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1. 发明申请

WO1996008463A1 DERIVATIVES OF 2-AMINO-1,2,3,4-TETRAHYDRONAPHTHALENE ACTIVE ON THE CARDIOVASCULAR SYSTEM 审中-公开
标题翻译： 2-氨基-1,2,3,4-四氢萘酮在心脏血管系统中的作用
公开(公告)号：WO1996008463A1
公开(公告)日：1996-03-21
申请号：PCT/EP1995003479
申请日：1995-09-05
申请人： ZAMBON GROUP S.P.A. , MONTANARI, Stefania , BOTTA, Daniela , CAVALLERI, Paolo , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07C215/44
CPC分类号： C07D213/38 , C07C215/64
摘要： Compounds of formula (I), wherein m is an integer number selected among 4, 5, 6, 7 and 8; R, R' and R" are hydrogen atoms or OH groups, provided that at least one among R, R' and R" is a hydrogen atom but R, R' and R" are not all contemporaneously hydrogen atoms and R' and R" are not both contemporaneously OH groups; R1 is a hydrogen atom or a C1-C4 alkyl group; R2 is a -(CH2)n-Ar group, wherein n is an integer number selected among 2, 3, 4 and 5; Ar is a pyridyl or a phenyl or R2 is a group of formula (a), wherein one or two among R3, R4, R5 and R6 are OH groups and the remaining are hydrogen atoms; R7 and R8 are hydrogen atoms or together can form a -CH2-CH2-chain; and pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of arterial hypertension and heart failure, of renal failure, of peripheral arteriopathies, of cerebrosvascular insufficiencies and of ischemic cardiopathy.
摘要翻译：式（I）化合物，其中m为选自4，5，6，7和8之间的整数; R，R'和R“是氢原子或OH基团，条件是R，R'和R”中的至少一个是氢原子，但R，R'和R“不全部同时为氢原子，R'和R “不是同时是OH组; R1是氢原子或C1-C4烷基; R2是 - （CH2）n-Ar基团，其中n是选自2,3,4和5中的整数; Ar是吡啶基或苯基或R2是式（a）的基团，其中R3，R4，R5和R6中的一个或两个是OH基团，其余是氢原子; R7和R8是氢原子或一起可以形成-CH 2 -CH 2 - 链; 及其药学上可接受的盐。式（I）化合物可用于治疗动脉高血压和心力衰竭，肾衰竭，外周动脉病变，脑血管功能不全和缺血性心脏病的治疗。

2. 发明申请

WO1997019102A1 PHOSPHONIC ACID DERIVATIVES WITH METALLOPEPTIDASE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有金属蛋白酶抑制活性的磷酸衍生物
公开(公告)号：WO1997019102A1
公开(公告)日：1997-05-29
申请号：PCT/EP1996004911
申请日：1996-11-11
申请人： ZAMBON GROUP S.P.A. , NORCINI, Gabriele , BOTTA, Daniela , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07K05/062
CPC分类号： C07K5/06191 , A61K38/00 , Y02P20/55
摘要： Compounds of formula (I) wherein R is an alkyl, aryl or arylalkyl group wherein the aryl is phenyl, naphthyl or heterocycle; R1 and R2, the same or different, are hydrogen atoms or alkyl groups; R3 is an aryl or arylalkyl group wherein the aryl is as above; R4 is a heterocycle optionally substituted with a heterocycle or phenyl, or it is a phenyl group substituted with a heterocycle (R4 is not imidazole or indole); X is a bond or -OCONH or -CONH- group, processes for their preparation and pharmaceutical compositions thereof, are described. The compounds of formula (I) are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：式（I）化合物，其中R是烷基，芳基或芳基烷基，其中芳基是苯基，萘基或杂环; R1和R2相同或不同，是氢原子或烷基; R3是芳基或芳基烷基，其中芳基如上所述; R4是任选被杂环或苯基取代的杂环，或它是被杂环取代的苯基（R4不是咪唑或吲哚）; X是键或-OCONH或-CONH-基，其制备方法及其药物组合物。式（I）化合物具有双重ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

