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1. 发明授权

US09809599B2 Aryl-quinoline derivatives 有权
公开(公告)号：US09809599B2
公开(公告)日：2017-11-07
申请号：US14938005
申请日：2015-11-11
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Aurelia Conte , Holger Kuehne , Bernd Kuhn , Werner Neidhart , Ulrike Obst Sander , Markus Rudolph
IPC分类号： C07D215/00 , C07D215/02 , C07D215/54 , C07D401/04 , C07D413/04 , C07D491/048 , C07D401/14 , C07D215/227 , C07D413/14
CPC分类号： C07D491/048 , C07D215/00 , C07D215/02 , C07D215/227 , C07D215/54 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

2. 发明申请

US20150259334A1 BENZISOXAZOLES 有权
标题翻译：苯唑沙司
公开(公告)号：US20150259334A1
公开(公告)日：2015-09-17
申请号：US14602541
申请日：2015-01-22
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： C07D413/14 , C07D231/12 , C07D401/04 , C07D413/04
CPC分类号： C07D413/14 , C07D231/12 , C07D401/04 , C07D413/04
摘要： The present invention relates to compounds of general formula wherein Ar1/Ar2 are phenyl or a 5 or 6-membered heteroaryl; R1/R2 is hydrogen, halogen, lower alkyl, CF3 or lower alkoxy; n,m are 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, with the exception of the compound 2,1-benzisoxazole, 3-(4-chlorophenyl)-5-(1-phenyl-1H-pyrazol-5 -yl)-. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major 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, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式的化合物，其中Ar 1 / Ar 2是苯基或5或6元杂芳基; R1 / R2是氢，卤素，低级烷基，CF3或低级烷氧基; n，m为1或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异构体和/或光学异构体反应，除了化合物2,1-苯并异恶唑，3-（4-氯苯基）-5-（1- 苯基-1H-吡唑-5-基） - 。这些化合物可用于治疗精神分裂症，强迫症人格障碍，重性抑郁症，双相障碍，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，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

3. 发明申请

US20150203472A1 BENZIMIDAZOLES AS CNS ACTIVE AGENTS 有权
标题翻译：苯并咪唑作为CNS活性剂
公开(公告)号：US20150203472A1
公开(公告)日：2015-07-23
申请号：US14675404
申请日：2015-03-31
申请人： HOFFMANN-LA ROCHE INC.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： C07D403/04 , C07D401/14
CPC分类号： C07D403/04 , C07D401/14
摘要： The present invention relates to compounds of general formula wherein R1 hydrogen, lower alkyl, halogen or lower alkyl substituted by halogen; R2 is hydrogen or halogen; X1 is N or CH; X2 is N or CH; with the proviso that only one of X1 or X2 is N; X3 is C(R) or N; and R is hydrogen, lower alkyl, halogen, lower alkyl substituted by halogen, lower alkoxy or SO2-lower alkyl; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major 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, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：本发明涉及通式的化合物，其中R 1为氢，低级烷基，卤素或被卤素取代的低级烷基; R2是氢或卤素; X1是N或CH; X2是N或CH; 条件是X1或X2中仅有一个为N; X3是C（R）或N; R为氢，低级烷基，卤素，被卤素取代的低级烷基，低级烷氧基或SO 2 - 低级烷基; 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。这些化合物可用于治疗精神分裂症，强迫症人格障碍，重性抑郁症，双相障碍，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，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

4. 发明申请

US20130116234A1 ARYL-QUINOLINE DERIVATIVES 有权
标题翻译：芳基喹啉衍生物
公开(公告)号：US20130116234A1
公开(公告)日：2013-05-09
申请号：US13666202
申请日：2012-11-01
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Aurelia Conte , Holger Kuehne , Bernd Kuhn , Werner Neidhart , Ulrike Obst Sander , Markus Rudolph
IPC分类号： A61K31/4709 , A61K31/47 , C07D413/14 , C07D401/14 , C07D215/54 , C07D401/04 , A61K31/5377 , C07D413/04
CPC分类号： C07D491/048 , C07D215/00 , C07D215/02 , C07D215/227 , C07D215/54 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
摘要翻译：本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所述，包括该化合物的组合物和使用该化合物的方法。本发明化合物可用作脂肪酸结合蛋白（FABP）4和/或5抑制剂，可用于治疗或预防脂肪营养不良，2型糖尿病，血脂异常，动脉粥样硬化，涉及炎症，脂肪变性和/或纤维化的肝脏疾病，如非酒精性脂肪性肝病，特别是非酒精性脂肪性肝炎，代谢综合征，肥胖，慢性炎性和自身免疫性炎性疾病。

