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1. 发明申请

WO1981001285A1 SUBSTITUTED CARBOXYLIC CETO-ACIDS,PROCESS FOR THE PREPARATION THEREOF,USE THEREOF AND MEDICINAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：取代的羧甲基纤维素，其制备方法，其用途及含有它们的药物组合物
公开(公告)号：WO1981001285A1
公开(公告)日：1981-05-14
申请号：PCT/EP1980000123
申请日：1980-10-31
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , KRAAS E , WOLF H
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH , LUDWIG G , RAPP E
IPC分类号： C07C51/09
CPC分类号： C07F3/08 , C07C29/36 , C07C59/84 , C07C59/88 , C07C59/90 , C07F3/02 , Y10S514/866 , C07C33/46
摘要： Substituted carboxylic ceto-acids having the formula I (FORMULA) wherein R1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl, lower alkyloxy or trifluoromethyl residue. R2 represents a hydrogen or halogen atom and n represents an integer from 3 to 8. These acids, as well as the salts thereof exhibit an hypoglycemic activity when applied to living homeothermic organisms. Preparation processes for these new compounds and intermediate compounds of the synthesis thereof are described. A preparation of medicinal compositions containing such acids or the salt thereof is also referred to.
摘要翻译： PCT No.PCT / EP80 / 00123 Sec。 371日期1981年6月29日第 102（e）日期1981年6月29日PCT提交1980年10月31日PCT公布。出版物WO81 / 01285 日期：1981年5月14日。式I的取代的氧代羧酸（I）其中R1表示氢原子，卤素原子，羟基，低级烷基，低级烷氧基或三氟甲基，R2表示氢原子或卤素原子，n表示3〜8的整数，它们的盐在温血动物中显示低血糖作用。描述了制备新化合物及其制备所需的中间产物以及相应药物的方法。

2. 发明申请

WO1979000586A1 W-(2-N-LOWER ALKYL-BENZAMIDO)-PHENYL)-ALKANOIC ACIDS,THEIR USE AND PREPARATION,AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译： W-（2-N-低级烷基 - 苯甲酰） - 苯基） - 甘草酸，其使用和制备，以及含有它们的药物
公开(公告)号：WO1979000586A1
公开(公告)日：1979-08-23
申请号：PCT/EP1979000006
申请日：1979-02-02
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , KRUEGER U , WOLF H , KLEMM K , KRAAS E , RAPP E
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH
IPC分类号： C07C103/84
CPC分类号： C07D215/227 , C07D223/16
摘要： //c-[-2-(N-lower alkyl-benzamido)-phenyl]-alkanoic acids of the general formula I: (FORMULA) wherein n denotes a positive whole number from 2 to 5, R s denotes a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylmercapto group, a trifluoromethyl group or a phenyl group which may be substituted by a halogen atom or a lower alkoxy group, R s denotes a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, R s denotes a lower alkyl group, R s denotes a hydrogen atom, a halogen atom, a hydroxy group, a lower alkyl group, a lower alkoxy group, a lower alkylmercapto group, a phenyl group which may be substituted by a halogen atom or a nitro group, a nitro group, an amino group which may be lower alkylated, a lower alkylcarbonyl group, a benzoyl group which may be substituted by a halogen atom, a trifluoromethyl group, a trifluoromethoxy group or a trifluoromethylmercapto group, R s denotes a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, R s denotes a hydrogen atom, a lower alkyl group or a lower alkoxy group, and their salts with inorganic or organic bases, are new compounds. They have a hypoglycaemic effect and inhibit the glucose formation in the liver. Processes for their preparation are stated.
摘要翻译：具有通式I的C 2- [N-（N-低级烷基 - 苯甲酰氨基） - 苯基] - 链烷酸：其中n表示2至5的正整数，R 1表示氢原子，卤素原子，低级烷基，低级烷氧基，低级烷基巯基，三氟甲基或可被卤素原子或低级烷氧基取代的苯基，R 2表示氢原子，卤素原子，低级烷基或低级烷氧基，R 3表示低级烷基，R 4表示氢原子，卤素原子，羟基，低级烷基低级烷氧基，低级烷基巯基，可以被卤素原子或硝基取代的苯基，硝基，可以低级烷基化的氨基，低级烷基羰基，苯甲酰基，可以是被卤素原子，三氟甲基，三氟甲氧基或三氟甲基巯基取代，R 5表示氢原子，卤素原子 m，低级烷基或低级烷氧基，R 6表示氢原子，低级烷基或低级烷氧基，它们与无机或有机碱的盐是新的化合物。它们具有低血糖作用并抑制肝脏中的葡萄糖形成。说明了其准备过程。

