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41. 发明申请

US20040006130A1 Calcium receptor antagonist 失效
标题翻译：钙受体拮抗剂
公开(公告)号：US20040006130A1
公开(公告)日：2004-01-08
申请号：US10344157
申请日：2003-02-10
发明人： Yuko Shinagawa , Takeo Katsushima , Takashi Nakagawa
IPC分类号： C07D317/44 , C07C255/50 , C07C215/46 , A61K031/277 , A61K031/137 , A61K031/335
CPC分类号： C07D213/30 , C07B2200/07 , C07C217/28 , C07C217/60 , C07C217/76 , C07C229/38 , C07C233/25 , C07C235/42 , C07C235/60 , C07C237/30 , C07C255/54 , C07C311/21 , C07C311/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D277/24 , C07D307/42 , C07D317/58 , C07D333/16 , C07D333/56
摘要： A compound of the formula nullInull 1 wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided. The compound of the present invention is useful as a therapeutic drug of diseases accompanied by abnormal calcium homeostasis, or osteoporosis, hypoparathyreosis, osteosarcoma, periodontal disease, bone fracture, steoarthrosis, chronic rheumatoid arthritis, Paget's disease, humoral hypercalcemia, autosomal dominant hypocalcemia and the like. In addition, an intermediate for the compound is provided.
摘要翻译：式[I]的化合物，其中R 1是任选取代的芳基或任选取代的杂芳基; R 2是任选取代的C 1-6烷基，C 3-7环烷基等; R 3是氢原子，C 1-6烷基，羟基等; R 4是氢原子，C 1-6烷基等; R 5和R 6各自为C 1-6烷基等; R 7是任选取代的芳基或任选取代的杂芳基; X 1，X 2和X 3各自为C 1-6亚烷基等; 和X 4和X 5各自为单键，亚甲基等，其盐，其溶剂合物或其前药，以及含有该化合物，特别是钙受体拮抗剂和治疗剂的药物组合物提供骨质疏松症药物。本发明的化合物可用作伴有异常钙稳态或骨质疏松症，hypoparathyreosis，骨肉瘤，牙周病，骨折，骨关节炎，慢性类风湿性关节炎，佩吉特氏病，体液性高钙血症，常染色体显性低钙血症的疾病的治疗药物喜欢。此外，还提供了化合物的中间体。

42. 发明申请

US20030049310A1 Cationic liposomes for gene transfer 失效
标题翻译：阳离子脂质体用于基因转移
公开(公告)号：US20030049310A1
公开(公告)日：2003-03-13
申请号：US10224706
申请日：2002-08-20
申请人： Vanderbilt University
发明人： Xiang Gao
IPC分类号： A61K048/00 , A61K009/127 , C07C229/04
CPC分类号： C07D295/088 , A61K9/1272 , A61K48/0025 , C07C211/09 , C07C211/14 , C07C211/21 , C07C211/63 , C07C217/08 , C07C217/28 , C07C219/06 , C07C219/08 , C07C229/12 , C07C229/16 , C07C233/36 , C07C233/38 , C07C237/06 , C07C237/10 , C07C237/12 , C07C237/20 , C07C255/24 , C07C271/22 , C07C275/16 , C07C279/24 , C07D295/13 , C07D295/24 , C07D295/30 , C07D295/32 , C12N15/88 , Y10S977/907 , Y10S977/923
摘要： The present invention relates to synthetic cationic lipids, liposome formulations and the use of such compounds to introduce functional bioactive agents into cultured cells.
摘要翻译：本发明涉及合成阳离子脂质，脂质体制剂和这些化合物在培养细胞中引入功能性生物活性剂的用途。

