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1. 发明授权

US5721217A Deoxy and oxygen-substituted sugar-containing 14-aminosteroid compounds 失效
标题翻译：脱氧和含氧取代的含糖的14-氨基甾体化合物
公开(公告)号：US5721217A
公开(公告)日：1998-02-24
申请号：US460348
申请日：1995-06-02
申请人： Song Liu , David Edward Portlock , Gilles Yves Genain , Jean-Jacques Koenig , Jacques de Rostolan
发明人： Song Liu , David Edward Portlock , Gilles Yves Genain , Jean-Jacques Koenig , Jacques de Rostolan
IPC分类号： A61K31/704 , A61P9/00 , C07D309/32 , C07J41/00 , C07J51/00 , A61K31/705 , C07H15/24
CPC分类号： C07J51/00 , C07D309/32 , C07J41/0011 , Y10S514/821 , Y10S514/824
摘要： Disclosed are 14-aminosteroid compounds, including pharmaceutically acceptable acid salts and esters thereof, useful in treating individuals afflicted with congestive heart failure, which compounds have the general formula: ##STR1## wherein R.sub.3 is a deoxy or oxygen-substituted monosaccharide sugar residue and R.sub.1, R.sub.2 and R.sub.4 are various other substituents as defined herein.
摘要翻译：公开了可用于治疗患有充血性心力衰竭的个体的14种氨基甾体化合物，包括其药学上可接受的酸式盐和酯，该化合物具有以下通式：其中R3是脱氧或氧取代的单糖糖残基，R1 ，R2和R4是如本文所定义的各种其它取代基。

2. 发明授权

US5235063A Process of preparing by condensation certain 失效
标题翻译：冷凝制备过程一定
公开(公告)号：US5235063A
公开(公告)日：1993-08-10
申请号：US732041
申请日：1991-07-18
申请人： Francois X. Jarreau , Vincenzo Rovei , Jean-Jacques Koenig , Alain R. Schoffs
发明人： Francois X. Jarreau , Vincenzo Rovei , Jean-Jacques Koenig , Alain R. Schoffs
IPC分类号： C07D263/24 , C07D413/12
CPC分类号： C07D263/24 , C07D413/10
摘要： The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and is 0 or 1 when X is a --CH.dbd.CH-- group;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl, benzyl, CHF.sub.2, CF.sub.3 or CF.sub.3 CF.sub.2 group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.4 -C.sub.7 cycloalkyl, phenyl or benzyl group;R'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain; andeach of R.sub.4 and R'.sub.4 independently is a C.sub.1 -C.sub.4 alkyl group or R.sub.4 and R'.sub.4 form together either a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain, a --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 -- chain substituted by one or two C.sub.1 -C.sub.4 alkyl groups, or a --(CH.sub.2).sub.2 -- chain substituted by one or two --CH.sub.2 --NH.sub.2 groups or by one or two --CH.sub.2 --NH.sub.2 groups N-substituted by one or two C.sub.1 -C.sub.4 alkyl groups,useful as drugs.
摘要翻译：下式的衍生物：其中：R 1是H或C 1 -C 4烷基; X是氧原子，亚甲基或-CH = CH-基团; 当X为氧原子或亚甲基时，n为1或2，当X为-CH = CH-基时，n为0或1; R3是C1-C4烷基，C3-C7环烷基，苯基，苄基，CHF2，CF3或CF3CF2基团; R 2和R 2各自独立地是氢原子或C 1 -C 4烷基，C 4 -C 7环烷基，苯基或苄基; R'2和R 3还可以一起形成 - （CH 2）3 - 或 - （CH 2）4 - 链; R 4和R 4各自独立地为C 1 -C 4烷基或R 4和R'4一起形成 - （CH 2）2 - 或 - （CH 2）3 - 链， - （CH 2）2 - 或被一个或两个C 1 -C 4烷基取代的（CH 2）3 - 链，或被一个或两个-CH 2 -NH 2基团取代的 - （CH 2）2 - 链或被一个或两个被取代的-CH 2 -NH 2基团一个或两个C 1 -C 4烷基，可用作药物。