3. 发明申请

WO1981000564A1 SUBSTITUTED QUINOLINONE-ALKANECARBOXYLIC ACIDS,THEIR PREPARATION AND USE,AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译：取代的喹啉酮 - 碱性羧酸，其制备和使用以及含有它们的药物
公开(公告)号：WO1981000564A1
公开(公告)日：1981-03-05
申请号：PCT/EP1980000086
申请日：1980-08-29
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , EISTETTER K , WOLF H , RAPP E
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH , KRAAS E , LUDWIG G , MIKLOVICH M
IPC分类号： C07D215/22
CPC分类号： C07D215/227 , C07D215/38
摘要： Quinolinone-alkanecarboxylic acids of the formula I (FORMULA) wherein R1, R2 and R3 are identical or different and denote a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group with 1 to 4 carbon atoms, an amino group, a dialkylamino group, the alkyl radicals having 1 to 4 carbon atoms, or a nitro group, R4 and R5 are identical or different and denote a hydrogen atom, a halogen atom, an alkoxy group with 1 to 4 carbon atoms, a hydroxyl group, an amino group or a dialkylamino group, the alkyl radicals having 1 to 4 carbon atoms, or R4 and R5 together denote a methylene-dioxy group bonded to two adjacent ring carbon atoms, and A denotes an alkylene group with 1 to 5 carbon atoms, and esters thereof with alkanols with 1 to 5 carbon atoms, and salts thereof with inorganic and organic bases are new compounds. They display a hyperglycaemic action in warm-blooded animals. Processes for the preparation of the new compounds are given.

4. 发明申请

WO1982003626A1 NEW DERIVATIVES OF PYRAZOLO(3,4-D)PYRIMIDINE,PREPARATION METHOD THEREOF AND REMEDY CONTAINING THEM 审中-公开
标题翻译：吡唑并[3,4-d]吡啶的新衍生物，其制备方法及其含有的补救
公开(公告)号：WO1982003626A1
公开(公告)日：1982-10-28
申请号：PCT/EP1982000085
申请日：1982-04-20
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , GAURI KAILASH KUMAR , ERBLER HANS
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH , ELTZE MANFRID
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Composes de formule generale I (FORMULE) dans laquelle R1 et R2, qui peuvent etre identiques ou differents signifient l'hydrogene ou les restes C1-C8-alkyle, C2-C8-alkenyle, C4-C8-alkyle-carbonyle-alkyle, C3-C8-alkyle-thio-alkyle et C3-C8-alkoxy-alkyle, qui peuvent etre substitues par halogene, hydroxy ou par le groupe di(C1-C2-alkyle)-amino, les symboles R1 et R2 ne pouvant cependant signifier en meme temps l'hydrogene; dans laquelle A signifie l'un des groupes (FORMULE) OU (FORMULE) dans lequel R3 signifie hydrogene ou C1-C4-alkyle, R4 signifie hydrogene, C1-C4-alkyle ou phenyle, qui peut etre substitue jusqu'a trois fois par C1-C2-alkoxy, R5 signifie l'hydrogene, C1-C6-alkyle, hydroxy-C1-C3-alkyle, di(C1-C2-alkyle)-amino-C1-C4-alkyle, C2-C6-alkenyle, phenyle, phenyle-C1-C2-alkyle ou benzoyle, les cycles phenyliques des trois derniers restes pouvant etre substitues jusqu'a trois fois par C1-C2-alkoxy, R5 signifiant par ailleurs C1-C3-alkyle-thio-C2-C4-alkyle ou alors hydroxy-, amino ou sulfo-C1-C3-alkyle-thio-C2-C4 alkyle; avec les conditions que R1, R2 et R5 ne peuvent simultanement signifier ethyle, R1 et R2 ne peuvent signifier en meme temps methyle, lorsque R3 ou R5 signifie butyle ou di(C1-C2-alkyle)-amino-ethyle, et la somme des atomes de carbone, d'oxygene, d'azote et de soufre des chaines laterales liees aux atomes d'azote de l'heterocycle etant au total au moins 6, ou au moins 5, lorsque R2 signifie isobutyle. Ces composes presentent une forte activite bronchospasmolytique, un effet inhibiteur sur la phosphodiesterase et un effet retinotrope. Ces composes ameliorent les proprietes rheologiques du sang et en fait la circulation sanguine peripherique. Ces composes se pretent donc a la preparation de medicaments. L'on decrit, par ailleurs, des procede de preparation de ces nouveaux composes.

