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1. 发明申请

WO2011120877A1 ARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES 审中-公开
标题翻译：芳基 - 环己基 - 四氮杂苯并[E]薁
公开(公告)号：WO2011120877A1
公开(公告)日：2011-10-06
申请号：PCT/EP2011/054582
申请日：2011-03-25
申请人： F. HOFFMANN-LA ROCHE AG , DOLENTE, Cosimo , SCHNIDER, Patrick
发明人： DOLENTE, Cosimo , SCHNIDER, Patrick
IPC分类号： C07D487/04 , A61K31/5517 , A61P15/12
CPC分类号： C07D487/04
摘要： The present invention is concerned with aryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I, wherein R 1 , R 2 and R 3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及式I的芳基 - 环己基 - 四氮杂苯并[e]薁，其中R 1，R 2和R 3如本文所述。根据本发明的化合物作为Via受体调节剂，特别是作为Via受体拮抗剂，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑，抑郁障碍，强迫症强迫症，自闭症谱系障碍，精神分裂症和侵略行为。

2. 发明申请

WO2010057795A1 ALKYLCYCLOHEXYLETHERS OF DIHYDROTETRAAZABENZOAZULENES 审中-公开
标题翻译：二氢AA EN ES ES ES ES
公开(公告)号：WO2010057795A1
公开(公告)日：2010-05-27
申请号：PCT/EP2009/064804
申请日：2009-11-09
申请人： F. HOFFMANN-LA ROCHE AG , SCHNIDER, Patrick
发明人： SCHNIDER, Patrick
IPC分类号： C07D487/04 , A61K31/5517 , A61P15/00 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention is concerned with alkylcyclohexylethers of dihydro-tetraazabenzoazulene derivatives, i.e. alkylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene derivatives of formula (I) wherein R 1 , R 2 and R 3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as VIa receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及二氢 - 四氮杂苯并薁衍生物的烷基环己基醚，即式（I）的5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁衍生物的烷基环己基醚，其中R 1，R 2和 R3如本文所述。根据本发明的化合物作为Via受体调节剂，特别是作为VIa受体拮抗剂，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑，抑郁障碍，强迫症强迫症，自闭症谱系障碍，精神分裂症和侵略行为。

3. 发明申请

WO2007054436A2 THIAZOLO[4,5-C]PYRIDINE DERIVATIVES 审中-公开
标题翻译：噻唑并[4,5-C]吡啶衍生物
公开(公告)号：WO2007054436A2
公开(公告)日：2007-05-18
申请号：PCT/EP2006067794
申请日：2006-10-26
申请人： HOFFMANN LA ROCHE , JAESCHKE GEORG , KOLCZEWSKI SABINE , PORTER RICHARD H P , SCHNIDER PATRICK , VIEIRA ERIC
发明人： JAESCHKE GEORG , KOLCZEWSKI SABINE , PORTER RICHARD H P , SCHNIDER PATRICK , VIEIRA ERIC
IPC分类号： C07D513/04 , A61K31/437 , A61P25/04
CPC分类号： C07D513/04
摘要： The invention relates to compounds of general formula (I) wherein R 1 , R 2 and R 3 are as defined in the description as metabotropic glutamate receptor antagonists which are useful in the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1，R 2和R 3是如代表性代谢型谷氨酸的描述中所定义的可用于治疗或预防mGluR5受体介导的病症的受体拮抗剂。

