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1. 发明授权

US4725691A 2-[8-quinolinyl]-sulphinyl-1H-benzimidazole 失效
标题翻译： 2- [8-喹啉基] - 亚磺酰基-1H-苯并咪唑
公开(公告)号：US4725691A
公开(公告)日：1988-02-16
申请号：US913689
申请日：1986-09-30
申请人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
发明人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/54 , A61P1/00 , A61P1/04 , A61P43/00 , C07D401/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/14 , C07D513/16 , C07D513/22
CPC分类号： C07D401/12 , C07D513/14
摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen preferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is a alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.

2. 发明授权

US4636499A Sulphenamides 失效
标题翻译：苯甲酰胺
公开(公告)号：US4636499A
公开(公告)日：1987-01-13
申请号：US739425
申请日：1985-05-30
申请人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
发明人： Arne E. Brandstrom , Per L. Lindberg , Bjorn Wallmark
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/54 , A61P1/00 , A61P1/04 , A61P43/00 , C07D401/12 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D495/04 , C07D513/14 , C07D513/16 , C07D513/22 , C07D513/04 , C07D513/12
CPC分类号： C07D401/12 , C07D513/14
摘要： Novel compounds of the formula IIIa ##STR1## wherein R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a are the same or different and are hydrogen, an alkyl, alkoxy optionally completely or predominantly substituted by fluorine or chlorine, halogen, --CN, --CF.sub.3, --NO.sub.2, --COR, --COOR, aryl, aryloxy or arylalkoxy group, or adjacent groups R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form a 5-, 6- or 7-membered monocyclic ring or a 9-, 10- or 11-membered bicyclic ring, which rings may be saturated or unsaturated and may contain 0-3 heteroatoms selected from N and O and which rings may be optionally substituted with 1-4 substitutents selected from alkyl groups with 1-3 carbon atoms, halogen perferably F or Cl, alkylene radicals containing 4-5 carbon atoms giving spiro compounds, or two or four of these substituents together form one or two oxy groups ##STR2## whereby if R.sup.1a, R.sup.2a, R.sup.3a and R.sup.4a together with the adjacent carbon atoms in the benzimidazole ring form two rings they may be condensed with each other, R.sup.5a is hydrogen or an alkyl group, R.sup.6a is hydrogen or an alkyl group or R.sup.5a and R.sup.6a are joined together to form an alkylene chain, R.sup.7a is hydrogen, an alkyl, alkoxy, alkenyloxy, or alkynyloxy group, R.sup.8a is hydrogen or an alkyl group, or R.sup.6a and R.sup.7a, or R.sup.7a and R.sup.8a together with the adjacent carbon atoms in the pyridinium ring form a ring wherein the part constituted by R.sup.6a and R.sup.7a or R.sup.7a and R.sup.8a, is --CH.dbd.CH--CH.dbd.CH--, --O--(CH.sub.2).sub.p --, --CH.sub.2 (CH.sub.2).sub.p --, --O--CH.dbd.CH--, --NH--CH.dbd.CH--, ##STR3## or --S--(CH.sub.2).sub.p --, wherein p is 2, 3 or 4 and the O, S and N atoms always are attached to position 3 in the compound IIIa, R is an alkyl, cycloalkyl, aryl or arylalkyl group, and X.sup.- is a pharmaceutically acceptable anion, process for preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine.
摘要翻译：新的式IIIa化合物其中R 1a，R 2a，R 3a和R 4a相同或不同，为氢，烷基，任选完全或主要被氟或氯取代的烷氧基，卤素，-CN，-CF 3 - NO 2，-COR，-COOR，芳基，芳氧基或芳烷氧基或相邻基团R 1a，R 2a，R 3a和R 4a与苯并咪唑环中的相邻碳原子一起形成5-，6-或7-元单环或 9,10,10或11元双环，该环可以是饱和或不饱和的，并且可以含有0-3个选自N和O的杂原子，哪些环可以任选被1-4个选自烷基的取代基取代， 3个碳原子，卤素优选为F或Cl，含有4-5个碳原子的烯基，得到螺环化合物，或两个或四个这些取代基一起形成一个或两个氧基“IMAGE”，如果R1a，R2a，R3a和R4a连同苯并咪唑环中相邻的碳原子形成它们的两个环相互稠合，R5a为氢或烷基，R6a为氢或烷基或R5a和R6a连接在一起形成亚烷基链，R7a为氢，烷基，烷氧基，烯氧基或炔氧基， R8a是氢或烷基，或R6a和R7a或R7a和R8a与吡啶鎓环中的相邻碳原子一起形成环，其中由R6a和R7a或R7a和R8a构成的部分是-CH = CH-CH = CH-，-O-（CH 2）p - ， - CH 2（CH 2）p - ， - O-CH = CH-，-NH-CH = CH-，其中p是2,3或4，并且O，S和N原子总是连接到化合物IIIa中的3位，R是烷基，环烷基，芳基或芳基烷基，X是药学上可接受的阴离子，含有这些化合物的药物组合物及其在药物中的用途。

