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1. 发明授权

US4916246A Paramagnetic chelates useful for NMR imaging 失效
标题翻译：用于NMR成像的顺磁性螯合物
公开(公告)号：US4916246A
公开(公告)日：1990-04-10
申请号：US2115
申请日：1987-01-12
申请人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorgio Vittadini
发明人： Ernst Felder , Fulvio Uggeri , Luciano Fumagalli , Giorgio 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 oris --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-(carboxy)alkyl radical, where the aryl or pyridyl radical may be substituted by hydroxyl, hydroxy alkyl, alkyl, halogen, carboxyl or SO.sub.3 H;R.sub.2 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--, --NH--, ##STR4## 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 --.
摘要翻译：适用于具有下式的NMR成像的化合物：其中a为2或3; b为0〜4的整数; Me（a +）是Fe（2+），Fe（3+），Gd（3+）或Mn（2+）; E（b +）是碱金属，碱土金属，烷基铵，链烷醇铵，多羟基烷基铵或碱性质子化氨基酸的离子，所述离子代表总电荷b; m为1〜5的整数; R是H，具有1至8个碳原子的烷基，具有1至8个碳原子的烷基，其中1至5个碳被OH取代; 具有1至4个脂族碳原子的芳烷基; 苯基或被卤素，羟基，羧基，羧酰胺，酯，SO 3 H，磺酰胺，低级烷基，低级羟基烷基，氨基，酰氨基取代的苯基; 具有1至50个氧原子和3至150个碳原子的（多）氧杂 - 烷基，其中1至5个氢原子可以被OH取代; R1与R2相同或为-CH2COOZ，-CH（CH3）COOZ，CH2CH2-N（CH2COOZ）2，羟基芳基烷基，羟基吡啶基烷基，羟基芳基（羧基）烷基或羟基吡啶基 - （羧基）烷基，芳基或吡啶基可以被羟基，羟基烷基，烷基，卤素，羧基或SO 3 H取代; R2是-CH2COOZ，-CH（CH3）COOZ，其中R3是-CH2COOZ，-CH（CH3）COOZ或具有结构X的单价基团是直接化学键，-O- ，-S-，-NH-， n为整数2或3，条件是当X表示直接键时，n为1,2或3; Z是氢或负电荷的单元， - （CH 2）m - 也可以是-CH 2 -C（CH 3）2 - 。

