公开(公告)号：WO2004110983A3

公开(公告)日：2004-12-23

申请号：PCT/EP2004/006330

申请日：2004-06-11

Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  FERNÁNDEZ SERRAT, Anna ,  SERRA COMAS, Carme ,  BALSA LÓPEZ, Dolors ,  LLEBARIA SOLDEVILA, Amadeu ,  FARRERONS GALLEMI, Carles ,  MIQUEL BONO, Ignacio José ,  CATENA RUIZ, Juan Lorenzo ,  LAGUNAS ARNAL, Carmen ,  CORDOMÍ MONTOYA, Arnau ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  MARRERO GONZÁLEZ, Pedro ,  HARO BAUTISTA, Diego ,  FERNÁNDEZ GARCÍA, Andrés

Inventor： FERNÁNDEZ SERRAT, Anna ,  SERRA COMAS, Carme ,  BALSA LÓPEZ, Dolors ,  LLEBARIA SOLDEVILA, Amadeu ,  FARRERONS GALLEMI, Carles ,  MIQUEL BONO, Ignacio José ,  CATENA RUIZ, Juan Lorenzo ,  LAGUNAS ARNAL, Carmen ,  CORDOMÍ MONTOYA, Arnau ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  MARRERO GONZÁLEZ, Pedro ,  HARO BAUTISTA, Diego ,  FERNÁNDEZ GARCÍA, Andrés

IPC: C07C235/52

Abstract: Compounds of general structure (I), wherein the central benzene ring may be substituted in the meta- or para-­position; -A is an optionally substituted hydroxyl, alkoxyl, hydroxylamine, alkoxylamine or amine radical; -W is an N- ­and C-linked biradical selected from several possibilities; and -Z is a carbon radical selected from several possibilities. These compounds are PPARϒ and PPARϒ/ PPARδ modulators and, therefore, are useful for the prophylactic and/or curative treatment of a condition or a disease mediated by these recetpcors.

公开(公告)号：WO2004110983A8

公开(公告)日：2005-08-11

申请号：PCT/EP2004006330

申请日：2004-06-11

Applicant: S A L V A T LAB SA ,  FERNANDEZ SERRAT ANNA ,  SERRA COMAS CARME ,  BALSA LOPEZ DOLORS ,  LLEBARIA SOLDEVILA AMADEU ,  FARRERONS GALLEMI CARLES ,  MIQUEL BONO IGNACIO JOSE ,  CATENA RUIZ JUAN LORENZO ,  LAGUNAS ARNAL CARMEN ,  CORDOMI MONTOYA ARNAU ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  MARRERO GONZALEZ PEDRO ,  HARO BAUTISTA DIEGO ,  FERNANDEZ GARCIA ANDRES

Inventor： FERNANDEZ SERRAT ANNA ,  SERRA COMAS CARME ,  BALSA LOPEZ DOLORS ,  LLEBARIA SOLDEVILA AMADEU ,  FARRERONS GALLEMI CARLES ,  MIQUEL BONO IGNACIO JOSE ,  CATENA RUIZ JUAN LORENZO ,  LAGUNAS ARNAL CARMEN ,  CORDOMI MONTOYA ARNAU ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  MARRERO GONZALEZ PEDRO ,  HARO BAUTISTA DIEGO ,  FERNANDEZ GARCIA ANDRES

IPC: A61P5/00 ,  C07C235/52 ,  C07D209/18 ,  C07D213/30 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D223/16 ,  C07D233/54 ,  C07D241/44 ,  C07D277/64 ,  C07D333/16 ,  A61K31/166 ,  A61K31/381 ,  A61K31/404 ,  A61K31/435 ,  A61K31/498 ,  C07D209/04 ,  C07D213/02 ,  C07D241/40 ,  C07D333/08

CPC classification number: C07D213/30 ,  C07C235/52 ,  C07D209/18 ,  C07D215/20 ,  C07D215/227 ,  C07D215/26 ,  C07D223/16 ,  C07D233/54 ,  C07D241/44 ,  C07D277/64 ,  C07D333/16

Abstract: Compounds of general structure (I), wherein the central benzene ring may be substituted in the meta- or para-­position; -A is an optionally substituted hydroxyl, alkoxyl, hydroxylamine, alkoxylamine or amine radical; -W is an N- ­and C-linked biradical selected from several possibilities; and -Z is a carbon radical selected from several possibilities. These compounds are PPARϒ and PPARϒ/ PPARdelta modulators and, therefore, are useful for the prophylactic and/or curative treatment of a condition or a disease mediated by these recetpcors.

