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51. 发明授权

US4675418A Process for preparing alkanoic acids or esters thereof by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt 失效
标题翻译：通过在质子介质中和非贵金属盐存在下重排α-卤代酮来制备链烷酸或其酯的方法
公开(公告)号：US4675418A
公开(公告)日：1987-06-23
申请号：US398586
申请日：1982-07-15
申请人： Claudio Giordano , Giovanni Villa , Fulvio Uggeri , Graziano Castaldi
发明人： Claudio Giordano , Giovanni Villa , Fulvio Uggeri , Graziano Castaldi
IPC分类号： C07C67/475 , B01J27/00 , C07B31/00 , C07B41/00 , C07B41/08 , C07B41/12 , C07B61/00 , C07C45/63 , C07C49/84 , C07C51/00 , C07C57/30 , C07C59/64 , C07C67/00 , C07C69/612 , C07C69/734 , C07D333/24 , C07C63/36 , C07C69/76
CPC分类号： C07C45/63 , C07C49/84 , C07C51/00
摘要： Process for preparing alkanoic acid or their esters by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt.The protic medium is preferably an aliphatic alcohol having low molecular weight or water and the reaction is carried out at a temperature from 0.degree. C. to the boiling-point of the diluent or of the diluents mixture.
摘要翻译：通过在质子介质中和在非贵金属盐存在下重新配置α-卤代酮来制备链烷酸或其酯的方法。质子介质优选为具有低分子量或水的脂族醇，并且反应在0℃至稀释剂或稀释剂混合物的沸点的温度下进行。

52. 发明授权

US4609766A Process for preparing esters of 2-(6'-methoxy-2'-naphtyl)-propionic acid via rearrangement of new ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-one and new esters of 2-(5'-bromo-6'-methoxy-2'-naphtyl)propionic acid thus prepared 失效
标题翻译：通过重新配置2-卤代-1-（6'-甲氧基-2'-萘基） - 丙-1-酮的新的缩酮来制备2-（6'-甲氧基-2'-萘基） - 丙酸的酯的方法和由此制备的2-（5'-溴-6'-甲氧基-2'-萘基）丙酸的新酯
公开(公告)号：US4609766A
公开(公告)日：1986-09-02
申请号：US735166
申请日：1985-05-17
申请人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
发明人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
IPC分类号： C07C43/174 , C07C43/225 , C07C43/30 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07C67/475 , C07C69/734 , C07D209/48 , C07D317/16 , C07D317/18 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/16 , C07D333/22
CPC分类号： C07D209/48 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07D317/16 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/22
摘要： Process for preparing esters of 2-(6'-methoxy-2'-naphtyl)-propionic acid via rearrangement of new ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-one in the presence of a Lewis acid.The esters thus obtained are useful as intermediate products for preparing Naproxen.The process involves the preparation of the following new compounds:ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-oneesters of 2-(5'-bromo-6'-methoxy-2'-naphtyl)-propionic acid1-(5'-bromo-6'-methoxy-2'-naphtyl)-propan-1-one2-halo-(5'-bromo-6'-methoxy-2'-naphtyl)-propan-1-one

53. 发明授权

US4582930A Process for the preparation of optically active alpha-arylalkanoic acids 失效
标题翻译：光学活性α-芳基链烷酸的制备方法
公开(公告)号：US4582930A
公开(公告)日：1986-04-15
申请号：US704407
申请日：1985-02-22
申请人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
发明人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
IPC分类号： C07C57/30 , C07B31/00 , C07B53/00 , C07C27/02 , C07C51/00 , C07C51/09 , C07C59/64 , C07C67/00 , C07C63/36
CPC分类号： C07C51/00
摘要： A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active alpha-(haloalkyl)-aryl-ketals and in submitting to hydrolysis the so-obtained esters of alpha-arylalkanoic acids.The rearrangement reaction is carried out under neutral or slightly alkaline conditions in a polar protic medium.
摘要翻译：公开了用于制备光学活性α-芳基链烷酸的方法，其包括光学活性α-（卤代烷基） - 芳基缩酮的重排，并且将所得的α-芳基链烷酸酯进行水解。重排反应在极性质子介质中在中性或弱碱性条件下进行。

