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1.发明授权公开(公告)号：US06221864B1
公开(公告)日：2001-04-24
申请号：US09446662
申请日：1999-12-23
IPC分类号： A61K315377
CPC分类号： A61K31/5377 , A61K31/535
摘要： The present invention relates to an agent for the prophylaxis and treatment of diseases caused by Helicobacter infections, which comprises (S)-1-cyclopropyl-1,4-dihydro-7-[2-(N,N-dimethylaminomethyl)morpholino]-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof. The prophylactic and therapeutic agent of the present invention is effective even when used alone in a small dose for a short time, is almost free of problematic side effects such as tolerance and diarrhea, and is low toxic and capable of safe and ensured bacterial eradication. It is useful for the prophylaxis and treatment of diseases caused by Helicobacter infections, particularly, gastritis, gastric ulcer, duodenal ulcer, malignant lymphoma and gastric cancer.
摘要翻译： 本发明涉及一种用于预防和治疗由幽门螺杆菌感染引起的疾病的药剂，其包含（S）-1-环丙基-1,4-二氢-7- [2-（N，N-二甲基氨基甲基）吗啉代] 6-氟-8-甲氧基-4-氧代喹啉-3-羧酸或其药学上可接受的盐。 本发明的预防和治疗剂即使在短时间内以小剂量单独使用也是有效的，几乎没有诸如耐受性和腹泻的副作用，并且毒性低，能够安全和确保细菌根除。 可用于预防和治疗由幽门螺杆菌感染引起的疾病，特别是胃炎，胃溃疡，十二指肠溃疡，恶性淋巴瘤和胃癌。
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2.发明授权2(4-n-Hexadecyl amino or oxy phenyl) 5 ethoxy oxazoleacetic acid derivatives 失效2（4-正十六烷基氨基或氧苯基）5乙氧基恶唑乙酸衍生物
公开(公告)号：US4365066A
公开(公告)日：1982-12-21
申请号：US253932
申请日：1981-07-28
申请人： Tsutomu Yamanaka , Mitsuharu Sano , Hiroshi Yasuda
发明人： Tsutomu Yamanaka , Mitsuharu Sano , Hiroshi Yasuda
IPC分类号： A61K31/42 , A61K31/421 , A61P3/06 , C07D263/42
CPC分类号： C07D263/42 , Y10S514/824 , Y10S514/96
摘要： Oxazoleacetic acid derivatives of the formula ##STR1## and salts thereof wherein R.sup.1 is a higher alkyl group having 10 to 20 carbon atoms, a higher alkenyl group, a benzyl group or a halogen substituted benzyl group; X is O, S or NH; R.sup.2 is a lower alkyl group, a phenyl group or a halogen-substituted phenyl group and R.sup.3 is a hydrogen atom or a lower alkyl group, having a hypolipidemic activity.
摘要翻译： PCT No.PCT / JP80 / 00287 Sec。 371日期1981年7月28日 102（e）日期1981年4月14日PCT提交1980年11月25日PCT公布。 公开号WO81 / 01553 日期：1981年6月11日。下式的化合物：其中R1是具有10-20个碳原子的高级烷基，较高的烯基，苄基或卤素取代的苄基; X是O，S或NH; R2是低级烷基，苯基或卤素取代的苯基，R3是具有降血脂活性的氢原子或低级烷基。
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3.发明授权3,4-dihydrothieno[2,3-d]pyrimidine compounds and their pharmaceutical use 失效3,4-二羟基（2,3-D）吡啶化合物及其药物用途
公开(公告)号：US5124331A
公开(公告)日：1992-06-23
申请号：US439044
申请日：1989-11-02
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： 3,4-Dihydrothieno[2,3-d]pyrimidine compounds having immunoregulating and carcinostatic actions of the general formula ##STR1## wherein A represents a C.sub.1-4 alkylene; R.sup.1 represents hydrogen, an alkyl, an aryl which may be substituted or --N(R.sup.7)(R.sup.8); R.sup.2, R.sup.3 and R.sup.4 represent hydrogen, a halogen, hydroxy, an alkyl which may be substituted by a halogen, an alkoxy, nitro, cyano or --N(R.sup.9)(R.sup.10); R.sup.5 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl or an alkoxycarbonyl; R.sup.6 represents hydrogen, a halogen, nitro, amino, cyano, an alkyl, an alkoxycarbonyl, a halogenosulfonyl or --SO.sub.2 N(R.sup.12)(R.sup.13); or R.sup.5 and R.sup.6 may, taken together, form a C.sub.3-6 alkylene chain, and their pharmaceutical use.
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公开(公告)号：US4720493A
公开(公告)日：1988-01-19
申请号：US799989
申请日：1985-11-20
IPC分类号： A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/535 , A61P1/04 , A61P25/08 , A61P25/20 , C07D333/00 , C07D333/22 , C07D333/38 , C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D333/22 , C07D333/38 , C07D417/14
摘要： Thienylthiazole compounds of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein: R is amino, guanidino, alkylamino, alkenylamino, unsubstituted or optionally substituted phenylamino or acylamino;A is amino, alkylamino, cyclic amino, alkanoylamino, a group of the formula: ##STR2## wherein each symbol is as defined in claim 1; Z is hydrogen or halogen; andm is 0 or 1 to 4,are useful in the treatment of peptic ulcer, acute or chronic gastritis, acute damage of gastric mucous membrane, dimentia and anxiety.
