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1. 发明申请

US20050245548A1 Alkynylated fused ring pyrimidine compounds 审中-公开
标题翻译：炔烃基稠环嘧啶化合物
公开(公告)号：US20050245548A1
公开(公告)日：2005-11-03
申请号：US11148880
申请日：2005-06-09
申请人： Bernard Gaudilliere , Henri Jacobelli , Joseph Picard , Michael Wilson
发明人： Bernard Gaudilliere , Henri Jacobelli , Joseph Picard , Michael Wilson
IPC分类号： A61K31/517 , A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/10 , A61P27/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D239/96 , C07D403/06 , C07D471/04 , C07D487/04 , C07D521/00 , C07F7/18
CPC分类号： C07D231/12 , A61K31/517 , C07D233/56 , C07D239/96 , C07D249/08 , C07D403/06 , C07D471/04 , C07D487/04 , C07F7/1804
摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基，环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W _{3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。}

2. 发明授权

US06962922B2 Alkynylated quinazoline compounds 失效
标题翻译：炔烃基喹唑啉化合物
公开(公告)号：US06962922B2
公开(公告)日：2005-11-08
申请号：US10269197
申请日：2002-10-11
申请人： Bernard Gaudilliere , Henri Jacobelli , Joseph Armand Picard , Michael William Wilson
发明人： Bernard Gaudilliere , Henri Jacobelli , Joseph Armand Picard , Michael William Wilson
IPC分类号： C07D239/96 , C07D403/06 , C07D471/04 , A61K31/517 , A61P19/02 , C07D401/10
CPC分类号： C07D403/06 , C07D239/96 , C07D471/04
摘要： A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2, monoalkylamino, dialkylamino, alkyl, alkenyl, alkynyl, aryl, arylalkyl, cycloalkylalkyl, heterocycle, these groups being optionally substituted, or W1 and W2 form together a group of formula —N═X4—W3— as defined in the description, X1, X2 and X3 represent N or C optionally substituted, n is 0 to 8, Z represents —CR12R13, wherein R12 and R13 are as defined in the description, A represents a ring system, the groups R2 represent hydrogen or various chemical groups as defined in the description, q is 0 to 7; R1 represents hydrogen, alkyl, alkenyl, alkynyl, or a ring system, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix metalloprotease.
摘要翻译：选自式（I）的化合物的化合物：其中W 1代表O，S或-NR 3，其中R 3表示氢，烷基，OH或CN; W 2表示选自氢，CF 3，NH 2，单烷基氨基，二烷基氨基，烷基，烯基，炔基，芳基，芳基烷基，环烷基烷基，杂环，这些基团任选被取代，或者W 1和W 2 2一起形成式-NX 4 -W _{3 < - >如描述中所定义，X 1，X 2和X 3表示N或C任选取代的n 是0至8，Z表示-CR 12 R 13，其中R 12和R 13定义同上在描述中，A表示环系，基团R 2表示氢或如说明书中定义的各种化学基团，q为0至7; R 1表示氢，烷基，烯基，炔基或环系，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐和药物产品含有它们的特异性抑制剂可用作13型基质金属蛋白酶的特异性抑制剂。}

