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1. 发明申请

WO1998003530A1 NOVEL ERYTHROMYCIN DERIVATIVES, METHOD FOR PREPARING SAME AND USE THEREOF AS DRUGS 审中-公开
标题翻译：新型红霉素衍生物，其制备方法和作为药物使用的方法
公开(公告)号：WO1998003530A1
公开(公告)日：1998-01-29
申请号：PCT/FR1997001372
申请日：1997-07-23
申请人： ROUSSEL UCLAF , AGOURIDAS, Constantin , CHANTOT, Jean-François , DENIS, Alexis , PEJAC, Jean-Marie
发明人： ROUSSEL UCLAF
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of formula (I), wherein R is hydrogen, alkyl optionally substituted by halogen or a (CH2)mAr radical or a radical (a), where m is an integer from 1 to 8, each of n and p, which are the same or different, is an integer from 0 to 6, each of A and B, which are the same or different, is hydrogen or halogen or alkyl, and Ar is aryl or heteroaryl, and Z is hydrogen or a carboxylic acid residue; a method for preparing same, and the use of said compounds as drugs, are disclosed.
摘要翻译：式（I）的化合物，其中R是氢，任选地被卤素或（CH 2）mAr基团或基团（a）取代的烷基，其中m是1至8的整数，n和p各自是相同或不同，为0至6的整数，A和B各自相同或不同，为氢或卤素或烷基，Ar为芳基或杂芳基，Z为氢或羧酸残基; 公开了其制备方法和所述化合物作为药物的用途。

2. 发明申请

WO1995029929A1 NOVEL ERYTHROMYCIN DERIVATIVES, METHOD FOR THEIR PREPARATION AND THEIR USE AS DRUGS 审中-公开
标题翻译：新型红霉素衍生物，其制备方法及其作为药物使用
公开(公告)号：WO1995029929A1
公开(公告)日：1995-11-09
申请号：PCT/FR1995000565
申请日：1995-05-02
申请人： ROUSSEL UCLAF , AGOURIDAS, Constantin , CHANTOT, Jean-François , DENIS, Alexis , GOUIN D'AMBRIERES, Solange , LE MARTRET, Odile
发明人： ROUSSEL UCLAF
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： Compounds of formula (I) in which R is a -(CH2)nAr radical, n is 3, 4 or 5, Ar is an optionally substituted heterocyclic radical and Z is a hydrogen atom or an acid residue. The compounds of formula (I) have useful antibiotic properties.
摘要翻译：其中R为 - （CH 2）n Ar基的式（I）化合物，n为3,4或5，Ar为任选取代的杂环基，Z为氢原子或酸残基。式（I）化合物具有有用的抗生素性质。

3. 发明申请

WO1995027720A1 NOVEL ERYTHROMYCIN DERIVATIVES, METHOD FOR PREPARING SAME AND USE THEREOF AS DRUGS 审中-公开
标题翻译：新型红霉素衍生物，其制备方法和作为药物使用的方法
公开(公告)号：WO1995027720A1
公开(公告)日：1995-10-19
申请号：PCT/FR1995000441
申请日：1995-04-06
申请人： ROUSSEL UCLAF , AGOURIDAS, Constantin , BENEDETTI, Yannick , CHANTOT, Jean-François , DENIS, Alexis , LE MARTRET, Odile
发明人： ROUSSEL UCLAF
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： Compounds of general formula (I), wherein R1 and R2, which are the same or different, are a hydrogen atom or a saturated or unsaturated hydrocarbon radical having up to 24 carbon atoms and being optionally interrupted by one or more heteroatoms and provided with one or more functional groupings; or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring optionally containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or R1 and R2, taken together, form a radical (a), wherein R'1 and R'2, which are the same or different, are a hydrogen atom or a saturated or unsaturated hydrocarbon radical having up to 23 carbon atoms and being optionally interrupted by one or more heteroatoms and provided with one or more functional groupings, and Z is a hydrogen atom or a carboxylic acid residue having up to 18 carbon atoms; as well as acid addition salts thereof. The compounds of formula (I) have valuable antibiotic properties.
摘要翻译：通式（I）的化合物，其中相同或不同的R 1和R 2是氢原子或具有至多24个碳原子的饱和或不饱和烃基，并且任选地被一个或多个杂原子中断并且具有一个或更多功能组; 或R 1和R 2与它们所连接的氮原子一起形成任选地含有一个或多个选自氮，氧和硫的杂原子的杂环; 或R 1和R 2一起形成基团（a），其中R 1和R 2相同或不同，为氢原子或具有至多23个碳原子的饱和或不饱和烃基，并且为任选被一个或多个杂原子中断并提供一个或多个官能团，Z是氢原子或具有至多18个碳原子的羧酸残基; 以及其酸加成盐。式（I）化合物具有有价值的抗生素特性。

