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1. 发明专利

CO4960641A1 DERIVADOS DE PIPERIDINA 1,4-DISUSTITUIDA CONTENIENDO FLUOR 未知
公开(公告)号：CO4960641A1
公开(公告)日：2000-09-25
申请号：CO97044382
申请日：1997-08-01
申请人： BANYU PHARMA CO LTD
发明人： YOSHIMI TSUCHIYA , NOMOTO TAKASHI , HIROKAZU OHSAWA , KUMIKO KAWAKAMI , OHWAKI KENJI , MASARU NISHIKIBE
IPC分类号： C07D211/46 , A61K31/445 , C07D211/58 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Está invención se refiere a nuevos derivados de piperidina1,4-disustituida que contienen flúor representados por la fórmula general [I] y sus sales farmacéuticamente aceptables. [donde: Ar representa un grupo de arilo o un grupo de heteroarilo que tiene entre 1 y 2 heteroátomos seleccionados de un grupo formado por nitrógeno, oxígeno y azufre (cualquiera de 1 a 3 átomos de hidrógeno sobre el anillo de dicho grupo de arilo o heteroarilo puede ser sustituido con un alquilo menor, trifluorometilo, ciano, hidroxilo, nitro, alcoxicarbonilo menor, halógeno, alcoxi menor, amino o alquilamino menor); R1 representa al cicloalquilo C3 -C6 cuyos 1 a 4 átomos de hidrógeno pueden estar sustituidos con átomo(s) de flúor; R2 representa grupos alifáticos saturados o no saturados de C5 -C15 cualquiera de cuyos 1 a 6 átomos de hidrógeno pueden sustituirse con átomo(s) de flúor, grupos de aralquilo, arilalquenilo, heteroarilalquilo o heteroarilalquenilo que tienen entre 1 y 2 heteroátomos seleccionados del grupo formado por nitrógeno, oxígeno y azufre (opcionalmente cualquiera de 1 a 3 átomos de hidrógeno en el anillo en dicho grupo aralquilo, arilalquenilo, heteroarilalquilo o heteroarilalquenilo puede estar sustituido con un alquilo menor, trifluorometilo, ciano, hidroxilo, nitro, alcoxicarbonilo menor, halógeno, alcoxi menor, amino o alquilamino menor), y X es O o NH, si al menos uno de R1 y R2 contiene uno o más átomos de flúor]. Los compuestos de la presente invención tienen no sólo un antagonismo potente y selectivo para los receptores M3 muscarínicos sino también tienen pocos efectos colaterales. Más aun, exhiben una excelente actividad oral, duración de acción y farmacocinética. Por lo tanto son útiles para el tratamiento y profilaxis de las enfermedades respiratorias, las enfermedades urinarias y enfermedades digestivas.

2. 发明专利

YU1299A 1,4-DISUPSTITUISANI DERIVATI PIPERIDINA KOJI SADRŽE FLUOR 未知
公开(公告)号：YU1299A
公开(公告)日：2002-03-18
申请号：YU1299
申请日：1997-07-28
申请人： BANYU PHARMA CO LTD
发明人： YOSHIMI TSUCHIYA , TAKASHI NOMOTO , HIROKAZU OHSAWA , KUMIKO KAWAKAMI , KENJI OHWAKI , MASARU NISHIKIBE
IPC分类号： C07D211/46 , C07D211/58 , C07D401/06 , C07D405/06 , C07D409/06
摘要： Ovaj pronalazak se odnosi na nove 1,4-disupstituisane derivate piperidina koji sadrze fluor, opisane opstom formulom (I) i na njihove farmaceutski prihvatljive soli, pri cemu: Ar predstavlja aril- ili heteroaril-grupu sa 1 do 2 hetero-atoma odabrana iz grupe koja se sastoji od azota, kiseonika i sumpora (od 1 do 3 atoma vodonika u prstenu navedene aril- ili heteroaril-grupe mogu da budu supstituisani nizom alkil-grupom, itd.); R1 predstavlja cikloalkil-grupu sa 3 do 6 atoma ugljenika, cijih od 1 do 4 atoma vodonika mogu da budu supstituisani fluorom; R2 predstavlja zasicenu ili nezasicenu alifaticnu ugljovodonicnu grupu sa 5 do 15 ugljenikovih atoma, cijih od 1 do 6 atoma vodonika mogu da budu supstituisani fluorom, aralkil-, arilalkenil-, heteroarilalkil- ili heteroarilalkenil-grupu sa 1 do 2 hetero-atoma odabrana iz grupe koja se sastoji od azota, kiseonika i sumpora (opciono, od 1 do 3 atoma vodonika u prstenu navedene aralkil-, arilalkenil-, heteroarilalkil- ili heteroarilalkenil-grupe mogu da budu supstituisani nizom alkil-, trifluormetil-, cijano-, hidroksi-, nitro-, nizom alkoksikarbonil-, halo-, nizom alkoksi- ili amino-grupom itd.; a X predstavlja O ili NH, pod uslovom da barem jedna od grupa R1, odnosno R2 sadrzi jedan ili vise atoma fluora. Jedinjenja iz ovog pronalaska pokazuju selektivno antagonisticko dejstvo prema muskarinskim M3 receptorima, kao i i odlicnu oralnu aktivnost, trajanje dejstva i farmakokinetiku, imaju malo sporednih efekata, bezbedna su i efikasna. Zbog toga su korisna pri lecenju ili profilaksi respiratornih, digestivnih i urinarnih oboljenja.

