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1. 发明授权

US4177344A Anhydro-sugars 失效
标题翻译：脱水糖
公开(公告)号：US4177344A
公开(公告)日：1979-12-04
申请号：US833795
申请日：1977-09-16
申请人： Gerhard Baschang , Jaroslav Stanek , Alberto Rossi , Alex Sele
发明人： Gerhard Baschang , Jaroslav Stanek , Alberto Rossi , Alex Sele
IPC分类号： C07D313/06 , A61K31/335 , A61P29/00 , C07H15/18 , C07H19/01 , C07H3/10
CPC分类号： C07H15/18 , C07H19/01 , Y10S514/822
摘要： The invention relates to novel 1,6-anhydro-.beta.-D-hexopyranose derivatives of the formula I ##STR1## in which R.sub.2 is hydrogen, methyl or aromatic acyl, R.sub.3 and R.sub.4 are alkyl, alkenyl or aralkyl and one of the radicals R.sub.3 and R.sub.4 is also an aroyl radical and R.sub.4 can also be hydrogen, with the proviso that the radicals R.sub.3 and R.sub.4 together contain at least 3 carbon atoms and, if R.sub.4 is the benzyl radical, the radical R.sub.3 contains at least 2 carbon atoms, and, if one of the radicals R.sub.3 and R.sub.4 is an aroyl radical, R.sub.2 is hydrogen.These compounds especially the 1,6-anhydro-3,4-di-O-benzyl-.beta.-D-glucopyranose or the 1,6-anhydro-.beta.-D-glucopyranose, can be used as fibrinolytic agents and thrombolytic agents.
摘要翻译：本发明涉及式Ⅰ的新颖的1,6-脱水-β-十六吡喃糖衍生物，其中R 2是氢，甲基或芳基酰基，R 3和R 4是烷基，链烯基或芳烷基，其中一个基团R 3 并且R4也是芳酰基，R4也可以是氢，条件是基团R3和R4一起含有至少3个碳原子，如果R 4是苄基，则基团R 3含有至少2个碳原子，和如果基团R 3和R 4中的一个是芳酰基，则R 2是氢。这些化合物尤其是1,6-脱水-3,4-二-O-苄基-β-D-吡喃葡萄糖或1,6-脱水-β-D-吡喃葡萄糖可用作纤维蛋白溶解剂和溶栓剂。

2. 发明授权

US4112075A Furanose-O-pyridylcarboxylic acid esters 失效
标题翻译：呋喃糖-O-吡啶羧酸酯
公开(公告)号：US4112075A
公开(公告)日：1978-09-05
申请号：US721738
申请日：1976-09-09
申请人： Gerhard Baschang , Alex Sele , Jaroslav Stanek , Alberto Rossi
发明人： Gerhard Baschang , Alex Sele , Jaroslav Stanek , Alberto Rossi
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61P29/00 , C07H9/04 , C07H13/10 , C07H15/04 , C07H15/18
CPC分类号： C07H9/04 , C07H13/10 , C07H15/04 , C07H15/18 , Y10S514/886
摘要： The invention relates to furanose-O-pyridylcarboxylic acid esters, such as the ethyl-2-O-methyl-3,5,6-tri-O-nicotinoyl-D-glucofuranoside, which have anti-inflammatory activity and are fibrinolysis activators. They can be used for the treatment of rheumatic and neuralgic complaints, and especially for the topical percutaneous treatment of localized inflammatory processes.
摘要翻译：本发明涉及具有抗炎活性并且是纤维蛋白溶解活化剂的呋喃糖-O-吡啶羧酸酯，例如乙基-2-O-甲基-3,5,6-三-O-氧代烟酰-D-葡萄糖呋喃糖苷。它们可用于治疗风湿性和神经痛症状，尤其适用于局部炎症过程的局部经皮治疗。