3. 发明授权

US4584289A 14-aminosteroid derivatives, application in therapy and process of preparation 失效
标题翻译： 14-氨基甾体衍生物，在治疗中的应用和制备过程
公开(公告)号：US4584289A
公开(公告)日：1986-04-22
申请号：US522957
申请日：1983-08-12
申请人： Francois-Xavier Jarreau , Jean-Jacques Koenig
发明人： Francois-Xavier Jarreau , Jean-Jacques Koenig
IPC分类号： C07J3/00 , C07J7/00 , C07J41/00 , C07J5/00
CPC分类号： C07J3/005 , C07J41/0011 , C07J7/007 , C07J7/0075
摘要： The present invention relates to new 14-aminosteroids and their application in therapy and also to a process for their preparation.
摘要翻译：本发明涉及新的14-氨基甾体及其在治疗中的应用，也涉及其制备方法。

4. 发明授权

US5376648A Derivatives of 4-(hetero)arylmethyloxy phenyl diazole, a method of preparing them and use thereof in therapy 失效
标题翻译： 4-（杂）芳基甲氧基苯基二唑的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US5376648A
公开(公告)日：1994-12-27
申请号：US119701
申请日：1993-09-10
申请人： Jean-Jacques Koenig , Luc L. Lebreton , Maryse F. Masson
发明人： Jean-Jacques Koenig , Luc L. Lebreton , Maryse F. Masson
IPC分类号： C07C243/38 , C07D257/04 , C07D271/10 , C07D271/113 , C07D401/12 , C07D273/02 , A61K31/41
CPC分类号： C07D257/04 , C07C243/38 , C07D271/113 , C07D401/12
摘要： Derivatives having the formula: ##STR1## in which R.sub.1 =C.sub.1 -C.sub.4 alkyl and Ar is an aryl or heteroaryl group chosen from among the following: ##STR2## where R.sub.2 represents a hydrogen atom one or two halogen atoms, a CN, NO.sub.2 or CF.sub.3 group, one, two or three C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups or an amino group substituted by two C.sub.1 -C.sub.4 alkyl groups, in which case the --W--V-- chain represents --N.dbd.N-- or ##STR3## and n=2-6; (ii) pyridyl, in which case the --W--V-- chain represents --N.dbd.N-- and n= 1-6, and acid addition salts of those derivatives (I) which are salt-forming.These derivatives are of use in therapy as agents for inhibiting type B monoamine oxydase.
摘要翻译：具有下式的衍生物：其中R 1 = C 1 -C 4烷基和Ar是选自以下的芳基或杂芳基：其中R 2表示氢原子一个或两个卤素原子，CN，NO 2或CF 3基团，一个，两个或三个C 1 -C 4烷基或C 1 -C 4烷氧基或被两个C 1 -C 4烷基取代的氨基，在这种情况下，-WV-链代表-N = N - 或，n = 2-6; （ii）吡啶基，在这种情况下，-W-V-链表示-N = N-和n = 1-6，以及这些衍生物（I）的酸加成盐，其是盐形成的。这些衍生物在治疗中用作抑制B型单胺氧化酶的药剂。