43. 发明授权

US06388134B1 Derivatives of 6-(4-phenylbutoxy)hexylamine and process for producing Salmeterol 有权
标题翻译： 6-（4-苯基丁氧基）己胺的衍生物及其生产沙美特罗的方法
公开(公告)号：US06388134B1
公开(公告)日：2002-05-14
申请号：US09806538
申请日：2001-03-28
申请人： Jordi Bessa Bellmunt , Pere Dalmases Barjoan , Francisco Marquillas Olondriz
发明人： Jordi Bessa Bellmunt , Pere Dalmases Barjoan , Francisco Marquillas Olondriz
IPC分类号： C07C21300
CPC分类号： C07D319/08 , C07C213/08 , C07C217/28 , C07C217/40 , C07C271/16 , Y02P20/55 , C07C217/10
摘要： The present invention refers to new derivatives of the 6-(4-phenylbutoxy)hexylamine of the general formula (I): wherein: R1 is CHO or CHOR3OR4, where R3 and R4 independently are C1-C6 alkyl, aralkyl, or they form 5 or 6 membered cyclic acetals; and R2 is H, benzyl or an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group; and to a process for its obtention. The invention also refers to a new process for obtaining Salmeterol or its pharmaceutically acceptable salts, characterized in that reaction of an organometallic compound of the general formula (13) is carried out in an inert solvent at low temperature with a synthetic intermediate of the general formula (I), wherein R1 is CHO, and R2 is an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group.
摘要翻译：本发明涉及通式（I）的6-（4-苯基丁氧基）己胺的新衍生物：其中：R1是CHO或CHOR3OR4，其中R3和R4独立地是C1-C6烷基，芳烷基或它们形成5 或6元环状缩醛; 并且R 2是H，苄基或烷氧基羰基，芳氧基羰基，芳烷氧基羰基或酰基;以及其获得的方法。本发明还涉及获得沙美特罗或其药学上可接受的盐的新方法，其特征在于通式（13）的有机金属化合物在惰性溶剂中在低温下与通式（I），其中R1是CHO，R2是烷氧基羰基，芳氧基羰基，芳烷氧基羰基或酰基。

44. 发明授权

US06300323B1 (Poly)ethereal ammonium salts of herbicides bearing acidic moieties and their use as herbicides 有权
标题翻译：（Poly）具有酸性部分的除草剂醚醚铵盐及其作为除草剂的用途
公开(公告)号：US06300323B1
公开(公告)日：2001-10-09
申请号：US09634630
申请日：2000-08-08
申请人： Takahiro Haga , Kevin E. Crosby , Jeffrey R. Schussler
发明人： Takahiro Haga , Kevin E. Crosby , Jeffrey R. Schussler
IPC分类号： A01N5712
CPC分类号： C07D213/64 , A01N25/30 , A01N33/08 , A01N39/02 , A01N39/04 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/84 , A01N57/20 , C07C215/08 , C07C215/14 , C07C215/18 , C07C217/08 , C07C217/16 , C07C217/28 , C07C217/42 , C07C219/04 , C07C219/08 , C07D213/80 , C07D231/20 , C07D239/34 , C07D295/088 , C07F9/3813 , C08G65/33306
摘要： A compound Wherein x, y, and z are integers from 0 to 3; and the (poly)ethereal amine is at least one selected from compounds of formula II1 through II5:
摘要翻译：复合物，其中x，y和z是0至3的整数; 和（多）醚胺是选自式II1至II5的化合物中的至少一种：