Abstract translation: 一般结构（I）的化合物，其中中间苯环可以在间位或对位取代; -A是任选取代的羟基，烷氧基，羟胺，烷氧基胺或胺基; -W是从几种可能性中选择的N-和C-连接的双基; -Z是选自几种可能性的碳根。 这些化合物是PPARγ和PPARγ/PPARδ调节剂，因此可用于预防性和/或治疗性治疗由这些重症患者介导的病症或疾病。

公开(公告)号：WO2004110983A2

公开(公告)日：2004-12-23

申请号：PCT/EP2004006330

申请日：2004-06-11

Applicant: S A L V A T LAB SA ,  FERNANDEZ SERRAT ANNA ,  SERRA COMAS CARME ,  BALSA LOPEZ DOLORS ,  LLEBARIA SOLDEVILA AMADEU ,  FARRERONS GALLEMI CARLES ,  MIQUEL BONO IGNACIO JOSE ,  CATENA RUIZ JUAN LORENZO ,  LAGUNAS ARNAL CARMEN ,  CORDOMI MONTOYA ARNAU ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  MARRERO GONZALEZ PEDRO ,  HARO BAUTISTA DIEGO ,  FERNANDEZ GARCIA ANDRES

Inventor： FERNANDEZ SERRAT ANNA ,  SERRA COMAS CARME ,  BALSA LOPEZ DOLORS ,  LLEBARIA SOLDEVILA AMADEU ,  FARRERONS GALLEMI CARLES ,  MIQUEL BONO IGNACIO JOSE ,  CATENA RUIZ JUAN LORENZO ,  LAGUNAS ARNAL CARMEN ,  CORDOMI MONTOYA ARNAU ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  MARRERO GONZALEZ PEDRO ,  HARO BAUTISTA DIEGO ,  FERNANDEZ GARCIA ANDRES

IPC: A61P5/00 ,  C07C235/52 ,  C07D209/18 ,  C07D213/30 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D223/16 ,  C07D233/54 ,  C07D241/44 ,  C07D277/64 ,  C07D333/16 ,  C07C235/00

CPC classification number: C07D213/30 ,  C07C235/52 ,  C07D209/18 ,  C07D215/20 ,  C07D215/227 ,  C07D215/26 ,  C07D223/16 ,  C07D233/54 ,  C07D241/44 ,  C07D277/64 ,  C07D333/16

Abstract: Compounds of general structure (I), wherein the central benzene ring may be substituted in the meta- or para-­position; -A is an optionally substituted hydroxyl, alkoxyl, hydroxylamine, alkoxylamine or amine radical; -W is an N- ­and C-linked biradical selected from several possibilities; and -Z is a carbon radical selected from several possibilities. These compounds are PPARϒ and PPARϒ/ PPARdelta modulators and, therefore, are useful for the prophylactic and/or curative treatment of a condition or a disease mediated by these recetpcors.

Abstract translation: 一般结构（I）的化合物，其中中间苯环可以在间位或对位取代; -A是任选取代的羟基，烷氧基，羟胺，烷氧基胺或胺基; -W是从几种可能性中选择的N-和C-连接的双基; -Z是选自几种可能性的碳根。 这些化合物是PPARγ和PPARγ/PPARδ调节剂，因此可用于预防性和/或治疗性治疗由这些重症患者介导的病症或疾病。