3. 发明申请

WO1996018633A1 ERYTHROMYCIN A 9-0-OXIME DERIVATIVES ENDOWED WITH ANTIBIOTIC ACTIVITY 审中-公开
标题翻译： ERYTHROMYCIN一种具有抗生素活性的9-0-氧化衍生物
公开(公告)号：WO1996018633A1
公开(公告)日：1996-06-20
申请号：PCT/EP1995004815
申请日：1995-12-07
申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , SCHIOPPACASSI, Giovanna , ALBINI, Enrico , BOTTA, Daniela , ROMAGNANO, Stefano , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of formula (I), wherein A, R1, R2, M, n , m and r have the meanings reported in the description, processes for their preparation and pharmaceutical compositions containing them as active ingredients are described. The compounds of formula (I) are useful in the treatment of infectious diseases.
摘要翻译：式（I）化合物，其中A，R 1，R 2，M，n，m和r'具有说明书中报道的含义，描述了其制备方法和含有它们作为活性成分的药物组合物。式（I）的化合物可用于治疗感染性疾病。

4. 发明申请

WO0042055A3 MACROLIDES WITH ANTI-INFLAMMATORY ACTIVITY 审中-公开
标题翻译：具有抗炎活性的抗体
公开(公告)号：WO0042055A3
公开(公告)日：2001-09-07
申请号：PCT/EP0000163
申请日：2000-01-12
申请人： ZAMBON SPA , PELLACINI FRANCO , BOTTA DANIELA , ROMAGNANO STEFANO , MORIGGI ERMANNO , PRADELLA LORENZO
发明人： PELLACINI FRANCO , BOTTA DANIELA , ROMAGNANO STEFANO , MORIGGI ERMANNO , PRADELLA LORENZO
IPC分类号： A61K31/70 , A61K31/7048 , A61P29/00 , C07H17/08
CPC分类号： C07H17/08
摘要： 3'-Des-dimethylamino-9-oxyimino macrolides of formula (I) endowed with anti-inflammatory activity and their pharmaceutical use are described.
摘要翻译：描述了具有抗炎活性的式（I）的3'-去二甲基氨基-9-氧亚氨基大环内酯，并描述了其药物用途。

5. 发明申请

WO1995035307A1 PEPTIDE DERIVATIVES WITH METALLOPEPTIDASE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有金属蛋白酶抑制活性的肽衍生物
公开(公告)号：WO1995035307A1
公开(公告)日：1995-12-28
申请号：PCT/EP1995002100
申请日：1995-06-02
申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , NORCINI, Gabriele , BOTTA, Daniela , ROMAGNANO, Stefano , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07K05/02
CPC分类号： C07K5/022 , A61K38/00
摘要： Compounds of formula (I) wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, nitro groups, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R1 is a hydrogen atom, a straigth or branched C1-C6 alkyl or an arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a biphenyl, a naphthyl or a 5- or 6-membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R2 is a straigth or branched C1-C6 alkyl optionally substituted by one or more substituents selected among amino, mono- or di-(C1-C6)alkylamino or aminocarbonyl groups, mono or di-(C1-C6)-alkylaminocarbonyl groups, an arylalkyl, an arylcarbonylaminoalkyl, an arylaminocarbonylalkyl or an arylalkylaminocarbonylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety, the aryl being optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; X is a single bond or an -N(R3)- group wherein R3 is a hydrogen atom or a straight or C1-C4 alkyl group; the carbon atoms marked with an asterisk are asymmetric carbon atoms; and their pharmaceutically acceptable salts, are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：式（I）化合物其中R是任选被一个或多个选自卤素原子，硝基，羟基，烷氧基，烷基，硫代烷基或具有1至6个碳原子的烷氧基羰基的一个或多个取代基取代的联苯基烷基部分中的原子，含有一个或多个氟原子的C 1 -C 3烷基，羧基，氨基或氨基羰基，酰氨基，氨基磺酰基，烷基部分中具有1至6个碳原子的单或二烷基氨基，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; R 1是烷基部分中的氢原子，直链或支链的C 1 -C 6烷基或具有1至6个碳原子的芳基烷基，其中芳基是苯基，联苯基，萘基或5或6元芳族具有一个或两个选自氮，氧和硫的杂原子的杂环，任选地被一个或多个选自具有1-6个碳原子的卤素原子，羟基，烷氧基，烷基，硫代烷基或烷氧基羰基中的相同或不同的取代基取代在烷基部分中，含有一个或多个氟原子，羧基，硝基，氨基或氨基羰基的C 1 -C 3烷基，酰氨基，氨基磺酰基，具有1至6个碳原子的单或二烷基氨基烷基部分，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; R 2是任选被一个或多个选自氨基，单 - 或二 - （C 1 -C 6）烷基氨基或氨基羰基，单或二 - （C 1 -C 6） - 烷基氨基羰基的取代基取代的直链或支链C 1 -C 6烷基，芳基烷基，芳基羰基氨基烷基，芳基氨基羰基烷基或在烷基部分具有1至6个碳原子的芳基烷基氨基羰基烷基，芳基任选被一个或多个相同或不同的取代基取代，选自卤素原子，羟基，烷氧基，烷基，在烷基部分具有1至6个碳原子的硫代烷基或烷氧基羰基，含有一个或多个氟原子的C 1 -C 3烷基，羧基，硝基，氨基或氨基羰基，酰氨基，氨基磺酰基，单或二在烷基部分具有1至6个碳原子的 - 烷基氨基，在烷基部分具有1至6个碳原子的单 - 或二 - 烷基氨基羰基; X是单键或-N（R3） - 基，其中R3是氢原子或直链或C1-C4烷基; 标有星号的碳原子是不对称碳原子; 及其药学上可接受的盐。式（I）化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