3. 发明授权

US5441968A Therapeutically active fluoro substituted benzimidazoles 失效
标题翻译：治疗活性氟取代的苯并咪唑
公开(公告)号：US5441968A
公开(公告)日：1995-08-15
申请号：US134255
申请日：1993-10-08
申请人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
IPC分类号： C07D401/12 , A61K31/44
CPC分类号： C07D401/12
摘要： The novel compounds of the formulas I and I' ##STR1## wherein F is in 5 or 6 position and ##STR2## wherein in both formulas R is the group --CH.sub.2 OCOOR.sup.1, wherein R.sup.1 is a straight or branched alkyl containing 1-6 carbon atoms or benzyl, or R.sup.1 is the group ##STR3## wherein n is 1-6 and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
摘要翻译：式I和I'的新颖化合物，其中F为5或6位且其中在两式中，R为基团-CH 2 OCOOR 1，其中R 1为含有1- 6个碳原子或苄基，或R1是其中n是1-6的基团，或其生理学上可接受的盐以及中间体，含有这些化合物作为活性成分的药物组合物，以及该化合物的用途在医学上。

4. 发明授权

US5019584A Therapeutically active chloro substituted benzimidazole 失效
标题翻译：治疗活性氯取代的苯并咪唑
公开(公告)号：US5019584A
公开(公告)日：1991-05-28
申请号：US454046
申请日：1989-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Carl I. Starke , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Carl I. Starke , Gunnel E. Sunden
IPC分类号： A61K9/08 , A61K9/20 , A61K9/48 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61P1/00 , A61P1/04 , C07D401/12
CPC分类号： C07D401/12
摘要： 5-Chloro-2-[[(3,4-dimethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole and physiologically acceptable salts thereof as well as an intermediate, pharmaceutical compositions containing such compound as active ingredient, and the use of the compound in medicine.
摘要翻译： 5-氯-2 - [[（3,4-二甲氧基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑及其生理学上可接受的盐，以及含有活性成分的化合物的中间体药物组合物，的药物中的化合物。

5. 发明授权

US5008278A Therapeutically active compound and a process for its preparation 失效
标题翻译：治疗活性化合物及其制备方法
公开(公告)号：US5008278A
公开(公告)日：1991-04-16
申请号：US454047
申请日：1989-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
IPC分类号： C07D401/12 , A61K31/4178 , A61K31/4184 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61P1/04 , C07D20060101 , C07D213/68 , C07D213/89 , C07D235/28
CPC分类号： C07D401/12 , C07D235/28
摘要： The novel compound 5-fluoro-2[[(4-cyclopropylmethoxy-2-pyridinyl) methyl]sulfinyl]-1H-benzimidazole and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing the compound as active ingredient, and the use of the compound in medicine.
摘要翻译：新化合物5-氟-2 [[（4-环丙基甲氧基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑及其生理学上可接受的盐以及中间体，含有该化合物作为活性成分的药物组合物，以及使用药物中的化合物。

6. 发明授权

US4689331A Substituted 2-pyridinyl benzimidazoles, and their use for inhibiting gastric acid secretion 失效
标题翻译：取代的2-吡啶基苯并咪唑，以及它们用于抑制胃酸分泌的用途
公开(公告)号：US4689331A
公开(公告)日：1987-08-25
申请号：US788768
申请日：1985-10-18
申请人： Kjell F. Ankner , Arne E. Brandstrom , Per L. Lindberg , Mats P. Nordberg , Bjorn M. G. Wallmark
发明人： Kjell F. Ankner , Arne E. Brandstrom , Per L. Lindberg , Mats P. Nordberg , Bjorn M. G. Wallmark
IPC分类号： A61K31/44 , A61K31/4427 , A61P1/04 , C07D401/04 , C07D401/14 , C12N9/99
CPC分类号： C07D401/04
摘要： Novel compounds of the formula I ##STR1## and its salts; process for the preparation thereof, pharmaceutical compositions containing such compounds and their use in medicine to affect gastric acid secretion and provide gastrointestinal cytoprotection.
摘要翻译：新的式I化合物及其盐; 其制备方法，含有这些化合物的药物组合物及其在药物中的用途，以影响胃酸分泌并提供胃肠细胞保护作用。