公开(公告)号：WO2003053966A2

公开(公告)日：2003-07-03

申请号：PCT/EP2002/014470

申请日：2002-12-18

Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  CATENA RUIZ, Juan Lorenzo ,  FARRERONS GALLEMI, Carles ,  FERNANDEZ SERRAT, Anna ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  LAGUNAS ARNAL, Carmen ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

Inventor： CATENA RUIZ, Juan Lorenzo ,  FARRERONS GALLEMI, Carles ,  FERNANDEZ SERRAT, Anna ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  LAGUNAS ARNAL, Carmen ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

IPC: C07D453/06

CPC classification number: A61K45/06 ,  C07D453/02

Abstract: Carbamate of general formula (I), wherein R1, R2 and R3 are H, OH, NO 2 , SH, CN, F, Cl, Br, I, COOH, CONH 2 , (C 1 -C 4 )-alkoxycarbonyl, (C 1 -C 4 )-alkylsulfanyl, (C 1 -C¿4)-alkylsulfinyl, (C 1 -C 4 )-alkylsulfonyl, (C 1 -C 4 )-alkoxyl optionally substituted with one or several F, and (C 1 -C 4 )-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C 5 -C 10 )-alkyl, a substituted (C 1 -C 10 )-alkyl; and X - is a physiologically acceptable anion. Carbamate (I) is selective M 3 receptor antagonists versus M 2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particulary, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.

Abstract translation: 通式（I）的氨基甲酸酯，其中R 1，R 2和R 3是H，OH，NO 2，SH，CN，F，Cl，Br，I，COOH，CONH 2，（C 1 -C 4） - 烷氧基羰基，（C 1 -C 4） - 烷基硫烷基，（C1-C4） - 烷基亚磺酰基，（C1-C4） - 烷基磺酰基，（C1-C4） - 烷氧基，任选被一个或多个F取代的（C1-C4） - 烷氧基和任意被一个或数个F或 哦; R4是环烷基，苯基，杂芳基或双环系统; R5是环烷基，（C5-C10） - 烷基，取代的（C1-C10） - 烷基; 而X - 是生理上可接受的阴离子。 氨基甲酸酯（I）是选择性M3受体拮抗剂对M2受体，可用于治疗尿失禁（特别是由膀胱过度活动引起的），肠易激综合征和呼吸系统疾病（特别是慢性阻塞性肺病，慢性支气管炎 ，哮喘，肺气肿和鼻炎）以及眼科干预。

公开(公告)号：WO03053966A8

公开(公告)日：2004-06-24

申请号：PCT/EP0214470

申请日：2002-12-18

Applicant: S A L V A T LAB SA ,  CATENA RUIZ JUAN LORENZO ,  FARRERONS GALLEMI CARLES ,  FERNANDEZ SERRAT ANNA ,  MIQUEL BONO IGNACIO JOSE ,  BALSA LOPEZ DOLORS ,  LAGUNAS ARNAL CARMEN ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  FERNANDEZ GARCIA ANDRES

Inventor： CATENA RUIZ JUAN LORENZO ,  FARRERONS GALLEMI CARLES ,  FERNANDEZ SERRAT ANNA ,  MIQUEL BONO IGNACIO JOSE ,  BALSA LOPEZ DOLORS ,  LAGUNAS ARNAL CARMEN ,  SALCEDO ROCA CAROLINA ,  TOLEDO MESA NATIVIDAD ,  FERNANDEZ GARCIA ANDRES

IPC: A61K31/439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/00 ,  A61K45/06 ,  A61P1/00 ,  A61P7/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/10 ,  A61P27/02 ,  A61P43/00 ,  C07D453/02 ,  C07D453/06 ,  A61K31/435

CPC classification number: A61K45/06 ,  C07D453/02

Abstract: Carbamate of general formula (I), wherein R1, R2 and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particulary, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.

