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1. 发明授权

US5472967A 4-pyrimidinone derivatives their preparation and their application in therapy 失效
标题翻译： 4-嘧啶酮衍生物的制备及其在治疗中的应用
公开(公告)号：US5472967A
公开(公告)日：1995-12-05
申请号：US294023
申请日：1994-08-24
申请人： Christian Hoornaert , Marc Daumas , Michel Aletru , Jean-Claude Muller
发明人： Christian Hoornaert , Marc Daumas , Michel Aletru , Jean-Claude Muller
IPC分类号： C07D239/36 , C07D239/52 , C07D403/10 , A61K31/505
CPC分类号： C07D239/36 , C07D239/52 , C07D403/10
摘要： Compounds which can be expressed as tautomeric forms and having the formulas (I), (I') and (I") ##STR1## wherein R.sub.1 =a straight or branched (C.sub.1-7) alkyl group or a straight or branched (C.sub.3-9) alkenyl group or a cyclo(C.sub.3-7)alkyl(C.sub.1-6) alkyl group, R.sub.2 =an atom of hydrogen, or a straight or branched (C.sub.1-7)alkyl group, or a cyclo(C.sub.3-7)alkyl(C.sub.1-3)alkyl group, or an aryl(C.sub.1-3)alkyl group optionally substituted on the ring, or an aryloxy(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylthio(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylsulfonyl(C.sub.1-3)alkyl group optionally substituted on the ring, or a heteroaryl(C.sub.1-3)alkyl group optionally substituted on the ring, R.sub.3 =CO.sub.2 H, 1H-tetrazol-5-yl, NHCOR.sub.11, NHSO.sub.2 R.sub.11, CONHSO.sub.2 R.sub.11 or CONHOR.sub.12 group where R.sub.11 =a methyl, trifluoromethyl, or phenyl group optionally substituted, R.sub.12 =a hydrogen atom, or a methyl or a phenyl group optionally substituted. The compounds are useful for antagonizing angiotensin II.
摘要翻译：可以表示为互变异构形式并具有式（I），（I'）和（I“）的化合物其中R 1 =直链或支链（C 1-7）烷基基团或直链或支链（C3-9）烯基或环（C3-7）烷基（C1-6）烷基，R2 =氢原子或直链或支链（C1-7）烷基，或环（C 3-7）烷基（C 1-3）烷基或任选在环上取代的芳基（C 1-3）烷基或任意在环上取代的芳氧基（C 1-3）烷基，或或环上任选取代的芳基磺酰基（C 1-3）烷基或环上任选取代的杂芳基（C 1-3）烷基，R 3 = CO 2 H ，1H-四唑-5-基，NHCOR 11，NHSO 2 R 11，CONHSO 2 R 11或CONHOR 12基团，其中R 11 =任选取代的甲基，三氟甲基或苯基，R 12 =氢原子或任选取代的甲基或苯基。该化合物可用于拮抗血管紧张素II。

2. 发明授权

US5447928A Benzoxazine derivatives and their application in therapy 失效
标题翻译：苯并恶嗪衍生物及其在治疗中的应用
公开(公告)号：US5447928A
公开(公告)日：1995-09-05
申请号：US201233
申请日：1994-02-24
申请人： Howard Williams , Lydia Zard , Thomas Purcell , Daniel Galtier , Jean-Claude Muller , Pascal George , Jonathan Frost , Patrick Pasau , Corinne Rousselle , Regine Bartsch
发明人： Howard Williams , Lydia Zard , Thomas Purcell , Daniel Galtier , Jean-Claude Muller , Pascal George , Jonathan Frost , Patrick Pasau , Corinne Rousselle , Regine Bartsch
IPC分类号： A61K31/535 , A61K31/538 , A61P9/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P35/00 , C07D265/36 , C07D413/06 , C07D413/12 , C07D413/14
CPC分类号： C07D413/06 , C07D265/36 , C07D413/12 , C07D413/14
摘要： Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.
摘要翻译：其中Y表示氢，氟，甲基或甲氧基的式（I）化合物，R 1表示被氟，甲基，甲氧基，三氟甲基或苯基取代的苯基，或R 1表示2-噻吩基，R 2表示甲基，或R 3表示（C 1 -C 4） - 烷基或在环上任选被2至3个甲氧基取代的苯基 - （C 1 -C 2） - 烷基或2-（2-吡啶基）乙基或R 2和R 3形式，相邻的氮，4-苯基（1-哌啶基），4-苯基甲基（1-哌啶基），1,2,3,4-四氢-2-异喹啉，6-甲氧基-1,2,3,4-四氢 - 2-异喹啉基，5,8-二甲氧基-1,2,3,4-四氢-2-异喹啉，6,7-二甲氧基-1,2,3,4-四氢-2-异喹啉，2,3,4,5 - 四氢-1H-3-苯并吖庚因-3-基或7,8-二甲氧基-2,3,4,5-四氢-1H-3-苯并吖庚因-3-基，X代表羰基或磺酰基，及其盐作为神经保护和抗感染药物是有用的。

