公开(公告)号：US20070015766A1

公开(公告)日：2007-01-18

申请号：US11426414

申请日：2006-06-26

申请人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Marie Gerard Nadler

发明人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Marie Gerard Nadler

IPC分类号： A61K31/496 ,  C07D403/02

CPC分类号： C07D401/12 ,  C07D215/52

摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: wherein: R1 is H or alkyl; R2 is aryl, cycloalkyl or heteroaryl; R3 is H or C1-3 alkyl, optionally substituted by one or more fluorines; R4 is H, R8NR9R10, R11R13 or R11R12R13; or R5 is branched or linear alkyl, cycloalkyl, aryl, arylalkyl, or a single or fused ring aromatic heterocyclic group; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and the use of such compounds and composition in medicine.

摘要翻译： 某些下式（I）化合物或其药学上可接受的盐或水合物：其中：R 1是H或烷基; R 2是芳基，环烷基或杂芳基; R 3是H或C 1-3烷基，任选被一个或多个氟取代; R 4是H，R 8 NR 9 R 10，R 11 R 13或13个R 12 R 13 13; 或R 5是支链或直链烷基，环烷基，芳基，芳烷基或单或稠环芳族杂环基; 制备这些化合物的方法，包含这些化合物的药物组合物和这些化合物的用途以及这些化合物和组合物在医药中的用途。

公开(公告)号：US06780875B2

公开(公告)日：2004-08-24

申请号：US10358938

申请日：2003-02-05

申请人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Marcel Morvan ,  Guy Marguerite Marie Gérard Nadler ,  Luca Francesco Raveglia

发明人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Marcel Morvan ,  Guy Marguerite Marie Gérard Nadler ,  Luca Francesco Raveglia

IPC分类号： A61K314709

CPC分类号： C07D401/06 ,  C07D215/52 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/10

摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or an optionally substituted C5-7 cycloalkyl group, or an optionally substituted single or fused ring aromatic heterocyclic group; R is hydrogen, linear or branched C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl; R1 represents hydrogen or up to three optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, amino or mono- and di-C1-6 alkylamino, R2 represents a moiety —(CH2)n—NYY2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from C1-6-alkyl; C1-6 alkyl substituted with hydroxy, alkoxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C3-6 cycloalkyl; C4-6 azacycloalkyl; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl, R5 represents hydrogen or halogen; a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

摘要翻译： 式（I）的化合物或其溶剂化物或其盐：其中，Ar为任选取代的芳基或C 5-7环二烯基，或任选取代的C 5-7环烷​​基，或任选取代的单或稠合 环芳族杂环基团; R是氢，直链或支链C 1-6烷基，C 3-7环烷基，C 3-7环烷基烷基; R 1代表氢或最多三个选自下列的任选取代基：C 1-6烷基， 6-烯基，芳基，C 1-6烷氧基，羟基，卤素，硝基，氰基，羧基，甲酰氨基，磺酰氨基，C 1-6烷氧基羰基，三氟甲基，酰氧基，氨基或单-C 1-6烷基氨基， （CH 2）n -NYY 2，其中n是1至9的整数，Y 1和Y 2独立地选自C 1-6 - 烷基; 被羟基，烷氧基，C 1-6烷基氨基或双（C 1-6烷基）氨基取代的C 1-6烷基; C3-6环烷基; C4-6氮杂环烷基; C 1-6 - 烯基; 芳基或芳基-C 1-6 - 烷基或Y1和Y2与它们所连接的氮原子一起表示任选取代的N-连接的单或稠环杂环基; R 3是支链或直链C 1-6烷基，C 3-7 环烷基，C 4-7环烷基烷基，任选取代的芳基或任选取代的单环或稠环芳族杂环基; R 4表示氢或C 1-6烷基，R 5表示氢或卤素; 制备这种化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。

公开(公告)号：US5254564A

公开(公告)日：1993-10-19

申请号：US553723

申请日：1990-07-16

申请人： Vittorio Vecchietti ,  Giuseppe Giardina ,  Roberto Colle

发明人： Vittorio Vecchietti ,  Giuseppe Giardina ,  Roberto Colle

IPC分类号： C07D217/06 ,  A61K31/47 ,  A61K31/472 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P25/04 ,  C07D217/14 ,  C07D221/16 ,  C07D221/20 ,  C07D217/26

CPC分类号： C07D221/20 ,  C07D217/14 ,  C07D221/16

摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.sub.1-6 alkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are not simultaneously hydrogen;R.sub.8 and R.sub.9, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.10, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.12, --NHSO.sub.2 R.sub.13, --CH.sub.2 SO.sub.2 NR.sub.14 R.sub.15, in which each of R.sub.10 to R.sub.15 is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl, is useful for the treatment of pain, and or hyponatraemic disease states and/or cerebral ischaemia.