54. 发明申请

US20120232151A1 Process for the Preparation of Gadobenate Dimeglumine Complex in a Solid Form 审中-公开
标题翻译：以固体形式制备钆酸二甲酚复合物的方法
公开(公告)号：US20120232151A1
公开(公告)日：2012-09-13
申请号：US13510409
申请日：2010-11-23
申请人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
发明人： Pier Lucio Anelli , Pierfrancesco Morisini , Silvia Ceragioli , Fulvio Uggeri , Luciano Lattuada , Roberta Fretta , Aurelia Ferrigato
IPC分类号： C07C227/00 , A61K31/197 , C07C229/36
CPC分类号： A61K49/1887 , A61K9/0019 , B29C67/24 , C07C213/10 , C07C227/38 , C07C227/40 , Y10T428/2982 , C07C229/22
摘要： The present invention discloses a process for the preparation of gadobenate dimeglumine complex in a solid form. In particular, said solid form is conveniently obtained by spray-drying a corresponding liquid suspension at a given temperature and concentration. The present invention is particularly advantageous for the industrial scale as the solid form may be obtained by employing water as a solvent, which is a non-toxic solvent, easy to handle and basically not requiring troublesome health or safety precautions.
摘要翻译：本发明公开了一种以固体形式制备钆酸二甲酚络合物的方法。特别地，所述固体形式通过在给定温度和浓度下喷雾干燥相应的液体悬浮液而方便地得到。本发明对于工业规模是特别有利的，因为固体形式可以通过使用水作为溶剂，其是无毒溶剂，易于处理并且基本上不需要麻烦的健康或安全预防措施来获得。

55. 发明授权

US5660814A Iodinated paramagnetic chelates, and their use as contrast agents 失效
标题翻译：碘化顺磁螯合物，以及它们作为造影剂的用途
公开(公告)号：US5660814A
公开(公告)日：1997-08-26
申请号：US448476
申请日：1995-05-30
申请人： Fulvio Uggeri , Pier Lucio Anelli , Franco Fedeli , Marcella Murru , Christoph De Haen
发明人： Fulvio Uggeri , Pier Lucio Anelli , Franco Fedeli , Marcella Murru , Christoph De Haen
IPC分类号： C07D257/02 , A61K49/00 , A61K49/04 , A61K49/08 , A61K51/00 , A61K51/04 , C07C237/04 , C07C237/10 , G01N31/00 , G01N33/48
CPC分类号： A61K49/10 , A61K49/0438 , A61K49/085 , A61K51/0497
摘要： Novel compounds containing a polyiodinated aromatic or heteroaromatic residue and their chelate complexes with ions of metal elements with atomic number from 20 to 31, 39, from 42 to 44, 49 and from 57 to 83, and their salts with physiologically tolerable organic and inorganic bases are useful contrast agents for preparation of diagnostic formulations to obtain images of organs and/or tissues of human and animal body through the use of nuclear magnetic resonance or X-rays or the combination of both nuclear magnetic resonance and X-rays.
摘要翻译： PCT No.PCT / EP94 / 01677 Sec。 371日期：1995年5月30日 102（e）日期1995年5月30日PCT 1994年5月25日PCT公布。公开号WO94 / 27644 日期1994年12月8日含有多碘化芳族或杂芳族残基的新型化合物及其与原子序数为20〜31,39,42,49和57〜83的金属元素离子的螯合络合物及其与生理盐可耐受的有机和无机碱是用于制备诊断制剂的有用的造影剂，以通过使用核磁共振或X射线或核磁共振和X-射线的组合来获得人体和动物的器官和/或组织的图像，射线

