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1. 发明授权

US4383996A Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it 失效
标题翻译：噻唑并[3,2-a]嘧啶的衍生物及其制备方法和含有它的药物
公开(公告)号：US4383996A
公开(公告)日：1983-05-17
申请号：US339460
申请日：1981-12-28
申请人： Takeo Oba , Kiyoshi Bannai , Toshio Tanaka , Kenzo Watanabe , Tatsuyuki Naruchi , Keiji Komoriya , Seizi Kurozumi , Kenji Hoshina
发明人： Takeo Oba , Kiyoshi Bannai , Toshio Tanaka , Kenzo Watanabe , Tatsuyuki Naruchi , Keiji Komoriya , Seizi Kurozumi , Kenji Hoshina
IPC分类号： C07D513/04 , A61K31/505
CPC分类号： C07D513/04 , Y10S514/825 , Y10S514/885
摘要： A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.
摘要翻译： PCT No.PCT / JP80 / 00090 Sec。 371日期：1981年12月28日 102（e）日期1981年12月28日PCT提交1980年4月28日PCT公布。公开号WO81 / 03174 1981年11月12日，由式（I）表示的噻唑并[3,2-a]嘧啶衍生物（I）（其中R表示苯基或具有卤素原子的苄基，较低烷基或低级烷氧基作为取代基，脂环基或芳乙基），以及制备式（I）化合物的方法，其包括使式（II）表示的化合物通过加热（II）（其中R的定义与式（I）的情况相同，R'表示卤素原子或低级烷氧基）。含有该化合物作为活性成分的药物可用于治疗自身免疫性疾病如类风湿性关节炎，肾炎等。

2. 发明授权

US4421914A Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效
公开(公告)号：US4421914A
公开(公告)日：1983-12-20
申请号：US311329
申请日：1981-10-14
申请人： Noriaki Okamura , Takeshi Toru , Takeo Oba , Toshio Tanaka , Kiyoshi Bannai , Kenzo Watanabe , Seizi Kurozumi , Tatsuyuki Naruchi , Keiji Komoriya
发明人： Noriaki Okamura , Takeshi Toru , Takeo Oba , Toshio Tanaka , Kiyoshi Bannai , Kenzo Watanabe , Seizi Kurozumi , Tatsuyuki Naruchi , Keiji Komoriya
IPC分类号： C07D513/04 , C07D513/14 , A61K31/505
CPC分类号： C07D513/04
摘要： A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.The thiazolo[3,2-a]pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined with regard to formula (I), and R.sup.4 and R.sup.5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms,with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or (b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid; and if desired, reacting the reaction product of (a) or (b) with an acid.The present invention provides also several processes for preparing enolate derivatives thereof.The thiazolo[3,2-a]pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.

3. 发明授权

US4472428A Halogenated prostacyclins pharmaceutical use thereof and hydroxy intermediates therefore 失效
标题翻译：因此，其卤化前列环素及其羟基中间体
公开(公告)号：US4472428A
公开(公告)日：1984-09-18
申请号：US327741
申请日：1981-12-04
申请人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
发明人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
IPC分类号： C07D307/937 , A61K31/557 , C07D307/935
CPC分类号： C07D307/937
摘要： Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.
摘要翻译： 5-或7-单卤代或5,7-二卤代6-PGI1和5-或7-单卤代或二卤代PGI2（5-单氟化PGI2除外）。新型卤代前列环素可用于控制血管作用，还可用于器官移植，体外循环等。本发明还提供了制备新型卤代前列环素的方法。

4. 发明授权

US4402975A Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical uses thereof 失效
公开(公告)号：US4402975A
公开(公告)日：1983-09-06
申请号：US284562
申请日：1981-07-17
申请人： Toru Takeshita , Kenji Hoshina , Akira Ohtsu , Tatsuyuki Naruchi
发明人： Toru Takeshita , Kenji Hoshina , Akira Ohtsu , Tatsuyuki Naruchi
IPC分类号： A61K31/135 , A61K31/195 , A61K31/24 , C07D295/18 , C07C101/34
CPC分类号： C07C229/34 , A61K31/135 , C07C225/18 , C07C233/51 , C07C2101/14 , Y10S514/927 , Y10S514/928
摘要： A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.2 represents an alkylene group having 1 to 5 carbon atoms which may be substituted by an alkyl group having 1 to 6 carbon atoms or an amino group; and R.sup.4 represents the group --COOR.sup.5, --CH.sub.2 OR.sup.6 or --CONR.sup.7 R.sup.8 in which R.sup.5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R.sup.6 represents a hydrogen atom or an acyl group having 1 to 6 carbon atoms, and R.sup.7 and R are identical or different and represent a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or taken together may form a 5- or 6-membered ring; or an acid addition salts of said compound wherein R.sup.1 represents a hydrogen atom or X.sup.2 represents an alkylene group having an amino group, or salts of said compound wherein R.sup.5 represents a hydrogen atom.The compounds represented by the above formula or their pharmaceutically acceptable salts are useful as anti-ulcer agents.The present invention also provides a process for producing the compounds or their pharmaceutically acceptable salts, which comprises acylating a protected derivative at the amino group of a corresponding acid halide with a corresponding substituted benzene in the presence of a Lewis acid; or reducing a corresponding compound in the presence of an inert solvent under conditions which induce reduction of the carbonyl group of said corresponding compound without substantially reducing the phenylene group of said corresponding compound; or dehydrating a corresponding compound.

