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1. 发明申请

US20100215727A1 STABILIZED PICOPLATIN DOSAGE FORM 审中-公开
标题翻译：稳定的PICPLATIN剂型
公开(公告)号：US20100215727A1
公开(公告)日：2010-08-26
申请号：US12635517
申请日：2009-12-10
申请人： Alistair J. Leigh , Ronald A. Martell , David A. Karlin , Cheni Kwok , Christopher A. Procyshyn , Hazel B. Breitz , Paul L. Weiden
发明人： Alistair J. Leigh , Ronald A. Martell , David A. Karlin , Cheni Kwok , Christopher A. Procyshyn , Hazel B. Breitz , Paul L. Weiden
IPC分类号： A61K9/127 , A61K31/555 , A61K39/395 , A61K31/7068 , A61P35/00 , A61P35/02
CPC分类号： A61K31/555 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K47/02 , A61K47/26
摘要： Methods for stabilizing aqueous solutions of picoplatin are provided. Such stable, preferably aseptic solutions are particularly useful for preparing unit dosages of picoplatin for oral or intravenous administration, preferably in combination with at least one additional non-platinum anti-cancer agent.
摘要翻译：提供了稳定吡铂水溶液的方法。这种稳定的，优选的无菌溶液特别可用于制备用于口服或静脉内给药的吡铂的单位剂量，优选与至少一种另外的非铂抗癌剂组合。

2. 发明申请

US20120123121A1 SYNTHESIS OF PICOPLATIN 审中-公开
标题翻译： PICOPLATIN合成
公开(公告)号：US20120123121A1
公开(公告)日：2012-05-17
申请号：US13322362
申请日：2010-06-11
申请人： Alistair J. Leigh , Steffen Jost
发明人： Alistair J. Leigh , Steffen Jost
IPC分类号： C07F15/00
CPC分类号： C07D213/60 , C07F15/0093
摘要： An improved method for the synthesis of the anticancer drug picoplatin is provided. Condensation of a tetrachloroplatinate salt (TCP), such as potassium tetrachloroplatinate, and 2-picoline, in a solvent, is catalyzed by the presence of oxygen, such as in air, and additionally catalyzed by the presence of a Pt+4 complex, such as potassium hexachloroplatinate. The oxygen can be introduced into the reaction mixture by sparging, optionally with high shear mixing and under an inert gas headspace. The product trichloropicolineplatinate salt (TCPP) is a key intermediate in the synthesis of picoplatin, to which it can be converted by reaction of the TCPP with ammonia.
摘要翻译：提供了一种用于合成抗癌药物吡铂的改进方法。四氯铂酸盐（TCP）如四氯铂酸钾和2-甲基吡啶在溶剂中的缩合是由氧气如空气中的存在而催化的，另外由Pt + 4络合物的存在催化，例如作为六氯铂酸钾。可以通过喷雾，任选地在高剪切混合下和在惰性气体顶部空间下将氧气引入反应混合物中。产物三氯吡啶磷酸盐（TCPP）是吡铂合成中的关键中间体，可通过TCPP与氨的反应转化。

3. 发明申请

US20110033528A1 STABILIZED PICOPLATIN ORAL DOSAGE FORM 审中-公开
标题翻译：稳定的PICOPLATIN口服剂型
公开(公告)号：US20110033528A1
公开(公告)日：2011-02-10
申请号：US12536335
申请日：2009-08-05
申请人： Alistair J. Leigh , Christopher A. Procyshyn , Ernest S.Y. Wong , Christen M. Giandomenico
发明人： Alistair J. Leigh , Christopher A. Procyshyn , Ernest S.Y. Wong , Christen M. Giandomenico
IPC分类号： A61K31/555 , A61K9/28 , A61K9/48 , A61P35/00
CPC分类号： A61K9/28 , A61J3/005 , A61K9/14 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2813 , A61K9/2826 , A61K9/2846 , A61K9/2866 , A61K9/4825 , A61K31/555
摘要： The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox-active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt % picoplatin wherein the picoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt % of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt % of a lubricant. The dosage form can further include a dispersant.
摘要翻译：本发明提供了包含核心和包衣的抗癌药物吡铂的口服剂型，所述剂型不含氧化还原活性金属盐。片剂的核心是包含约10至60重量％的吡铂的基本干燥的粉末，其中吡铂是平均粒径小于约10微米的颗粒，约40-80重量％的包含基本上水溶性的，水分散性或吸水性碳水化合物，有效量至多约5重量％的润滑剂。剂型还可包括分散剂。