5. 发明授权

US5262432A Derivatives of 4-(hetero)arylmethyloxy phenyl diazole, a method of preparing them and use thereof in therapy 失效
标题翻译： 4-（杂）芳基甲氧基苯基二唑的衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US5262432A
公开(公告)日：1993-11-16
申请号：US878557
申请日：1992-05-05
申请人： Jean-Jacques Koenig , Luc L. Lebreton , Maryse F. Masson
发明人： Jean-Jacques Koenig , Luc L. Lebreton , Maryse F. Masson
IPC分类号： C07C243/38 , C07D257/04 , C07D271/10 , C07D271/113 , C07D401/12 , C07D257/02 , A61K31/41 , A61K31/47
CPC分类号： C07D257/04 , C07C243/38 , C07D271/113 , C07D401/12
摘要： Derivatives having the formula: ##STR1## in which R.sub.1 =C.sub.1 -C.sub.4 alkyl and Ar is an aryl or heteroaryl group chosen from among the following:(i) ##STR2## where R.sub.2 represents a hydrogen atom one or two halogen atoms, a CN, NO.sub.2 or CF.sub.3 group, one, two or three C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy groups or an amino group substituted by two C.sub.1 -C.sub.4 alkyl groups, in which case the --W--V-- chain represent ##STR3## and n=2-6; (ii) pyridyl, in which case the --W--V-- chain represents --N.dbd.N--and n=1-6, and acid addition salts of those derivatives (I) which are salt-forming.These derivatives are of use in therapy as agents for inhibiting type B monoamine oxydase.
摘要翻译：具有下式的衍生物：其中R 1 = C 1 -C 4烷基和Ar是选自以下的芳基或杂芳基：（ⅰ）其中R 2表示氢原子一个或两个卤原子，CN，NO 2或CF 3基团，一个，两个或三个C 1 -C 4烷基或C 1 -C 4烷氧基或被两个C 1 -C 4烷基取代的氨基，在这种情况下，-WV-链代表＆lt; IMAGE＆gt;和 n = 2-6; （ⅱ）吡啶基，在这种情况下，-W-V-链表示-N = N-和n = 1-6，以及形成盐的那些衍生物（Ⅰ）的酸加成盐。这些衍生物在治疗中用作抑制B型单胺氧化酶的药剂。

6. 发明授权

US5171747A 3-aryloxazolidinone derivatives, process for their preparation and their use in therapy 失效
标题翻译： 3-ARYLOXAZOLIDINONE衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US5171747A
公开(公告)日：1992-12-15
申请号：US598254
申请日：1990-10-16
申请人： Francois X. Jarreau , Vincenzo Rovei , Jean-Jacques Koenig , Alain R. Schoffs
发明人： Francois X. Jarreau , Vincenzo Rovei , Jean-Jacques Koenig , Alain R. Schoffs
IPC分类号： C07D263/24 , A61K31/42 , A61K31/421 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D413/10 , C07D413/12
CPC分类号： C07D413/12 , C07D263/24
摘要： The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;D is an oxygen atom or a NOR group, wherein R.dbd.H or C.sub.1 -C.sub.4 alkyl;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group; andR'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain,useful as drugs.

7. 发明授权

US4578382A 4-acylamino-1-azaadamantanes, and compositions for use thereof in medicine 失效
标题翻译： 4-酰基氨基-1-氮杂金刚烷及其用于医药的组合物
公开(公告)号：US4578382A
公开(公告)日：1986-03-25
申请号：US427343
申请日：1982-09-29
申请人： Francois X. Jarreau , Jean-Jacques Koenig
发明人： Francois X. Jarreau , Jean-Jacques Koenig
IPC分类号： A61K31/435 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/12 , C07D471/18
CPC分类号： C07D471/18
摘要： The invention relates to 4-acylamino-1-azaadamantanes represented by general formula (I): ##STR1## wherein R represents an alkyl group, a substituted alkyl group, an aryl group or a substituted aryl group, useful in particular, for the treatment of cardiovascular diseases.
摘要翻译：本发明涉及由通式（I）表示的4-酰基氨基-1-氮杂金刚烷：其中R表示烷基，取代的烷基，芳基或取代的芳基，特别有用，用于治疗心血管疾病。

