公开(公告)号：WO2012159992A1

公开(公告)日：2012-11-29

申请号：PCT/EP2012/059272

申请日：2012-05-18

Applicant: INTERQUIM, S.A. ,  BERZOSA RODRÍGUEZ, Xavier ,  MARQUILLAS OLONDRIZ, Francisco ,  LLEBARIA SOLDEVILLA, Amadeo ,  SERRA COMAS, Carme

Inventor： BERZOSA RODRÍGUEZ, Xavier ,  MARQUILLAS OLONDRIZ, Francisco ,  LLEBARIA SOLDEVILLA, Amadeo ,  SERRA COMAS, Carme

IPC: C07D413/10 ,  C07D413/14

CPC classification number: C07D413/14 ,  C07D413/10

Abstract: This invention relates to a procedure for obtaining a thiophene-2-carboxamide compound, specifically rivaroxaban, which comprises the (i) fragmentation of the N=C bond of a compound of formula 23 where R1 is selected among hydrogen, halogen, and (C1-C6)alkyl; and (ii) acylation of the resulting intermediate with 5-chloro-tiofen-2-carbonyl chloride in a solvent medium, in the presence of a base. The invention also relates to the compounds of formula 23 and their use in the obtention of rivaroxaban.

Abstract translation: 本发明涉及获得噻吩-2-甲酰胺化合物，特别是利伐沙班的方法，其包括（i）式23化合物的N = C键的断裂，其中R1选自氢，卤素和（C1 1 -C 6）烷基; 和（ii）在溶剂介质中，在碱的存在下，用5-氯 - 噻吩-2-碳酰氯将得到的中间体酰化。 本发明还涉及式23化合物及其在获得利伐沙班的用途。

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：WO2010139827A1

公开(公告)日：2010-12-09

申请号：PCT/ES2010/000258

申请日：2010-06-04

Applicant: LABORATORIOS SALVAT, S.A. ,  CATENA RUIZ, Juan Lorenzo ,  SERRA COMAS, Carme ,  REY PUIGGROS, Oscar ,  ANTOLIN HERNANDEZ, Albert ,  MONLLEO MAS, Ester

Inventor： CATENA RUIZ, Juan Lorenzo ,  SERRA COMAS, Carme ,  REY PUIGGROS, Oscar ,  ANTOLIN HERNANDEZ, Albert ,  MONLLEO MAS, Ester

IPC: C07D295/104 ,  A61K31/4709 ,  A61K31/472

CPC classification number: C07D217/16 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  C07D215/08 ,  C07D215/14 ,  C07D215/20 ,  C07D215/58 ,  C07D217/06 ,  C07D217/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06

Abstract: Los compuestos de fórmula (I) son derivados de perhidroquinolina y perhidroisoquinolina y son útiles como principios activos farmacéuticos para Ia profilaxis o tratamiento de enfermedades causadas por trastornos asociados con Ia enzima 11 beta-hidroxiesteroide deshidrogenasa de tipo 1 (11 beta- HSD1), tales como glaucoma, presión ocular elevada, trastornos metabólicos, obesidad, síndrome metabólico, dislipidemia, hipertensión, diabetes, aterosclerosis, síndrome de Cushing, psoriasis, artritis reumatoide, alteraciones de Ia cognición, enfermedad de Alzheimer o neurodegeneración.

Abstract translation: 式（I）化合物衍生自全氢喹啉和全氢异喹啉，可用作预防或治疗由与11-β-羟基类固醇脱氢酶1型酶（11-β-HSD1）相关的疾病引起的疾病的药物活性成分。 例如青光眼，眼压升高，代谢紊乱，肥胖，代谢综合征，血脂异常，高血压，糖尿病，动脉粥样硬化，库兴综合征，牛皮癣，类风湿性关节炎，认知变化，阿尔茨海默病或神经变性。

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：IL318651A

公开(公告)日：2025-03-01

申请号：IL31865125

申请日：2025-01-28

Applicant: SANIFIT THERAPEUTICS S A ,  SALCEDO ROCA CAROLINA ,  P?REZ FERRER MAR?A DEL MAR ,  FERRER REYN?S MIQUEL DAVID ,  SERRA COMAS CARME ,  CATENA RUIZ JUAN LORENZO ,  LLEBARIA SOLDEVILA AMADEU ,  PERELL? BESTARD JOAN ,  BASSISSI MOHAMAD FIRAS

Inventor： SALCEDO ROCA CAROLINA ,  P?REZ FERRER MAR?A DEL MAR ,  FERRER REYN?S MIQUEL DAVID ,  SERRA COMAS CARME ,  CATENA RUIZ JUAN LORENZO ,  LLEBARIA SOLDEVILA AMADEU ,  PERELL? BESTARD JOAN ,  BASSISSI MOHAMAD FIRAS

IPC: A61P19/00 ,  A61P43/00 ,  C07C35/16 ,  C07C43/188 ,  C07C43/196

Abstract: The present invention provides IP5 substituted compounds of general formula I, their methods of synthesis and their uses. The IP5 substituted compounds of the invention are characterized for having -O(alkyl)nX, and -O(alkyl)yCy(alkyl)y'-Z chains in positions R1, R2, R4, and R5. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.