3. 发明授权

US5432283A Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US5432283A
公开(公告)日：1995-07-11
申请号：US295469
申请日：1994-08-25
申请人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
发明人： Gerard Cremer , Pascale Goberville , Jean-Claude Muller
IPC分类号： C07D215/12 , C07D401/14 , C07D403/10 , C07D215/16
CPC分类号： C07D401/14 , C07D215/12
摘要： The present invention provides a compound which is a quinoline derivative of the formula (I) ##STR1## in which R.sub.1 represents either 1H-tetrazol-5-yl, or CO.sub.2 H,R.sub.2 represents either (C.sub.1-7)alkyl or (C.sub.2-6)alkenyl,R.sub.3 and R.sub.4 represent, independently of each other, hydrogen, halogen, cyano group, (C.sub.1-7)alkyl, (C.sub.3-7)cycloalkyl(C.sub.1-4)alkyl, aryl, aryl(C.sub.1-4)alkyl, aryl(C.sub.2-6)alkenyl, --(CH.sub.2).sub.m --COR.sub.5 in which m=0 to 4 and R.sub.5 represents hydrogen, --OH, --(C.sub.1-6)alkoxy, or --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 representing, independently of each other, hydrogen or --(C.sub.1-4)alkyl group, or a --(CH.sub.2).sub.n --R.sub.6 group in which n=1 to 4 and R.sub.6 represents --OH, --(C.sub.1-6)alkoxy, --(C.sub.1-4)alkoxy(C.sub.1-4)alkoxy, or (C.sub.3-7)cycloalkyl(C.sub.1-4)alkoxy group, or a pharmaceutically acceptable salt thereof and their therapeutic applications.
摘要翻译：本发明提供一种化合物，其为式（I）的喹啉衍生物，其中R 1表示1H-四唑-5-基或CO 2 H，R 2表示（C 1-7）烷基或（ C2-6）烯基，R3和R4彼此独立地表示氢，卤素，氰基，（C1-7）烷基，（C3-7）环烷基（C1-4）烷基，芳基，芳基（C1-4 ）烷基，芳基（C2-6）烯基， - （CH2）m-COR5，其中m = 0至4，R5表示氢，-OH， - （C1-6）烷氧基或-NR7R8，R7和R8表示，氢或 - （C1-4）烷基或其中n = 1-4的R6为R6，R6为-OH的 - （CH2）n-R6基， - （C1-6）烷氧基， - （C1 -4）烷氧基（C 1-4）烷氧基或（C 3-7）环烷基（C 1-4）烷氧基或其药学上可接受的盐及其治疗应用。

4. 发明授权

US5001159A N-aminobutyl-n-phenylarylamide compounds and their application in therapy 失效
标题翻译： N-氨基丁基 - 正苯基芳酰胺化合物及其在治疗中的应用
公开(公告)号：US5001159A
公开(公告)日：1991-03-19
申请号：US517419
申请日：1990-05-02
申请人： Christian Hoornaert , Jean-Claude Muller , Nigel Beeley
发明人： Christian Hoornaert , Jean-Claude Muller , Nigel Beeley
IPC分类号： A61K31/165 , A61K31/357 , A61K31/36 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P1/04 , A61P9/00 , A61P11/08 , A61P25/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/08 , C07C231/12 , C07C233/88 , C07C235/68 , C07D211/14 , C07D213/38 , C07D213/74 , C07D213/82 , C07D215/50 , C07D217/04 , C07D217/26 , C07D295/12 , C07D295/13 , C07D317/58
CPC分类号： C07D213/74 , C07D211/14 , C07D213/82 , C07D215/50 , C07D217/04 , C07D217/26 , C07D295/13
摘要： A compound of formula (I) ##STR1## in which: X denotes hydrogen, a halogen, a trifluoromethyl group, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group;R.sub.1 denotes a linear or branched C.sub.2 -C.sub.8 alkyl group, a C.sub.3 -C.sub.5 cycloalkyl group or a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 5 carbon atoms;R.sub.2 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl group;R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group, an optionally substituted phenylalkyl group or a pyridylalkyl group;or R.sub.2 and R.sub.3 denote, together with the nitrogen to which they are attached, a pyrrolidinyl, piperidyl, morpholinyl, perhydrothiazinyl, piperazinyl or 4-methylpiperazinyl ring; andAr denotes a phenyl group, optionally having from one to three substituents, each of which is, independently, a halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, nitro or cyano group, or Ar denotes a naphthyl, pyridyl, quinolinyl or isoquinolinyl group;or a pharmacologically acceptable acid addition salt thereof.
摘要翻译：式（I）化合物其中：X表示氢，卤素，三氟甲基，C 1 -C 4烷基或C 1 -C 4烷氧基; R1表示环烷基部分具有3至5个碳原子的直链或支链C 2 -C 8烷基，C 3 -C 5环烷基或环烷基甲基; R2表示氢或C1-C4烷基; R3表示氢，C1-C4烷基，任选取代的苯基烷基或吡啶基烷基; 或R 2和R 3与它们所连接的氮一起表示吡咯烷基，哌啶基，吗啉基，全氢噻嗪基，哌嗪基或4-甲基哌嗪基; 并且Ar表示任选具有一至三个取代基的苯基，其各自独立地为卤素或C 1 -C 4烷基，C 1 -C 4烷氧基，三氟甲基，硝基或氰基，或Ar表示萘基，吡啶基，喹啉基或异喹啉基; 或其药理学上可接受的酸加成盐。