5. 发明授权

US09440962B2 Benzisoxazoles 有权
标题翻译：苯并恶唑
公开(公告)号：US09440962B2
公开(公告)日：2016-09-13
申请号：US14602541
申请日：2015-01-22
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Juergen Wichmann
IPC分类号： A61K31/41 , C07D413/14 , C07D413/04 , C07D231/12 , C07D401/04
CPC分类号： C07D413/14 , C07D231/12 , C07D401/04 , C07D413/04
摘要： The present invention relates to compounds of general formula wherein Ar1/Ar2 are phenyl or a 5 or 6-membered heteroaryl; R1/R2 is hydrogen, halogen, lower alkyl, CF3 or lower alkoxy; n,m are 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, with the exception of the compound 2,1-benzisoxazole, 3-(4-chlorophenyl)-5-(1-phenyl-1H-pyrazol-5 -yl)-. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major 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, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine.
摘要翻译：这些化合物可用于治疗精神分裂症，强迫症人格障碍，重症抑郁症，双相障碍，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，恐慌症，帕金森病，痴呆，阿尔茨海默病，轻度认知障碍，化疗诱导的认知功能障碍，唐氏综合征，自闭症谱系障碍，听力损失，耳鸣，脊髓小脑共济失调，肌萎缩性侧索硬化，多发性硬化，亨廷顿氏病，中风，放射治疗，慢性压力，滥用神经活性药物，如酒精，阿片剂，甲基苯丙胺，苯环利定和可卡因。

6. 发明授权

US09278918B2 Urea derivatives and their use as fatty-acid binding protein (FABP) inhibitors 有权
标题翻译：尿素衍生物及其作为脂肪酸结合蛋白（FABP）抑制剂的用途
公开(公告)号：US09278918B2
公开(公告)日：2016-03-08
申请号：US14857007
申请日：2015-09-17
申请人： Hoffmann-La Roche Inc.
发明人： Bernd Buettelmann , Simona M. Ceccarelli , Aurelia Conte , Holger Kuehne , Bernd Kuhn , Werner Neidhart , Ulrike Obst Sander , Hans Richter
IPC分类号： C07C275/28 , C07C273/18 , G01N33/53
CPC分类号： C07C275/28 , C07C273/1863 , C07C275/30 , C07C2601/02 , C07C2601/04 , C07C2601/08 , G01N33/5304
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, W, A and B are as described herein, compositions including the compounds and methods of using the compounds.
摘要翻译：本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，W，A和B如本文所述，包括该化合物的组合物和使用该化合物的方法。

7. 发明申请

US20160060270A1 New Aryl-Quinoline Derivatives 有权
标题翻译：新型芳基 - 喹啉衍生物
公开(公告)号：US20160060270A1
公开(公告)日：2016-03-03
申请号：US14938005
申请日：2015-11-11
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Aurelia Conte , Holger Kuehne , Bernd Kuhn , Werner Neidhart , Ulrike Obst Sander , Markus Rudolph
IPC分类号： C07D491/048 , C07D413/14 , C07D401/14 , C07D215/54 , C07D401/04
CPC分类号： C07D491/048 , C07D215/00 , C07D215/02 , C07D215/227 , C07D215/54 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
摘要翻译：本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所述，包括该化合物的组合物和使用该化合物的方法。本发明化合物可用作脂肪酸结合蛋白（FABP）4和/或5抑制剂，可用于治疗或预防脂肪营养不良，2型糖尿病，血脂异常，动脉粥样硬化，涉及炎症，脂肪变性和/或纤维化的肝脏疾病，如非酒精性脂肪性肝病，特别是非酒精性脂肪性肝炎，代谢综合征，肥胖，慢性炎性和自身免疫性炎性疾病。