Abstract translation: 通式（I）的氨基甲酸酯，其中R 1，R 2和R 3是H，OH，NO 2，SH，CN，F，Cl，Br，I，COOH，CONH 2，（C 1 -C 4） - 烷氧基羰基，（C 1 -C 4） ，（C 1 -C 4） - 烷基亚磺酰基，（C 1 -C 4） - 烷基磺酰基，任选被一个或几个F取代的（C 1 -C 4） - 烷氧基和任选被一个或几个F或OH取代的（C 1 -C 4） - 烷基; R4是环烷基，苯基，杂芳基或双环系统; R5是环烷基，（C5-C10） - 烷基，取代的（C1-C10） - 烷基; 而X - 是生理上可接受的阴离子。 氨基甲酸酯（I）是选择性M3受体拮抗剂对M2受体，可用于治疗尿失禁（特别是由膀胱过度活动引起的），肠易激综合征和呼吸系统疾病（特别是慢性阻塞性肺病，慢性支气管炎 ，哮喘，肺气肿和鼻炎）以及眼科干预。

公开(公告)号：WO2003053966A3

公开(公告)日：2003-07-03

申请号：PCT/EP2002/014470

申请日：2002-12-18

Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  CATENA RUIZ, Juan Lorenzo ,  FARRERONS GALLEMI, Carles ,  FERNANDEZ SERRAT, Anna ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  LAGUNAS ARNAL, Carmen ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

Inventor： CATENA RUIZ, Juan Lorenzo ,  FARRERONS GALLEMI, Carles ,  FERNANDEZ SERRAT, Anna ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  LAGUNAS ARNAL, Carmen ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

IPC: C07D453/06

Abstract: Carbamate of general formula (I), wherein R1, R2 and R3 are H, OH, NO 2 , SH, CN, F, Cl, Br, I, COOH, CONH 2 , (C 1 -C 4 )-alkoxycarbonyl, (C 1 C 4 )-alkylsulfanyl, (C 1 -C 4 )-alkylsulfinyl, (C 1 C 4 )-alkylsulfonyl, (C 1 -C 4 )-alkoxyl optionally substituted with one or several F, and (C 1 -C 4 )-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C 5 -C 10 )-alkyl, a substituted (C 1 -C 10 )-alkyl; and X - is a physiologically acceptable anion. Carbamate (I) is selective M 3 receptor antagonists versus M 2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particulary, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.

公开(公告)号：WO2003008395A1

公开(公告)日：2003-01-30

申请号：PCT/ES2002/000358

申请日：2002-07-17

Applicant: LABORATORIOS S.A.L.V.A.T., S.A. ,  FARRERONS GALLEMI, Carles ,  LAGUNAS ARNAL, Carmen ,  FERNANDEZ SERRAT, Anna ,  CATENA RUIZ, Juan Lorenzo ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

Inventor： FARRERONS GALLEMI, Carles ,  LAGUNAS ARNAL, Carmen ,  FERNANDEZ SERRAT, Anna ,  CATENA RUIZ, Juan Lorenzo ,  MIQUEL BONO, Ignacio José ,  BALSA LOPEZ, Dolors ,  SALCEDO ROCA, Carolina ,  TOLEDO MESA, Natividad ,  FERNANDEZ GARCIA, Andrés

IPC: C07D261/08

CPC classification number: C07D413/12 ,  C07D261/08 ,  C07D413/14 ,  C07D417/14

Abstract: Los compuestos de fórmula (I), donde X es O, S, NH, OCO, NH-CO, NH-COO, NH-CO-NH, NH-CS o NH-CS-NH; R4 es H, (C 1 -C 3 )-alquilo opcionalmente sustituido por halógeno, o un radical heterocíclico de carbono seleccionado entre varias posibilidades; R1 y R3 son H o F; y R2 es un radical heterocíclico de nitrógeno o carbono, son útiles para el tratamiento de infecciones microbianas en el cuerpo humano o animal.

Abstract translation: 本发明涉及具有式（I）的化合物，其中X是O，S，NH，OCO，NH-CO，NH-COO，NH-CO-NH，NH-CS或NH-CS-NH; R4是H，（C 1 -C 3） - 烷基，其任选被卤素或选自各种可能性的杂环碳基团取代; R1和R3是H或F; 并且R 2是杂环氮或碳基团。 所述化合物可用于治疗人或动物体内的微生物感染。