4. 发明申请

WO1997031929A1 NOVEL ERYTHROMYCIN DERIVATIVES, METHOD FOR PREPARING SAME, AND USE THEREOF AS DRUGS 审中-公开
标题翻译：新型红霉素衍生物，其制备方法及其作为药物的用途
公开(公告)号：WO1997031929A1
公开(公告)日：1997-09-04
申请号：PCT/FR1997000351
申请日：1997-02-27
申请人： ROUSSEL UCLAF , AGOURIDAS, Constantin , CHANTOT, Jean-François
发明人： ROUSSEL UCLAF
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of formula (I), wherein X is a CH2 or SO2 radical or an oxygen atom, Y is a (CH2)m-(CH=CH)n(CH2)o radical, where m + n + o
摘要翻译：式（I）的化合物，其中X是CH 2或SO 2基团或氧原子，Y是（CH 2）m - （CH = CH）n（CH 2）o基团，其中m + n + n = 0或1，Ar为芳基，W为氢原子或氨基甲酸酯官能残基。式（I）化合物具有有价值的抗生素特性。

5. 发明申请

WO1997047634A1 NOVEL AROMATIC DERIVATIVES SUBSTITUTED BY A RIBOSE, THEIR METHOD OF PREPARATION AND APPLICATION AS MEDICINE 审中-公开
标题翻译：由RIBOSE取代的新型芳香衍生物，其作为药物的制备和应用方法
公开(公告)号：WO1997047634A1
公开(公告)日：1997-12-18
申请号：PCT/FR1997001022
申请日：1997-06-10
申请人： ROUSSEL UCLAF , KLICH, Michel , LAURIN, Patrick , MUSICKI, Branislav , SCHIO, Laurent
发明人： ROUSSEL UCLAF
IPC分类号： C07H17/075
CPC分类号： C07H15/04 , C07H17/075
摘要： The invention discloses the compounds of formula (I): R1 = H, OH, alkyl, alkenyl or alkynyl optionally substituted or alkoxy; R2 = H, Hal; R3 = H, alkyl, Hal, R4 = (a) where Rg and Rh are H, alkyl, an aryl heterocycle; R5 = H or O-alkyl; R6 = alkyl or CH2-O-alkyl; R7 = H or alkyl. The compounds of formula (I) have antibiotic properties.
摘要翻译：本发明公开了式（I）的化合物：R1 = H，OH，烷基，烯基或炔基任选取代或烷氧基; R2 = H，Hal; R3 = H，烷基，Hal，R4 =（a）其中Rg和Rh为H，烷基，芳基杂环; R5 = H或O-烷基; R6 =烷基或CH2-O-烷基; R7 = H或烷基。式（I）化合物具有抗生素特性。

6. 发明申请

WO1997032897A1 NOVEL RADIOACTIVE PEPTIDES USEFUL FOR SCREENING ENDOTHELIN-CONVERTING ENZYME INHIBITORS 审中-公开
标题翻译：用于筛选内皮素转化酶抑制剂的新型放射性肽
公开(公告)号：WO1997032897A1
公开(公告)日：1997-09-12
申请号：PCT/FR1997000368
申请日：1997-03-03
申请人： ROUSSEL UCLAF , INSERM , DUMAS, Jacques , ROQUES, Bernard, Pierre
发明人： ROUSSEL UCLAF , INSERM
IPC分类号： C07K14/575
CPC分类号： C07K14/57536
摘要： Products of formula (IA), wherein X is particularly a (2,3) H-propionyl radical, the use thereof in an endothelin-converting enzyme inhibitor identification test, and the rapid determination of the inhibitory activity of such compounds, are disclosed. When systematically applied, the test enables a large number of assays to be carried out.
摘要翻译：式（IA）的产物，其中X特别是（2,3）3H-丙酰基，其用于内皮素转化酶抑制剂鉴定试验中，并且快速测定这些化合物的抑制活性，被披露。当系统应用时，该测试可以进行大量测定。

7. 发明申请

WO1997027846A1 BIPHENYL COMPOUNDS AND USE THEREOF AS OESTROGENIC AGENTS 审中-公开
标题翻译：联苯化合物及其作为致癌剂的用途
公开(公告)号：WO1997027846A1
公开(公告)日：1997-08-07
申请号：PCT/FR1997000183
申请日：1997-01-30
申请人： ROUSSEL UCLAF , LESUISSE, Dominique , TEUTSCH, Jean-Georges
发明人： ROUSSEL UCLAF
IPC分类号： A61K31/055
CPC分类号： C07C217/20 , C07C39/15 , C07C39/24 , C07C39/367 , C07C39/373 , C07C43/23 , C07C45/00 , C07C45/59 , C07C45/67 , C07C45/673 , C07C45/68 , C07C47/57 , C07C47/575 , C07C49/83 , C07C205/20 , C07C205/26 , C07C205/58 , C07C205/59 , C07C215/54 , C07C215/78
摘要： Compounds of formula (I), wherein R5 is an [A]-CH3, -[A]-C(OH)ZZ' or -[A]-C(O)Z" grouping where -[A]- is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z' and Z" are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R1, R2, R3, R4, R6, R7 and R8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.
摘要翻译：式（I）化合物，其中R 5是[A] -CH 3， - [A] -C（OH）ZZ'或 - [A] -C（O）Z“基团，其中 - [A] 亚烯基或亚炔基或单键，Z，Z'和Z“为氢原子或任选取代的烷基，烯基，炔基或芳基; 并且R1，R2，R3，R4，R6，R7和R8如说明书中所定义; 公开了其作为药物的用途，含有它们的药物组合物，其制备方法和所述方法的中间体。