公开(公告)号：US4954509A

公开(公告)日：1990-09-04

申请号：US312648

申请日：1989-02-17

申请人： Vittorio Vecchietti ,  Giuseppe Giardina

发明人： Vittorio Vecchietti ,  Giuseppe Giardina

IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P25/04 ,  C07D217/14 ,  C07D409/06

CPC分类号： C07D409/06 ,  C07D217/14

摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.sub.1-6 alkyl group.R.sub.6 and R.sub.6a, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.6b, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.6d, --NHSO.sub.2 R.sub.6e, --CH.sub.2 SO.sub.2 NR.sub.6f R.sub.6g, in which each of R.sub.6b to R.sub.6g is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.6a are not simultaneously hydrogen,is useful for the treatment of pain.

公开(公告)号：US20070259882A1

公开(公告)日：2007-11-08

申请号：US11768338

申请日：2007-06-26

申请人： Carlo FARINA ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Marisa Martinelli

发明人： Carlo FARINA ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Marisa Martinelli

IPC分类号： A61K31/497 ,  A61P25/00 ,  C07D401/00

CPC分类号： C07D215/50 ,  C07D215/16 ,  C07D215/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/06 ,  C07D487/04

摘要： A compound of formula (I) below or a pharmaceutically acceptable salt or solvate thereof:

摘要翻译： 下式（I）的化合物或其药学上可接受的盐或溶剂合物：

公开(公告)号：US20060229315A1

公开(公告)日：2006-10-12

申请号：US11426956

申请日：2006-06-28

申请人： Carlo FARINA ,  Stefania GAGLIARDI ,  Giuseppe GIARDINA ,  Marisa MARTINELLI

发明人： Carlo FARINA ,  Stefania GAGLIARDI ,  Giuseppe GIARDINA ,  Marisa MARTINELLI

IPC分类号： A61K31/496 ,  C07D403/02

CPC分类号： C07D215/50 ,  C07D215/16 ,  C07D215/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/06 ,  C07D487/04

摘要： A compound of formula (I) below or a pharmaceutically acceptable salt or solvate thereof:

摘要翻译： 下式（I）的化合物或其药学上可接受的盐或溶剂合物：

公开(公告)号：US20060161004A1

公开(公告)日：2006-07-20

申请号：US11331623

申请日：2006-01-13

申请人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Marguerite Nadler

发明人： Carlo Farina ,  Giuseppe Giardina ,  Mario Grugni ,  Guy Marguerite Nadler

IPC分类号： A61K31/4709 ,  C07D401/02

CPC分类号： C07D401/06 ,  C07D401/14

摘要： Certain compounds of formula (I): or a pharmaceutically acceptable salt or hydrate thereof, a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

摘要翻译： 某些式（I）化合物：或其药学上可接受的盐或水合物，制备此类化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。