4. 发明申请

US20100062056A1 ENCAPSULATED PICOPLATIN 审中-公开
标题翻译：封闭的PICPLATIN
公开(公告)号：US20100062056A1
公开(公告)日：2010-03-11
申请号：US12536311
申请日：2009-08-05
申请人： Alistair J. Leigh , Christopher A. Procyshyn , Angelica Phillips , Hazel B. Breitz
发明人： Alistair J. Leigh , Christopher A. Procyshyn , Angelica Phillips , Hazel B. Breitz
IPC分类号： A61K31/555 , A61K9/48 , A61P35/00
CPC分类号： A61K9/4816 , A61K9/1652 , A61K9/4825 , A61K9/4833 , A61K9/4858 , A61K9/4866 , A61K31/28 , A61K31/44 , A61K31/555 , A61K33/24
摘要： The invention provides an encapsulated unit dosage form for picoplatin that is adapted for oral administration of the picoplatin containing a substantially dry powder with about 20 to 55 wt % picoplatin in the physical form of a picoplatin particulate wherein an average picoplatin particle diameter is less than about 10 microns. The picoplatin particles are dispersed within the powder of the formulation which includes a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate and an effective amount of up to about 5 wt % of a lubricant.
摘要翻译：本发明提供了一种用于吡铂的胶囊化单位剂量形式，其适于口服给药皮质素，其含有基本上干燥的粉末，其具有皮质颗粒物理形式的约20至55重量％的吡铂，其中平均吡铂粒径小于约 10微米。皮普铂颗粒分散在制剂的粉末中，其包括基本上水溶性，水分散性或吸水性碳水化合物和有效量的至多约5重量％的润滑剂。

5. 发明授权

US6020337A Electronegative-substituted long chain xanthine compounds 失效
标题翻译：电负性取代长链黄嘌呤化合物
公开(公告)号：US6020337A
公开(公告)日：2000-02-01
申请号：US950810
申请日：1997-09-16
申请人： Alistair J. Leigh , John Michnick , Anil M. Kumar , J. Peter Klein , Gail Underiner
发明人： Alistair J. Leigh , John Michnick , Anil M. Kumar , J. Peter Klein , Gail Underiner
IPC分类号： C07D209/48 , C07D239/54 , C07D239/96 , C07D473/10 , A61K31/52 , C07D473/00
CPC分类号： C07D209/48 , C07D239/54 , C07D239/96 , C07D473/10
摘要： Therapeutic compounds, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, having a formula: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, halo, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic groups, wherein the substituents of substituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl are other than halo; n is an integer from one to sixteen; R.sub.1, R.sub.2, and R.sub.3 are independently selected from the group consisting of a halo; haloacetoxy; hydrogen; hydroxy; oxo; --N.dbd.C.dbd.S; --N.dbd.C.dbd.O; --0--C.tbd.N; --C.tbd.N; --N.dbd.N.dbd.N; and --C--(R.sub.5).sub.3, R.sub.5 being independently a halo or hydrogen, at least one R.sub.5 being halo, at least one of R.sub.1, R.sub.2, and R.sub.3 being halo, cyano, isocyano, isothiocyano, azide or haloacetoxy group; R.sub.4 is hydrogen, C.sub.(1-6) alkyl, C.sub.(1-6) alkenyl, cyclo C.sub.(4-6) alkyl, or phenyl; one or more hydrogen atoms of (CH.sub.2).sub.n --CH.sub.a --CH.sub.b --CH.sub.c may be replaced with: i) at least one of halogen atom, hydroxyl, oxo, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyalkyl, or C.sub.(2-10) alkenyl; or ii) one or more unsaturated bonds; and any two adjacent carbon atoms of (CH.sub.2).sub.n --CH.sub.a --CH.sub.b --CH.sub.c may be instead separated by at least one oxygen atom. These compounds are useful in treating or preventing diseases by inhibiting selective second messenger pathways.
摘要翻译：具有下式的治疗化合物，包括拆分的对映异构体和/或非对映异构体，水合物，盐，溶剂合物及其混合物，其中R 0选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，环状或杂环基团，其中取代的C（1-10）烷基，C（2-10）烯基的取代基不是卤素; n是从1到16的整数; R 1，R 2和R 3独立地选自卤素; 卤代乙酰氧基; 氢; 羟基; 氧代 -N = C = S; -N = C = O; -0-C 3BOND N; -C 3BOND N; -N = N = N; 和 - （R 5）3，R 5独立地为卤素或氢，至少一个R 5为卤素，R 1，R 2和R 3中的至少一个为卤素，氰基，异氰基，异硫氰基，叠氮基或卤代乙酰氧基; R4是氢，C（1-6）烷基，C（1-6）烯基，环C（4-6）烷基或苯基; （CH 2）n -CH-CHB-CHc的一个或多个氢原子可以被：i）卤素原子，羟基，氧代，取代或未取代的C（1-10）烷基，C（1-10 ）烷氧基烷基或C（2-10）烯基; 或ii）一个或多个不饱和键; 并且（CH 2）n -CH CH-CH c CH 2的任何两个相邻的碳原子可以被至少一个氧原子隔开。这些化合物可用于通过抑制选择性第二信使途径来治疗或预防疾病。

