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1. 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。

2. 发明申请

WO1996012706A1 NOVEL ACID PYRAZOLE AND PYRAZOLONE DERIVATIVES FOR USE AS ENDOTHELIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：用作内皮素受体拮抗剂的新型吡咯和吡唑啉酮衍生物
公开(公告)号：WO1996012706A1
公开(公告)日：1996-05-02
申请号：PCT/FR1995001386
申请日：1995-10-20
申请人： ROUSSEL UCLAF , FORTIN, Michel , ZHANG, Jidong
发明人： ROUSSEL UCLAF
IPC分类号： C07D231/20
CPC分类号： C07D405/06 , C07D231/22
摘要： Products of formula (I) wherein R1 and R2 are hydrogen or optionally substituted alkyl, aryl, arylalkyl or alkylaryl, R3, R4 and R5 are keto, -(CH2)n-R6, -CH=CH-(CH2)n-R6 or -C &cir& C-(CH2)n-R6, where n is 0-4 and R6 is hydroxyl, a lkoxy and aryloxy, alkylthio, arylthio, carboxy, cyano, alkyl, aryl, amino, mono- or dialkylamino, acylamino, and (a), -(NH)m-SO2-W, where m is 0 or 1, W is -NH-R7, (b), (c), (d) or -R7, R7 is hydrogen, alkyl or aryl and R8 is R7 except for hydrogen, or one of R3, R4 and R5 is hydrogen, and all the possible isomeric forms of the products of formula (I), are disclosed.
摘要翻译：式（I）的产物，其中R 1和R 2是氢或任选取代的烷基，芳基，芳基烷基或烷基芳基，R 3，R 4和R 5是酮， - （CH 2）n -R 6，-CH = CH-（CH 2）n -R 6 或-C（C 1 -C 6 - ） - （CH 2）n -R 6，其中n为0-4且R 6为羟基，烷氧基和芳氧基，烷硫基，芳硫基，羧基，氰基，烷基，芳基，氨基，单或二烷基氨基，酰氨基，和（a）， - （NH）m -SO 2 -W，其中m为0或1，W为-NH-R7，（b），（c），（d）或-R7，R7为氢，烷基或芳基和R 8为R 7，除了氢，或者R 3，R 4和R 5中的一个为氢，并且公开了式（I）的产物的所有可能的异构形式。

3. 发明申请

WO1997017340A1 NOVEL IMIDAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, RESULTING INTERMEDIATES, PHARMACEUTICAL COMPOSITIONS AND USE OF SAID DERIVATIVES AS ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译：新咪唑衍生物，其制备方法，中成药，药物组合物和作为内皮素拮抗剂的上述衍生物的使用
公开(公告)号：WO1997017340A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001750
申请日：1996-11-07
申请人： ROUSSEL UCLAF , HECKMANN, Bertrand , JOUQUEY, Simone , VEVERT, Jean-Paul , ZHANG, Jidong
发明人： ROUSSEL UCLAF
IPC分类号： C07D405/06
CPC分类号： C07D405/06
摘要： Novel compounds of formula (I), wherein R1 is alkyl, A is a sulphur or oxygen atom, R2 is carboxy, tetrazolyl or alkyl, alkoxy and alkylthio substituted by carboxy or tetrazolyl, Hal1 is halogen, q is an integer from 0 to 4, R3 is formyl, carboxy or tetrazolyl, Y is phenyl substituted by a dioxol radical and optionally by a halogen atom, or by an alkyl or alkoxy radical, and all possible isomeric, i.e. racemic, enantiomeric and diastereoisomeric forms thereof, as well as addition salts of said compounds of formula (I), are disclosed.
摘要翻译：式（I）的新型化合物，其中R 1是烷基，A是硫或氧原子，R 2是羧基，四唑基或烷基，被羧基或四唑基取代的烷氧基和烷硫基，Hal 1是卤素，q是0-4的整数，R 3是甲酰基，羧基或四唑基，Y是被二氧杂环己基和任选地被卤素原子取代的苯基，或被烷基或烷氧基取代的苯基，以及所有可能的异构体，即外消旋，对映体和非对映异构形式，以及加成公开了所述式（I）化合物的盐。