4. 发明申请

WO2006089658A2 NK1 ANTAGONISTS 审中-公开
标题翻译： NK1拮抗剂
公开(公告)号：WO2006089658A2
公开(公告)日：2006-08-31
申请号：PCT/EP2006/001310
申请日：2006-02-14
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN, Torsten , SCHNIDER, Patrick
发明人： HOFFMANN, Torsten , SCHNIDER, Patrick
IPC分类号： C07D213/75 , A61K31/44 , A61P25/18
CPC分类号： C07D213/75 , C07D213/82
摘要： The present invention relates to compounds of the formula (I), wherein R 1 /R 1’ are hydrogen or methyl; X is -C(O)N(CH 3 )- or -N(CH 3 )C(O)-; and to pharmaceutically acceptable acid addition salts thereof for the treatment of numerous inflammatory conditions, migraine, rheumatoid arthritis, asthma, inflammatory bowel disease, mediation of the emetic reflex, Parkinson's disease, anxiety, depression, psychosis, motion sickness, induced vomiting, pain, headache, migraine, Alzheimer's disease, multiple sclerosis, attenuation of morphine withdrawal, cardiovascular changes, oedema, such as oedema caused by thermal injury, chronic inflammatory diseases such as rheumatoid arthritis, asthma/bronchial hyperreactivity and other respiratory diseases including allergic rhinitis, inflammatory diseases of the gut including ulcerative colitis and Crohn's disease, ocular injury and ocular inflammatory diseases, traumatic brain injury, motion sickness, emesis and psychoimmunologic or psychosomatic disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 1，R 2， X是-C（O）N（CH 3） - 或-N（CH 3）C（O） - ; 以及其药学上可接受的酸加成盐，用于治疗许多炎性病症，偏头痛，类风湿性关节炎，哮喘，炎症性肠病，呕吐反射调节，帕金森病，焦虑症，抑郁症，精神病，运动病，诱导性呕吐，疼痛，头痛，偏头痛，阿尔茨海默病，多发性硬化，吗啡戒断减轻，心血管改变，水肿，如热损伤引起的水肿，慢性炎性疾病如类风湿性关节炎，哮喘/支气管高反应性和其他呼吸系统疾病，包括过敏性鼻炎，炎性疾病的肠道，包括溃疡性结肠炎和克罗恩病，眼部损伤和眼部炎症性疾病，创伤性脑损伤，运动病，呕吐和心理免疫或心身疾病。

5. 发明申请

WO2006013050A1 DUAL NK1/NK3 ANTAGONISTS AGAINST SCHIZOPHRENIA 审中-公开
标题翻译：双抗NK1 / NK3抗体针对SCHIZOPHRENIA
公开(公告)号：WO2006013050A1
公开(公告)日：2006-02-09
申请号：PCT/EP2005/008144
申请日：2005-07-27
申请人： F. HOFFMANN-LA ROCHE AG , SCHNIDER, Patrick
发明人： SCHNIDER, Patrick
IPC分类号： A61K31/44
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4436 , A61K31/4439 , A61K31/444 , C07D213/89 , C07D401/04 , C07D409/04
摘要： The present invention relates to the use of compounds of the general formula (I) wherein R 1 is lower alkyl or halogen; R 2 is hydrogen or halogen; R 3 -(CHR') n OH, phenyl, optionally substituted by -(CHR') n OH, or is a saturated, partial saturated or aromatic 5-or 6-membered heterocyclic ring with one heteroatom, selected from the group consisting of-N(R 4 )-, -N=, formula (II), -S- or -S(O) 2 , and which rings are optionally substituted by - (CHR’) n OH ; R’ is independently from “n” hydrogen or - (CH 2 ) n OH; R 4 is hydrogen, -S(O 2 )-lower alkyl or -C(O)-lower alkyl; X is -O-, -CH 2 O-, -S- or a bond; n is 1 or 2; or to pharmaceutically active acid-addition salts thereof, for the preparation of medicaments for the treatment of schizophrenia.
摘要翻译：本发明涉及通式（I）的化合物，其中R