3. 发明授权

US4192868A Novel aryl-hexafuranosides and processes for their preparation 失效
标题翻译：新型芳基六氢呋喃糖苷及其制备方法
公开(公告)号：US4192868A
公开(公告)日：1980-03-11
申请号：US880255
申请日：1978-02-22
申请人： Jean M. J. Tronchet , Bruno Baehler , Alberto Rossi , Gerhard Baschang , Alex Sele
发明人： Jean M. J. Tronchet , Bruno Baehler , Alberto Rossi , Gerhard Baschang , Alex Sele
IPC分类号： A61K31/70 , A61K31/7028 , A61P25/04 , A61P29/00 , C07H15/04 , C07H15/00
CPC分类号： C07H15/04
摘要： The invention relates to processes for the preparation of novel aryl-hexafuranosides of the formula ##STR1## in which R.sub.1 is lower alkyl or cycloalkyl and R.sub.2 is hydrogen, lower alkyl or acyl, or R.sub.1 and R.sub.2 together are alkylidene or cycloalkylidene, R.sub.3 is hydrogen, lower alkyl, lower alkenyl or aryl-lower alkyl, R.sub.5a and R.sub.6a independently of one another are hydrogen or lower alkyl, R.sub.5b and R.sub.6b independently of one another are hydrogen, hydroxyl, lower alkoxy or amino, or R.sub.5b and R.sub.6b together are a C--C bond, epoxy or lower alkylidene, and R.sub.6c is aryl, by methods known per se.These novel compounds have an anti-inflammatory and/or antinociceptive action.
摘要翻译：本发明涉及制备式（I）的新型芳基 - 六氢蒽醌的方法，其中R 1是低级烷基或环烷基，R 2是氢，低级烷基或酰基，或者R 1和R 2一起是亚烷基或亚环烷基， R3是氢，低级烷基，低级烯基或芳基 - 低级烷基，R5a和R6a彼此独立地是氢或低级烷基，R5b和R6b彼此独立地是氢，羟基，低级烷氧基或氨基，或R5b和R6b在一起是CC键，环氧基或低级亚烷基，R6c是芳基，通过本身已知的方法。这些新化合物具有抗炎和/或抗伤害感受作用。

4. 发明授权

US4297358A Novel 4,7-phenanthroline derivatives and pharmaceutical compositions containing them and their use 失效
标题翻译：新颖的4,7-菲咯啉衍生物和含有它们的药物组合物及其用途
公开(公告)号：US4297358A
公开(公告)日：1981-10-27
申请号：US109715
申请日：1980-01-04
申请人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
发明人： Georges Haas , Knut A. Jaeggi , Alberto Rossi , Alex Sele
IPC分类号： A61K31/47 , A61P37/08 , C07D215/26 , C07D215/38 , C07D471/04 , C07D487/04 , A61K31/435
CPC分类号： C07D215/38 , C07D215/26 , C07D471/04
摘要： New 4,7-phenanthroline derivatives of the formula (I) ##STR1## in which Ch represents an optionally substituted 5,6-quinolinylene radical of which the 6-position is joined to the --N(R.sub.E)-- group, andR represents an optionally esterified or amidated carboxy group,and in which eitherR.sub.A and R.sub.B together represent oxo,R.sub.C and R.sub.D together represent an additional link, andR.sub.E represents a radical R.sub.1 which is hydrogen, or an aliphatic, cycloaliphatic, araliphatic or heterocyclic-aliphatic radical, orR.sub.A represents an optionally etherified hydroxy group andR.sub.B together with R.sub.C and R.sub.D together with R.sub.E in each case represents an additional link,and salts of salt-forming compounds of the formula (I), compounds of the formula (I) or the salts thereof have anti-allergic properties. They can be prepared in accordance with processes known per se and may be used as active substances in pharmaceutical preparations.
摘要翻译：式（I）的新的4,7-菲咯啉衍生物其中Ch表示6位与-N（RE） - 基团连接的任意取代的5,6-喹啉基，并且R表示任选酯化或酰胺化的羧基，并且其中RA和RB一起表示氧代，RC和RD一起表示另外的连接，并且RE表示基团R 1，其为氢或脂族，脂环族，芳脂族或杂环脂族基团，或RA表示任选醚化的羟基，RB与RC和RD一起连同RE一起代表另外的连接，式（I）的成盐化合物的盐，式（I）的化合物）或其盐具有抗过敏性质。它们可以根据本身已知的方法制备，并且可以用作药物制剂中的活性物质。

5. 发明授权

US4327091A N,N-Di and N,N,N-tri(hydroxy-lower alkyl) ammonium salts of substituted 3,4-dihydro-2H-1,2-benzothiazine 1,1 dioxide and pharmaceutical compositions thereof 失效
标题翻译：取代的3,4-二氢-2H-1,2-苯并噻嗪一氧化碳的N，N-Di和N，N，N-三（羟基 - 低级烷基）铵盐及其药物组合物
公开(公告)号：US4327091A
公开(公告)日：1982-04-27
申请号：US116200
申请日：1980-01-28
申请人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
发明人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
IPC分类号： A61K31/54 , A61P29/00 , C07D417/12
CPC分类号： C07D417/12
摘要： 3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R.sub.1 represents hydrogen or a substituted or unsubstituted hydrocarbon radical of aliphatic character, and their salts, possess antiinflammatory properties and are useful as medicaments.
摘要翻译：式（Ⅰ）的3,4-二氢-2H-1,2-苯并噻嗪1,1-二氧化物，其中Ph表示取代或未取代的1,2-亚苯基，R表示取代或未取代的苯并吡喃酮基， R 1表示氢或取代或未取代的脂肪族烃基，它们的盐具有抗炎性质，可用作药物。

