公开(公告)号：EP0281261A3

公开(公告)日：1989-11-23

申请号：EP88301073.8

申请日：1988-02-09

申请人： H. LUNDBECK A/S

发明人： Boegesoe, Klaus Peter ,  Perregaard, Jens Kristian

IPC分类号： C07C215/46 ,  C07C217/54 ,  C07C219/26 ,  C07C271/00 ,  C07D307/81 ,  C07D333/58 ,  C07D209/14 ,  A61K31/13 ,  A61K31/22 ,  A61K31/325 ,  A61K31/34

CPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58

摘要： Indane-, dihydrobenzofurane-, dihydrobenzothiophene-, and indoline- derivatives of the following formula:
wherein X, R¹, R², R³ and R⁴ are as defined in Claim 1,
are effective at presynaptic DA receptors, or both at pre- and postsynaptic DA receptors, indicating usefulness in the treatment of disorders of the central nervous system (CNS) such as schizophrenia or Parkinson's disease. The 1-aminomethyl derivatives of Formula I exist as optical isomers, and the useful effects are often found in the single enantiomers to a different degree. A method for the preparation of compounds of Formula I is described.

公开(公告)号：EP1490324A4

公开(公告)日：2007-10-10

申请号：EP03716197

申请日：2003-02-27

申请人： TEVA PHARMA

发明人： BLAUGRUND ERAN ,  HERZIG YAACOV ,  STERLING JEFFREY

IPC分类号： A61P15/10 ,  A61K31/216 ,  A61K31/22 ,  A61P21/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C215/64 ,  C07C219/26 ,  C07C271/44 ,  C07D265/12 ,  C07C211/00 ,  A01N33/02 ,  A01N47/10 ,  A61K31/135 ,  A61K31/27 ,  C07C261/00 ,  C07C269/00 ,  C07C271/00

CPC分类号： C07C215/64 ,  C07C219/26 ,  C07C2602/08 ,  C07D265/12

公开(公告)号：EP1278736A1

公开(公告)日：2003-01-29

申请号：EP00986918.1

申请日：2000-12-15

申请人： UCB FARCHIM S.A.

发明人： CHOI, Lewis, Siu, Leung ,  BEATCH, Gregory, N. ,  PAGE, Clive, P.

IPC分类号： C07D295/195 ,  C07D295/10 ,  C07D295/08 ,  C07C237/34 ,  C07C219/26 ,  C07D295/18 ,  A61K31/16 ,  A61P11/14 ,  C07C219/14

CPC分类号： C07D295/088 ,  C07C229/60 ,  C07C229/64 ,  C07C237/34 ,  C07D295/13

摘要： In one aspect, the present invention concerns the use of certain quaternary ammonium compounds as active ingredient in the manufacture of a medicament for use in the treatment and/or prevention of cough in warm-blooded animals, including humans, such as compounds of the following formula (I): Y— J— E An- wherein J is independently selected from a group represented by one of formulae (II), (III) and (IV).

公开(公告)号：EP0717620A4

公开(公告)日：1997-05-28

申请号：EP94925190

申请日：1994-08-05

申请人： DISCOVERY THERAPEUTICS INC

发明人： SLEEVI MARK C ,  MINASKANIAN GEVORK ,  MOSES L MEREDITH

IPC分类号： C07D317/58 ,  A61K31/215 ,  A61K31/34 ,  A61K31/341 ,  A61K31/35 ,  A61K31/351 ,  A61K31/357 ,  A61K31/36 ,  A61P25/00 ,  A61P27/02 ,  A61P27/06 ,  C07C217/08 ,  C07C217/12 ,  C07C219/26 ,  C07D307/14 ,  C07D309/04 ,  C07D309/06 ,  C07D317/70 ,  A61K31/275 ,  A61K31/335 ,  A61K31/38 ,  A61K31/655 ,  C07C211/00 ,  C07C217/00 ,  C07D307/02 ,  C07D315/00 ,  C07D317/44

CPC分类号： C07D309/06 ,  C07C217/08 ,  C07C217/12 ,  C07C219/26 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/10 ,  C07D307/14 ,  C07D309/04 ,  C07D317/70

摘要： Optically active or racemic compounds represented by formula (I) wherein R1, R2, R3, R5 and n are defined as in the specification, and pharmaceutically acceptable salts thereof. These compounds are useful for alleviating Parkinsonism, glaucoma, hyperprolactinemia and for inducing weight loss in mammals.