5. 发明授权

US4256886A Process for the preparation of oxadiazolopyrimidine derivatives 失效
标题翻译：制备恶二唑并嘧啶衍生物的方法
公开(公告)号：US4256886A
公开(公告)日：1981-03-17
申请号：US123145
申请日：1980-02-21
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： A61K31/505 , A61P9/08 , A61P9/12 , C07D239/48 , C07D401/04 , C07D498/04
CPC分类号： C07D239/48 , Y10S514/929
摘要： A process for preparing oxadiazolopyrimidines of the formula ##STR1## wherein R is alkyl or alkoxyalkyl, by reacting a compound of the formula ##STR2## wherein R is as set forth above, with phosgene, is described.
摘要翻译：其中R是烷基或烷氧基烷基，通过将其中R如上所述的式Ⅺ化合物与光气反应，制备式ⅩⅧ的恶二唑并嘧啶的方法。

6. 发明授权

US4220772A Process for the preparation of oxadiazolopyrimidine derivatives 失效
标题翻译：制备恶二唑并嘧啶衍生物的方法
公开(公告)号：US4220772A
公开(公告)日：1980-09-02
申请号：US55230
申请日：1979-07-06
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： A61K31/505 , A61P9/08 , A61P9/12 , C07D239/48 , C07D401/04 , C07D498/04
CPC分类号： C07D239/48 , Y10S514/929
摘要： A process for preparing oxadiazolopyrimidines of the formula ##STR1## wherein R is alkyl or alkoxyalkyl, by reacting a compound of the formula ##STR2## wherein R is as set forth above, with phosgene, is described.
摘要翻译：其中R是烷基或烷氧基烷基，通过使其中R如上所述的式Ⅺ化合物与光气反应，制备式ⅩⅧ的恶二唑并嘧啶的方法。

7. 发明授权

US4150131A Substituted oxadiazolopyrimidines 失效
标题翻译：取代的恶二唑并嘧啶
公开(公告)号：US4150131A
公开(公告)日：1979-04-17
申请号：US873183
申请日：1978-01-27
申请人： Jean-Claude Muller , Henri Ramuz
发明人： Jean-Claude Muller , Henri Ramuz
IPC分类号： A61K31/505 , A61P9/08 , A61P9/12 , C07D498/04 , C07D498/22
CPC分类号： C07D498/04
摘要： Oxadiazolopyrimidine derivatives of the formula ##STR1## wherein R and R.sub.1 are as hereinafter described, prepared, inter alia, by cyclizing a compound of the formula ##STR2## wherein R and R.sub.1 are as hereinafter described. The end products are useful in the treatment of vascular-conditioned hypertension or as vasodilators in the case of peripheral blood supply disorders.
摘要翻译：其中R和R 1如下文所述，其中R 1和R 2如下文所述，其中R 1和R 1如下文所述，其中R 1和R 2如下文所述，通过使下式化合物环化来制备。