6. 发明授权

US4288450A Process for the preparation of novel benzopyrane derivatives 失效
标题翻译：制备新型苯并吡喃衍生物的方法
公开(公告)号：US4288450A
公开(公告)日：1981-09-08
申请号：US110077
申请日：1980-01-07
申请人： Georges Haas , Alberto Rossi , Knut A. Jaeggi , Alex Sele
发明人： Georges Haas , Alberto Rossi , Knut A. Jaeggi , Alex Sele
IPC分类号： C07D311/74 , A61K31/352 , C07D311/22 , C07D311/30 , C07D311/94 , C07D501/20 , C07D501/38 , A61K31/35
CPC分类号： C07D311/22 , C07D311/30 , C07D311/94 , Y10S514/826 , Y10S514/861
摘要： The present invention relates to novel benzopyrane derivatives, especially 3-oxaloamino-4-oxo-4H-1-benzopyrane derivatives of the formula I ##STR1## in which Ph is substituted or unsubstituted 1,2-phenylene, R is free, esterified or amidated carboxyl and R.sub.1 is hydrogen or a substituted or substituted hydrocarbon radical, in the free from or in the form of a salt, exhibit antiallergic activities and are accordingly useful as active ingredients of antiallergic pharmaceutical preparations.
摘要翻译：本发明涉及新的苯并吡喃衍生物，特别是其中Ph为取代或未取代的1,2-亚苯基，R为游离基的式I（I）的3-氧代氨基-4-氧代-4H-1-苯并吡喃衍生物，酯化或酰胺化的羧基，R 1是氢或取代或取代的烃基，以盐形式存在或以盐形式，表现出抗过敏活性，因此可用作抗过敏药物制剂的活性成分。

7. 发明授权

US4216155A Process for the preparation of novel benzopyrane derivatives 失效
标题翻译：制备新型苯并吡喃衍生物的方法
公开(公告)号：US4216155A
公开(公告)日：1980-08-05
申请号：US923522
申请日：1978-07-11
申请人： Georges Haas , Alberto Rossi , Knut A. Jaeggi , Alex Sele
发明人： Georges Haas , Alberto Rossi , Knut A. Jaeggi , Alex Sele
IPC分类号： C07D311/74 , A61K31/352 , C07D311/22 , C07D311/30 , C07D311/94 , C07D501/20 , C07D501/38 , A61K31/35 , C07D311/78 , C07D493/04
CPC分类号： C07D311/22 , C07D311/30 , C07D311/94 , Y10S514/826 , Y10S514/861
摘要： The present invention relates to novel benzopyrane derivatives, especially 3-oxaloamino-4-oxo-4H-1-benzopyrane derivatives of the formula I ##STR1## in which Ph is substituted or unsubstituted 1,2-phenylene, R is free, esterified or amidated carboxyl and R.sub.1 is hydrogen or a substituted or substituted hydrocarbon radical, in the free form or in the form of a salt, exhibit antiallergic activities and are accordingly useful as active ingredients of antiallergic pharmaceutical preparations.
摘要翻译：本发明涉及新的苯并吡喃衍生物，特别是其中Ph为取代或未取代的1,2-亚苯基，R为游离基的式I（I）的3-氧代氨基-4-氧代-4H-1-苯并吡喃衍生物，酯化或酰胺化的羧基，R 1是氢或取代或取代的烃基，以游离形式或盐形式，表现出抗过敏活性，因此可用作抗过敏药物制剂的活性成分。