45. 发明授权

US5723497A Amine derivative and dermatologic preparation containing the same 失效
标题翻译：胺衍生物和含有相同的皮肤病学制剂
公开(公告)号：US5723497A
公开(公告)日：1998-03-03
申请号：US513872
申请日：1995-09-18
申请人： Yukihiro Ohashi , Yukihiro Yada , Yoshinori Takema , Taketoshi Fujimori , Akira Kawamata , Hiroyuki Ohsu , Kazuhiko Higuchi , Genji Imokawa , Hiroshi Kusuoku , Ayumi Ogawa , Tsutomu Fujimura
发明人： Yukihiro Ohashi , Yukihiro Yada , Yoshinori Takema , Taketoshi Fujimori , Akira Kawamata , Hiroyuki Ohsu , Kazuhiko Higuchi , Genji Imokawa , Hiroshi Kusuoku , Ayumi Ogawa , Tsutomu Fujimura
IPC分类号： A61K8/41 , A61K8/46 , A61K8/49 , A61K8/68 , A61K31/13 , A61Q17/04 , A61Q19/00 , A61Q19/08 , C07C215/08 , C07C215/10 , C07C215/12 , C07C217/28 , C07C219/06 , C07C229/12 , C07C229/24 , C07C233/18 , C07C235/10 , C07C237/06 , C07C323/25 , C07D295/088 , C07D311/58 , C07D311/72 , C07D317/22 , C07F7/08 , C07F9/09 , C07H15/04
CPC分类号： C07C323/25 , A61K8/41 , A61K8/46 , A61K8/49 , A61K8/68 , A61Q19/00 , A61Q19/08 , C07C215/08 , C07C215/10 , C07C215/12 , C07C217/28 , C07C219/06 , C07C229/12 , C07C229/24 , C07C233/18 , C07C235/10 , C07D295/088 , C07D311/58 , C07D311/72 , C07D317/22 , C07F7/0818 , C07F7/0847 , C07F7/0852 , C07F9/091 , C07H15/04 , A61Q17/04 , Y10S514/844 , Y10S514/845 , Y10S514/873
摘要： The present invention relates to an amine derivative represented by the following general formula (I) or (II): ##STR1## wherein R.sup.1 means a heteroatom-containing C.sub.1 -C.sub.40 hydrocarbon group which may have a ring structure, or the like; R.sup.2 -R.sup.5 each denote a C.sub.1 -C.sub.20 hydrocarbon group, hydrogen or the like; A.sup.1 represents ##STR2## or R.sup.15 --Z--.sup.16 --(CH.sub.2).sub.n --; B.sup.1 stands for hydrogen, a C.sub.1 -C.sub.10 hydrocarbon group, nitrogen or the like; C.sup.1 denotes hydrogen, a C.sub.1 -C.sub.10 hydrocarbon group, nitrogen, alcohol residue, phosphoric acid residue or the like; a dermatologic preparation containing the same; and a process for producing the amine derivative. This amine derivative has excellent effects of smoothing or removing wrinkles and improving keratinization.
摘要翻译： PCT No.PCT / JP94 / 00436 Sec。 371 1995年9月18日第 102（e）1995年9月18日PCT PCT 1994年3月17日PCT公布。公开号WO94 / 21595 日期：1994年9月29日本发明涉及由以下通式（I）或（II）表示的胺衍生物：其中R 1表示含杂原子的C 1 -C 40烃可以具有环结构的基团等; R2-R5各自表示C1-C20烃基，氢等; A1表示或R15-Z-16-（CH2）n-; B1代表氢，C1-C10烃基，氮等; C1表示氢，C1-C10烃基，氮，醇残基，磷酸残基等; 含有该皮肤病的制剂; 和胺衍生物的制造方法。该胺衍生物具有优异的平滑或去除皱纹和改善角质化的效果。

46. 发明授权

US5521136A Process for the preparation of organotitanium compounds and their use in cathodically depositable electrodeposition coating materials 失效
标题翻译：用于制备有机钛化合物的方法及其在阴极沉积电沉积涂料中的应用
公开(公告)号：US5521136A
公开(公告)日：1996-05-28
申请号：US294863
申请日：1994-08-29
申请人： Roland Feola , Willibald Paar , Johann Gmoser
发明人： Roland Feola , Willibald Paar , Johann Gmoser
IPC分类号： C07C31/28 , C07C213/04 , C07C217/28 , C07F7/00 , C09D5/44 , B01J31/00
CPC分类号： C07C213/04 , C07C217/28 , C07C31/28 , C07F7/006 , C09D5/4492
摘要： A process for the preparation of organotitanium compounds and to their use as crosslinking catalysts in cathodically depositable electro-deposition coating materials is described. The organotitanium compounds are obtained by first carrying out partial transesterification of tetraalkyl orthotitanates with alkylene glycols which are capable of forming chelates, and then completing the transesterification of the resulting intermediate with hydroxyl compounds based on modified mono- and/or diepoxide compounds.Cathodically depositable electrodeposition coating materials which contain the organotitanium compounds prepared in accordance with the invention provide, after curing in a temperature range from 160.degree. to 180.degree. C., coating films having excellent stability and the like properties, without the need to use additional crosslinking catalysts based on heavy metals such as lead or tin.
摘要翻译：描述了制备有机钛化合物的方法及其作为阴极沉积的电沉积涂料中的交联催化剂的用途。有机钛化合物通过首先进行四烷基原钛酸酯与能够形成螯合物的亚烷基二醇的部分酯交换获得，然后基于改性的单 - 和/或二环氧化合物完成所得中间体与羟基化合物的酯交换反应。包含根据本发明制备的有机钛化合物的阴极沉积的电沉积涂料在160℃至180℃的温度范围内固化后，提供具有优异稳定性和类似性能的涂膜，而不需要使用额外的交联基于重金属如铅或锡的催化剂。