56. 发明授权

US5132409A Macrocyclic chelating agents and chelates thereof 失效
标题翻译：大环螯合剂及其螯合物
公开(公告)号：US5132409A
公开(公告)日：1992-07-21
申请号：US449883
申请日：1989-11-27
申请人： Ernst Felder , Carlo Musu , Luciano Fumagalli , Fulvio Uggeri
发明人： Ernst Felder , Carlo Musu , Luciano Fumagalli , Fulvio Uggeri
IPC分类号： A61K49/06 , C07D257/02
CPC分类号： A61K49/06 , C07D257/02
摘要： Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH.sub.2 CH.sub.2).sub.1-4-, Me(OCH.sub.2 CH.sub.2).sub.1-4-, or Et(OCH.sub.2 CH.sub.2).sub.1-4- group, X or O--R.sub.1, in which R.sub.1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR.sub.2 R.sub.3, in which R.sub.2 and R.sub.3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B.sub.1, B.sub.2 and B.sub.3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R.sub.4 is H or alkyl, Y is a O--R.sub.5 group, wherein R.sub.5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR.sub.6 R.sub.7 group, wherein R.sub.6 and R.sub.7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. ##STR1##
摘要翻译：其中A为下式（Ⅱ）基团，其中R为H或烷基或任意取代的苄基或H（OCH 2 CH 2）1的式（I）的基团，其通式（I）的1,4,7,10-四氮杂环十二烷的大环衍生物 -4-，Me（OCH 2 CH 2）1-4 - 或Et（OCH 2 CH 2）1-4 - 基，X或O-R 1，其中R 1是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或多氧杂烷基或X是 -NR2R3，其中R2和R3为H或烷基，羟烷基，烷氧基烷基或烷氧基羟烷基，B1，B2和B3与A相同，或为H或下式（III）的基团，其中R4为H或烷基，Y是O-R5基团，其中R5是H或烷基，羟基烷基，烷氧基烷基，烷氧基羟基烷基或聚氧杂烷基，或Y是-NR6R7基团，其中R6和R7是H或烷基，羟基烷基，烷氧基烷基或烷氧基羟烷基所述衍生物任选地被盐化，并且其络合盐用作药物和/或诊断剂。（一）图像（二）<图像>（三）

57. 发明授权

US4980502A Paramagnetic chelates 失效
标题翻译：顺磁螯合物
公开(公告)号：US4980502A
公开(公告)日：1990-12-25
申请号：US411906
申请日：1989-09-25
申请人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorio Vittadini
发明人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorio Vittadini
IPC分类号： A61K49/00 , A61K31/28 , C07C229/22 , C07C229/40 , C07C229/46 , C07C233/10 , C07D401/12 , C07F5/00 , C07F13/00 , C07F15/02
CPC分类号： A61K31/28
摘要： Compounds suitable for NMR imaging having the formula: ##STR1## wherein a is 2 or 3;b is an integer from 0 to 4;Me.sup.(a+) is Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+), or Mn.sup.(2+) ;E.sup.(b+) is an ion of an alkali metal, alkaline earth metal, alkyl ammonium, alkanol ammonium, polyhydroxyalkyl ammonium, or basic protonated amino acid, said ions representing a total charge of b;m is an integer from 1 to 5;R is H, alkyl with from 1 to 8 carbon atoms, alkyl with from 1 to 8 carbon atoms wherein from 1 to 5 carbons are substituted with OH; aralkyl with 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, hydroxyl, carboxyl, carboxamide, ester, SO.sub.3 H, sulfonamide, lower alkyl, lower hydroxy alkyl, amino, acylamino; (poly)oxa-alkyl with 1 to 50 oxygen atoms and from 3 to 150 carbon atoms, wherein 1 to 5 hydrogen atoms may be substituted by OH; R.sub.1 is the same as R.sub.2 or is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, CH.sub.2 CH.sub.2 --N(CH.sub.2 COOZ).sub.2, a hydroxy arylalkyl, hydroxy pyridylalkyl, hydroxy aryl(carboxy)alkyl or hydroxy pyridyl-(carboxyl)-alkyl radical, where the aryl or pyridyl radical may be substituted by hydroxyl, hydroxy alkyl, alkyl, halogen, carboxyl or SO.sub.3 H; is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ, ##STR2## wherein R.sub.3 is --CH.sub.2 COOZ, --CH(CH.sub.3)COOZ or a monovalent radical having the structure ##STR3## X is a direct chemical bond, --O--, --S--, 13 NH--, n is the integer 2 or 3, with the proviso that when X represents a direct bond, n is 1, 2 or 3;Z is hydrogen or a unit of negative charge, and --(CH.sub.2).sub.m -- may also be --CH.sub.2 --C(CH.sub.3).sub.2 --.