6. 发明申请

WO0006606A3 ERYTHROMYCIN DERIVATIVES WITH ANTIBIOTIC ACTIVITY 审中-公开
标题翻译：具有抗生素活性的红霉素衍生物
公开(公告)号：WO0006606A3
公开(公告)日：2000-05-04
申请号：PCT/EP9905485
申请日：1999-07-27
申请人： ZAMBON SPA , PELLACINI FRANCO , BOTTA DANIELA , ALBINI ENRICO , UNGHERI DOMENICO
发明人： PELLACINI FRANCO , BOTTA DANIELA , ALBINI ENRICO , UNGHERI DOMENICO
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： The invention discloses erythromycin derivatives with antibiotic activity and pharmaceutically acceptable salts thereof, a process for preparing them and pharmaceutical compositions containing them as active principle (I).
摘要翻译：本发明公开了具有抗生素活性的红霉素衍生物及其药学上可接受的盐，其制备方法和含有它们作为活性成分（I）的药物组合物。

7. 发明申请

WO9932449A3 BENZAZINE DERIVATIVES AS PHOSPHODIESTERASE 4 INHIBITORS 审中-公开
标题翻译：苯并噻唑衍生物作为磷酸二酯酶4抑制剂
公开(公告)号：WO9932449A3
公开(公告)日：1999-09-30
申请号：PCT/EP9808292
申请日：1998-12-17
申请人： ZAMBON SPA , NAPOLETANO MAURO , NORCINI GABRIELE , BOTTA DANIELA , GRANCINI GIANCARLO , MORAZZONI GABRIELE
发明人： NAPOLETANO MAURO , NORCINI GABRIELE , BOTTA DANIELA , GRANCINI GIANCARLO , MORAZZONI GABRIELE
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/4725 , A61P11/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D401/06 , A61K31/44 , A61K31/47
CPC分类号： C07D401/06
摘要： Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by (C1-4)alkyl, (C1-4)alkoxy or -COOR', and necessarily substituted by a -B-Cy group wherein B is methylene, ethylene, amino, CONH or a bond; and is a 5- or 6-membered heterocycle containing from 1 to 3 nitrogen atom(s) optionally substituted by one or more halogen(s); R1 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R2 is aryl, aryl-(C1-10)-alkyl or a (C4-7)-cycloalkyl group optionally containing an oxygen atom and optionally substituted by a polar substituent; and the N}O derivatives and pharmaceutically acceptable salts thereof; are PDE 4 and TNF alpha inhibitors.
摘要翻译：式（I）的化合物，其中A是任选被（C 1-4）烷基，（C 1-4）烷氧基或-COOR'取代并且必须被-B-Cy基取代的正己基杂环，其中B是亚甲基，亚乙基，氨基，CONH或键; 并且是含有1-3个任选被一个或多个卤素取代的氮原子的5-或6-元杂环; R1是（C1-6）烷基或多氟（C1-6）烷基; R2是芳基，芳基 - （C1-10） - 烷基或任意含有氧原子并任选被极性取代基取代的（C 4-7） - 环烷基; 和N} O衍生物及其药学上可接受的盐; 是PDE4和TNFα抑制剂。

