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1. 发明授权

US5459254A Process for preparing synthetic intermediates of 2-alkynyladenosines and 2-alkynyladenosines 失效
标题翻译：制备2-炔基腺苷和2-炔基腺苷合成中间体的方法
公开(公告)号：US5459254A
公开(公告)日：1995-10-17
申请号：US149943
申请日：1993-11-10
申请人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Takanori Miyashita , Shinji Sakata , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/067
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2,[V] A=NHR.sup.4,wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译：本发明涉及可用作2-炔基腺苷合成中间体的下式[I]表示的新型化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷[Ⅳ]的方法。此外，本发明涉及具有优异的储存稳定性的由下式[V]表示的2-炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。 [I] A =离去基团，[II] A = NH 2，[V] A = NHR 4，其中R 1至R 4表示氢原子或保护基，n表示1至15的整数， R1至R4同时不表示氢原子。

2. 发明授权

US5283327A Tri-O-acetyl-2-alkynyladenosines 失效
标题翻译：三-O-乙酰基-2- alkynyladenosines
公开(公告)号：US5283327A
公开(公告)日：1994-02-01
申请号：US655354
申请日：1991-04-17
申请人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
发明人： Toyofumi Yamaguchi , Toichi Abiru , Akira Matsuda , Tohru Ueda , Kentaro Kogi
IPC分类号： C07H19/16 , C07H19/167
CPC分类号： C07H19/16 , Y02P20/55
摘要： The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine.The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound.Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.
摘要翻译： PCT No.PCT / JP90 / 00807 Sec。 371日期：1991年4月17日 102（e）中的日期1991年4月17日提交的PCT 1990年6月20日的PCT公布。出版物WO90 / 15812 PCT 日本1990年12月27日。本发明涉及可用作2-炔基腺苷合成中间体的下式（I）表示的新化合物。本发明还涉及该化合物的制备方法和通过该化合物制备2-炔基腺苷（Ⅳ）的方法。此外，本发明涉及具有优异储存稳定性的下式（V）表示的2-链炔基腺苷衍生物，以及以该衍生物的形式存储2-炔基腺苷的方法。（*化学结构*）（*化学结构*）其中R1至R4表示氢原子或保护基，n表示1至15的整数，条件是R1至R4同时不表示氢原子。

3. 发明授权

US5270304A Therapeutic 2-alkynyl adenosine agent for ischemic diseases of the heart or brain 失效
标题翻译：用于心脏或脑部缺血性疾病的治疗性2-炔基腺苷
公开(公告)号：US5270304A
公开(公告)日：1993-12-14
申请号：US700156
申请日：1991-05-15
申请人： Kentaro Kogi , Toichi Abiru , Toyofumi Yamaguchi
发明人： Kentaro Kogi , Toichi Abiru , Toyofumi Yamaguchi
IPC分类号： C07H19/16 , A61K31/52
CPC分类号： A61K31/70 , C07H19/16
摘要： The present invention concerns a therapeutic-prophylactic agent for ischemic diseases of the heart or brain, comprising as an active ingredient a 2-alkynyladenosine represented by the following formula: ##STR1## wherein n represents an integer of from 2 to 15.
摘要翻译： PCT No.PCT / JP89 / 01158 Sec。 371日期1991年5月15日 102（e）日期1991年5月15日PCT提交1989年11月15日PCT公布。出版物WO90 / 05526 日期：1990年5月31日本发明涉及心脏或脑的缺血性疾病的治疗性预防剂，其包含作为活性成分的下式表示的2-炔基腺苷：其中n表示整数从2到15。

