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公开(公告)号：US20090176819A1
公开(公告)日：2009-07-09
申请号：US12273917
申请日：2008-11-19
IPC分类号： C07D491/052 , A61K31/436 , A61P35/00
CPC分类号： C07D498/18
摘要： The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39-methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及新的39-脱甲氧基-39-甲基雷帕霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-脱甲氧基-39-甲基雷帕霉素衍生物在治疗癌症和/或B细胞恶性肿瘤中的应用，诱导或维持免疫抑制，移植排斥治疗，移植物抗 - 宿主病，自身免疫性疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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2.发明申请36-Des(3-Methoxy-4-Hydroxycyclohexyl) 36-(3-Hydroxycycloheptyl) Derivatives of Rapamycin for the Treatment of Cancer and Other Disorders 审中-公开用于治疗癌症和其他疾病的雷帕霉素36-去（3-甲氧基-4-羟基环己基）36-（3-羟基环庚基）衍生物公开(公告)号：US20090209572A1
公开(公告)日：2009-08-20
申请号：US12273990
申请日：2008-11-19
IPC分类号： A61K31/436 , C07D491/153
CPC分类号： C07D493/18
摘要： The present invention relates to novel 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 36-des(3-methoxy-4-hydroxycyclohexyl)-36-(3-hydroxycycloheptyl)rapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及新的36-des（3-甲氧基-4-羟基环己基）-36-（3-羟基环庚基）雷帕霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些36-des（3-甲氧基-4-羟基环己基）-36-（3-羟基环庚基）雷帕霉素衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导 或维持免疫抑制，移植排斥，移植物抗宿主病，自身免疫性疾病，炎症疾病，血管疾病和纤维化疾病的治疗，刺激神经元再生或治疗真菌感染。
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公开(公告)号：US20100081682A1
公开(公告)日：2010-04-01
申请号：US12630251
申请日：2009-12-03
申请人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
发明人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
IPC分类号： A61K31/436
CPC分类号： C07D498/18
摘要： The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及39-去甲氧基嘧啶霉素衍生物及其用途。 本发明提供了这些化合物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症疾病，血管 疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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公开(公告)号：US08008318B2
公开(公告)日：2011-08-30
申请号：US12630251
申请日：2009-12-03
申请人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
发明人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
IPC分类号： A61P35/00
CPC分类号： C07D498/18
摘要： The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及39-去甲氧基嘧啶霉素衍生物及其用途。 本发明提供了这些化合物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症疾病，血管 疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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公开(公告)号：US07648996B2
公开(公告)日：2010-01-19
申请号：US11908250
申请日：2006-03-10
申请人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
发明人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
IPC分类号： C07D498/18 , A61K31/436
CPC分类号： C07D498/18
摘要： The present invention relates to novel 39-desmethoxyrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxyrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及新型的39-去甲氧基嘧啶霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-去甲氧基丙酰胺衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫的治疗 疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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6.发明申请公开(公告)号：US20090209494A1
公开(公告)日：2009-08-20
申请号：US12094240
申请日：2006-12-22
申请人： Christine Janet Martin , Barrie Wilkinson , Sabine Gaisser , Ming-Oiang Zhang , Rose Mary Sheridan , Lesley Sarah Sheehan , Rachel Edith Lill , Mohammed Nur-E-Alam , William Alexander Vousden
发明人： Christine Janet Martin , Barrie Wilkinson , Sabine Gaisser , Ming-Oiang Zhang , Rose Mary Sheridan , Lesley Sarah Sheehan , Rachel Edith Lill , Mohammed Nur-E-Alam , William Alexander Vousden
IPC分类号： A61K31/66 , C12P17/10 , C12N1/21 , A61K31/395 , A61K31/4745 , A61K31/175 , A61K31/135 , C07D225/06
CPC分类号： C07D225/06
摘要： The present invention relates to 21-deoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and or prophylaxis of cancer or B-cell malignancies.