8. 发明申请

WO1997018197A1 NEW PROCESS FOR THE PREPARATION OF PHENYLIMIDAZOLIDINE DERIVATIVES 审中-公开
标题翻译：制备苯基咪唑衍生物的新方法
公开(公告)号：WO1997018197A1
公开(公告)日：1997-05-22
申请号：PCT/FR1996001794
申请日：1996-11-14
申请人： ROUSSEL UCLAF , BOUCHET, Raphaël , DELTHIL, Michel , GUILMARD, Daniel , MACKIEWICZ, Philippe
发明人： ROUSSEL UCLAF
IPC分类号： C07D233/72
CPC分类号： C07D491/10 , C07D233/72 , Y02P20/55
摘要： The invention relates to a process for the preparation of products having formula (I) wherein R1 and R2 represent particularly hydrogen, cyano, halogen or amino, R3 is particularly hydrogen or hydroxyl alkyl, R4 and R5 are particularly optionally substituted alkyl, X and Y are oxygen or sulfur, characterized in that a product having formula (A) is prepared; in formula (A), W is a halogen atom or a derivative of hydantoin which is subjected to various reactions in order to obtain the products of formula (I), all isomers and salts thereof.
摘要翻译：本发明涉及一种制备具有式（I）的产物的方法，其中R 1和R 2特别表示氢，氰基，卤素或氨基，R 3特别是氢或羟基烷基，R 4和R 5特别是任选取代的烷基，X和Y 是氧或硫，其特征在于制备具有式（A）的产物; 在式（A）中，W是为了获得式（I）的产物而进行各种反应的卤素原子或乙内酰脲的衍生物，其全部异构体和盐。

9. 发明申请

WO1997015570A1 NOVEL ACID PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREFOR, USE THEREOF AS DRUGS, NOVEL USE THEREFOR, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH DERIVATIVES 审中-公开
标题翻译：新型吡唑衍生物，其制备方法，其作为药物，其新用途及含有这些衍生物的药物组合物
公开(公告)号：WO1997015570A1
公开(公告)日：1997-05-01
申请号：PCT/FR1996001615
申请日：1996-10-16
申请人： ROUSSEL UCLAF , DIDIERLAURENT, Stanislas , FORTIN, Michel , ZHANG, Jidong
发明人： ROUSSEL UCLAF
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07D405/14 , C07D409/14
摘要： Products of formula (I), wherein one of A and B is a nitrogen atom while the other of A and B is a methine radical, such that A is either nitrogen substituted particularly by alkyl, or methine substituted particularly by phenyl, thienyl or pyridyl, and B is either nitrogen substituted particularly by cyclohexylalkyl, or methine substituted particularly by alkylthio, R1 is particularly carboxy, and R is particularly halogen, as well as isomers and salts of said products of formula (I), are disclosed.
摘要翻译：式（I）的产物，其中A和B中的一个是氮原子，而A和B中的另一个是次甲基，使得A特别是被烷基取代的氮或特别被苯基取代的次甲基，噻吩基或吡啶基并且B是特别是被环己基烷基取代的氮或特别由烷硫基取代的次甲基，R 1特别是羧基，R特别是卤素，以及所述式（I）产物的异构体和盐。

10. 发明申请

WO1995023791A1 NOVEL TETRASUBSTITUTED IMIDAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, RESULTING NOVEL INTERMEDIATES, USE THEREOF AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新型四唑基咪唑衍生物，其制备方法，结果新颖的中间体，作为药物使用，以及含有其的药物组合物
公开(公告)号：WO1995023791A1
公开(公告)日：1995-09-08
申请号：PCT/FR1995000227
申请日：1995-02-27
申请人： ROUSSEL UCLAF , CORBIER, Alain , DEPREZ, Pierre , FORTIN, Michel , GUILLAUME, Jacques , HECKMANN, Bertrand
发明人： ROUSSEL UCLAF
IPC分类号： C07D233/84
CPC分类号： C07D403/06 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/90 , C07D403/12 , C07D405/04 , C07D409/06 , C07D409/12 , C07D413/04
摘要： Products of formula (I), wherein R1 is particularly an alkyl, alkylthio and alkoxy radical; R2 is e.g. a halogen atom or radicals -S-R, -O-R and (a), where R may be an alkyl or alkenyl radical; R3 is a radical (b), where X is an oxygen or sulphur atom; and R4 is particularly an optionally substituted guanidinosulphonyl radical.
摘要翻译：式（I）的产物，其中R 1特别是烷基，烷硫基和烷氧基; R2是例如卤素原子或基团-S-R，-O-R和（a），其中R可以是烷基或烯基; R3是基团（b），其中X是氧或硫原子; 并且R4特别是任选取代的胍基磺酰基。

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