4. 发明授权

US4874760A 4,7-dihydroisothiazolo(5,4-b)pyridine derivatives and cardiovascular treating agents containing said derivatives 失效
标题翻译： 4,7-二氢异噻唑（5,4-b）吡啶衍生物和含有所述衍生物的心血管治疗剂
公开(公告)号：US4874760A
公开(公告)日：1989-10-17
申请号：US140999
申请日：1988-01-05
申请人： Shin-ichi Yamada , Takao Goto , Toshihisa Mashiko , Kentaro Kogi , Yukiko Oguchi , Senichi Narita
发明人： Shin-ichi Yamada , Takao Goto , Toshihisa Mashiko , Kentaro Kogi , Yukiko Oguchi , Senichi Narita
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A 4,7-dihydroisothiazole[5,4-b]pyridine derivative represented by the general formula ##STR1## wherein R.sup.1 represents an alkyl group which may be substituted,R.sup.2 represents a hydrogen atom, a hydroxyl group, a benzyloxy group, a lower alkoxy group, a group of the formula ##STR2## in which R.sup.3 and R.sup.4 are identical or different and each represents a hydrogen atom, a lower alkyl group, an aralkyl group, an aralkynyl group, an aryloxyalkyl group, an arylaminoalkyl group, a pyridylalkyl group or a benzazolylalkyl group, or R.sup.3 and R.sup.4 form a ring and represent a group of the formula ##STR3## where X represents a methine group, a nitrogen atom or an oxygen atom, n is an integer of 1 or 2, and when X is a methine group or a nitrogen atom, R.sup.5 represents a hydrogen atom, a lower alkyl group, a lower hydroxyalkyl group, an aryl group, an aryloxy group, an aralkyl group, a furoyl group, a pyridyl group or a diphenylmethane group each of which group may be substituted, andm is an integer of 1 to 3,or an acid addition salt thereof. Processes for producing said derivative and a cardiovascular treating agent comprising said derivative as an active ingredient are also provided.

5. 发明授权

US5117037A Cis-bicyclo[4,3.0]non-2-end derivatives 失效
标题翻译： CIS-BICYCLO（4,3.0）非2-D衍生物
公开(公告)号：US5117037A
公开(公告)日：1992-05-26
申请号：US622471
申请日：1990-12-05
申请人： Masakatsu Shibasaki , Takahashi Atsuo , Tuyoshi Aoki , Hiroyasu Sato , Shin-ichi Yamada , Michiko Kudo , Takaji Yamaguchi , Kentaro Kogi , Sen-ichi Narita
发明人： Masakatsu Shibasaki , Takahashi Atsuo , Tuyoshi Aoki , Hiroyasu Sato , Shin-ichi Yamada , Michiko Kudo , Takaji Yamaguchi , Kentaro Kogi , Sen-ichi Narita
IPC分类号： C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , C07C69/738 , C07C405/00
CPC分类号： C07C69/738 , C07C405/0083 , C07C59/46 , C07C59/62 , C07C69/712 , C07C69/732 , Y02P20/55
摘要： A cis-bicyclo[4.3.0]non-2-ene derivative of the formula: ##STR1## wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R.sup.1 is a hydrogen atom, A C.sub.1 -C.sub.12 straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a C.sub.6 -C.sub.12 aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is --CH.dbd.CH--CH.sub.2 --, or --CH.sub.2 --CH.sub.2 --O--, R.sup.2 is a C.sub.3 -C.sub.10 straight or branched chain alkyl group, a C.sub.1 -C.sub.3 alkyl group substituted by an aryloxy group which may be substituted, a C.sub.3 -C.sub.12 straight or branched chain alkenyl group, a C.sub.3 -C.sub.8 straight or branched chain alkynyl group, a C.sub.1 -C.sub.3 alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a C.sub.1 -C.sub.6 alkoxy group or by a C.sub.5 -C.sub.8 cycloalkyl group, R.sup.3 is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.

6. 发明授权

US06258829B1 Cycloalka[b]pyridine-3-carbonylguanidine derivatives, process for producing the same, and drugs containing the same 有权
标题翻译：环烷基[b]吡啶-3-羰基胍衍生物，其制备方法和含有它们的药物
公开(公告)号：US06258829B1
公开(公告)日：2001-07-10
申请号：US09367873
申请日：1999-09-03
申请人： Atsuo Takahashi , Kaoru Genkyou , Sachiko Yoneyama , Kazuyuki Aihara , Takashi Satoh , Fumiya Yoneyama , Jun Sasamori , Shin-ichi Yamada , Tetsuo Kimura , Kentaro Kogi
发明人： Atsuo Takahashi , Kaoru Genkyou , Sachiko Yoneyama , Kazuyuki Aihara , Takashi Satoh , Fumiya Yoneyama , Jun Sasamori , Shin-ichi Yamada , Tetsuo Kimura , Kentaro Kogi
IPC分类号： A61K31435
CPC分类号： C07D221/04 , C07D215/54 , C07D215/60 , C07D401/04 , C07D401/06 , C07D401/12 , C07D409/06 , C07D491/04 , C07D491/10 , C07F7/1804
摘要： This invention relates to a cycloalka[b]pyridine-3-carbonylguanidine derivative represented by the following general formula (1): and a salt thereof, which can provide a drug having sodium/proton (Na+/H+) exchange transport inhibitory action.
摘要翻译：本发明涉及可以提供具有钠/质子（Na + / H +）交换转运抑制作用的药物的由以下通式（1）表示的环烷并[b]吡啶-3-羰基胍衍生物及其盐。