2. 发明授权

US5182370A Paramagnetic chelates 失效
标题翻译：顺磁螯合物
公开(公告)号：US5182370A
公开(公告)日：1993-01-26
申请号：US450225
申请日：1989-12-13
申请人： Ernst Felder , Luciano Fumagalli , Fulvio Uggeri , Giorgio Vittadini
发明人： Ernst Felder , Luciano Fumagalli , Fulvio Uggeri , Giorgio 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： Comounds having the formula ##STR1## wherein: a is 2 or 3; b is an integer from 0 to 4;Me.sup.(a+) is an ion of an element of atomic number from 57 to 70 or an ion of a transition metal of atomic number 21-29, 42 or 44;E.sup.(b+) is one or more physiologically biocompatible cation of an inorganic or an organic base or amino acid, said cation representing a total positive charge of b units;S is the group --A--O--R wherein:A is --(CH.sub.2).sub.m --; --CH.sub.2 --C(CH.sub.3).sub.2 --; m is an integer from 1 to 5; R is H; linear or branched alkyl of 1 to 8 carbon atoms, said carbon atoms being unsubstituted or substituted by one or more hyroxy group; aralkyl of 1 to 4 aliphatic carbon atoms; phenyl or phenyl substituted by halogen, amino, hydroxy or trifluoromethyl; (poly)-oxa-alkyl of 1 to 10 oxygen atoms and from 3 to 30 carbon atoms;R.sub.1 is R.sub.2 or --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; --(CH.sub.2).sub.n --N(CH.sub.2 COOZ).sub.2 ; hydroxy-arylalkyl radical in which the aryl radical is unsubstituted or substituted by hydroxy;R.sub.2 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; with the proviso that when R.sub.1 is --CH.sub.2 COOZ or --CH(CH.sub.3)COOZ, R.sub.2 is other than --CH.sub.2 COOZ and --CH(CH.sub.3)--COOZ ##STR2## wherein: R.sub.3 is --CH.sub.2 COOZ; --CH(CH.sub.3)COOZ; a monovalent radical having the structure S--CH--COOZ;X is a direct chemical bond; --O--; --S--; --NH--; --N--CH.sub.2 COOZ; --N--CH(CH.sub.3)COOZ;n is the integer 2 or 3, with the proviso that when X is a direct chemical bond, n is 1, 2 or 3;Z is H or a negative charge;with the proviso that, unless R represents a trifluoromethyl substituted phenyl or R.sub.1 is R.sub.2, Me.sup.(a+) is different from Fe.sup.(2+), Fe.sup.(3+), Gd.sup.(3+) and Mn.sup.(2+) and with the proviso that when R.sub.1 is R.sub.2 every molecule can contain not more than 500 nitrogen atoms.
摘要翻译：具有式的化合物，其中：a为2或3; b为0〜4的整数; Me（a +）是原子序数为57〜70的元素的离子或原子序数21-29,42或44的过渡金属的离子; E（b +）是无机或有机碱或氨基酸的一种或多种生理生物相容阳离子，所述阳离子表示b单元的总正电荷; S是基团-A-O-R，其中：A是 - （CH 2）m - ; -CH 2 -C（CH 3）2 - ; m为1〜5的整数; R为H; 1至8个碳原子的直链或支链烷基，所述碳原子未被取代或被一个或多个羟基取代; 1至4个脂族碳原子的芳烷基; 苯基或被卤素，氨基，羟基或三氟甲基取代的苯基; 具有1至10个氧原子和3至30个碳原子的（多） - 氧代 - 烷基; R1是R2或-CH2COOZ; -CH（CH 3）COOZ; - （CH 2）n -N（CH 2 COOZ）2; 其中芳基未被取代或被羟基取代的羟基 - 芳基烷基; R2是-CH2COOZ; -CH（CH 3）COOZ; 条件是当R1是-CH2COOZ或-CH（CH3）COOZ时，R2不是-CH2COOZ和-CH（CH3）-COOZ其中：R3是-CH2COOZ; -CH（CH 3）COOZ; 具有结构S-CH-COOZ的单价基团; X是直接化学键; -O-; -S-; -NH-; -N-CH 2 COOZ; -N-CH（CH 3）COOZ; n为整数2或3，条件是当X为直接化学键时，n为1,2或3; Z为H或负电荷; 条件是，除非R代表三氟甲基取代的苯基或R1是R2，Me（a +）不同于Fe（2+），Fe（3+），Gd（3+）和Mn（2+）条件是当R1为R2时，每个分子可含有不超过500个氮原子。

3. 发明授权

US4273931A Reduction of alkyl esters of carbonic-carboxylic anhydrides to alcohols 失效
标题翻译：将碳酸酐的烷基酯还原成醇
公开(公告)号：US4273931A
公开(公告)日：1981-06-16
申请号：US105537
申请日：1979-12-20
申请人： Aldo Garzia , Giorgio Vittadini , Andrea Bottazzi , Domenico Pelagalli , Costantino Coccoli
发明人： Aldo Garzia , Giorgio Vittadini , Andrea Bottazzi , Domenico Pelagalli , Costantino Coccoli
IPC分类号： C07C29/149 , C07C45/29 , C07C65/24 , C07D213/30 , C07D233/54 , C07D239/48 , C07D239/49 , C07C33/20
CPC分类号： C07D213/30 , C07C41/26 , C07C45/298 , C07C65/24 , C07D233/54 , C07D239/49
摘要： There is disclosed the reduction of alkyl esters of carbonic-carboxylic acid anhydrides at elevated temperature and pressure in the presence of platinum group metal catalysts, especially palladium on activated carbon, to make alcohols. Novel alkyl esters of carbonic-carboxylic acid anhydrides are disclosed, and can be used to make the corresponding alcohols, e.g., substituted benzyl alcohols. The alcohols can be converted to the corresponding halo, e.g., chloro, compounds. The substituted benzyl halides can be reacted with di(lower alkoxy)propionitriles, and the resulting 5-benzyl pyrimidines such as trimethoprim, 2,4-diamino-5-(3,4,5-trimethoxybenzyl)-pyrimidine, which is a known anti-bacterial agent, are especially useful in combination with sulfa drugs such as sulfamethoxazole. Other alcohols that can be made in accordance with the invention include 2,6-pyridine dimethanol which can be used to make pyridinol carbamate, an anti-inflammatory agent and an anti-arteriosclerotic agent and 1-aceto-4-hydroxymethyl-5-methyl imidazole, which can be converted into cimetidine.
摘要翻译：公开了在铂族金属催化剂，特别是钯活性炭存在下，在升高的温度和压力下还原碳酸羧酸酐的烷基酯以制备醇。公开了新的碳 - 羧酸酐的烷基酯，并且可用于制备相应的醇，例如取代的苄醇。醇可以转化为相应的卤素，例如氯，化合物。取代的苄基卤可以与二（低级烷氧基）丙腈反应，得到的5-苄基嘧啶如甲氧苄啶，2,4-二氨基-5-（3,4,5-三甲氧基苄基） - 嘧啶，这是已知的抗菌剂，特别适用于磺胺类药物如磺胺甲恶唑。可以根据本发明制备的其它醇包括可用于制备吡啶酚氨基甲酸酯的2,6-吡啶二甲醇，抗炎剂和抗动脉硬化剂和1-乙酰-4-羟甲基-5-甲基咪唑，可以转化成西咪替丁。