6. 发明申请

WO2011141396A1 HETEROARYL-CYCLOHEXYL-TETRAAZABENZO[E]AZULENES 审中-公开
标题翻译：杂芳基 - 环己基 - 四氮杂苯并[E]薁
公开(公告)号：WO2011141396A1
公开(公告)日：2011-11-17
申请号：PCT/EP2011/057368
申请日：2011-05-09
申请人： F. HOFFMANN-LA ROCHE AG , DOLENTE, Cosimo , SCHNIDER, Patrick
发明人： DOLENTE, Cosimo , SCHNIDER, Patrick
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P9/00 , A61P9/04 , A61P9/12 , A61P1/16 , A61P15/10
CPC分类号： C07D487/04
摘要： The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula (I) wherein R 1 , R 2 and R 3 are as described herein. The compounds according to the invention act as Via receptor modulators, and in particular as Via receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及其中R 1，R 2和R 3如本文所述的式（I）的杂芳基 - 环己基 - 四氮杂苯并[e]薁。根据本发明的化合物作为Via受体调节剂，特别是作为Via受体拮抗剂，它们的制备，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑，抑郁障碍，强迫症强迫症，自闭症谱系障碍，精神分裂症和侵略行为。

7. 发明申请

WO2011128265A1 ARYL - /HETEROARYL - CYCLOHEXENYL - TETRAAZABENZO [E] AZULENES AS VASOPRESSIN ANTAGONISTS 审中-公开
标题翻译： ARYL - / HETEROARYL - 环己酮 - 四氮唑[E]亚油酸酯作为血管紧张素拮抗剂
公开(公告)号：WO2011128265A1
公开(公告)日：2011-10-20
申请号：PCT/EP2011/055516
申请日：2011-04-08
申请人： F. HOFFMANN-LA ROCHE AG , DOLENTE, Cosimo , SCHNIDER, Patrick
发明人： DOLENTE, Cosimo , SCHNIDER, Patrick
IPC分类号： C07D487/04 , A61K31/5517 , A61P15/00 , A61P9/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention is concerned with aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes of formula I wherein R 1 , R 2 and R 3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
摘要翻译：本发明涉及式I的芳基 - 杂芳基 - 环己烯基 - 四氮杂苯并[e]薁，其中R 1，R 2和R 3如本文所述。根据本发明的化合物作为V1a受体调节剂，特别是作为V1a受体拮抗剂，它们的制造，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用作在痛经，男性或女性性功能障碍，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，焦虑，抑郁障碍，强迫症强迫症，自闭症谱系障碍，精神分裂症和侵略行为。

8. 发明申请

WO2008068183A1 INDOLES 审中-公开
标题翻译：吲哚
公开(公告)号：WO2008068183A1
公开(公告)日：2008-06-12
申请号：PCT/EP2007/062983
申请日：2007-11-29
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , MASCIADRI, Raffaello , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D401/04 , C07D413/14 , A61K31/404 , A61P29/00
CPC分类号： C07D401/04 , C07D413/14
摘要： The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders 5 and other diseases. Present invention is concerned with compounds of the general formula (I), A: (a), (b), (c) wherein R 1 to R 6 , R 8 to R 14 , R 12' , R 13' , X and Y are as defined in the specification.
摘要翻译：本发明涉及作为V1a受体拮抗剂的新的吲哚-2-基 - 羰基 - 哌啶衍生物，其制备方法，含有它们的药物组合物及其作为药物的用途。本发明的活性化合物可用于预防和/或治疗焦虑和抑郁障碍5及其它疾病。本发明涉及通式（I）的化合物：A：（a），（b），（c）其中R 1至R 6， R 8，R 14，R 12，R 13，X和Y如说明书中所定义。