8. 发明申请

WO1995035302A1 PHOSPHINIC ACID DERIVATIVES WITH METALLOPEPTIDASE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有金属蛋白酶抑制活性的磷酸衍生物
公开(公告)号：WO1995035302A1
公开(公告)日：1995-12-28
申请号：PCT/EP1995002343
申请日：1995-06-16
申请人： ZAMBON GROUP S.P.A. , NORCINI, Gabriele , BOTTA, Daniela , SANTANGELO, Francesco , MORAZZONI, Gabriele
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07F09/30
CPC分类号： C07F9/301
摘要： Compounds of formula (I), wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R1 is a hydrogen atom, a straight or branched C1-C6 alkyl group or an arylalkyl group having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a biphenyl, a naphtyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted with one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R2 is a straight or branched C1-C6 alkyl group, optionally containing one or more fluorine atoms or one or more -NH- groups, an arylalkyl, an arylcarbonylaminoalkyl, an arylalkylcarbonylaminoalkyl or an arylaminocarbonylalkyl group having from 1 to 6 carbon atoms and optionally one or more -NH- groups in the alkyl moiety, the aryl being optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl, thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C1-C3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylaminocarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; m is 0 or 1; X is a hydrogen or fluorine atom; the carbon atom marked with an asterisk is an asymmetric carbon atom; and their pharmaceutically acceptable salts, are described. The compounds of formula (I) are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.
摘要翻译：式（I）化合物，其中R是任选被一个或多个选自卤原子，羟基，烷氧基，烷基硫代烷基或具有1至6个碳原子的烷氧基羰基的相同或不同的取代基取代的联苯基，烷基部分，含有一个或多个氟原子的C 1 -C 3烷基，羧基，硝基，氨基或氨基羰基，酰氨基，氨基磺酰基，烷基部分中具有1至6个碳原子的双 - 或二烷基氨基，在烷基部分具有1至6个碳原子的单 - 或二烷基氨基 - 羰基; R1是氢原子，在烷基部分中具有1至6个碳原子的直链或支链C 1 -C 6烷基或芳烷基，其中芳基是苯基，联苯基，萘基或5或6元芳族杂环其中一个或两个选自氮，氧和硫的杂原子，任选被一个或多个相同或不同的选自卤原子，羟基，烷氧基，烷基，硫代烷基或具有1-6个碳原子的烷氧基羰基的取代基取代，烷基部分，含有一个或多个氟原子的C 1 -C 3烷基，羧基，硝基，氨基或氨基羰基，酰氨基，氨基磺酰基，烷基中具有1至6个碳原子的单或二烷基氨基部分，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; R 2是任选地含有一个或多个氟原子或一个或多个-NH-基团，芳基烷基，芳基羰基氨基烷基，芳基烷基羰基氨基烷基或具有1至6个碳原子的芳基氨基羰基烷基的直链或支链C 1 -C 6烷基，或更多的-NH-基团，芳基任选被一个或多个选自具有1至6个碳原子的卤素原子，羟基，烷氧基，烷基，硫代烷基或烷氧基羰基中的相同或不同的取代基取代在烷基部分中，含有一个或多个氟原子，羧基，硝基，氨基或氨基羰基的C 1 -C 3烷基，酰氨基，氨基磺酰基，具有1至6个碳原子的单或二烷基氨基烷基部分，在烷基部分具有1至6个碳原子的单或二烷基氨基羰基; m为0或1; X是氢或氟原子; 标有星号的碳原子是不对称碳原子; 及其药学上可接受的盐。式（I）化合物具有混合的ACE抑制和NEP抑制活性，可用于治疗心血管疾病。

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