7. 发明授权

US5049674A Therapeutically active fluoro substituted benzimidazoles 失效
标题翻译：治疗活性氟取代的苯并咪唑
公开(公告)号：US5049674A
公开(公告)日：1991-09-17
申请号：US454048
申请日：1989-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/495 , A61P1/00 , A61P1/04 , C07D20060101 , C07D401/12
CPC分类号： C07D401/12
摘要： The novel compounds of the formulas I and I' ##STR1## wherein F is in 5 or 6 position and ##STR2## wherein in both formulas R is the group --CH.sub.2 OCOOR.sup.1, wherein R.sup.1 is a straight or branched alkyl containing 1-6 carbon atoms or benzyl, or R.sup.1 is the group ##STR3## --(CH.sub.2).sub.n COOH or --(CH.sub.2).sub.n SO.sub.3 H wherein n is 1-6 and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
摘要翻译：式I和I'的新颖化合物，其中F为5或6位且其中在两式中，R为基团-CH 2 OCOOR 1，其中R 1为含有1- 6个碳原子或苄基，或R1是基团，其中n是1-6，其生理学上可接受的盐以及中间体，含有活性的化合物的药物组合物是（CH 2）n COOH或 - （CH 2）n SO 3 H 成分，以及在药物中使用的化合物。

8. 发明授权

US5039808A Therapeutically active cyclopropyl substituted compound 失效
标题翻译：治疗活性环丙基取代的化合物
公开(公告)号：US5039808A
公开(公告)日：1991-08-13
申请号：US633007
申请日：1990-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
IPC分类号： C07D401/12 , A61K31/4178 , A61K31/4184 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61P1/04 , C07D20060101 , C07D213/68 , C07D213/89 , C07D235/28
CPC分类号： C07D401/12 , C07D235/28
摘要： The novel compound 5-fluoro-2[[(4-cyclopropylmethoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing the compound as active ingredient, and the use of the compound in medicine.

9. 发明授权

US5025024A Therapeutically active fluoro-substituted compound 失效
标题翻译：治疗活性氟取代的化合物
公开(公告)号：US5025024A
公开(公告)日：1991-06-18
申请号：US453960
申请日：1989-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Gunnel E. Sunden
IPC分类号： C07D233/84 , A61K31/415 , A61K31/44 , A61K31/4427 , A61P1/04 , C07D235/28 , C07D401/12
CPC分类号： C07D401/12 , C07D235/28
摘要： The novel compound 4-fluoro-2-[[(4-methoxy-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compound in medicine.
摘要翻译：新化合物4-氟-2 - [[（4-甲氧基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑及其生理学上可接受的盐以及中间体，含有这些化合物作为活性成分的药物组合物和使用的药物中的化合物。

10. 发明授权

US4965269A Therapeutically active chloro substituted benzimidazoles 失效
标题翻译：治疗活性氯取代的苯并咪唑
公开(公告)号：US4965269A
公开(公告)日：1990-10-23
申请号：US454049
申请日：1989-12-20
申请人： Arne E. Brandstrom , Per L. Lindberg , Carl I. Starke , Gunnel E. Sunden
发明人： Arne E. Brandstrom , Per L. Lindberg , Carl I. Starke , Gunnel E. Sunden
IPC分类号： C07D417/12
CPC分类号： C07D417/12 , Y10S514/925 , Y10S514/926
摘要： The novel compounds of the formula I ##STR1## wherein Cl is in 5 or 6 position and whereby R is the group --CH.sub.2 OCOOR.sup.1, wherein R.sup.1 is a straight or branched alkyl containing 1-6 carbon atoms or benzyl,or R.sup.1 is the group --(CH.sub.2).sub.n ##STR2## --(CH.sub.2).sub.n COOH or --(CH.sub.2).sub.n SO.sub.3 H wherein n is 1-6 and physiologically acceptable salts thereof as well as intermediates, pharmaceutical compositions containing such compounds as active ingredient, and the use of the compounds in medicine.
摘要翻译：其中Cl为5或6位，其中R为基团-CH 2 OCOOR 1，其中R 1为含1-6个碳原子的直链或支链烷基或苄基，或R1为基团 - （CH 2）n COOH或 - （CH 2）n SO 3 H，其中n为1-6及其生理上可接受的盐以及中间体，含有这些化合物作为活性成分的药物组合物，以及药物中的化合物。

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