3. 发明专利

EE9900038A 未知
公开(公告)号：EE9900038A
公开(公告)日：1999-08-16
申请号：EE9900038
申请日：1997-07-28
申请人： BANYU PHARMA CO LTD
发明人： YOSHIMI TSUCHIYA , TAKASHI NOMOTO , HIROKAZU OHSAWA , KUMIKO KAWAKAMI , KENJI OHWAKI , MASARU NISHIKIBE
IPC分类号： C07D211/46 , C07D211/58 , C07D401/06 , C07D405/06 , C07D409/06 , A61K31/445 , C07C59/56 , C07D213/75
摘要： This invention relates to novel fluorine-containing 1,4-disubstituted piperidine derivatives represented by a general formula ÄIÜ and pharmaceutically acceptable salts thereof, Äwherein: Ar represents an aryl group or a hetero-aryl group having 1 to 2 hetero atoms selected from a group consisting of nitrogen, oxygen and sulfur (any 1 to 3 hydrogen atoms on the ring of said aryl or heteroaryl group may be substituted with lower alkyl, etc.); R represents C3-C6 cycloalkyl whose any 1-4 hydrogen atmos may be substituted with fluorine atoms(s); R represents C5-C15 saturated or unsaturated aliphatic hydrocarbon groups whose any 1 to 6 hydrogen atoms may be substituted with fluorine atom(s), aralkyl, arylalkenyl, heteroarylalkyl or heteroarylalkenyl group having 1 to 2 hetero atoms selected from a group consisting of nitrogen, oxygen and sulfur (optionally any 1 to 3 hydrogen atoms on the ring in said aralkyl, arylalkenyl, hetero-arylalkyl or heteroarylalkenyl group may be substituted with lower alkyl, trifluoromethyl, cyano, hydroxyl, nitro, lower alkoxycarbonyl, halogen, lower alkoxy or amino, etc. ; and X stands for O or NH, provided that at least either one of R and R contains one or more fluorine atomsÜ. The compounds of the present invention have selective antagonistic activity for muscarinic M3 receptors, and exhibit excellent oral activity, duration of action and pharmacokinetics, so that they have little side effects and are safe and effective. Therefore they are useful for treatment or prophylaxis of respiratory diseases, urinary diseases and digestive diseases.