7. 发明授权

US5728835A Substituted cyclic amine compound, production process thereof and pharmaceutical composition for circulatory organ use containing the same 失效
标题翻译：取代的环胺化合物，其制备方法和含有其的循环器官用途的药物组合物
公开(公告)号：US5728835A
公开(公告)日：1998-03-17
申请号：US575062
申请日：1995-12-19
申请人： Tsuyoshi Aoki , Atsuo Takahashi , Hiroyasu Sato , Eiji Shimanuki , Kaoru Gengyou , Toyoki Nishimata , Sachiko Ishigami , Shin-ichi Yamada , Takahiro Yamaguchi , Yoichi Manome , Isamu Sato , Kentaro Kogi , Sen-ichi Narita
发明人： Tsuyoshi Aoki , Atsuo Takahashi , Hiroyasu Sato , Eiji Shimanuki , Kaoru Gengyou , Toyoki Nishimata , Sachiko Ishigami , Shin-ichi Yamada , Takahiro Yamaguchi , Yoichi Manome , Isamu Sato , Kentaro Kogi , Sen-ichi Narita
IPC分类号： A61K31/445 , C07D211/32
CPC分类号： A61K31/445 , C07D211/32
摘要： A substituted cyclic amine compound represented by the following general formula (1) ##STR1## wherein each of R.sup.1 to R.sup.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or .dbd.N(.fwdarw.O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.
摘要翻译：由下列通式（1）表示的取代环胺化合物其中R 1至R 5各自表示氢原子，卤素原子，低级烷基，低级烷氧基等，A表示羰基或磺酰基，B表示次甲基部分或氮原子，D表示次甲基部分，氮原子或= N（ - O） - ，n为2〜3的整数。及其合成方法。本发明化合物可用于预防和治疗诸如高血压，缺血性心脏病，脑血管病，外周血循环疾病等循环器官相关疾病。