47. 发明授权

US5334761A Cationic lipids 失效
标题翻译：阳离子脂质
公开(公告)号：US5334761A
公开(公告)日：1994-08-02
申请号：US937508
申请日：1992-08-28
申请人： Gulilat Gebeyehu , Joel A. Jessee , Valentina C. Ciccarone , Pamela Hawley-Nelson , Anna Chytil
发明人： Gulilat Gebeyehu , Joel A. Jessee , Valentina C. Ciccarone , Pamela Hawley-Nelson , Anna Chytil
IPC分类号： C12N5/10 , A61K9/127 , A61K47/18 , C07C27/28 , C07C217/28 , C07C219/06 , C07C219/08 , C07C237/10 , C07C323/25 , C07C233/36
CPC分类号： C07C237/10 , A61K47/48046 , A61K9/1272 , C07C217/28
摘要： The present invention discloses cationic lipids useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Also disclosed are lipids useful both for the delivery of macromolecules and also useful as intermediates for making other such lipids.
摘要翻译：本发明公开了用于制备用于将大分子和其它化合物递送到细胞中的脂质聚集体的阳离子脂质。它们对细胞的DNA依赖性转化特别有用。还公开了可用于递送大分子的脂质，也可用作制备其它这种脂质的中间体。

48. 发明授权

US5288833A Liquid catalysts for rapid polymerization of liquid compositions bases on polyisocyanates and epoxides 失效
标题翻译：用于液体组合物快速聚合的液体催化剂基于多异氰酸酯和环氧化物
公开(公告)号：US5288833A
公开(公告)日：1994-02-22
申请号：US886599
申请日：1992-05-20
申请人： Fabrizio Parodi , Carlo Belgiovine , Carla Zannoni
发明人： Fabrizio Parodi , Carlo Belgiovine , Carla Zannoni
IPC分类号： C08G18/16 , C07C215/90 , C07C217/08 , C07C217/28 , C07C217/30 , C07C219/08 , C07C229/26 , C08G18/00 , C08G18/18 , C08G18/58 , C08G59/40 , C08G59/68
CPC分类号： C08G18/003 , C07C215/90 , C07C217/28 , C07C217/30 , C08G18/1875 , C08G59/4028 , C08G59/686
摘要： The present invention relates to quaternary .beta.-hydroxy-alkyl-ammonium halides and quaternary .beta.-hydroxy-cycloalkylammonium halides, which are liquid at temperatures lower than 60.degree. C., are easily and rapidly miscible in liquid epoxides, as well as in liquid poly-isocianates, generating liquid compositions which spontaneously polymerize, with fast polymerization rate, already at temperatures comprised within the range of from 0.degree. C. to 60.degree. C., yielding a solid, insoluble polymeric material endowed with very high values of softening temperature.
摘要翻译：本发明涉及在低于60摄氏度的温度下为液体的季（β） - 羟基 - 烷基 - 卤化铵和季（β） - 羟基 - 环烷基卤化物，在液体环氧化物中容易且快速地混溶如在液体聚异氰酸酯中，产生以快速聚合速率自发聚合的液体组合物已经在0℃至60℃的温度范围内，产生具有非常高的值的固体，不溶性聚合物的软化温度。

49. 发明授权

US4931596A Process for preparing hydroxylated amines 失效
标题翻译：制备羟基化胺的方法
公开(公告)号：US4931596A
公开(公告)日：1990-06-05
申请号：US292831
申请日：1989-01-03
申请人： Kathleen S. Laurenzo
发明人： Kathleen S. Laurenzo
IPC分类号： C07C213/00 , C07C215/08 , C07C215/18 , C07C217/28 , C07C271/02
CPC分类号： C07C215/18 , C07C213/00 , C07C215/08 , C07C217/28 , C07C271/02
摘要： Hydroxylated primary amines corresponding to the formula:R--X--CH.sub.2 --CH(OH)--CH.sub.2 NH.sub.2 (I)in which R is a saturated or unsaturated straight chain C.sub.5 -C.sub.18 aliphatic radical and X represents --O--, --S--, --NH-- or --CH.sub.2 -- are prepared by reacting an epoxide of the formula: ##STR1## in which R and X are as defined previously and R.sub.1 and R.sub.2 together represent an epoxy radical with ammonium carbamate to form the corresponding substituted ammonium carbamate of the formula: ##STR2## in which R and X are as defined previously and thereafter heating the substituted ammonium carbamate thus formed at a temperature and for a length of time sufficient to form the corresponding hydroxylated primary amine of formula (I).The hydroxylated primary amines of formula (I) and the salts of these compounds, particularly the hydrohalide, acetate and quaternary alkyl ammonium salts thereof are useful as medicaments, anticeptics, sterilizing agents and preservatives.
摘要翻译：对应于式为RX-CH2-CH（OH）-CH2NH2（I）的羟基化的伯胺，其中R是饱和或不饱和直链C 5 -C 18脂族基，X表示-O - ， - S - ， - NH- 或-CH 2 - 是通过使下式的环氧化物反应制备的：其中R和X如前所定义，R 1和R 2一起代表环氧基与氨基甲酸铵，形成相应的取代的氨基甲酸铵其中R和X如前所定义，然后在如此形成的取代的氨基甲酸铵的温度下加热足够长的时间以形成相应的羟基化的伯胺（I）的胺。式（I）的羟基化伯胺和这些化合物的盐，特别是其氢卤化物，乙酸盐和季烷基铵盐可用作药物，防腐剂，杀菌剂和防腐剂。