8. 发明授权

US09199938B2 Aryl-quinoline derivatives 有权
标题翻译：芳基 - 喹啉衍生物
公开(公告)号：US09199938B2
公开(公告)日：2015-12-01
申请号：US13666202
申请日：2012-11-01
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Aurelia Conte , Holger Kuehne , Bernd Kuhn , Werner Neidhart , Ulrike Obst Sander , Markus Rudolph
IPC分类号： C07D413/14 , C07D401/14 , C07D215/54 , C07D401/04 , C07D413/04 , C07D215/227 , C07D215/00 , C07D215/02 , C07D491/048
CPC分类号： C07D491/048 , C07D215/00 , C07D215/02 , C07D215/227 , C07D215/54 , C07D401/04 , C07D401/14 , C07D413/04 , C07D413/14
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.
摘要翻译：本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所述，包括该化合物的组合物和使用该化合物的方法。本发明化合物可用作脂肪酸结合蛋白（FABP）4和/或5抑制剂，可用于治疗或预防脂肪营养不良，2型糖尿病，血脂异常，动脉粥样硬化，涉及炎症，脂肪变性和/或纤维化的肝脏疾病，如非酒精性脂肪性肝病，特别是非酒精性脂肪性肝炎，代谢综合征，肥胖，慢性炎性和自身免疫性炎性疾病。

9. 发明申请

US20140323462A1 AZETIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 有权
标题翻译： AZETIDINE化合物，组合物和使用方法
公开(公告)号：US20140323462A1
公开(公告)日：2014-10-30
申请号：US14328033
申请日：2014-07-10
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Carine Guerot , Henner Knust
IPC分类号： C07D487/10 , C07D487/04 , C07D205/12
CPC分类号： C07D487/10 , C07D205/12 , C07D487/04
摘要： Provided are compounds of Formula I, R1-L1-A-L2-R2 (I), and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein A, L1, L2, R1 and R2 are defined herein. The present invention also provides a pharmaceutical composition and methods of using such compounds. The compounds are useful for therapy and/or prophylaxis in a patient, and in particular to inhibitors of Soluble Epoxide Hydrolase (sEH).
摘要翻译：提供式I，R1-L1-A-L2-R2（I）的化合物及其立体异构体，互变异构体及其药学上可接受的盐，其中A，L1，L2，R1和R2如本文所定义。本发明还提供药物组合物和使用这些化合物的方法。该化合物可用于患者的治疗和/或预防，特别是可溶性环氧化物水解酶（sEH）的抑制剂。

10. 发明授权

US09586903B2 Isoquinoline derivatives 有权
公开(公告)号：US09586903B2
公开(公告)日：2017-03-07
申请号：US14926387
申请日：2015-10-29
申请人： Hoffmann-La Roche Inc.
发明人： Simona M. Ceccarelli , Ravi Jagasia , Roland Jakob-Roetne , Rainer E. Martin , Juergen Wichmann
IPC分类号： C07D217/14 , C07D405/12 , A61K9/00 , A61K9/20 , A61K9/48 , A61K47/10 , C07D401/06 , C07D401/12 , C07D405/04 , C07D417/06 , C07D217/26 , C07D401/04 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K31/472 , A61K31/4725
CPC分类号： C07D217/14 , A61K9/0019 , A61K9/2018 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K47/10 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D417/06
摘要： The present invention relates to the use of compounds of general formula wherein R1 is phenyl or pyridinyl, which are optionally substituted by halogen, cyano or lower alkyl substituted by halogen, or is dihydro-pyran-4-yl; R2 is hydrogen or lower alkyl; R3 is —(CHR)n-phenyl, optionally substituted by lower alkoxy or S(O)2-lower alkyl, or is heterocycloalkyl, optionally substituted by ═O and lower alkyl, or is —(CH2)n-five or six membered heteroaryl, optionally substituted by lower alkyl, or is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —NR—S(O)2-lower alkyl, —(CH2)n-cycloalkyl or —(CH2)n—S(O)2-lower alkyl; or R2 and R3 form together with the N-atom to which they are attached a heterocycloalkyl ring, selected from the group consisting of 1,1-dioxo-thiomorpholinyl, morpholinyl, or pyrrolidinyl, optionally substituted by hydroxyl; R is hydrogen or lower alkyl; n is 0, 1 or 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, such as alcohol, opiates, methamphetamine, phencyclidine or cocaine.

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