8. 发明授权

US4526895A 3-Pyridyl-5-alkoxy-pyrazole derivatives and pharmaceutical composition for use as a cardiotonic medication 失效
标题翻译： 3-吡啶基-5-烷氧基 - 吡唑衍生物和用作强心药物的药物组合物
公开(公告)号：US4526895A
公开(公告)日：1985-07-02
申请号：US513190
申请日：1983-07-12
申请人： Francois-Xavier Jarreau , Jean-Jacques Koenig
发明人： Francois-Xavier Jarreau , Jean-Jacques Koenig
IPC分类号： C07D401/04 , A61K31/44
CPC分类号： C07D401/04
摘要： The invention relates to new 3-pyridyl-5-alkoxy-pyrazole derivatives of the following formula: ##STR1## wherein R.sub.1 represents a 4-pyridyl, 3-pyridyl or 2-pyridyl group which is unsubstituted or which may be substituted with one or two lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl group; and R.sub.3 represents a lower alkyl group, a phenyl group or an aralkyl group; and the acid addition salts thereof. The derivatives may be prepared by alkylation of a 3-pyridyl-5-pyrazolone. The derivatives are medicinally useful, particularly for the treatment of cardiac deficiency.
摘要翻译：本发明涉及下式的新的3-吡啶基-5-烷氧基 - 吡唑衍生物：其中R 1表示未被取代的4-吡啶基，3-吡啶基或2-吡啶基，或者可以被一个或多个两个低级烷基; R2表示氢原子或低级烷基; R3代表低级烷基，苯基或芳烷基; 及其酸加成盐。衍生物可以通过3-吡啶基-5-吡唑啉酮的烷基化来制备。该衍生物在医学上是有用的，特别是用于治疗心脏缺陷。

9. 发明授权

US4410525A Alkoxy pyrazole derivatives and compositions 失效
标题翻译：烷氧基吡唑衍生物和组合物
公开(公告)号：US4410525A
公开(公告)日：1983-10-18
申请号：US427344
申请日：1982-09-29
申请人： Francois X. Jarreau , Jean-Jacques Koenig
发明人： Francois X. Jarreau , Jean-Jacques Koenig
IPC分类号： A61K31/415 , A61P9/06 , C07D231/20 , A61K31/535 , C07D413/12
CPC分类号： C07D231/20 , Y10S514/821
摘要： The invention relates to 3-aryl-5-alkoxy-pyrazoles, represented by general formula (I): ##STR1## wherein Ar represents an aryl group which may be substituted; R represents a hydrogen atom or an alkyl, phenyl or benzyl group; R.sub.1 and R.sub.2 which may be the same or different, each represent a hydrogen atom or an alkyl group, or together form a 5 or 7 membered heterocyclic ring with the nitrogen atom to which they are attached; and n is an integer of from 1 to 4; and the pharmaceutically acceptable acid salts thereof, useful in particular, in the treatment of cardiac arrhythmias.
摘要翻译：本发明涉及由通式（I）表示的3-芳基-5-烷氧基 - 吡唑：其中Ar表示可被取代的芳基; R代表氢原子或烷基，苯基或苄基; R 1和R 2可以相同或不同，各自表示氢原子或烷基，或一起形成与它们相连的氮原子的5或7元杂环; n为1〜4的整数，及其药学上可接受的酸盐，特别用于治疗心律失常。

10. 发明授权

US4093619A Method for oxidizing cinchona alkaloids 失效
标题翻译：氧化苦参碱生物碱的方法
公开(公告)号：US4093619A
公开(公告)日：1978-06-06
申请号：US743257
申请日：1976-11-19
申请人： Francois Xavier Jarreau , Jean-Jacques Koenig
发明人： Francois Xavier Jarreau , Jean-Jacques Koenig
IPC分类号： C07D453/04 , C07D401/06 , C07G5/00
CPC分类号： C07D453/04
摘要： Method of oxidizing cinchona alkaloids by reacting specific ketone with cinchona alkaloid in the presence of a strong base and aprotic solvent; following oxidation the oxo compound is reduced to the corresponding stereoisomer.
摘要翻译：通过在强碱和非质子溶剂的存在下，使特定的酮与苦参碱生物碱反应来氧化苦参碱生物碱的方法; 氧化后，将氧代化合物还原为相应的立体异构体。

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