50. 发明授权

US4343745A Process for solubilizing organic or mineral salts in organic solvents 失效
标题翻译：将有机溶剂或无机盐溶解在有机溶剂中的方法
公开(公告)号：US4343745A
公开(公告)日：1982-08-10
申请号：US125775
申请日：1980-02-29
申请人： Gerard Soula
发明人： Gerard Soula
IPC分类号： B01F1/00 , B01D20060101 , B01D11/04 , B01F20060101 , C07B31/00 , C07B61/00 , C07C20060101 , C07C67/00 , C07C213/00 , C07F1/00 , C07F5/06 , C07F15/00 , C22B20060101 , C07C85/16 , C07C87/20
CPC分类号： C07F15/004 , C07C217/28 , C07F11/005 , C07F15/0053 , C07F15/0066 , C07F15/008 , C07F15/0093 , C07F15/025 , C07F15/045 , C07F15/065 , C07F3/003 , C07F7/006
摘要： The invention provides a process for solubilizing an organic or mineral salt in an organic solvent, said process comprising contacting an organic or mineral salt of the formula A.sup.- M.sup.+, wherein A.sup.- represents a mineral or organic anion and M.sup.+ represents a cation selected from the group consisting of the cation NH.sub.4.sup.+ and its derivatives and the cations derived from the metals of the groups I.sub.A, II.sub.A, III.sub.A, IV.sub.A, V.sub.A, VI.sub.A, VII.sub.A, VIII, I.sub.B, II.sub.B, III.sub.B, IV.sub.B and V.sub.B of the periodic table, with at least one sequestering agent which is soluble in said organic solvent, said sequestering agent having the formula:N[CHR.sub.1 --CHR.sub.2 --O--(CHR.sub.3 --CHR.sub.4 --O).sub.n --R.sub.5 ].sub.3 (I)wherein n is an integer from 0 to 10 inclusive; R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which can be the same or different, are each a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms; R.sub.5 is an alkyl radical having 1 to 12 carbon atoms, a cycloalkyl radical having 3 to 12 carbon atoms, a phenyl radical, a radical of the formula ##STR1## or a radical of the formula ##STR2## and m is an integer from 1 to 12 inclusive. The process makes it possible to utilize the A.sup.- M.sup.+ salt as a reactant in solvents in which such reaction has not heretofore been possible, or to extract the A.sup.31 M.sup.+ salt from a solution containing it.
摘要翻译：本发明提供了将有机或无机盐溶解在有机溶剂中的方法，所述方法包括使式A-M +的有机盐或矿物盐接触，其中A-代表矿物或有机阴离子，M +表示选自由阳离子NH4 +及其衍生物组成的基团和衍生自元素周期表IA，IIA，IIIA，IVA，VA，VIA，VIIA，VIII，IB，IIB，IIIB，IVB和VB族金属的阳离子，至少一种可溶于所述有机溶剂的螯合剂，所述螯合剂具有下式：N [CHR 1 -CHR 2 -O-（CHR 3 -CHR 4 -O）n -R 5] 3（I）其中n是0的整数至10包可以相同或不同的R 1，R 2，R 3和R 4各自为氢原子或具有1至4个碳原子的烷基; R 5是具有1至12个碳原子的烷基，具有3至12个碳原子的环烷基，苯基，式“IMAGE”基团或式“IMAGE”基团，m是1的整数至12包括该方法可以将A-M +盐作为反应物在其中尚未达到此类反应的溶剂中或从含有该溶液的溶液中提取A31M +盐成为可能。

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