6. 发明申请

US20130202690A1 ENCAPSULATED PICOPLATIN 审中-公开
标题翻译：封闭的PICPLATIN
公开(公告)号：US20130202690A1
公开(公告)日：2013-08-08
申请号：US13629108
申请日：2012-09-27
申请人： Alistair J. Leigh , Christopher A. Procyshyn , Angelica F. Phillips , Hazel B. Breitz
发明人： Alistair J. Leigh , Christopher A. Procyshyn , Angelica F. Phillips , Hazel B. Breitz
IPC分类号： A61K9/48 , A61K31/555
CPC分类号： A61K9/4816 , A61K9/1652 , A61K9/4825 , A61K9/4833 , A61K9/4858 , A61K9/4866 , A61K31/28 , A61K31/44 , A61K31/555 , A61K33/24
摘要： The invention provides an encapsulated unit dosage form for picoplatin that is adapted for oral administration of the picoplatin containing a substantially dry powder with about 20 to 55 wt % picoplatin in the physical form of a picoplatin particulate wherein an average picoplatin particle diameter is less than about 10 microns. The picoplatin particles are dispersed within the powder of the formulation which includes a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate and an effective amount of up to about 5 wt % of a lubricant.
摘要翻译：本发明提供了一种用于吡铂的胶囊化单位剂量形式，其适于口服给药皮质素，其含有基本上干燥的粉末，其具有皮质颗粒物理形式的约20至55重量％的吡铂，其中平均吡铂颗粒直径小于约 10微米。皮普铂颗粒分散在制剂的粉末中，其包括基本上水溶性，水分散性或吸水性碳水化合物和有效量的至多约5重量％的润滑剂。