公开(公告)号：EP1530461B1

公开(公告)日：2007-10-03

申请号：EP04725614.4

申请日：2004-04-03

申请人： SCHWARZ PHARMA AG

发明人： BREITENBACH, Armin ,  MEESE, Claus ,  WOLFF, Hans-Michael ,  DREWS, Roland

IPC分类号： A61K9/70 ,  A61K31/403 ,  C07C219/26

CPC分类号： A61K9/7053 ,  A61K31/403

摘要： The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among C1-6 alkyl, C3-10 cycloalkyl, or phenyl, each of which can be substituted by C1-3 alkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments.

公开(公告)号：EP1127871A1

公开(公告)日：2001-08-29

申请号：EP99953994.3

申请日：1999-11-04

申请人： VITA-INVEST, S.A.

发明人： DEL CASTILLO NIETO, Juan Carlos ,  CHALAUX FREIXA, Maria ,  HUGUET CLOTET, Joan ,  MOURELLE MANCINI, Marisabel ,  DE RAMON AMAT, Elisabet

IPC分类号： C07C219/26 ,  C07D207/337 ,  A61K31/24

CPC分类号： C07C271/44 ,  C07B2200/07 ,  C07C219/28 ,  C07C219/30 ,  C07C2601/14 ,  C07C2601/16 ,  C07D487/04

摘要： New csters derived from substituted phenyl cyclohexyl compounds, which are derived from Tramadol, process for obtaining them and their use for preparing a drug with analgesic properties. These new compounds of general formula (I) have a higher analges activcity, a lower toxicity and a longer effective time period than Tramadol.

摘要翻译： 衍生自衍生自曲马多的取代的苯基环己基化合物的新型化合物获得它们的方法及其用于制备具有止痛性质的药物的用途。 这些新型通式（I）化合物与曲马多相比具有较高的镇痛活性，较低的毒性和较长的有效期。

公开(公告)号：EP0281261B1

公开(公告)日：1992-05-06

申请号：EP88301073.8

申请日：1988-02-09

申请人： H. LUNDBECK A/S

发明人： Boegesoe, Klaus Peter ,  Perregaard, Jens Kristian

IPC分类号： C07C215/46 ,  C07C217/54 ,  C07C219/26 ,  C07C271/00 ,  C07D307/81 ,  C07D333/58 ,  C07D209/14 ,  A61K31/13 ,  A61K31/22 ,  A61K31/325 ,  A61K31/34

CPC分类号： C07D209/14 ,  C07D307/81 ,  C07D333/58

公开(公告)号：EP1530461A1

公开(公告)日：2005-05-18

申请号：EP04725614.4

申请日：2004-04-03

申请人： SCHWARZ PHARMA AG

发明人： BREITENBACH, Armin ,  MEESE, Claus ,  WOLFF, Hans-Michael ,  DREWS, Roland

IPC分类号： A61K9/70 ,  A61K31/403 ,  C07C219/26

CPC分类号： A61K9/7053 ,  A61K31/403

摘要： The invention relates to a device for transdermally administering a compound of formula (I), wherein A represents hydrogen or deuterium, R represents a group selected among C1-6 alkyl, C3-10 cycloalkyl, or phenyl, each of which can be substituted by C1-3 alkoxy, fluoride, chlorine, bromine, iodine, nitro, amino, hydroxy, oxo, mercapto, or deuterium, the C atom marked by * (asterisk) being provided in the R configuration. The invention is characterized in that the compound of general formula (I) is provided in a polymer matrix and is released at a dose of 0.5 to 20 mg per day through human skin. The invention further relates to the use of said compounds of formula (I) for producing transdermal medicaments.

