—N(O)X— where X is S, O or NR. One embodiment is directed to COX-2 inhibitors where a tertiary carbon atom and/or an oxygen atom and/or a sulfur atom is nitrosylated.

摘要翻译： 单体基团的分子量范围为约225至约1,000（约225至约600）的C-亚硝基化合物，其中亚硝基连接到叔碳上，其通过碳的亚硝基化获得 pKa小于约25的酸可用作NO供体。 在另一种情况下，C-亚硝基化合物包含部分<？in-line-formula description =“In-line Formulas”end =“lead”？> CN（O）X - <？in-line-formula description = “In-line Formulas”end =“tail”？>其中X是S，O或NR。 一个实施方案涉及其中叔碳原子和/或氧原子和/或硫原子被亚硝酰化的COX-2抑制剂。

公开(公告)号：US20010005762A1

公开(公告)日：2001-06-28

申请号：US09748924

申请日：2000-12-27

发明人： Tetsuya Shintaku ,  Masahide Tanaka ,  Nobushige Itaya

IPC分类号： C07C205/00 ,  C07C207/00 ,  C07C051/16 ,  C07C051/235

CPC分类号： C07C201/16 ,  C07C205/51 ,  C07C205/53

摘要： The present invention provides a method of producing easily and in a high yield a threo-2-hydroxy-3-nitrobutanoic acid compound or a mixture of a threo- and an erythro-2-hydroxy-3-nitrobutanoic acid compounds, this mixture having an erythro compound:threo compound ratio of about 1:1, which method includes reacting, in a solvent, a 2-hydroxy-3-nitrobutanoic acid compound having the formula (I) 1 wherein R is optionally substituted alkyl or optionally substituted aryl, with not less than 1 equivalent of a base to isomerize (i) the erythro compound into the threo compound, or (ii) the threo compound into the erythro compound, and a method for separating the erythro and the threo compounds easily and in a high yield. The separation method includes reacting the mixture of threo- and erythro-compounds with not more than 1 equivalent of potassium carbonate per threo compound in a solvent. According to the method of the present invention, useful pharmaceuticals can be produced easily in a high yield.

摘要翻译： 本发明提供了一种容易且高产率地制备苏-22-羟基-3-硝基丁酸化合物或苏 - 和 - 赤-2-羟基-3-硝基丁酸化合物的混合物的方法，该混合物具有 红霉素化合物：苏化合物比例为约1:1，该方法包括在溶剂中使具有式（I）的2-羟基-3-硝基丁酸化合物（其中R是任选取代的烷基或任选取代的芳基）与 不少于1当量的碱，将（i）赤式化合物异构化为苏化合物，或（ii）苏化合物进入赤式化合物，以及容易且高收率地分离赤式和苏式化合物的方法 。 分离方法包括在溶剂中使苏氨酸和赤式化合物的混合物与不多于1当量的碳酸钾/苏化合物反应。 根据本发明的方法，可以容易地以高产率制备有用的药物。

公开(公告)号：US5136081A

公开(公告)日：1992-08-04

申请号：US405232

申请日：1989-09-11

申请人： Paul H. Briner

发明人： Paul H. Briner

IPC分类号： C07C67/333 ,  B01J23/04 ,  C07B61/00 ,  C07C45/63 ,  C07C45/74 ,  C07C49/697 ,  C07C49/747 ,  C07C49/753 ,  C07C51/353 ,  C07C61/39 ,  C07C61/40 ,  C07C62/32 ,  C07C62/34 ,  C07C62/38 ,  C07C63/331 ,  C07C67/00 ,  C07C67/293 ,  C07C67/475 ,  C07C69/753 ,  C07C69/757 ,  C07C69/76 ,  C07C201/12 ,  C07C205/45 ,  C07C205/55 ,  C07C227/02 ,  C07C227/16 ,  C07C229/46 ,  C07C231/12 ,  C07C235/84 ,  C07C253/30 ,  C07C255/57 ,  C07C315/04 ,  C07C317/24 ,  C07C317/44 ,  C07C319/20 ,  C07C323/22 ,  C07C323/62 ,  C07C255/50 ,  C07C205/00 ,  C07C207/00 ,  C07C211/00 ,  C07C315/00 ,  C07C317/00 ,  C07C321/00 ,  C07C323/00

CPC分类号： C07C45/63 ,  C07C45/74 ,  C07C49/697 ,  C07C49/753 ,  C07C2101/08 ,  C07C2101/10 ,  C07C2101/14

摘要： The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.

公开(公告)号：US4621126A

公开(公告)日：1986-11-04

申请号：US731499

申请日：1985-05-07

申请人： William J. Middleton

发明人： William J. Middleton

IPC分类号： C07C17/00 ,  C07C17/093 ,  C07C17/26 ,  C07C17/269 ,  C07C17/275 ,  C07C17/281 ,  C07C17/358 ,  C07C19/08 ,  C07C19/10 ,  C07C19/14 ,  C07C21/18 ,  C07C22/08 ,  C07C23/06 ,  C07C23/08 ,  C07C207/00 ,  C07C381/12 ,  C07D295/26 ,  C08F4/00 ,  C08F18/10

CPC分类号： C07C381/12 ,  C07C17/00 ,  C07C17/358 ,  C07C19/08 ,  C07C201/00 ,  C07C23/06 ,  C07C23/08 ,  C07C23/10 ,  C07C23/18 ,  C07C245/06 ,  C07D295/26

摘要： Tris(disubstituted amino)sulfonium perfluorocarbanion salts, process for their preparation and the use thereof as catalysts in group transfer polymerization.

摘要翻译： 三（二取代氨基）锍全氟碳酸盐，其制备方法及其在组转移聚合中的用途。

公开(公告)号：US4615876A

公开(公告)日：1986-10-07

申请号：US488184

申请日：1983-04-25

申请人： David E. Troutner ,  Wynn A. Volkert

发明人： David E. Troutner ,  Wynn A. Volkert

IPC分类号： A61K51/00 ,  A61K51/04 ,  C07B59/00 ,  C07C51/363 ,  C07C53/19 ,  C07C207/00 ,  C07C251/70 ,  C07D295/13 ,  C07D295/15 ,  C07F13/00 ,  G21G4/08 ,  A61K43/00 ,  A61K49/00

CPC分类号： C07D295/13 ,  A61K51/04 ,  C07C51/363 ,  C07C53/19 ,  C07D295/15 ,  C07F13/005 ,  A61K2123/00

摘要： Stable neutral-lipophilic complexes of technetium-99m (Tc-99m) useful as diagnostic radionuclidic imaging agents are formed by complexing technetium-99m pertechnetate with alkylene amine oximes (viz. propylene amine oxime) in aqueous solutions under reducing conditions. The complexes have a zero charge, contain an O--H--O ring closure bond, and are sufficiently stable for parental administration in imaging by scintillation scanning. Substituents can be attached to the C.sub.2 to C.sub.4 alkylene carbon backbone of the tetradentate amine oxime ligands to structurally modify them and produce a variety of Tc-99m-radiopharmaceuticals with specific body imaging applications.

摘要翻译： 通过在还原条件下在水溶液中将99吨高锝酸锝与亚胺胺肟（即丙烯胺肟）络合来形成用作诊断性放射性核素显像剂的锝-99m（Tc-99m）稳定的中性 - 亲脂性络合物。 络合物具有零电荷，含有O-H-O闭环键，并且通过闪烁扫描在成像中对于亲本施用是足够稳定的。 取代基可以连接到四齿胺肟配体的C2至C4亚烷基碳主链上，以对其进行结构修饰并产生具有特定身体成像应用的各种Tc-99m放射性药物。