公开(公告)号：US5041451A

公开(公告)日：1991-08-20

申请号：US440883

申请日：1989-11-22

申请人： Roberto Colle ,  Giuseppe Giardina

发明人： Roberto Colle ,  Giuseppe Giardina

IPC分类号： C07D209/44 ,  A61K31/47 ,  A61K31/472 ,  A61P3/00 ,  A61P7/10 ,  A61P25/04 ,  C07D217/14 ,  C07D495/04

CPC分类号： C07D495/04 ,  C07D217/14

摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which R represents a group of formula (II) ##STR2## in which R.sub.x is the remainder of a heterocyclic group, or an optionally substituted phenyl group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5, which may be located on the same or different carbon atoms, are independently hydrogen, C.sub.1-6 alkyl, or phenyl;m is 1, 2 or 3;R.sub.7 is hydrogen or C.sub.1-6 alkyl;n is 0, 1 or 2;X is direct bond, or O, S or NR.sub.6 in which R.sub.6 is hydrogen or C.sub.1-6 alkyl;Y is >C.dbd.O, >CHOH, >S.dbd.O or >SO.sub.2 ;each is R.sub.8 and R.sub.9 is C.sub.1-6 alkyl, or R.sub.8 and R.sub.9 are linked together and R.sub.8 represents --(Z).sub.p -- where p is 0 or 1 and Z is O, S or NR.sub.z where R.sub.z is hydrogen or C.sub.1-6 alkyl;and R.sub.9 represents --(CH.sub.2).sub.q -- where q is an integer of from 1 to 4,is useful for the treatment of pain or hyponatraemic disease states.

公开(公告)号：US20070197546A1

公开(公告)日：2007-08-23

申请号：US11691899

申请日：2007-03-27

申请人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

发明人： Giuseppe Giardina ,  Mario Grugni ,  Davide Graziani ,  Luca Raveglia

IPC分类号： A61K31/4709 ,  A61K31/496 ,  C07D401/02

CPC分类号： C07D401/06 ,  C07D215/50 ,  C07D215/52 ,  C07D251/52 ,  C07D491/10 ,  C07D491/113

摘要： A compound, or a solvate or a salt thereof, of formula (I): wherein, Ar is an optionally substituted aryl or a C5-7 cycloalkdienyl group, or a C5-7 cycloalkyl group or an optionally substituted single or fused ring aromatic heterocyclic group,; R is C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkylalkyl, optionally substituted phenyl or phenyl C1-6 alkyl, an optionally substituted five-membered heteroaromatic ring comprising up to four heteroatoms selected from O and N, hydroxy C1-6 alkyl, amino C1-6 alkyl, C1-6 alkylaminoalkyl, di C1-6 alkylaminoalkyl, C1-6 acylaminoalkyl, C1-6 alkoxyalkyl, C1-6 alkylcarbonyl, carboxy, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, aminocarbonyl, C1-6 alkylaminocarbonyl, di C1-6 alkylaminocarbonyl, halogeno C1-6 alkyl; or R is a group —(CH2)p— wherein p is 2 or 3 which group forms a ring with a carbon atom of Ar; R1 represents hydrogen or up to four optional substituents selected from the list consisting of: C1-6 alkyl, C1-6 alkenyl, aryl, C1-6 alkoxy, hydroxy, halogen, nitro, cyano, carboxy, carboxamido, sulphonamido, C1-6 alkoxycarbonyl, trifluoromethyl, acyloxy, phthalimido, amino or mono- and di-C1-6 alkylamino; R2 represents a moiety —(CH2)n—NY1Y2 wherein n is an integer in the range of from 1 to 9, Y1 and Y2 are independently selected from hydrogen; C1-6-alkyl; C1-6 alkyl substituted with hydroxy, C1-6 alkylamino or bis (C1-6 alkyl) amino; C1-6-alkenyl; aryl or aryl-C1-6-alkyl or Y1 and Y2 together with the nitrogen atom to which they are attached represent an optionally substituted N-linked single or fused ring heterocyclic group; R3 is branched or linear C1-6 alkyl, C3-7 cycloalkyl, C4-7 cycloalkylalkyl, optionally substituted aryl, or an optionally substituted single or fused ring aromatic heterocyclic group; and R4 represents hydrogen or C1-6 alkyl; a pharmaceutical composition comprising such a compound, process for preparing such a compound and the use of such a compound in medicine.

公开(公告)号：US20060223819A1

公开(公告)日：2006-10-05

申请号：US11425508

申请日：2006-06-21

申请人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Nadler

发明人： Carlo Farina ,  Stefania Gagliardi ,  Giuseppe Giardina ,  Mario Grugni ,  Marisa Martinelli ,  Guy Marguerite Nadler

IPC分类号： A61K31/496 ,  C07D403/02

CPC分类号： C07D401/06 ,  A61K31/495 ,  C07D215/52 ,  C07D409/14 ,  C07D493/04

摘要： Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: a process for preparing such compounds, a pharmaceutical composition comprising such compounds and the use of such compounds and composition in medicine.

摘要翻译： 某些下面的式（I）化合物或其药学上可接受的盐或水合物：制备此类化合物的方法，包含这些化合物的药物组合物以及这些化合物和组合物在医药中的用途。