8. 发明授权

US4213980A Azathianaphthalenes 失效
标题翻译：氮杂萘
公开(公告)号：US4213980A
公开(公告)日：1980-07-22
申请号：US4113
申请日：1979-01-17
申请人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
发明人： Alex Sele , Pier G. Ferrini , Georges Haas , Knut A. Jaeggi , Alberto Rossi
IPC分类号： A61K31/54 , A61P29/00 , C07D417/12 , C07D279/02
CPC分类号： C07D417/12
摘要： 3,4-Dihydro-2H-1,2-benzothiazine 1,1-dioxides of the formula ##STR1## wherein Ph represents a substituted or unsubstituted 1,2-phenylene radical, R represents a substituted or unsubstituted benzopyrone radical, and R.sub.1 represents hydrogen or a substituted or unsubstituted hydrocarbon radical of aliphatic character, and their salts, possess antiinflammatory properties and are useful as medicaments.
摘要翻译：式（Ⅰ）的3,4-二氢-2H-1,2-苯并噻嗪1,1-二氧化物，其中Ph表示取代或未取代的1,2-亚苯基，R表示取代或未取代的苯并吡喃酮基， R 1表示氢或取代或未取代的脂肪族烃基，它们的盐具有抗炎性质，可用作药物。

9. 发明授权

US4188396A New phenylazacycloalkanes 失效
标题翻译：新的苯基氮杂环烷烃
公开(公告)号：US4188396A
公开(公告)日：1980-02-12
申请号：US867644
申请日：1978-01-06
申请人： Georges Haas , Alberto Rossi , Pier G. Ferrini , Oswald Schier
发明人： Georges Haas , Alberto Rossi , Pier G. Ferrini , Oswald Schier
IPC分类号： A61K20060101 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/24 , A61P25/26 , A61P43/00 , C07D20060101 , C07D211/08 , C07D211/12 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/30 , C07D211/32 , C07D211/52 , C07D211/62 , C07D211/70 , C07D211/74 , C07D211/76 , C07D211/78 , C07F3/02
CPC分类号： C07C255/00 , C07D211/12 , C07D211/14 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/52 , C07D211/70 , C07D211/74 , C07D211/78 , C07F3/02
摘要： New 4-(phenyl)-piperidine compounds of the general formula I ##STR1## in which R.sub.1 represents hydrogen or lower alkyl, Ph represents a p-phenylene group optionally substituted by lower alkyl, lower alkoxy, nitro and/or halogen, and R.sub.2 represents lower alkyl, and pharmaceutically acceptable acid addition salts thereof are useful as antidepressant agents.
摘要翻译：新的式（I）的4-（苯基） - 哌啶化合物，其中R 1表示氢或低级烷基，Ph表示任选被低级烷基，低级烷氧基，硝基和/或卤素取代的对亚苯基，R2表示低级烷基，其药学上可接受的酸加成盐可用作抗抑郁剂。

10. 发明授权

US3933835A New aliphatically substituted aryl-chalcogeno-hydrocarbon derivatives 失效
标题翻译：新的脂肪族取代芳基 - 硫属烃衍生物
公开(公告)号：US3933835A
公开(公告)日：1976-01-20
申请号：US409192
申请日：1973-10-24
申请人： Georges Haas , Roland Jaques , Alberto Rossi , Martin Ruegg
发明人： Georges Haas , Roland Jaques , Alberto Rossi , Martin Ruegg
IPC分类号： C07C69/708 , C07C59/72 , C07C67/00 , C07C69/66 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/06 , C07C253/00 , C07C255/13 , C07C301/00 , C07C303/02 , C07C303/22 , C07C303/36 , C07C303/40 , C07C309/11 , C07C311/00 , C07C313/00 , C07C317/18 , C07C319/14 , C07C323/52 , C07D213/55
CPC分类号： C07C59/72
摘要： Compounds of the formula IR.sub.1 -- Ph -- X -- alk -- R.sub.2 (I)wherein R.sub.1 is adamantyl, Ph is phenylene which is optionally substituted by amino, nitro, lower alkyl, lower alkoxy, halogen or trifluoromethyl, X is oxy or thio, alk is alkylene with 1 to 20 C atoms or alkenylene with 2 to 20 C atoms and R.sub.2 is free, esterfied or amidised carboxyl, sulpho or sulphonamido and therapeutically acceptable salts thereof are useful as anti-allergic and hypolipidaemic agents.
摘要翻译：硝基，低级烷基，低级烷氧基，卤素或三氟甲基，X是氧基或硫基，其中R 1是金刚烷基，Ph是任选被氨基，硝基，低级烷基，低级烷氧基，卤素或三氟甲基取代的亚苯基，烷基是具有1至20个碳原子的亚烷基或具有2至20个碳原子的亚烯基，R2是游离的，酯化的或酰胺化的羧基，磺基或磺酰胺基，其治疗上可接受的盐可用作抗过敏和降血脂药。

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