7. 发明授权

US5817662A Substituted amino alkyl compounds 失效
标题翻译：取代的氨基烷基化合物
公开(公告)号：US5817662A
公开(公告)日：1998-10-06
申请号：US468656
申请日：1995-06-06
申请人： J. Peter Klein , Gail E. Underiner , Alistair J. Leigh
发明人： J. Peter Klein , Gail E. Underiner , Alistair J. Leigh
IPC分类号： A61K31/522 , A61K31/52
CPC分类号： A61K31/522 , Y10S424/824 , Y10S424/825
摘要： Compounds and pharmaceutical compositions thereof comprise the formula: (R)j-(core moiety), including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, wherein J is an integer from one to three, the core moiety is non-cyclic or comprises at least one, five- to seven-membered ring structure, R may be selected from the group consisting of hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted benzyl, alkyl (C.sub.1-6) or alkenyl (C.sub.1-6), and at least one R has the formula I: ##STR1## wherein n is an integer from four to eighteen; each R'.sub.1 and R'.sub.2 is independently hydrogen, alkyl (C.sub.1-4) or alkenyl (C.sub.1-4), the alkyl or alkenyl groups being preferably substituted by a halogen, hydroxyl, ketone or dimethylamino group and/or may be interrupted by an oxygen or hydrogen atom or an alkyl (C.sub.1-4) group; and each R'.sub.3 and R'.sub.4 is independently hydrogen or methyl. Preferably, n is an integer from six to ten, R'.sub.1 and R'.sub.2 are independently hydrogen or methyl and R'.sub.3 and R'.sub.4 are hydrogen. The compounds are useful in treating or preventing, for example, sepsis syndrome, hematopoietic or organ toxicity, baldness, hair loss or allopecia caused by cytotoxic therapies, and progression of an inflammatory or autoimmune disease.
摘要翻译：化合物及其药物组合物包含式（R）j-（核心部分），包括拆分的对映异构体和/或非对映异构体，水合物，盐，溶剂合物及其混合物，其中J为1至3的整数，核心部分为非环状或包含至少一个五元至七元环结构，R可以选自氢，卤素，羟基，氨基，取代或未取代的苄基，烷基（C 1-6）或烯基（C 1 -6），并且至少一个R具有式I：其中n是从4到18的整数; 每个R'1和R'2独立地是氢，烷基（C1-4）或烯基（C1-4），烷基或烯基优选被卤素，羟基，酮或二甲基氨基取代和/或可被中断通过氧或氢原子或烷基（C 1-4）基团; 并且每个R'3和R'4独立地是氢或甲基。优选地，n是6至10的整数，R'1和R'2独立地是氢或甲基，R'3和R'4是氢。该化合物可用于治疗或预防例如败血症综合症，造血或器官毒性，秃发，由细胞毒性治疗引起的脱发或脱发，以及炎性或自身免疫性疾病的进展。

8. 发明授权

US6100271A Therapeutic compounds containing xanthinyl 失效
标题翻译：含有黄原素的治疗化合物
公开(公告)号：US6100271A
公开(公告)日：2000-08-08
申请号：US483871
申请日：1995-06-07
申请人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
发明人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar
IPC分类号： C07D239/54 , A61K31/42 , A61K31/421 , A61K31/496 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/10 , A61P9/14 , A61P11/16 , A61P13/02 , A61P15/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07C47/198 , C07C47/277 , C07C49/175 , C07C49/255 , C07C57/46 , C07C59/64 , C07C65/21 , C07C69/06 , C07C69/14 , C07C69/24 , C07C69/608 , C07C69/612 , C07C225/06 , C07C233/01 , C07D239/56 , C07D241/18 , C07D263/30 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D513/04 , C07D521/00
CPC分类号： C07D487/04 , C07D473/04 , C07D473/06 , C07D473/10 , C07D513/04
摘要： Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyallyl; --A(R.sub.5).sub.m, A being N or O, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.
摘要翻译：具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中：或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟基烯基; -A（R5）m，A是N或O，m是一个或两个，R5是氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

9. 发明申请

US20130183433A1 STABILIZED PICOPLATIN ORAL DOSAGE FORM 审中-公开
标题翻译：稳定的PICOPLATIN口服剂型
公开(公告)号：US20130183433A1
公开(公告)日：2013-07-18
申请号：US13587711
申请日：2012-08-16
申请人： Alistair J. Leigh , Christopher A. Procyshyn , Ernest S.Y. Wong , Christen M. Giandomenico
发明人： Alistair J. Leigh , Christopher A. Procyshyn , Ernest S.Y. Wong , Christen M. Giandomenico
IPC分类号： A61J3/00
CPC分类号： A61K9/28 , A61J3/005 , A61K9/14 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2813 , A61K9/2826 , A61K9/2846 , A61K9/2866 , A61K9/4825 , A61K31/555
摘要： The invention provides an oral dosage form for the anti-cancer drug picoplatin comprising a core and a coating, the dosage form being free of redox- active metal salts. The core of the tablet is a substantially dry powder comprising about 10 to 60 wt % picoplatin wherein the pieoplatin is a particulate of less than about 10 microns average particle diameter, about 40-80 wt % of a filler comprising a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate, and an effective amount of up to about 5 wt % of a lubricant. The dosage form can further include a dispersant.
摘要翻译：本发明提供了抗癌药物吡铂的口服剂型，其包含核心和涂层，所述剂型不含氧化还原活性金属盐。片剂的核心是包含约10至60重量％的吡铂的基本干燥的粉末，其中压铂是平均粒径小于约10微米的颗粒，约40-80重量％的包含基本上水溶性的，水分散性或吸水性碳水化合物，有效量至多约5重量％的润滑剂。剂型还可包括分散剂。

