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1. 发明申请

WO1997024341A1 THIOL DERIVATIVES WITH METALLOPEPTIDASE (ACE/NEP) INHIBITORY ACTIVITY 审中-公开
标题翻译：具有金属蛋白酶（ACE / NEP）抑制活性的THIOL衍生物
公开(公告)号：WO1997024341A1
公开(公告)日：1997-07-10
申请号：PCT/EP1996005496
申请日：1996-12-09
申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , ROMAGNANO, Stefano , NORCINI, Gabriele , SANTANGELO, Francesco , SEMERARO, Claudio
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07D275/02
CPC分类号： C07D333/24 , C07D213/55 , C07D277/30
摘要： Compounds of formula (I) wherein R, R1, R2, R3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients 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：描述了其中R，R 1，R 2，R 3具有本说明书中报道的含义，其制备方法和含有它们作为活性成分的药物组合物的式（I）化合物。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。

2. 发明申请

WO1997024342A1 THIOL 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THIOL衍生物
公开(公告)号：WO1997024342A1
公开(公告)日：1997-07-10
申请号：PCT/EP1996005663
申请日：1996-12-17
申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , FANTUCCI, Mario , NORCINI, Gabriele , ROMAGNANO, Stefano , SANTANGELO, Francesco , SEMERARO, Claudio
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07D277/30
CPC分类号： C07D239/26 , C07D213/55 , C07D241/12 , C07D277/30 , C07D307/54 , C07D333/24 , C07D417/12
摘要： Compounds of formula (I), wherein R, R1, R2, and R3 have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients 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：描述了式（I）化合物，其中R，R 1，R 2和R 3具有本说明书中报道的含义，其制备方法和含有它们作为活性成分的药物组合物。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。

3. 发明申请

WO1996022998A1 THIOL 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THIOL衍生物
公开(公告)号：WO1996022998A1
公开(公告)日：1996-08-01
申请号：PCT/EP1996000251
申请日：1996-01-23
申请人： ZAMBON GROUP S.P.A. , PELLACINI, Franco , ROMAGNANO, Stefano , NORCINI, Gabriele , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07K05/06
CPC分类号： C07D307/54 , C07C323/60 , C07C327/32 , C07D213/56 , C07D261/08
摘要： Compounds of formula (I) wherein R, R1, R2, R3, R4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients 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：其中R，R 1，R 2，R 3，R 4，n和n n的式（I）化合物具有说明书中报道的含义，其制备方法和药物组合物含有它们作为活性成分被描述。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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO1995028417A1 PHOSPHONYLDIPEPTIDES USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISEASES 审中-公开
标题翻译：用于治疗心血管疾病的磷酰胆碱
公开(公告)号：WO1995028417A1
公开(公告)日：1995-10-26
申请号：PCT/EP1995001322
申请日：1995-04-11
申请人： ZAMBON GROUP S.P.A. , NORCINI, Gabriele , MORAZZONI, Gabriele , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07K05/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： Compounds of formula (II) 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 or thioalkyl groups having from 1 to 6 carbon atoms in the alkyl moiety, carboxylic groups, nitro groups, amino, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety; R1 is a hydrogen atom or a straight or branched C1-C4 alkyl; R2 is a straight or branched C1-C6 alkyl or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a naphthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted as above indicated for the R substituent; R3 is a straight or branched C1-C6 alkyl, optionally containing one or more fluorine atoms, or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety; the carbon atoms marked with an asterisk are asymmetric carbon atoms; and their pharmaceutically acceptable salts, are described. The compounds of formula (II) are useful in the treatment of cardiovascular diseases.
摘要翻译：式（II）化合物其中R是任选被一个或多个选自在烷基部分中具有1至6个碳原子的卤素原子，羟基，烷氧基，烷基或硫代烷基中的一个或多个相同或不同的取代基取代的联苯基，羧基，硝基，氨基，在烷基部分具有1至6个碳原子的一或二烷基氨基; R1是氢原子或直链或支链C 1 -C 4烷基; R2是直链或支链的C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基，其中芳基是苯基，萘基或具有一个或两个选自氮，氧和硫，任选地被如上述R取代基所取代; R3是任选地含有一个或多个氟原子的直链或支链C 1 -C 6烷基或在烷基部分具有1至6个碳原子的芳基烷基; 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（II）的化合物可用于治疗心血管疾病。

8. 发明申请

WO1994003461A1 DIPHOSPHATES OF CATECHOLAMINES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：羧甲基纤维素的二磷酸酯和含有它们的药物组合物
公开(公告)号：WO1994003461A1
公开(公告)日：1994-02-17
申请号：PCT/EP1993001927
申请日：1993-07-21
申请人： ZAMBON GROUP S.P.A. , SANTANGELO, Francesco , CASAGRANDE, Cesare , NORCINI, Gabriele
发明人： ZAMBON GROUP S.P.A.
IPC分类号： C07F09/12
CPC分类号： C07F9/12
摘要： Diphosphates of catecholamines having formula (I) wherein R, R1, R2, R3, R4, R5, R6, R7 and X have the meanings reported in the description, are useful in the therapy of cardiovascular and renal diseases.
摘要翻译：式（I）的儿茶酚胺的二磷酸盐其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7和X具有说明书中报道的含义，可用于治疗心血管和肾脏疾病。

9. 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。

10. 发明申请

WO1996008228A2 DERIVATIVES OF 2-AMINO-1,2,3,4-TETRAHYDRO-NAPHTHALENE ACTIVE ON THE CARDIOVASCULAR SYSTEM 审中-公开
标题翻译： 2-氨基-1,2,3,4-四氢萘-1-酮对心脏血管系统活性的衍生物
公开(公告)号：WO1996008228A2
公开(公告)日：1996-03-21
申请号：PCT/EP1995003562
申请日：1995-09-11
申请人： ZAMBON GROUP S.P.A. , MONTANARI, Stefania , CAVALLERI, Paolo , FRAIRE, Cristina , GRANCINI, Gian, Carlo , NAPOLETANO, Mauro , SANTANGELO, Francesco
发明人： ZAMBON GROUP S.P.A.
IPC分类号： A61K00/00
CPC分类号： C07D277/68 , C07C59/90 , C07C215/64 , C07C215/80 , C07C217/20 , C07C217/60 , C07C217/74 , C07C229/38 , C07C233/43 , C07C235/20 , C07C235/34 , C07C237/22 , C07C237/30 , C07C271/30 , C07C309/46 , C07C311/08 , C07C311/37 , C07C317/22 , C07C317/44 , C07C323/25 , C07D209/08 , C07D217/14 , C07D277/82 , C07D295/13 , C07D317/58 , C07D319/20
摘要： Derivatives of 2-amino-1,2,3,4-tetrahydro-naphtalene according to formula (I) for the treatment of arterial hypertension, congestive heart failure, renal failure, peripheral arteriopathies or cerebro-vascular insufficiencies.
摘要翻译：用于治疗动脉高血压，充血性心力衰竭，肾衰竭，外周动脉病或脑血管功能不全的根据式（I）的2-氨基-1,2,3,4-四氢 - 萘的衍生物。

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