3. 发明授权

US06849637B2 Triazolo compounds as MMP inhibitors 失效
标题翻译：三唑酚化合物作为MMP抑制剂
公开(公告)号：US06849637B2
公开(公告)日：2005-02-01
申请号：US10075654
申请日：2002-02-14
申请人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
发明人： Charles Andrianjara , Francine Breuzard , Bernard Gaudilliere , Henri Jacobelli
IPC分类号： A61K31/519 , A61P1/02 , A61P1/04 , A61P9/04 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： A compound selected from those of formula (I): in which: W represents N or C—R1; in which R1 is as defined in the description, X represents N or C—R2 in which R2 is as defined in the description, Y represents a group selected from oxygen, sulfur, —NH, and —Nalkyl, Z represents a group selected from oxygen, sulphur, —NR8 in which R8 is as defined in the description, and optionally carbon depending the definition of Y, n is an integer from 0 to 8 inclusive, Z1 represents a group —CR9R10 wherein R9 and R10, are as defined in the description, which group contains optionally multiple bonds or heteroatomes, A represents a cyclic group, m is an integer from 0 to 7 inclusive, the group(s) R4 is (are) as defined in the description, R3 represents a group selected from hydrogen, alkyl, alkenyl, alkynyl, and the group of formula: in which p, Z2, B, q, and R13 are as defined in the description, optionally, its racemic forms, isomers thereof, N-oxydes thereof, and its the pharmaceutically acceptable salts thereof, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：其中：W表示N或C-R 1; 其中R1如说明书中所定义，X表示N或C-R2，其中R2如说明书中所定义，Y表示选自氧，硫，-NH和-N烷基的基团，Z表示选自氧，硫，-NR 8，其中R8如说明书中所定义，可选地取决于Y的定义，n为0至8的整数，其中Z 1为基团-CR 9 R 10，其中R 9和R 10如描述，该组包含任选的多个键或杂原子，A表示环状基团，m是0至7的整数，包括端值，其中R 4是如在说明书中所定义的（是），R 3表示选自氢，烷基，烯基，炔基和下式的基团：其中p，Z2，B，q和R13如说明书中所定义，任选地，其外消旋形式，异构体，其N-氧化物及其其药学上可接受的盐和含有它们的药物可用作特异性抑制剂的13型基质金属蛋白酶。

4. 发明授权

US06239130B1 Phosphodiesterase 4-inhibiting diazepinoindolones 失效
标题翻译：磷酸二酯酶4抑制二氮芥基吲哚酮
公开(公告)号：US06239130B1
公开(公告)日：2001-05-29
申请号：US09380883
申请日：1999-11-10
申请人： Yves Pascal , Catherine Burnouf , Bernard Gaudilliere , Henry Jacobelli , Alain Calvet , Adrian Payne , Svein Dahl
发明人： Yves Pascal , Catherine Burnouf , Bernard Gaudilliere , Henry Jacobelli , Alain Calvet , Adrian Payne , Svein Dahl
IPC分类号： C07D48706
CPC分类号： C07D487/06
摘要： The present invention presents compounds that inhibit phosphodiesterase 4 having Formula (I). The present invention also provides methods of using the compounds of Formula (I) to prevent or treat asthma, atopic dermatitis, rheumatoid arthritis, inflammatory bowel disorders, pulmonary hypertension, liver injury, bone loss, septic shock, or multiple sclerosis, and to pharmaceutical compositions that contain the compounds of Formula (I).
摘要翻译：本发明提供抑制具有式（I）的磷酸二酯酶4的化合物。本发明还提供了使用式（I）化合物来预防或治疗哮喘，特应性皮炎，类风湿性关节炎，炎性肠病，肺动脉高压，肝损伤，骨丢失，败血性休克或多发性硬化的方法，以及药物含有式（I）化合物的组合物。