公开(公告)号：EP1362844A4

公开(公告)日：2004-05-26

申请号：EP02716323

申请日：2002-01-22

申请人： SANKYO CO

发明人： KOYAMA KAZUO ,  MARUMOTO SHINJI ,  TODA NARIHIRO ,  KOGEN HIROSHI ,  SUZUKI KEIKO

IPC分类号： C07D295/20 ,  A61K31/222 ,  A61K31/27 ,  A61K31/277 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/47 ,  A61K31/5375 ,  A61P25/00 ,  A61P25/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07C219/22 ,  C07C219/26 ,  C07C219/30 ,  C07C271/44 ,  C07C323/20 ,  C07C323/25 ,  C07C323/32 ,  C07C333/04 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/73 ,  C07D215/20 ,  C07D217/16 ,  C07D223/16 ,  C07D233/46 ,  C07D233/88 ,  C07D249/14 ,  C07D295/205 ,  C07D317/58 ,  C07D317/64 ,  C07D333/38 ,  C07D333/40 ,  C07D401/06 ,  C07D413/06 ,  C07D487/04 ,  C07D521/00 ,  A61K31/137

CPC分类号： C07C219/30 ,  C07C271/44 ,  C07C323/20 ,  C07C323/25 ,  C07C333/04 ,  C07D213/64 ,  C07D213/68 ,  C07D215/20 ,  C07D317/58 ,  C07D333/38

摘要： A compound represented by the general formula (I) (wherein R1 represents C¿1-6? alkyl, etc.; R?2 and R3¿ are the same or different and each represents hydrogen, etc.; Ra represents C¿1-6? alkyl, etc.; Arom represents aryl, etc.; A represents C1-6 alkylene; E represents a single bond, oxygen, sulfur, etc.; and X?1 and X2¿ are the same or different and each represents oxygen or sulfur); or a pharmacologically acceptable salt or ester of the compound.

摘要翻译： 由通式（I）表示的化合物（其中R1代表C1-6烷基等; R12和R3相同或不同并且各代表氢等; Ra代表C1- 6代表烷基等; Arom代表芳基等; A代表C 1-6亚烷基; E代表单键，氧，硫等; X 1和X 2相同或不同，各代表氧 或硫）; 或该化合物的药理学上可接受的盐或酯。

公开(公告)号：EP1127871B1

公开(公告)日：2003-09-10

申请号：EP99953994.3

申请日：1999-11-04

申请人： LABORATORIOS VITA, S.A.

发明人： DEL CASTILLO NIETO, Juan Carlos ,  CHALAUX FREIXA, Maria ,  HUGUET CLOTET, Joan ,  MOURELLE MANCINI, Marisabel ,  DE RAMON AMAT, Elisabet

IPC分类号： C07C219/26 ,  C07D207/337 ,  A61K31/24

CPC分类号： C07C271/44 ,  C07B2200/07 ,  C07C219/28 ,  C07C219/30 ,  C07C2601/14 ,  C07C2601/16 ,  C07D487/04

摘要： New esters derived from substituted phenyl-cyclohexyl compounds, derived from tramadol, process for obtaining such esters and use of said compounds for the fabrication of a medicament having analgesic properties. These new products having the general formula (I) have an analgesic activity which is higher than that of tramadol, a lesser toxicity and longer duration of activity.

摘要翻译： 衍生自衍生自曲马多的取代的苯基环己基化合物的新酯，其获得方法及其用于制备具有止痛性质的药物的用途。 这些通式（I）的这些新化合物具有比曲马多更高的镇痛活性，更低的毒性和更长的有效时间。