6. 发明专利

YU41100A N-ACIL DERIVATI CIKLIČNIH AMINA 未知
公开(公告)号：YU41100A
公开(公告)日：2002-06-19
申请号：YU41100
申请日：1999-02-03
申请人： BANYU PHARMA CO LTD
发明人： YOSHIMI TSUCHIYA , TAKASHI NOMOTO , HIROKAZU OHSAWA , KUMIKO KAWAKAMI , KENJI OHWAKI , MASARU NISHIKIBE
IPC分类号： C07D211/26 , C07D211/58 , C07D211/70 , C07D221/20 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10
摘要： Pronalazak se odnosi na jedinjenja prikazana opstom formulom [I] u kojoj Ar oznacava aril-grupu iil heteroaril-grupu koja moze da bude supstituisana atomom halogena, nizom alkil-grupom i nizom alkoksi-grupom; R1 oznacava cikloalkil-grupu sa 3 do 6 atoma ugljenika koja moze da bude supstituisana atomom fluora; R2 i R4 oznacavaju atom vodonika, grupe prikazane formulom -(A1)m-NH-B i slicno; R3 i R5 oznacavaju atom vodonika, alifaticnu ugljovodonicnu grupu sa 1 do 6 atoma ugljenika ili slicno, koja moze da bude supstituisana sa jednom ili vise nizih alkil-grupa; n oznacava 0 ili 1; a X oznacava atom kiseonika ili sumpora. Jedinjenja iz ovog pronalaska, posto ne samo da ispoljavaju selektivnu antagonisticku aktivnost prema muskarinskim M3 receptorima, vec imaju i izuzetnu oralnu aktivnost, trajsnot dejstva i farmakokinetiku, veoma su korisna kao bezbedna i efikasna sredstva protiv respiratornih, urinarnih i digestivnih oboljenja, pri cemu ne ispolajvaju znacajne sporedne efekte.

7. 发明专利

NZ227042A SUBSTITUTED ALKYLAMINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：NZ227042A
公开(公告)日：1991-05-28
申请号：NZ22704288
申请日：1988-11-22
申请人： BANYU PHARMA CO LTD
发明人： HIROSHI TAKEZAWA , MASAHIRO HAYASHI , YOSHIKAZU IWASAWA MASAAKI HOSO , YOSHIAKI IIDA , YOSHIMI TSUCHIYA , MASAHIRO HORIE , TOSHIO KAMEI
IPC分类号： C07C211/27 , C07C211/30 , C07C211/46 , C07C211/49 , C07C217/48 , C07C217/54 , C07C217/58 , C07C233/20 , C07C233/64 , C07C235/42 , C07C237/40 , C07C255/36 , C07C255/54 , C07C323/32 , C07D213/30 , C07D213/38 , C07D213/64 , C07D215/14 , C07D231/12 , C07D261/08 , C07D263/32 , C07D277/24 , C07D277/28 , C07D307/12 , C07D307/42 , C07D307/68 , C07D307/80 , C07D333/16 , C07C87/28 , C07D207/335 , C07D307/52 , C07D333/20 , A61K31/13 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44
摘要： A substituted alkylamine derivative represented by the general formula wherein A represents a methine group, a nitrogen atom, an oxygen atom or a sulfur atom; Q represents a group which may contain one or two hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms and forms a 5- or 6-membered aromatic ring together with the adjacent carbon atoms and A (the aromatic ring may contain one substituent, or two identical or different substituents, selected from the class consisting of halogen atoms, hydroxyl groups, lower alkyl groups and lower alkoxy groups); X and Y may be identical or different and each represents an oxygen atom, a sulfur atom, a carbonyl group, a group of the formula -CHR - in which R represents a hydrogen atom or a lower alkyl group, or a group of the formula -NR - in which R represents a hydrogen atom or a lower alkyl group, or when taken together, X and Y represent a vinylene or ethynylene group; R represents a lower alkenyl group which may be substituted, a cycloalkenyl group which may be substituted, a lower alkynyl group which may be substituted, an aryl group which may be substituted, or a heterocyclic group which may be substituted; R represents a hydrogen atom or a lower alkyl group; R represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a cycloalkyl group; R and R may be identical or different and each represents a hydrogen atom or a halogen atom; and R represents an acyclic hydrocarbon group which may be substituted (which may contain 1 or 2 unsaturated bonds selected from double and triple bonds); a cycloalkyl group which may be substituted, or a phenyl group which may be substituted; provided that when either one of X and Y represents an oxygen or sulfur atom, or the group -NR - in which R is as defined above, the other represents a carbonyl group or the group -CHR - in which R is as defined above, and a nontoxic salt thereof. The said compound is useful as pharmaceuticals, particularly for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.

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