5. 发明申请

WO1982000822A1 SUBSTITUTED OXIRANECARBOXYLIC ACIDS,THEIR PREPARATION AND THEIR USE AS MEDICAMENTS 审中-公开
标题翻译：取代的氧化丙烯酸，其制备及其作为药物使用
公开(公告)号：WO1982000822A1
公开(公告)日：1982-03-18
申请号：PCT/EP1981000137
申请日：1981-08-24
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , EISTETTER K , RAPP E
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH
IPC分类号： C07D303/48
CPC分类号： C07D303/48 , C07C17/16 , Y10S514/866 , C07C22/00
摘要： Epoxycycloalkylalkanecarboxylic acids of the general formula I (FORMULA) wherein R denotes a hydrogen atom or a lower alkyl group, Y denotes an oxygen atom (-O-) or a methylene group (-CH u-), m denotes an integer from 0 to 6, n denotes an integer from 0 to6and p denotes an integer from 2 to 11 (and m cannot be 0 or 1 if Y represents an oxygen atom, and the sum of the numbers m, n and p is an integer from 6 to 15), and also the salts of the carboxylic acids, are new compounds. They exhibit a hypoglycaemic action on warmblooded animals. Processes for the preparation of the new compounds are described.
摘要翻译：通式I（式）的环氧环烷基烷烃羧酸其中R表示氢原子或低级烷基，Y表示氧原子（-O-）或亚甲基（-CH u-），m表示整数 0至6，n表示0至6的整数，p表示2至11的整数（如果Y表示氧原子，则m不能为0或1，并且数m，n和p的和为 6至15），以及羧酸的盐也是新的化合物。他们对温血动物表现出低血糖作用。描述了制备新化合物的方法。

6. 发明申请

WO1982000293A1 SUBSTITUTED ADENOSINE-3',5'-PHOSPHOBENZYL TRIESTER DERIVATIVES,METHOD FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING SUCH COMPOUNDS 审中-公开
标题翻译：取代的腺苷-3'，5'-磷酰胆碱衍生物，其制备方法和含有这些化合物的药物
公开(公告)号：WO1982000293A1
公开(公告)日：1982-02-04
申请号：PCT/EP1981000098
申请日：1981-07-15
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , ENGELS J
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH
IPC分类号： C07H19/20
CPC分类号： C07H19/20
摘要： Derives substitues de l'adenosine-3',5'-phosphobenzyl-triester de formule generale I (FORMULE) dans laquelle R1 signifie soit halogene, soit SR3, ou R3 designe un reste en chaine droite ou ramifiee alkyle C1-C5 ou alkanyle C2-C5, qui peuvent etre substitues par hydroxy ou un reste phenyle, qui lui peut porter les substituants halogene, methyle, ethyle, methoxy, ethoxy ou nitro, R3 peut signifier egalement un reste cyclo-alkyle C4-C7, phenyle ou naphthyle, ces derniers restes peuvent etre substitues dans le cycle par halogene, methyle, ethyle, methoxy ou ethoxy, soit SeR4, ou R4 signifie un reste en chaine droite ou ramifiee alkyle C1-C5 ou un reste benzyle, ce dernier pouvant etre substitue dans le cycle par halogene, methyle, ethyle, methoxy, ethoxy ou nitro, soit NR5R6, ou R5 et R6, qui sont egaux ou differents, signifient l'hydrogene ou le reste R3, ou alors qui constituent ensemble en commun avec l'atome d'azote un reste cyclique piperidino ou morpholino; dans laquelle R2 signifie un reste phenyle, qui lui peut etre substitue par des groupements livrant des electrons ou enlevant des electrons. Ces composes sont nouveaux et presentent des activites pharmacologiques interessantes, comme par exemple une activite inotrope, une activite relaxante sur le tractus respiratoire et les vaisseaux sanguins. L'on decrit la preparation de ces composes et leur formulation en remedes.

7. 发明申请

WO1982001133A1 INHALATION DEVICE 审中-公开
标题翻译：吸入装置
公开(公告)号：WO1982001133A1
公开(公告)日：1982-04-15
申请号：PCT/EP1981000157
申请日：1981-10-06
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH , SCHWEITZER M
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH
IPC分类号： A61M15/00
CPC分类号： A61M15/0091 , A61M2205/42
摘要： Les proprietes d'utilisation d'un appareil d'inhalation connus avec liberation commandee par la respiration des ingredients actifs sont ameliorees par des mesures de l'insonorisation et de l'amortissement des mouvements du mecanisme de detente.