5. 发明授权

US4690931A Therapeutically useful 1-phenyl-2-piperidinoalkanol derivatives 失效
标题翻译：治疗上有用的1-苯基-2-哌啶子基链烷醇衍生物
公开(公告)号：US4690931A
公开(公告)日：1987-09-01
申请号：US773926
申请日：1985-09-09
申请人： Alexander Wick , Jonathan Frost , Bernard Gaudilliere , Jean Bertin , Regis Dupont , Jean Rousseau
发明人： Alexander Wick , Jonathan Frost , Bernard Gaudilliere , Jean Bertin , Regis Dupont , Jean Rousseau
IPC分类号： C07D211/12 , A61K31/445 , A61K31/451 , A61P9/08 , A61P25/24 , A61P25/26 , A61P25/28 , C07C45/00 , C07C45/45 , C07C45/54 , C07C45/63 , C07C45/71 , C07C49/76 , C07C49/80 , C07C49/825 , C07C49/84 , C07C63/70 , C07C67/00 , C07C69/76 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/28 , C07D211/30 , C07D211/32 , C07D211/62 , C07D213/50 , C07D213/78 , C07D317/18 , C07D317/30
CPC分类号： C07D211/22 , C07C45/004 , C07C45/45 , C07C45/54 , C07C45/63 , C07C45/71 , C07C49/80 , C07C49/825 , C07C49/84 , C07D211/14 , C07D211/18
摘要： Compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, trifluoromethyl, alkyl, hydroxyl, alkyoxy, benzyloxy, alkanoyloxy, or benzoyloxy, or when R.sub.2 is hydroxyl or methoxy in the 4-position and R.sub.3 is hydrogen, R.sub.1 may also represent hydroxymethyl carbamoyl or alkoxycarbonyl,R.sub.2 is hydrogen, halogen, alkyl, hydroxyl, or alkoxy,R.sub.3 is hydrogen or alkyl,R.sub.4 is alkyl (in which case the compounds are (.+-.)-erythro) or when R.sub.3 represents hydrogen, R.sub.4 may also be hydrogen, and R.sub.5 is hydrogen, halogen, alkyl, alkoxy, or three methoxy groups in the 3-, 4- and 5-positions and pharmaceutically acceptable acid addition salts thereof, with the exclusion of compounds wherein:(a) one of R.sub.1 and R.sub.2 is in the 4-position and is hydroxyl, alkoxy or benzyloxy, the other is in the 3-position and is hydrogen, hydroxyl, alkoxy or benzyloxy, and R.sub.3 and R.sub.5 are hydrogen and wherein:(b) R.sub.1 is in the 4-position and is halogen, R.sub.4 is methyl and R.sub.2, R.sub.3 and R.sub.5 are hydrogen, are useful as medicaments.
摘要翻译：下式的化合物：其中R 1为氢，卤素，三氟甲基，烷基，羟基，烷氧基，苄氧基，烷酰氧基或苯甲酰氧基，或当R 4为4-位的羟基或甲氧基且R 3为氢时， R1还可以表示羟甲基氨基甲酰基或烷氧基羰基，R2是氢，卤素，烷基，羟基或烷氧基，R3是氢或烷基，R4是烷基（在这种情况下，化合物是（+/-） - 赤式）氢，R 4也可以是氢，R 5是氢，卤素，烷基，烷氧基或三个甲氧基的3-，4-和5-位及其药学上可接受的酸加成盐，其中：（ a）R1和R2中的一个是4-位，羟基，烷氧基或苄氧基，另一个是3-位，是氢，羟基，烷氧基或苄氧基，R3和R5是氢，其中：（b ）R1为4-位且为卤素，R4为甲基，R2，R3和R5为氢，可用作药物。

6. 发明授权

US06828315B1 1-Amino triazoloc4,3-a! quinazoline-5-ones and/or -5-thiones inhibiting phosphodiesterase IV 失效
标题翻译： 1-氨基三唑并[3,4-a] 喹唑啉-5-酮和/或5-硫代磷酸二酯酶IV
公开(公告)号：US06828315B1
公开(公告)日：2004-12-07
申请号：US09980540
申请日：2001-10-25
申请人： Bernard Gaudilliere , Remi Lavalette , Charles Andrianjara , Francine Breuzard
发明人： Bernard Gaudilliere , Remi Lavalette , Charles Andrianjara , Francine Breuzard
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives. The compounds act as inhibitors of phosphodiesterase IV (PDE-4) and, as such, have utility in treating asthma, chronic bronchitis, acutte pulmonary attack, atopic dermatitis, pulmonary hypertension, pulmonary insufficiency, cardiac insufficiency, psoriasis, inflammatory conditions of the digestive system such as haemorrhagic rectocolitis and Crohn's disease, acute respiratory distress syndrome, acute pancreatitis, benign hypertrophy of the prostate, rheumatoid arthritis, multiple sclerosis, depression, ischaemia-induced neuronal damage, partial cerebral ischaemia, and cancer such as malignant tumor and chronic lymphoid leukemia.
摘要翻译：本发明涉及式I和式II的三唑并[4,3-a]喹唑啉-5-酮和5-硫杂，其中I和II是氮3或4上基团R的位置异构体。任选地，本发明也涉及其外消旋形式，异构体和药学上可接受的盐。本发明还涉及其制备方法和含有所述衍生物的组合物。这些化合物作为磷酸二酯酶IV（PDE-4）的抑制剂，因此可用于治疗哮喘，慢性支气管炎，急性肺部发作，特应性皮炎，肺动脉高压，肺功能不全，心功能不全，牛皮癣，消化道炎症状况系统如出血性直肠结肠炎和克罗恩病，急性呼吸窘迫综合征，急性胰腺炎，前列腺良性肥大，类风湿性关节炎，多发性硬化症，抑郁症，局部缺血诱发的神经元损伤，部分脑缺血和恶性肿瘤和慢性淋巴细胞癌白血病。