摘要翻译： 下式的噻吩噻唑化合物及其药学上可接受的酸加成盐，其中：R为氨基，胍基，烷基氨基，烯基氨基，未取代或任选取代的苯基氨基或酰氨基; A是氨基，烷基氨基，环状氨基，烷酰基氨基，下式的基团：其中每个符号如权利要求1中所定义; Z是氢或卤素; m为0或1〜4，可用于治疗消化性溃疡，急性或慢性胃炎，胃粘膜急性损伤，疼痛和焦虑。
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公开(公告)号：US20100298550A1
公开(公告)日：2010-11-25
申请号：US12681658
申请日：2008-10-03
IPC分类号： C07H15/04 , C07H19/067 , C07H1/00 , C07H3/08
CPC分类号： C07H5/02 , C07H13/06 , C07H15/04 , C07H19/067
摘要： It is an object of the present invention to provide a process for producing 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose in an industrially appropriate manner. The present invention provides a process for producing a 1,2,3-tri-O-acetyl-5-deoxy-ribofuranose which comprises hydrogenating a compound represented by the formula (1) or formula (2) in the presence of a metal catalyst: wherein P1 and P2 independently represent a hydrogen atom or an acyl group, OP1 and OP2 may together form an acetal group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group; wherein X1 represents Br or I, P3 and P4 independently represent a hydrogen atom or an acyl group, and R represents a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an acyl group.
摘要翻译： 本发明的目的是提供以工业上合适的方式制备1,2,3-三-O-乙酰基-5-脱氧 - 呋喃核糖的方法。 本发明提供了一种制备1,2,3-三-O-乙酰基-5-脱氧 - 呋喃核糖的方法，该方法包括在金属催化剂存在下氢化由式（1）或式（2）表示的化合物 ：其中P1和P2独立地表示氢原子或酰基，OP1和OP2可以一起形成缩醛基，R表示氢原子，烷基，芳基，芳烷基或酰基; 其中X1表示Br或I，P3和P4独立地表示氢原子或酰基，R表示氢原子，烷基，芳基，芳烷基或酰基。
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公开(公告)号：US5616581A
公开(公告)日：1997-04-01
申请号：US460666
申请日：1995-06-02
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/333 , A61K31/44 , A61K31/535
CPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/3332
摘要： A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobacter pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.
摘要翻译： 式（I）的吡啶化合物其中R 1是氢，卤素，烷基，烷氧基等，R 2和R 3各自是氢，卤素或烷基，-P = Q-是 -CH = CH-，-N = CH-或-CH = N-，A是氧原子，硫原子或其中R4是氢，烷基等的N（R4），n是0,1或2， B是S（O）p，其中p是0,1或2，D是单键，亚烷基等，E是烷氧基烷基或-N（R6）（R7），其药学上可接受的盐具有抗菌性 针对幽门螺杆菌的活性，抗溃疡活性，胃肠细胞保护活性，溃疡复发，复发预防活性和胃酸分泌抑制活性，可用作药物制剂。
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公开(公告)号：US5504082A
公开(公告)日：1996-04-02
申请号：US352183
申请日：1994-12-01
IPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/333 , A61K31/44 , A61K31/535 , C07D413/14
CPC分类号： C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C08G65/3332
摘要： A pyridine compound of the formula ##STR1## wherein R.sup.1 is a hydrogen, a halogen, an alkyl, an alkoxy or the like, R.sup.2 and R.sup.3 are each a hydrogen, a halogen or an alkyl, --P.dbd.Q-- is --CH.dbd.CH--, --N.dbd.CH-- or --CH.dbd.N--, A is an oxygen atom, a sulfur atom or N(R.sup.4) wherein R.sup.4 is hydrogen, alkyl or the like, n is 0, 1 or 2, B is S(O)p wherein p is 0, 1 or 2, D is a single bond, an alkylene or the like and E is an alkoxyalkyl or --N(R.sup.6)(R.sup.7), and a pharmaceutically acceptable salt thereof have antibacterial activity against Helicobater pylori, antiulcer activity, gastrointestinal cytoprotective activity, ulcer recurrence, relapse-preventive activity and gastric acid secretion-suppressive activity and are useful as pharmaceutical preparations.
摘要翻译： 式（I）的吡啶化合物其中R 1是氢，卤素，烷基，烷氧基等，R 2和R 3各自是氢，卤素或烷基，-P = Q-是 -CH = CH-，-N = CH-或-CH = N-，A是氧原子，硫原子或其中R4是氢，烷基等的N（R4），n是0,1或2， B是S（O）p，其中p是0,1或2，D是单键，亚烷基等，E是烷氧基烷基或-N（R6）（R7），其药学上可接受的盐具有抗菌性 针对幽门螺旋杆菌的活性，抗溃疡活性，胃肠细胞保护活性，溃疡复发，复发预防活性和胃酸分泌抑制活性，可用作药物制剂。
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