5. 发明授权

US5229422A Extemporaneous preparation type kit of a pharmaceutical substance-containing fat emulsion 失效
标题翻译：含药物脂肪乳剂的临时制剂型试剂盒
公开(公告)号：US5229422A
公开(公告)日：1993-07-20
申请号：US715018
申请日：1991-06-13
申请人： Ken Takahashi , Yuji Makino , Yoshiki Suzuki , Tatsuyuki Naruchi
发明人： Ken Takahashi , Yuji Makino , Yoshiki Suzuki , Tatsuyuki Naruchi
IPC分类号： A61K9/107
CPC分类号： A61K9/1075 , Y10S514/943
摘要： An extemporaneous kit of pharmaceutical substance-containing fat emulsion which consists of a fat emulsion and (a) a pharmaceutical substance composition containing pharmaceutical substance and at least one solvent selected from the group consisting of water, liquid polyalkylene glycols, liquid alkylethanolamines, and liquid polyhydric alcohols, or (b) a pharmaceutical substance composition containing pharmaceutical substance and saccharides and/or 30 amino acids as an excipient, and a process for preparation of a pharmaceutical substance-containing fat emulsion therefrom.
摘要翻译： PCT No.PCT / JP88 / 00889 Sec。 371日期：1989年5月4日 102（e）日期1989年5月4日PCT提交1988年9月5日PCT公布。出版物WO89 / 02265 日期：1989年3月23日。一种含药物脂肪乳剂的临时试剂盒，由脂肪乳液和（a）含有药物和至少一种选自水，液体聚亚烷基二醇的溶剂的药物组合物组成，液体烷基乙醇胺和液体多元醇，或（b）含有药物和糖类和/或30个氨基酸作为赋形剂的药物组合物及其制备含药物的脂肪乳剂的方法。

6. 发明授权

US4364941A Method for regulating bone metabolism of warm-blooded animals, and pharmaceutical compositions thereof 失效
标题翻译：调节温血动物骨代谢的方法及其药物组合物
公开(公告)号：US4364941A
公开(公告)日：1982-12-21
申请号：US297975
申请日：1981-08-31
申请人： Mamoru Kiyoki , Hiroyoshi Endo , Tatsuyuki Naruchi , Yoshinobu Hashimoto
发明人： Mamoru Kiyoki , Hiroyoshi Endo , Tatsuyuki Naruchi , Yoshinobu Hashimoto
IPC分类号： A61K31/59 , A61P3/00 , A61P3/02
CPC分类号： A61K31/59
摘要： A method for regulating the bone metabolism of a warm-blooded animal, which comprises administering pharmaceutically effective amounts of 1.alpha., 24-dihydroxycholecalciferol (1.alpha., 24-DHCC) and 24,25-dihydroxycholecalciferol (24,25-DHCC) to said warm-blooded animal, and a pharmaceutical composition comprising 1.alpha.,24-DHCC, 24,25-DHCC and a pharmaceutically acceptable carrier.According to the invention, a condition of abnormal bone metabolism requiring long-term therapy, such as osteoporosis, can be safely treated by administering 1.alpha., 24-DHCC and 24,25-DHCC over a long period of time because no substantial adverse effect of 1.alpha., 24-DHCC on the metabolis of 24,25-DHCC is observed.
摘要翻译：一种用于调节温血动物的骨代谢的方法，其包括将药学有效量的1α，24-二羟基胆钙化甾醇（1α，24-DHCC）和24,25-二羟基胆钙化甾醇（24,25-DHCC）施用于所述温血动物，以及包含1α，24-DHCC，24,25-DHCC和药学上可接受的载体的药物组合物。根据本发明，通过长期施用1α，24-DHCC和24,25-DHCC可以安全地治疗需要长期治疗的骨质疏松症如骨质疏松症的病症，因为没有实质的不利影响的1α，24-DHCC对24,25-DHCC的代谢。

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