10. 发明授权

US6043250A Methods for using therapeutic compounds containing xanthinyl 失效
标题翻译：使用含有黄原素的治疗化合物的方法
公开(公告)号：US6043250A
公开(公告)日：2000-03-28
申请号：US472296
申请日：1995-06-07
申请人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar , Glenn C. Rice
发明人： J. Peter Klein , Alistair J. Leigh , Gail E. Underiner , Anil M. Kumar , Glenn C. Rice
IPC分类号： C07D239/54 , A61K31/42 , A61K31/421 , A61K31/496 , A61K31/505 , A61K31/52 , A61K31/522 , A61P9/10 , A61P9/14 , A61P11/16 , A61P13/02 , A61P15/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P31/18 , A61P35/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07C47/198 , C07C47/277 , C07C49/175 , C07C49/255 , C07C57/46 , C07C59/64 , C07C65/21 , C07C69/06 , C07C69/14 , C07C69/24 , C07C69/608 , C07C69/612 , C07C225/06 , C07C233/01 , C07D239/56 , C07D241/18 , C07D263/30 , C07D473/04 , C07D473/06 , C07D473/10 , C07D487/04 , C07D513/04 , C07D521/00 , A61K3/52
CPC分类号： C07D487/04 , C07D473/04 , C07D473/06 , C07D473/10 , C07D513/04
摘要： Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C(.sub.1-10) alkyl, C(.sub.2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C(.sub.1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.2 and R.sub.4 join to form a substituted or unsubstituted heterocycle having four to seven ring atoms, the ether group --O-- of --CHR.sub.4 O-- being a member of the heterocycle. R.sub.2 is selected from the group consisting of hydrogen; halogen; substituted or unsubstituted C.sub.(1-10) alkyl; C.sub.(1-10) alkoxyl; C.sub.(2-10) alkenyl; C.sub.(1-10) hydroxyalkyl; --A(R.sub.5).sub.m, A being N or 0, m being one or two and R.sub.5 being hydrogen, a substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl or C.sub.(1-10) hydroxyalkyl), or carbocyclic or heterocyclic group. At least one of R.sub.1 is NR.sub.3, O or --CHR.sub.4 O--, or R.sub.2 is --A(R.sub.5).sub.m. The compounds and pharmaceutical compositions thereof are useful as therapies for diseases advanced via intracellular signaling through specific intracellular signaling pathways by mediating a signaling response to an external stimuli.
摘要翻译：具有至少一个羧酸，酯或酰胺取代的侧链的治疗化合物具有下式：CORE MOIETY - （R）j，其中j是1至3的整数。核心部分是非环状或环状的（碳环或杂环）。 R可以选自氢，卤素，羟基，氨基，取代或未取代的C（1-10）烷基，C（2-10）烯基，碳环或杂环基，并且至少一个R具有式I：其中：或两个p为整数，否则p为2; n为3〜20的整数。 R1选自取代和未取代的CH 2; NR 1，R 3为氢，取代或未取代的C 1-20烷基，C（1-20）烷氧基，C（2-20）烯基或C（1-20）羟基烷基或碳环或杂环基; O; -CHR4O-，R4是取代或未取代的C（1-20）烷基，C（1-20）烷氧基，C（2-20）烯基，C（1-20）羟基烷基或R2和R4连接形成取代的或具有4-7个环原子的未取代的杂环，-CHR4O-的醚基-O-是杂环的成员。 R2选自氢; 卤素; 取代或未取代的C（1-10）烷基; C（1-10）烷氧基; C（2-10）烯基; C（1-10）羟烷基; -A（R5）m，A为N或0，m为一个或两个，R5为氢，取代或未取代的C（1-10）烷基，C（1-10）烷氧基，C（2-10）烯基或C（1-10）羟烷基）或碳环或杂环基。 R 1中的至少一个为NR 3，O或-CHR 4 O-，或R 2为-A（R 5）m。这些化合物及其药物组合物可用作通过介导对外部刺激的信号反应的特异性细胞内信号通路的细胞内信号传导的疾病的治疗。

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