会员体验
专利管家（专利管理）
工作空间（专利管理）
风险监控（情报监控）
数据分析（专利分析）
侵权分析（诉讼无效）
联系我们
交流群
官方交流：
QQ群： 891211   
微信请扫码    >>>
现在联系顾问~
下载
著录项
PDF全文
热词
    • 8. 发明公开
      EP2346834A1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 有权
    • 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES
    • 3-氨基 - 吲唑或3-氨基-4,5,6,7-四氢 - 吲唑衍生物
    • EP2346834A1
    • 2011-07-27
    • EP09783046.7
    • 2009-09-15
    • F.Hoffmann-La Roche AG
    • BENSON, Gregory, Martin , BLEICHER, Konrad , FENG, Song , GRETHER, Uwe , KUHN, Bernd , MARTIN, Rainer, E. , PLANCHER, Jean-Marc , RICHTER, Hans , RUDOLPH, Markus , TAYLOR, Sven
    • C07D231/56 , A61K31/416 , A61P3/06 , A61P3/10 , C07D401/12 , C07D407/12
    • C07D231/56 , C07D401/12 , C07D407/12
    • This invention relates to novel indazole derivatives of formula (I), wherein R
      1 to R
      7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be use as medicaments. The compounds are selective modulators of the farnesoid-X-receptor, preferably agonists u j[ιe farnesoid-X-receptor (FXR) is a member of the nuclear hormone receptor superfamily of transcription factors. Diseases which are affected by FXR modulators include increased lipid and cholesterol levels, particularly high LDL-cholesterol, high triglycerides, low HDL-cholesterol, dyslipidemia, diseases of cholesterol absorption, atherosclerotic disease, peripheral occlusive disease, ischemic, stroke, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, diabetic nephropathy, obesity, cholesterol gallstone disease, cholestasis/fibrosis of the liver, non alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), psoriasis, cancer, particularly gastrointestinal cancer, osteoporosis, Parkinson's disease and Alzheimer's disease. Preferred diseases (and conditions) which are affected by FXR modulators are prevention or treatment of high LDL cholesterol levels high triglycerides, dyslipidemia, cholesterol gallstone disease, cancer, non-insulin dependent diabetes mellitus and metabolic syndrome. Particularly preferred diseases which arc affected by FXR modulators arc high LDL cholesterol, high triglyceride levels and dyslipidemia.
    • 本发明涉及式（I）的新型吲唑衍生物，其中R 1至R 7如说明书和权利要求书中所定义，及其生理上可接受的盐。 这些化合物是FXR调节剂，可用作药物。 该化合物是法尼醇-X-受体的选择性调节剂，优选激动剂，其中法尼醇-X-受体（FXR）是转录因子核激素受体超家族的成员。 受FXR调节剂影响的疾病包括增加的脂质和胆固醇水平，特别是高LDL-胆固醇，高甘油三酯，低HDL-胆固醇，血脂异常，胆固醇吸收疾病，动脉粥样硬化疾病，外周阻塞病，局部缺血，中风，糖尿病，特别是非 胰岛素依赖性糖尿病，代谢综合征，糖尿病肾病，肥胖症，胆固醇胆结石病，肝胆汁淤积/纤维化，非酒精性脂肪性肝炎（NASH），非酒精性脂肪肝病（NAFLD），牛皮癣，癌症，特别是胃肠癌， 骨质疏松症，帕金森病和阿尔茨海默病。 受FXR调节剂影响的优选疾病（和条件）是预防或治疗高LDL胆固醇水平高甘油三酯，血脂异常，胆固醇胆石病，癌症，非胰岛素依赖型糖尿病和代谢综合征。 特别优选的受FXR调节剂影响的疾病是高LDL胆固醇，高甘油三酯水平和血脂异常。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明公开
      EP2922540A1 SUBSTITUTED 1,6-NAPHTHYRIDINES 审中-公开