7. 发明授权

US5023266A Method of treatment of psychotic disorders 失效
标题翻译：治疗精神病的方法
公开(公告)号：US5023266A
公开(公告)日：1991-06-11
申请号：US469783
申请日：1990-01-24
申请人： Salomon Z. Langer , Jonathan R. Frost , Johannes Schoemaker , Bernard Gaudilliere , Jean Bertin , Jean Rousseau , Regis Dupont , Alexander E. Wick
发明人： Salomon Z. Langer , Jonathan R. Frost , Johannes Schoemaker , Bernard Gaudilliere , Jean Bertin , Jean Rousseau , Regis Dupont , Alexander E. Wick
IPC分类号： C07D211/14 , A61K31/445 , A61K31/451 , A61P25/18 , C07D211/18
CPC分类号： A61K31/445
摘要： Ifenprodil and its analogues are useful for the treatment of psychoses such as schizophrenia.
摘要翻译： Ifenprodil及其类似物可用于治疗精神病如精神分裂症。

8. 发明授权

US4950670A 6-phenyl-3-(piperazinyalalkyl)-2,4(1H,3H)-pyrimidinedione derivatives, their preparation and their application in therapy 失效
标题翻译： 6-苯基-3-（哌嗪烷基）-2,4（1H，3H） - 嘧啶二酮衍生物，其制备及其在治疗中的应用
公开(公告)号：US4950670A
公开(公告)日：1990-08-21
申请号：US352342
申请日：1989-05-16
申请人： Jonathan Frost , Bernard Gaudilliere , Jean Rousseau , Regis Dupont , Philippe Manoury , Daniel Obitz
发明人： Jonathan Frost , Bernard Gaudilliere , Jean Rousseau , Regis Dupont , Philippe Manoury , Daniel Obitz
IPC分类号： A61K31/505 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D217/22 , C07D239/54 , C07D401/12
CPC分类号： C07D239/54 , C07D401/12
摘要： A pyrimidinedione derivative which is a compound of formula (I): ##STR1## in which: R1 denotes hydrogen, a halogen, a methyl group or a methoxy group,R2 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a benzyl group,n denotes 2, 3 or 4,X denotes a CH group or nitrogen, andR3 denotes hydrogen, a halogen or a methoxy group when X denotes a CH group, with the proviso that R3 denotes hydrogen when X denotes nitrogen,or a pharmacologically acceptable acid addition salt thereof.
摘要翻译：作为式（I）的化合物的嘧啶二酮衍生物：其中：R1表示氢，卤素，甲基或甲氧基，R2表示氢，C1-C4烷基或苄基，n 表示2,3或4，X表示CH基或氮，当X表示CH基时，R 3表示氢，卤素或甲氧基，条件是当X表示氮时，R3表示氢，或药理学上可接受的酸加成盐。