摘要翻译： 本发明涉及21-脱氧山梨醇类似物，其可用于，例如， 在治疗癌症，B细胞恶性肿瘤，疟疾，真菌感染，中枢神经系统疾病和神经变性疾病，依赖于血管生成的疾病，自身免疫性疾病或作为癌症的预防性预处理。 本发明还提供了这些化合物的制备方法及其在医药中的用途，特别是治疗和/或预防癌症或B细胞恶性肿瘤的方法。
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公开(公告)号：US07897608B2
公开(公告)日：2011-03-01
申请号：US12273917
申请日：2008-11-19
IPC分类号： C07D498/18 , A61K31/436
CPC分类号： C07D498/18
摘要： The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39 -methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及新的39-脱甲氧基-39-甲基雷帕霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-脱甲氧基-39-甲基雷帕霉素衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥治疗，移植物抗 - 宿主病，自身免疫性疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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公开(公告)号：US20080188511A1
公开(公告)日：2008-08-07
申请号：US11908250
申请日：2006-03-10
申请人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
发明人： Christoph Hendrik Beckmann , Steven James Moss , Rose Mary Sheridan , Mingqiang Zhang , Barrie Wilkinson
IPC分类号： A61K31/436 , C07D498/18 , A61P35/04
CPC分类号： C07D498/18
摘要： The present invention relates to novel 39-desmethoxyrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxyrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.
摘要翻译： 本发明涉及新型的39-去甲氧基嘧啶霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-去甲氧基丙酰胺衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫的治疗 疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。
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公开(公告)号：US08207167B2
公开(公告)日：2012-06-26
申请号：US13063950
申请日：2009-09-18
申请人： Iain Robert Greig , Rose Mary Sheridan , Raymond Fisher , Matthew John Tozer , Juha Andrew Clase , Andrew Smith , Andrew Robert Tuffnell , Robert Jurgen Van 't Hof
发明人： Iain Robert Greig , Rose Mary Sheridan , Raymond Fisher , Matthew John Tozer , Juha Andrew Clase , Andrew Smith , Andrew Robert Tuffnell , Robert Jurgen Van 't Hof
IPC分类号： A61K31/5375 , A61K31/18 , C07D265/30 , C07C311/01
CPC分类号： C07D303/36 , C07C311/21 , C07C311/39 , C07C2601/02 , C07D239/26 , C07D239/30 , C07D263/20 , C07D295/135
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumor, etc.
摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些芳基 - 苯基 - 亚磺酰氨基 - 亚苯基化合物（本文统称为“APSAP化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体瘤等。
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公开(公告)号：US20110190302A1
公开(公告)日：2011-08-04
申请号：US13063950
申请日：2009-09-18
申请人： Iain Robert Greig , Rose Mary Sheridan , Raymond Fisher , Matthew John Tozer , Juha Andrew Clase , Andrew Smith , Andrew Robert Tuffnell , Robert Jurgen Van 't Hof
发明人： Iain Robert Greig , Rose Mary Sheridan , Raymond Fisher , Matthew John Tozer , Juha Andrew Clase , Andrew Smith , Andrew Robert Tuffnell , Robert Jurgen Van 't Hof
IPC分类号： A61K31/5375 , C07C311/21 , C07D303/36 , C07D295/135 , C07C255/58 , C07D263/14 , A61K31/18 , A61K31/245 , A61K31/196 , A61K31/336 , A61K31/421 , A61P29/00 , A61P19/02 , A61P17/06 , A61P11/00 , A61P9/10 , A61P35/00 , A61P35/02 , A61P19/08 , A61P19/10
CPC分类号： C07D303/36 , C07C311/21 , C07C311/39 , C07C2601/02 , C07D239/26 , C07D239/30 , C07D263/20 , C07D295/135
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-phenylene compounds of the following formula (I) (collectively referred to herein as “APSAP compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc.
摘要翻译： 本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些芳基 - 苯基 - 亚磺酰氨基 - 亚苯基化合物（本文统称为“APSAP化合物”）。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内在治疗例如炎症和/或关节破坏和/或骨丢失中的用途; 由免疫系统的过度和/或不适当和/或延长的激活介导的疾病; 炎性和自身免疫性疾病，例如类风湿性关节炎，牛皮癣，牛皮癣关节炎，慢性阻塞性肺病（COPD），动脉粥样硬化，炎性肠病，强直性脊柱炎等; 与骨丢失相关的疾病，例如与类风湿性关节炎中的过度破骨细胞活性相关的骨丢失，骨质疏松症，癌症相关的骨病，佩吉特氏病等; 和癌症，如血液恶性肿瘤，实体瘤等。
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