58. 发明授权

US4810819A Process for the preparation of optically active alpha-acrylalkanoic acids and novel intermediates thereof 失效
标题翻译：制备光学活性α-丙烯酰基链烷酸的方法及其新型中间体
公开(公告)号：US4810819A
公开(公告)日：1989-03-07
申请号：US81688
申请日：1987-08-05
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： C07C45/46 , C07C49/807 , C07C51/00 , C07D317/32 , C07C69/76
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.
摘要翻译：描述了通过以下方法制备光学活性α-芳基链烷酸的新的对映选择性方法：（a）在缩酮的α-脂肪族碳原子上卤化式（ⅠA）的缩酮，其中Ar表示任选取代的芳基; R代表C1-C4烷基; R1和R2表示羟基，O-M +，OR3或NR4R5基团; 由星号表示的碳原子同时为（R）或（S）构型。该反应是非对映选择性的，因此获得了α-二酮的混合物，其中两个差向异构体中的一个占优势，并且通常强大地占优势。（b）通过式（IMA）的（C）（C）的酯，将单体或两个连续阶段中的X为Cl，Br或I的式（A）所示的配子重新排列成α-芳基链烷酸）化合物（A）和（C）都是新的化合物。重新布置步骤（b）可以在新的创造条件下进行。式（C）的酯具有类似于相应的α-芳基链烷酸的药理活性。

59. 发明授权

US4620031A Process for preparing alpha-aryl-alkanoic acids 失效
标题翻译：制备α-芳基 - 链烷酸的方法
公开(公告)号：US4620031A
公开(公告)日：1986-10-28
申请号：US697449
申请日：1985-02-01
申请人： Fulvio Uggeri , Graziano Castaldi , Claudio Giordano
发明人： Fulvio Uggeri , Graziano Castaldi , Claudio Giordano
IPC分类号： C07B41/08 , C07C51/00 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/64 , C07C59/84 , C07C67/00 , C07D333/24 , C07C63/36
CPC分类号： C07D333/24 , C07C51/00
摘要： Alpha-alkyl-alkanoic acids are prepared by heating at boiling temperature a mixture of an alpha-halogen-alkyl-arylketone in a saturated aliphatic diol or in a mixture of saturated aliphatic diols in the presence of a Broensted's acid and by successively alkalifying the reaction mixture.
摘要翻译： α-烷基 - 链烷酸通过在沸石温度下加热饱和脂肪族二醇中的α-卤代烷基 - 芳基酮或饱和脂族二醇的混合物，在布朗斯台德酸的存在下并通过连续碱化反应来制备混合物。

60. 发明授权

US4560777A Preparation of esters of 2-(6'-methoxy-2'-naphthyl)-propionic acid via rearrangement of ketals of 2-halo-1-(6'-methoxy-2'-naphthyl)-propan-1-one 失效
标题翻译：通过2-卤代-1-（6'-甲氧基-2'-萘基） - 丙-1-酮的缩酮的重排制备2-（6'-甲氧基-2'-萘基） - 丙酸的酯
公开(公告)号：US4560777A
公开(公告)日：1985-12-24
申请号：US520190
申请日：1983-08-04
申请人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
发明人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
IPC分类号： C07C43/174 , C07C43/225 , C07C43/30 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07C67/475 , C07C69/734 , C07D209/48 , C07D317/16 , C07D317/18 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/16 , C07D333/22 , C07D317/00
CPC分类号： C07D209/48 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07D317/16 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/22
摘要： Process for preparing esters of 2-(6'-methoxy-2'-naphtyl)-propionic acid via rearrangement of new ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-one in the presence of a Lewis acid.The esters thus obtained are useful as intermediate products for preparing Naproxen.The process involves the preparation of the following new compounds:ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-oneesters of 2-(5'-bromo-6'-methoxy-2'-naphtyl)-propionic acid1-(5'-bromo-6'-methoxy-2'-naphtyl)-propan-1-one2-halo-(5'-bromo-6'-methoxy-2'-naphtyl)-propan-1-one.

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