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![(PYRIDO/THIENO)-[f]-OXAZEPINE-5-ONE DERIVATIVES](/abs-image/US/2009/06/25/US20090163473A1/abs.jpg.150x150.jpg)
公开(公告)号：US20090163473A1
公开(公告)日：2009-06-25
申请号：US12389968
申请日：2009-02-20
IPC分类号： A61K31/553 , A61P25/24 , A61P25/28
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R 4和R 5独立地为H或（C 1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素 和氧代; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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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：US20080139529A1
公开(公告)日：2008-06-12
申请号：US11924451
申请日：2007-10-25
IPC分类号： A61K31/553 , A61P25/00
CPC分类号： C07D515/04
摘要： The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or S02; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
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14.发明申请公开(公告)号：US20180319714A1
公开(公告)日：2018-11-08
申请号：US15773768
申请日：2016-06-17
申请人： Mingqiang Zhang
发明人： Mingqiang Zhang
CPC分类号： C05F7/005 , C05F17/00 , C05F17/0018 , C05G3/04 , Y02W30/43
摘要： A micro-carbon bio-fertilizer for rapidly increasing a soil granular structure and a preparation method thereof are provided. The formula composition of the micro-carbon bio-fertilizer by mass percentage is: 30-60% of micro carbons, and 40-70% of plant fibers. The preparation process includes is that: preparation of raw materials; filtration and purification of the raw materials; biodegradation; canning of semi-finished product; dispensing and mixing; sedimentation and achievement of finished product. The macromolecular carbohydrates contained in the industrial wastewater rich in organic matters are activated into micro carbons of 100 μm in average through biotechnologies. The micro carbons have natural affinity with soil and split the soil into small particles which are gathered to form a granular structure. Such a granular structure mitigates the degree of soil hardening and acidification, while quickly increasing soil fertility and improving crop quality and yield.
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![(Pyrido/thieno)-[f]-oxazepine-5-one derivatives](/abs-image/US/2011/10/11/US08034804B2/abs.jpg.150x150.jpg)
公开(公告)号：US08034804B2
公开(公告)日：2011-10-11
申请号：US12389968
申请日：2009-02-20
IPC分类号： A61K31/553 , A61P25/28
CPC分类号： C07D498/14
摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4)-alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R4和R5独立地是H或（C1-4） - 烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4） - 烷氧基，羟基，卤素 和氧代; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。
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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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18.发明授权公开(公告)号：US07504390B2
公开(公告)日：2009-03-17
申请号：US11924451
申请日：2007-10-25
CPC分类号： C07D515/04
摘要： The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.
摘要翻译： 本发明涉及具有通式I的苯并氧氮杂衍生物，其中X代表CO或SO2; R1，R2，R3和R4独立地选自H，（C1-4）烷基，（C1-4）烷氧基，（C1-4）烷氧基（C1-4）烷基，卤素，硝基，氰基，NR8R9，NR8COR10， 并且CONR 8 R 9，R 5，R 6和R 7独立地为H或（C 1-4）烷基; R8和R9独立地为H或（C1-4）烷基; 或R8和R9与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有另外选自O，S或NR11的杂原子; R 10为（C 1-4）烷基; R11为（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，羟基，卤素和 氧代 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些苯并恶氮平衍生物在治疗神经系统疾病和精神病学障碍中的应用，所述神经疾病和精神疾病对中枢神经系统中AMPA受体介导的突触应答的增强有反应。
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公开(公告)号：US6011033A
公开(公告)日：2000-01-04
申请号：US191549
申请日：1998-11-13
申请人： Henk Timmerman , Mingqiang Zhang , Kazuhiro Onogi , Masahiro Tamura , Tsutomu Toma , Yasushi Wada
发明人： Henk Timmerman , Mingqiang Zhang , Kazuhiro Onogi , Masahiro Tamura , Tsutomu Toma , Yasushi Wada
IPC分类号： C07D215/22 , C07D215/227 , C07D215/26 , C07D215/54 , C07D239/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D487/04 , A61K31/54 , C07D279/16
CPC分类号： C07D215/227 , C07D215/26 , C07D215/54 , C07D239/74 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D487/04
摘要： This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l --, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.
摘要翻译： 本发明涉及由下式（1）表示的亚苯基衍生物或其盐，以及含有它作为有效成分的药物。 其中R1表示H或卤素; A表示-CH = CH-，-CH = N-，-N（R 2） - ， - O-或-S-; W表示-CH = CH-或-CH 2 O-; X表示-CH 2 O - ， - CH 2 S - ， - CH 2 N（R 3） - ， - CH = N - ， - COO-或-CONH-; Y表示B 1表示-C（R 7）（R 8）（CH 2）1 - ， - S（O）m（CH 2）n - 或-CH = C（R 9） B2表示-CH 2 CH 2 - 或-CH 2 CH 2 CH 2 - ; Z1和Z2各自表示O或S; 亚苯衍生物或其盐具有抗白细胞增多作用和抗组胺作用，并且可用作诸如哮喘预防或治疗药物。
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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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