4. 发明申请

WO1997017339A1 NOVEL IMIDAZOLE N-BENZYLDIOXOL DERIVATIVES, METHOD FOR PREPARING SAME, RESULTING INTERMEDIATES, PHARMACEUTICAL COMPOSITIONS AND USE OF SAID DERIVATIVES AS ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译：新型咪唑烷N-苯甲醛衍生物，其制备方法，结果中间体，药物组合物和作为内皮素拮抗剂的上述衍生物的使用
公开(公告)号：WO1997017339A1
公开(公告)日：1997-05-15
申请号：PCT/FR1996001749
申请日：1996-11-07
申请人： ROUSSEL UCLAF , HECKMANN, Bertrand , JOUQUEY, Simone , VEVERT, Jean-Paul , 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： Novel compounds of formula (I), wherein R1 is optionally substituted alkyl or cycloalkyl optionally interrupted by heteroatoms, both of R2 and R3 are or carry an acid isostere or acid function, and Y is phenyl particularly substituted by a dioxol radical, said compounds being in all isomeric and salt forms, for use as drugs.
摘要翻译：式（I）的新型化合物，其中R 1是任选被取代的烷基或任选被杂原子中断的环烷基，R 2和R 3都是或具有酸等势线或酸官能团，Y是特别被二氧杂环己基取代的苯基，所述化合物是以所有异构体和盐形式，用作药物。

5. 发明申请

WO1996004275A1 NOVEL IMIDAZOLE DERIVATIVES, METHOD FOR PREPARING SAME, NOVEL INTERMEDIATES THUS OBTAINED, MEDICINAL APPLICATIONS OF SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新咪唑衍生物，其制备方法，获得的新型中间体，其药物应用和含有其的药物组合物
公开(公告)号：WO1996004275A1
公开(公告)日：1996-02-15
申请号：PCT/FR1995001033
申请日：1995-08-01
申请人： ROUSSEL UCLAF , HECKMANN, Bertrand , VEVERT, Jean-Paul , ZHANG, Jidong
发明人： ROUSSEL UCLAF
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07D405/14
摘要： Novel products of formula (I), wherein R1 is hydrogen, hydroxy, alkoxy, formyl, dioxol, aryl, arylcarbonyl, arylthio, alkylcarbonyl, R2 and R3 are halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R4, -OR4, and R4 are hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, -(CH2)m1-S(O)m2-X-R10, wherein m1 = 0-4, m2 = 0-2, X is a single bond or -NH-, -NH-CO-, -NH-CO-NH- and R10 is alkyl, alkenyl or aryl, and Y is optionally substituted aryl, said products being obtained in all the isomeric forms, their salts, and their novel use as medicines.
摘要翻译：式（I）的新产物，其中R1是氢，羟基，烷氧基，甲酰基，二氧杂环戊烯，芳基，芳基羰基，芳硫基，烷基羰基，R2和R3是卤素，巯基，酰基，羧基，硝基，氰基，氨基，氨基甲酰基，R4 ，-OR4和R4为氢，烷基，烯基，炔基，酰基，氨基， - （CH2）m1-S（O）m2-X-R10，其中m1 = 0-4，m2 = 0-2，X为单键或-NH-，-NH-CO-，-NH-CO-NH-和R10是烷基，烯基或芳基，Y是任选取代的芳基，所述产物以所有异构体形式获得，其盐，和他们的小说用作药物。

6. 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。

7. 发明申请

WO1996008483A1 GALLIC ACID DERIVATIVES, METHOD FOR THEIR PREPARATION AND THEIR USE AS DRUGS 审中-公开
标题翻译：糖苷衍生物，其制备方法及其作为药物使用
公开(公告)号：WO1996008483A1
公开(公告)日：1996-03-21
申请号：PCT/FR1995001185
申请日：1995-09-15
申请人： ROUSSEL UCLAF , FORTIN, Michel , HAESSLEIN, Jean-Luc
发明人： ROUSSEL UCLAF
IPC分类号： C07D317/46
CPC分类号： C07C69/92 , C07C233/81 , C07C309/65 , C07C309/67 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/21 , C07C327/26 , C07D317/46
摘要： Products of formula (ID), in which R1 is hydrogen, carboxy, formyl, alkyl, hydroxyalkyl, alkoxyalkyl, carbamoyl, N-alkyl-carbamoyl, NNdialkylcarbamoyl, alkoxycarbothioate or alkylcarbonyl, V1 is oxygen or -NH-, V2 is -V1H or hydrogen and A is optionally substituted alkyl or aryl, the products of formula (ID) being in all the possible isomeric forms. The invention also concerns the acid addition salts and bases of the products of formula (ID).
摘要翻译：式（ID）的产物，其中R 1是氢，羧基，甲酰基，烷基，羟基烷基，烷氧基烷基，氨基甲酰基，N-烷基 - 氨基甲酰基，N，N-二烷基氨基甲酰基，烷氧基硫代酯或烷基羰基，V1是氧或-NH-，V2是-V1H或氢和A是任选取代的烷基或芳基，式（ID）的产物具有所有可能的异构形式。本发明还涉及式（ID）的产物的酸加成盐和碱。