8. 发明授权

US4119540A Counter-current automatic cleaning filter 失效
标题翻译：逆流自动清洗过滤器
公开(公告)号：US4119540A
公开(公告)日：1978-10-10
申请号：US859182
申请日：1977-12-09
申请人： Jean-Claude Muller
发明人： Jean-Claude Muller
IPC分类号： B01D46/24 , B01D29/11 , B01D29/46 , B01D29/62 , B01D29/66 , B01D29/38
CPC分类号： B01D29/117 , B01D2201/0438 , B01D2201/287
摘要： The filter has a filtering chamber in which a number of hollow filtering elements are arranged on a circle about the axis of the filter. The chamber has a liquid inlet and a liquid outlet and the hollow filtering elements communicate in parallel with the inlet and outlet. A hollow arm defining a passageway is rotatable about the axis of the filter and the passageway is capable of putting all the inlets of the filtering elements successively in communication with an impurities discharging chamber in which prevails a pressure lower than the pressure of the filtered liquid. The arm is connected to rotate with the driven member of a unidirectional step-by-step drive mechanism. The arm is also connected to rotate with the driven member of a second unidirectional step-by-step drive mechanism in the same direction as with the first drive mechanism.
摘要翻译：过滤器具有过滤室，其中多个中空过滤元件围绕过滤器的轴线布置在圆周上。腔室具有液体入口和液体出口，并且中空过滤元件与入口和出口平行地连通。限定通道的空心臂可围绕过滤器的轴线旋转，并且通道能够将过滤元件的所有入口连续地与杂质排出室连通，其中压力低于过滤液体的压力。臂与单向逐步驱动机构的从动构件连接以旋转。臂也被连接成与第二单向逐步驱动机构的从动构件沿与第一驱动机构相同的方向旋转。

9. 发明授权

US4045213A Method of injecting a powder containing carbon into a metal bath 失效
标题翻译：将含有碳的粉末注入金属浴中的方法
公开(公告)号：US4045213A
公开(公告)日：1977-08-30
申请号：US762944
申请日：1977-01-27
申请人： Pierre Leroy , Jean Bastien , Jean-Claude Muller , Roger Kieger
发明人： Pierre Leroy , Jean Bastien , Jean-Claude Muller , Roger Kieger
IPC分类号： C21C5/34 , C21C7/00 , C21C7/06
CPC分类号： C21C7/06 , C21C5/34 , C21C7/0025
摘要： In a method of deoxidizing and/or carburizing a metal, particularly steel, bath using an immersed nozzle consisting of two concentric tubes, the central tube of the nozzle is fed with an oxidizing gas during the or each oxidation phase, then with a scavenging gas, then with a neutral gas carrying carbon powder or powder containing carbon during the or each deoxidation or carburization phase and finally with a scavenging gas, the outer tube of the nozzle being fed with a protective fluid or different protective fluids during both the oxidation and deoxidation or carburization phases.
摘要翻译：在使用由两个同心管组成的浸渍喷嘴的金属，特别是钢，浴的脱氧和/或渗碳的方法中，在该氧化阶段或每个氧化阶段期间，喷嘴的中心管被供给氧化气体，然后用清除气体然后在该脱氧或渗碳阶段期间用中性气体携带碳粉或含有碳的粉末，最后用清除气体，在氧化和脱氧过程中，喷嘴的外管被供给保护流体或不同的保护流体或渗碳阶段。

10. 发明授权

US5457112A 3-(6-quinolylmethyl)-4H-imidazol-4-one derivatives, their preparation and their application in therapy 失效
标题翻译： 3-（6-喹啉基甲基）-4H-咪唑-4-酮衍生物，其制备及其在治疗中的应用
公开(公告)号：US5457112A
公开(公告)日：1995-10-10
申请号：US165648
申请日：1993-12-13
申请人： Gerard Cremer , Jean Claude Muller
发明人： Gerard Cremer , Jean Claude Muller
IPC分类号： C07D401/14 , C07D215/04 , A61K31/47
CPC分类号： C07D401/14
摘要： 3-(6-Quinolylmethyl)-4H-imidazol-4-one derivatives corresponding to the formula (I): ##STR1## in which R.sub.1 represents an unbranched or branched (C.sub.2 -C.sub.5) alkyl group,R.sub.2 and R.sub.3 represent, each independently of one another, either a hydrogen atom, or an unbranched or branched (C.sub.1 -C.sub.5)alkyl group, or a (CH.sub.2).sub.n -aryl group where n=0 to 3, or R.sub.2 and R.sub.3 with the imidazole ring can form a spirocyclo(C.sub.3 -C.sub.8)alkyl group,as well as their addition salts with pharmaceutically acceptable acids and bases.
摘要翻译：对应于式（I）的3-（6-喹啉基甲基）-4H-咪唑-4-酮衍生物：其中R 1表示无支链或支链（C2-C5）烷基，R2和R3表示（C 1 -C 5）烷基或其中n = 0至3的（CH 2）n - 芳基或具有咪唑环的R 2和R 3可彼此独立地为氢原子，形成螺环（C 3 -C 8）烷基，以及它们与药学上可接受的酸和碱的加成盐。

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