4. 发明授权

US4939207A Blends based on vinyl-aromatic polymers endowed with high tenacity and chemical resistance 失效
标题翻译：基于乙烯基芳族聚合物的共混物赋予了高强度和耐化学性
公开(公告)号：US4939207A
公开(公告)日：1990-07-03
申请号：US193587
申请日：1988-05-13
申请人： Gian C. Fasulo , Annibale Vezzoli , Giorgio Vittadini
发明人： Gian C. Fasulo , Annibale Vezzoli , Giorgio Vittadini
IPC分类号： C08L25/04 , C08F297/02 , C08F297/04 , C08L23/00 , C08L51/00 , C08L51/04 , C08L51/06 , C08L53/00 , C08L53/02
CPC分类号： C08L51/06
摘要： Blends based on vinyl-aromatic polymers endowed with high tenacity and good chemical resistance, comprising:40 to 98% by weight of a vinyl-aromatic polymer containing from 0.5 to 5% by weight of a vinyl-aromatic monomer conjugated diene block copolymer;1-54% by weight of a polyolefine; and1-20% by weight of a vinyl-aromatic monomer-conjugated diene star block copolymer; the sum of the three components being equal to 100%.

5. 发明授权

US4814374A Polymeric blends based on vinyl-aromatic polymers endowed with high tenacity and chemical resistance 失效
标题翻译：基于乙烯基芳族聚合物的聚合物共混物具有高韧性和耐化学性
公开(公告)号：US4814374A
公开(公告)日：1989-03-21
申请号：US147122
申请日：1988-01-21
申请人： Gianfranco Biglione , Andrea Mattiussi , Giorgio Vittadini
发明人： Gianfranco Biglione , Andrea Mattiussi , Giorgio Vittadini
IPC分类号： C08L25/00 , C08L1/00 , C08L7/00 , C08L21/00 , C08L23/00 , C08L25/02 , C08L27/00 , C08L27/06 , C08L33/00 , C08L33/02 , C08L51/00 , C08L51/02 , C08L51/04 , C08L55/02 , C08L77/00 , C08L101/00
CPC分类号： C08L27/06 , C08L51/04 , C08L55/02
摘要： Polymeric blends based on vinyl-aromatic polymers endowed with high tenacity and chemical resistance comprising:from 10 to 90% by weight of a vinyl-chloride polymer;from 90 to 10% by weight of a vinyl-aromatic copolymer containing from 2 to 25% by weight of an ethylenically unsaturated nitrile and a quantity not exceeding 15% by weight of a rubber, are disclosed.
摘要翻译：基于乙烯基芳族聚合物的聚合物共混物具有高强度和耐化学性，包括：10至90重量％的氯乙烯聚合物; 公开了90至10重量％的含有2至25重量％烯属不饱和腈和不超过15重量％橡胶量的乙烯基芳族共聚物。

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