8. 发明授权

US5149702A Cycloheptenopyridine derivatives, process for preparation thereof and antiulcer agents containing the same 失效
标题翻译：环庚烯并吡啶衍生物，其制备方法和含有它们的抗溃疡剂
公开(公告)号：US5149702A
公开(公告)日：1992-09-22
申请号：US618943
申请日：1990-11-27
申请人： Shin-ichi Yamada , Takao Goto , Rie Yorita , Eizi Shimanuki , Takaji Yamaguchi , Kentaro Kogi , Senichi Narita
发明人： Shin-ichi Yamada , Takao Goto , Rie Yorita , Eizi Shimanuki , Takaji Yamaguchi , Kentaro Kogi , Senichi Narita
IPC分类号： C07D401/12 , C07D471/04
CPC分类号： C07D401/12 , C07D471/04 , Y02P20/55 , Y10S514/926 , Y10S514/927
摘要： Provided are cycloheptenopyridine derivatives represented by the general formula ##STR1## [wherein R represents a hydrogen atom or lower alkyl group; R.sup.1 represents a hydrogen atom, halogen atom, lower cycloalkoxy group, amido group, substituted phenoxy group, substituted benzyloxy group, lower alkoxy group optionally containing halogen atoms(s), nitro group, hydroxyl group, lower alkenyloxy group, lower alkylthio group, or a group--NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or lower alkyl group, or R.sup.4 and R.sup.5 mutually combine together with the nitrogen atom adjacent thereto to form a 5- or 6-membered heterocyclic group); R.sup.2 represents a hydrogen atom, halogen atom, lower alkyl group optionally containing a halogen atom, lower alkoxy group optionally containing a halogen atom, hydroxyl group, acyl group, lower alkoxycarbonyl group, nitro group or amino group; R.sup.3 represents a hydrogen atom, a lower alkyl group, lower alkoxymethyl group, lower alkylcarbonyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkylcarbamoyl group, lower alkylcarbonylmethyl group, lower alkoxycarbonyl group, lower acyloxymethyl group, lower alkylsulfonyl group, or physiologically acceptable protective group eliminatable in an acid medium or under a physiological condition; n represents 0 or 1; and A represents a methine carbon or nitrogen atom] or their salts. These derivatives and their salts are useful as antiulcer agents.
摘要翻译：提供由通式[IMAGE] [I]表示的环庚烯并吡啶衍生物[其中R表示氢原子或低级烷基; R1表示氢原子，卤素原子，低级环烷氧基，酰胺基，取代苯氧基，取代的苄氧基，任选含有卤原子的低级烷氧基，硝基，羟基，低级链烯氧基，低级烷硫基，或基团-NR 4 R 5（其中R 4和R 5可以相同或不同，各自表示氢原子或低级烷基，或者R 4和R 5与与其相邻的氮原子相互结合形成5-或6-元杂环基）; R2表示氢原子，卤素原子，任选含有卤原子的低级烷基，任选含有卤素原子的低级烷氧基，羟基，酰基，低级烷氧基羰基，硝基或氨基; R3表示氢原子，低级烷基，低级烷氧基甲基，低级烷基羰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基羰基甲基，低级烷氧基羰基，低级酰氧基甲基，低级烷基磺酰基或生理上可接受的保护性组在酸性培养基中或在生理条件下可消除; n表示0或1; A表示次甲基碳或氮原子]或其盐。这些衍生物及其盐可用作抗溃疡剂。

9. 发明授权

US4837342A Prostacyclin analogue, and blood circulation improving agent and anti-ulcer composition containing it as active ingredient 失效
公开(公告)号：US4837342A
公开(公告)日：1989-06-06
申请号：US14591
申请日：1987-02-13
申请人： Masakatsu Shibasaki , Atsuo Takahashi , Tuyoshi Aoki , Kentaro Kogi , Yozo Nishimiya , Takeshi Nara , Takashi Yamaguchi
发明人： Masakatsu Shibasaki , Atsuo Takahashi , Tuyoshi Aoki , Kentaro Kogi , Yozo Nishimiya , Takeshi Nara , Takashi Yamaguchi
IPC分类号： C07C405/00
CPC分类号： C07C405/0083
摘要： A prostacyclin analogue having the formula: ##STR1## wherein R.sup.1 is --CO.sub.2 R.sup.5 (wherein R.sup.5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or --CONR.sup.6 R.sup.7 (wherein each of R.sup.6 and R.sup.7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom, form a 5- or 6-membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 --O--CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --O--CH.sub.2 -- or --CH.dbd.CHCH.sub.2 CH.sub. 2 --; B is trans --CH.dbd.CH-- or --C.tbd.C--; R.sup.2 is a straight chain or branched alkyl group having from 3 to 10 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a straight chain or branched alkenyl group having from 3 to 12 carbon atoms, a straight chain or branched alkynyl group having from 3 to 8 carbon atoms, or an alkyl group having from 1 to 3 carbon atoms substituted by a substituted or unsubstituted phenyl or phenoxy group, by an alkoxy group having from 1 to 6 carbon atoms or by a cycloalkyl group having from 5 to 8 carbon atoms; R.sup.3 is a hydrogen atom, a methyl group or a vinyl group; and R.sup.4 is a hydrogen atom, an acyl group having from 1 to 7 carbon atoms, a tri-C.sub.1 -C.sub.7 hydrocarbon-silyl group or a group capable of forming an acetal bond together with the oxygen atom of a hydroxyl group; provided that the double bond in a substituent for A is E or Z, or a mixture thereof; the asymmetric center in a substituent for R.sup.2 assumes a R-conformation or a S-conformation, or a mixture thereof; and the bonds shown by dotted lines at the 2-3 and 3-4 positions mean that either one of them is a double bond.

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