9. 发明授权

US06894057B2 Oxo-azabicyclic compounds 失效
标题翻译：氧氮杂双环化合物
公开(公告)号：US06894057B2
公开(公告)日：2005-05-17
申请号：US10384115
申请日：2003-03-07
申请人： Bernard Gaudilliere , Henry Jacobelli , Catherine Kostlan , Jack Jie Li , Wen-Song Yue
发明人： Bernard Gaudilliere , Henry Jacobelli , Catherine Kostlan , Jack Jie Li , Wen-Song Yue
IPC分类号： C07D239/91 , C07D401/06 , C07D403/06 , C07D403/10 , C07D471/04 , A61K31/5025
CPC分类号： C07D401/06 , C07D239/91 , C07D403/06 , C07D403/10 , C07D471/04
摘要： A compound selected from those of formula (I): wherein: X1, X2, and X3, represent N or —CR3 in which R3 is as described in the description, G1 represents a group selected from those of formulae (i/a) and (i/b): in which R4, R5, and R6 are as defined in the description, G2 represents a group selected from carbon—carbon triple bond, —CH═C═CH—, C═O, C═S, S(O)n1 in which n1 represents an integer from 0 to 2 inclusive, or a group of formula (i/c): in which Y1 represents O, S, —NH or -Nalkyl, and Y2 represents O, S, —NH or -Nalkyl, n is an integer from 0 to 6 inclusive, and m is an integer from 0 to 7 inclusive, Z1 represents —CR9R10, wherein R9 and R10 are as defined in the description, A represents a ring system, R1 represents a group selected from H, alkyl, alkenyl, alkynyl, optionally substituted and the group of formula (i/d): in which p, Z2, B, q and G3 are as defined in the description and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of type-13 matrix mettaloprotease.
摘要翻译：选自式（I）的化合物：其中：X 1，X 2和X 3代表N或-CR 3，其中R 3 3如说明书中所述，其中G 1表示选自式（i / a）和（i / b）：其中R 4，R 5和R 6如描述中所定义，G 2，表示选自碳 - 碳三键，-CH-C-CH-，CO，CS，S（O）n1N的基团，其中n1表示0〜2的整数，或者式（I / c）的基团：其中Y 1表示O，S，-NH或-N烷基，Y 2表示O，S，-NH或 -N烷基，n为0〜6的整数，m为0〜7的整数，Z 1表示-CR 9 R 10，其中R 9和R 10如在说明书中所定义，A表示环系，R 1表示所选择的基团由H，烷基，烯基，炔基，任选的其中p，Z 2，B，q和G 3 3如在说明书中所定义，并且任选地，其光学异构体，N-氧化物及其与药学上可接受的酸或碱的加成盐，以及含有它们的药物可用作13型基质金属蛋白酶的特异性抑制剂。

10. 发明授权

US4711899A 2-(4-benzoyl-1-piperidyl)-1-phenylalkanol derivatives 失效
标题翻译： 2-（4-苯甲酰基-1-哌啶基）-1-苯基链烷醇衍生物
公开(公告)号：US4711899A
公开(公告)日：1987-12-08
申请号：US862715
申请日：1986-05-13
申请人： Bernard Gaudilliere , Jean Rousseau
发明人： Bernard Gaudilliere , Jean Rousseau
IPC分类号： A61K31/443 , A61K31/445 , A61K31/451 , A61K31/455 , A61P9/08 , A61P25/28 , C07C49/80 , C07C49/82 , C07C49/84 , C07C67/00 , C07C213/00 , C07C225/22 , C07C233/33 , C07C255/56 , C07C301/00 , C07C303/40 , C07C311/16 , C07C313/00 , C07C323/32 , C07D211/32 , C07D317/00 , C07D405/04
CPC分类号： C07D211/32
摘要： Compound of general formula I ##STR1## in which R is hydrogen, R.sub.1 is unsubstituted phenyl, 4-methoxy - 3,5-dimethylphenyl or phenyl substituted at one of the 2-, 3- or 4- positions by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, benzyloxy, trifluoromethyl, cyano, nitro, amino, acetylamino, methylthio, methylsulphonyl or aminosulphonyl and R.sub.2 is unsubstituted phenyl, 2,4,6-trimethoxyphenyl or phenyl substituted at either the 3- or the 4- positions by fluorine, chlorine, methyl or methoxy, or an acid addition salt thereof.
摘要翻译：通式I的化合物其中R是氢，R 1是未取代的苯基，4-甲氧基-3,5-二甲基苯基或在2-，3-或4-位的一个被卤素取代的苯基， C 1-4烷基，C 1-4烷氧基，羟基，苄氧基，三氟甲基，氰基，硝基，氨基，乙酰氨基，甲硫基，甲基磺酰基或氨基磺酰基，R2是未取代的苯基，2,4,6-三甲氧基苯基或在3- 或氟，氯，甲基或甲氧基的4-位，或其酸加成盐。

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