8. 发明申请

WO1996004276A1 NOVEL USE AND NOVEL DERIVATIVES OF IMIDAZOLE, METHOD FOR PREPARING SAME, NOVEL INTERMEDIATES THUS OBTAINED, MEDICINAL APPLICATIONS OF SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：咪唑唑的新用途和新型衍生物，其制备方法，获得的新型中间体，其药物应用和含有其的药物组合物
公开(公告)号：WO1996004276A1
公开(公告)日：1996-02-15
申请号：PCT/FR1995001034
申请日：1995-08-01
申请人： ROUSSEL UCLAF , HECKMANN, Bertrand , VEVERT, Jean-Paul , ZHANG, Jidong
发明人： ROUSSEL UCLAF
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , A61K31/4178
摘要： Novel products of formula (I), wherein R1 is hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, formyl, cycloalkyl optionally interrupted by heteroatoms, R2 and R3 are halogen, mercapto, acyl, carboxy, nitro, cyano, amino, carbamoyl, R4, -OR4, and R4 are hydrogen, alkyl, alkenyl, alkynyl, acyl, amino, -(CH2)m1-S(O)m2-X-R10, wherein m1 = 0-4, m2 = 0-2, X is a single bond or -NH-, -NH-CO-, -NH-CO-NH- and R10 is alkyl, alkenyl or aryl, and Y is optionally substituted aryl, said products being obtained in all the isomeric forms, their salts, and their novel use as medicines.
摘要翻译：式（I）的新产物，其中R 1是羟基，烷基，烯基，炔基，烷氧基，烷硫基，甲酰基，任选地被杂原子中断的环烷基，R 2和R 3是卤素，巯基，酰基，羧基，硝基，氰基，氨基，氨基甲酰基，R 4，-OR 4和R 4为氢，烷基，烯基，炔基，酰基，氨基， - （CH 2）m1-S（O）m 2 -X-R 10，其中m1 = X是单键或-NH-，-NH-CO-，-NH-CO-NH-，R 10是烷基，烯基或芳基，Y是任选取代的芳基，所述产物以所有异构形式获得，它们盐和它们作为药物的新颖用途。

9. 发明申请

WO1995023792A1 USE OF IMIDAZOLE DERIVATIVES FOR TREATING DISORDERS INVOLVING ANGIOTENSIN RECEPTORS AT1 AND AT2, CERTAIN SUCH PRODUCTS, PREPARATION THEREOF, USE THEREOF AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：使用咪唑衍生物治疗参与ANGIOTENSIN受体AT1和AT2的某些产物，其制备方法及其作为药物的药物和含有其的药物组合物
公开(公告)号：WO1995023792A1
公开(公告)日：1995-09-08
申请号：PCT/FR1995000228
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： C07D233/64 , C07D233/68 , C07D233/84 , C07D233/90
摘要： Products of formula (I), wherein R1 is particularly alkyl, alkylthio or alkoxy; R2 is particularly halogen, -S-R, -O-R or -C(OH)(R)-COOH, where R is alkyl or alkenyl; R3 is particularly carboxy, acyl, halogen, alkyl, alkenyl or alkylthio; and R4 is particularly -(CH2)m1-COOR14, -(CH2)m1-CONHR14, -(CH2)m1-CN, -SO2-NH-SO2-R14, -NH-SO2-R14, -PO3R14, or -NH-SO2-CF3, where m1 is 0-4 and R14 is hydrogen, alkyl or alkenyl; are useful for preparing pharmaceutical compositions for treating disorders resulting from abnormal stimulation of angiotensin II receptors AT1 and AT2.
摘要翻译：式（I）的产物，其中R 1特别是烷基，烷硫基或烷氧基; R2特别是卤素，-S-R，-O-R或-C（OH）（R）-COOH，其中R是烷基或烯基; R3特别是羧基，酰基，卤素，烷基，烯基或烷硫基; （CH2）m1-COOR14， - （CH2）m1-CONHR14， - （CH2）m1-CN，-SO2-NH-SO2-R14，-NH-SO2-R14，-PO3R14或-NH -SO2-CF3，其中m1为0-4且R14为氢，烷基或烯基; 可用于制备用于治疗由血管紧张素II受体AT1和AT2的异常刺激引起的疾病的药物组合物。

10. 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。

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