    • SUBSTITUTED 1,6-NAPHTHYRIDINES
    • 替代物1,6-萘啶
    • EP2922540A1
    • 2015-09-30
    • EP13795705.6
    • 2013-11-18
    • F.Hoffmann-La Roche AG
    • CECCARELLI, Simona, M. , JAGASIA, Ravi , JAKOB-ROETNE, Roland , MARTIN, Rainer, E. , PETERS, Jens-Uwe , WICHMANN, Juergen
    • A61K31/4375 , A61P25/24 , A61P25/28 , A61P25/30
    • C07D471/04 , A61K31/4375 , A61K31/444 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541
    • The present invention relates to the use of compounds of general formula wherein R′ is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)—NH-lower alkyl, CH2—C(O)—NH-lower alkyl, CH2—NH—C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH—S(O)2—CH3, —(CH2)m—O-lower alkyl or —(CH2)n—S(O)2—CH3; or is —(CR2)n-phenyl, optionally substituted by —S(O)2CH3 or lower alkoxy; or is —(CH2)n-heterocycloalkyl, optionally substituted by lower alkyl and ═O; or is —(CH2)n-heteroaryl, optionally substituted by one or two lower alkyl groups; or is —(CH2)n-cycloalkyl, optionally substituted by cyano; or R2 and R3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1,1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson's disease, dementia, Alzheimer's disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.
    • 本发明涉及通式化合物的用途，其中R'是氢或低级烷基; R1是卤素，低级烷基，环烷基或氰基; 或者为被卤素取代的低级烷基，被低级烷氧基取代的低级烷氧基，卤素，氰基，氰基，羟基，C（O）-NH-低级烷基，CH 2 - C（O）-NH-低级烷基，CH 2 -NH-C（O） - 低级烷基，CH 2 NH 2，S（O）2 CH 3，S（O）2 N（CH 3）2或杂环烷基; 或是任选被低级烷基取代的吡唑-1,4或5-基; 或是任选被一个或两个低级烷基取代的噻唑-5-基; 或任选被低级烷基，低级烷氧基，卤素或N（CH 3）2取代的吡啶2,3或4-基; 或是3,6-二氢-2H-吡喃; 或者是苯并[d] [1,3]二氧杂环戊烯-5-基; 或是2,3-二氢苯并[b] [1,4]二恶英-6-基; R2是氢，被烷氧基取代的低级烷基或低级烷基; R 3是氢，低级烷基，被卤素取代的低级烷基，被羟基取代的低级烷基，NH-S（O）2 -CH 3， - （CH 2）m -O-低级烷基或 - （CH 2）n -S（O） 2-CH 3; 或是 - （CR 2）n - 苯基，任选被-S（O）2 CH 3或低级烷氧基取代; 或是 - （CH 2）n - 杂环烷基，任选地被低级烷基取代和= = O; 或是 - （CH 2）n - 杂芳基，任选被一个或两个低级烷基取代; 或为 - （CH 2）n - 环烷基，任选被氰基取代; 或R 2和R 3与它们所连接的N原子一起形成杂环，该杂环选自吗啉，哌啶，1,1-二氧代硫代吗啉或哌嗪，其可被低级烷基或C（O）O-低级烷基取代 ，或可形成任选被羟基取代的吡咯烷环; R独立地为氢或低级烷基; n为0,1,2,3; m为2; 或其药学上可接受的酸加成盐与外消旋混合物或其相应的对映体和/或光学异构体反应，用于治疗精神分裂症，强迫症人格障碍，抑郁症，双相性精神障碍，焦虑症，正常老化，癫痫， 视网膜变性，创伤性脑损伤，脊髓损伤，创伤后应激障碍，惊恐障碍，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱发的认知功能障碍（“chemobrain”），唐氏综合征，自闭症谱系障碍， 听力损失，耳鸣，脊髓小脑性共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿舞蹈病，中风以及由于放射治疗引起的干扰，慢性应激，视神经病变或黄斑变性，或滥用选自酒精，阿片剂，甲基苯丙胺的神经活性药物 ，苯环利定或可卡因。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
每页展示10个专利
每页展示10个专利
每页展示20个专利
每页展示50个专利
每页展示100个专利

IPRDB

最新中国发明专利 最新美国发明专利 技术领域 专利库 专利分类库 国际专利分类库

热门服务

会员版试用 API 数据接口 找代理 知嘟嘟专利交易 排行榜 大学排行榜 专利百科

关于我们

平台介绍 战略合作 网站地图

友情链接

知嘟嘟专利交易 国家知识产权局 中国商标网

联系方式


©2019-2023 上海吉码数字技术有限公司 版权所有，并保留所有权利 沪ICP备20016256号-6 沪公网安备31011702005475号