9. 发明申请

WO2007113155A1 PROCESS FOR PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC Β-ARYL OR HETEROARYL CARBOXYLIC ACIDS 审中-公开
标题翻译：制备环境友好型循环型马来酰亚胺或羟基羧酸的方法
公开(公告)号：WO2007113155A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/052855
申请日：2007-03-26
申请人： F. HOFFMANN-LA ROCHE AG , BACHMANN, Stephan , SCALONE, Michelangelo , SCHNIDER, Patrick
发明人： BACHMANN, Stephan , SCALONE, Michelangelo , SCHNIDER, Patrick
IPC分类号： C07D211/60 , C07D207/16
CPC分类号： C07C51/36 , C07D207/16 , C07D211/60 , C07D401/04
摘要： The present invention relates to a process for the preparation of cis substituted cyclic β- aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme (Formula I, II) wherein X is -C(R)(R')-, -N(R")-, -O-, -S(O)0-, C(O)N(R"), -N(R")C(O)- or -C(O)-; R and R' are independently from each other hydrogen, C 1-7 -alkyl, C 1-7 -alkyl substituted by halogen, C 1-7 -alkoxy, hydroxy or -(CH 2 ) P -Ar; R" is hydrogen, C 1-7 -alkyl, C 1-7 -alkyl substituted by halogen, -S(O) 0 -C 1-7 -alkyl, -S(O) 0 -Ar, -S(O) 0 -NRR', -(CH 2 ) P -Ar, -C(O)-C 1-7 -alkyl, -C(O)-Ar, -C(O)-NRR' or -C(O)O-C 1-7 -alkyl; Ar is aryl 1 or heteroaryl 1 ; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; o is 0, 1 or 2; p is 0, 1, or 2; and corresponding salts thereof.
摘要翻译：本发明涉及按照以下方案（式I，II）通过对映选择性氢化制备具有高非对映选择性的顺式取代的环状β-芳基或杂芳基羧酸衍生物的方法，其中X是-C（R ）（R'） - ， - （R“） - ， - O - ， - S（O）O-，C（O）N（R” C（O） - ; R和R'彼此独立地为氢，C 1-7 - 烷基，被卤素取代的C 1-7 - 羟基或 - （CH 2）n -Ar; R“是氢，C 1-7 - 烷氧基， C 1 -C 6烷基，C 1-4烷基，被卤素取代的C 1-7 - 烷基，-S（O）0 -C 1-7 - 烷基，-S（O）O -Ar，-S（O）NRR 2 - ， - （CH 2） -C（O）-C 1-7 - 烷基，-C（O）-Ar，-C（O）-NRR'或-C（O）OC _{1-7 - 烷基; Ar是芳基，或杂芳基; n为0,1,2或3; m为0,1,2或3; o为0,1或2; p为0,1或2; 及其相应的盐。}

10. 发明申请

WO2007077122A1 INDOL-3-YL-CARBONYL-SPIRO-PIPERIDINE DERIVATIVES 审中-公开
标题翻译：吲哚-3-基 - 碳 - 螺 - 哌啶衍生物
公开(公告)号：WO2007077122A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/069897
申请日：2006-12-19
申请人： F. HOFFMANN-LA ROCHE AG , BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
发明人： BISSANTZ, Caterina , GRUNDSCHOBER, Christophe , RATNI, Hasane , ROGERS-EVANS, Mark , SCHNIDER, Patrick
IPC分类号： C07D471/10 , C07D498/10 , A61K31/438 , A61P9/02
CPC分类号： C07D471/10
摘要： This invention relates to indol-3-yl-carbonyl-spiro-piperidine derivatives which act as V1a receptor antagonists and which are represented by Formula (I) wherein the spiropiperidine-head group A and the residues R 1 , R 2 and R 3 are as defined herein. The invention further relates to pharmaceutical compositions containing such compounds, their use in medicaments against dysmenorrhea, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, obsessive compulsive disorder, anxiety and depressive disorders, and methods of preparation thereof.
摘要翻译：本发明涉及作为V1a受体拮抗剂的吲哚-3-基 - 羰基 - 螺 - 哌啶衍生物，其由式（I）表示，其中spiropiperidine-head基团A和残基R 1 R 2和R 3如本文所定义。本发明还涉及含有这些化合物的药物组合物，其用于抗痛经，高血压，慢性心力衰竭，不适当的血管加压素分泌，肝硬化，肾病综合征，强迫症，焦虑和抑郁障碍的药物中的用途及其制备方法。

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