8. 发明申请

WO1981003173A1 THIENO-TRICYCLIC COMPOUNDS,METHOD FOR THE PREPARATION THEREOF,UTILIZATION OF SUCH COMPOUNDS AND DRUGS CONTAINING THEM 审中-公开
标题翻译：三烯三氯化合物，其制备方法，这些化合物的使用和含有它们的药物
公开(公告)号：WO1981003173A1
公开(公告)日：1981-11-12
申请号：PCT/EP1981000042
申请日：1981-05-06
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH , FIGALA VOLKER , RIEDEL RICHARD , RAINER GEORG , KLEMM KURT
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The new compounds, defined as thieno-benzodiazepinones, are represented by the general formula I, (FORMULA) wherein R1 represents a hydrogen atom or an alkyl residue from C1 to C4, R2 represents a halogen atom or has the same representation as R1, and R3 represents a halogen atom or a group-N (R4)R5, wherein R4 represents an alkyl residue from C1 to C4 or an alkenyl residue from C3 to C5 and wherein R5 has one of the representations of R4 or represents a group having the partial formula -(CH2)m-N (R6)R7, or wherein R4 and R5 in common, including the nitrogen atom to which they are bound, represent a morpholino, pyrrolidino, piperidino group, a hexa-hydro-azepin-1-yl group, a piperazine-1-yl group optionally substituted in position 4 by methyl or ethyl or benzyl, a 2, 4-dimethyl-piperazine-1-yl group or an hexa-hydro-1H-1, 4-diazepin-1-yl group substituted in position 4 by methyl or ethyl, the symbol R6 representing an alkyl group in C1 to C4 and R7 representing an alkyl group in C1 to C4, the symbol A of the formula I represents an alkylen group with a straight or branched chain C1 to C5 and the symbol m hereabove is 2 or 3; their addition salts may also be formed. All these compounds exhibit a pharmacologic activity for the protection of the stomach and intestine organs and are therefore appropriate for the treatment of diseases affecting the stomach or intestine organs; these compounds may also be used as intermediary products. There are also disclosed methods for the preparation of said new compounds which exhibit an interesting pharmacological activity and also form intermediary products.

9. 发明申请

WO1981000568A1 BENZODIAZEPINONES,A PROCESS FOR THEIR PREPARATION,THEIR USE AND MEDICAMENTS CONTAINING THEM 审中-公开
标题翻译：苯并嗪酮，其制备方法，其使用和药物含有它们
公开(公告)号：WO1981000568A1
公开(公告)日：1981-03-05
申请号：PCT/EP1980000075
申请日：1980-08-07
申请人： BYK GULDEN LOMBERG CHEM FAB GMBH
发明人： BYK GULDEN LOMBERG CHEM FAB GMBH , SCHAEFER H , ELTZE M , KLEMM K , RIEDEL R , SENN J
IPC分类号： C07D487/04
CPC分类号： C07D239/42 , C07D487/04
摘要： Benzodiazepinones of the general formula I (FORMULA) wherein R denotes a hydrogen atom or a phenyl group, R s denotes a hydrogen atom or an alkyl radical with 1 to 4 carbon atoms, R s denotes the group -CO-C uH unR s or (when R is a phenyl group) a hydrogen atom, R s denotes a halogen atom or the group -N(R s)R s, R s denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms, R s denotes an alkyl radical with 1 to 4 carbon atoms, which may be substituted by a dialkylamino group with 1 to4 carbon atoms in the alkyl radicals, or an alkenyl radical with 3 to 5 carbon atoms, or R s and R s together, and including the nitrogen atom, denote a pyrrolidino, piperidino, morpholino or perhydroazepino radical, a piperazino radical which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group or a homopiperazino radical which is optionally substituted in the 4-position by a methyl group, and n represents 1 or 2, and their N-oxides and their acid addition salts with inorganic and organic acids are new compounds. They are used in the pharmaceutical industry as intermediate products and for the preparation of medicaments with protective action on the stomach and the intestines.
摘要翻译：通式I（式）的苯并二氮杂酮其中R表示氢原子或苯基，R 1表示氢原子或具有1至4个碳原子的烷基，R 2表示基团-CO 或者（当R是苯基时）氢原子，R 3表示卤素原子或基团-N（R 4）s R 5， s s表示具有1至4个碳原子的烷基或具有3至5个碳原子的烯基，R 5表示具有1至4个碳原子的烷基，其可以被取代在烷基中具有1至4个碳原子的二烷基氨基或具有3至5个碳原子的烯基或R 4和R 5一起并且包括氮原子表示吡咯烷子基，哌啶子基，吗啉代或全氢氮杂基，哌嗪基，其任选在4-位被甲基，乙基或苄基取代，或任选在4-位被甲基取代的高哌嗪基，n代表 nts 1或2，它们的N-氧化物及其与无机和有机酸的酸加成盐是新化合物。它们用于制药工业中作为中间产品，并用于制备具有对胃和肠的保护作用的药物。

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