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~
热词
    • 14. 发明授权
    • β-lactam compounds process for reproducing the same and serum cholesterol-lowering agents containing the same
    • 用于再现相同的β-内酰胺化合物的方法和含有它们的血清胆固醇降低剂
    • US07045515B2
    • 2006-05-16
    • US10450171
    • 2002-02-20
    • Hiroshi TomiyamaMasayuki YokotaAtsushi NodaAkira Ohno
    • Hiroshi TomiyamaMasayuki YokotaAtsushi NodaAkira Ohno
    • C07D205/08A61K31/397A61P3/06
    • C07D405/10C07D405/12
    • Novel β-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A1, A3 and A4 represent each hydrogen, halogen C1-5 alkyl, C1-5 alkoxy, —COOR1, a group represented by the following general formula (b): (b) wherein R1 represents hydrogen or C1-5 alkyl, or a group represented by the following general formula (a): (a) wherein R2 represents —CH2OH, —CH2OC(O)—R1 or —CO2—R1; R3 represents —OH or —OC(O)—R1; R4 represents —(CH2)kR5(CH2)1- wherein K and 1 are each 0 or an integer of 1 or above provided k+1 is an integer of not more than 10; and R5 represents a single bond, —CH═CH—, —OCH2—, carbonyl or —CH(OH)—; provided that at least one of A1, A3 and A4 is a group represented by the above formula (a); A2 represents C1-5 alkyl, C1-5 alkoxy, C1-5 alkenyl, C1-5 hydroxyalkyl or C1-5 carbonylalkyl; and n, p, q and r are each an integer of 0, 1 or 2.
    • 由下式(I)表示的新型β-内酰胺化合物或其药学上可接受的盐可用作血清降胆固醇剂:(I)其中A 1,A 3, >和A 4各自表示氢,卤素C 1-5烷基,C 1-5烷氧基,-COOR 1, (b)表示的基团:(b)其中R 1表示氢或C 1-5烷基,或由以下通式(b)表示的基团: 以下通式(a):(a)其中R 2代表-CH 2 OH,-CH 2 OC(O)-R' SUB> 1或-CO 2 -R 1; R 3表示-OH或-OC(O)-R 1; R 4表示 - (CH 2)2 R 5(CH 2)2 - (CH 2) 其中K和1各自为0或1或更高的整数,k + 1为不大于10的整数; 和R 5表示单键,-CH-CH-,-OCH 2 - ,羰基或-CH(OH) - ; 条件是A 1,A 3和A 4中的至少一个是由上述式(a)表示的基团。 A 2表示C 1-5烷基,C 1-5烷氧基,C 1-5 - 烯基,C 1-5个羟基烷基或C 1-5烷基羰基; 并且n,p,q和r各自为0,1或2的整数。
    • 15. 发明申请
    • Process for Preparing Optically Active Alcohols
    • 光学活性醇制备方法
    • US20090062527A1
    • 2009-03-05
    • US12224098
    • 2007-02-13
    • Hiroshi TomiyamaMasayuki Yokota
    • Hiroshi TomiyamaMasayuki Yokota
    • C07D205/08C07D263/24C07C69/732
    • C07D263/14C07B53/00C07B2200/07C07C67/31C07D205/08C07C69/732
    • This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity at large scale production. Aromatic ketones represented by formula (I) [wherein, R1 are selected from hydrogen atom, halogen atom, lower alkyl group etc. R2 is —(CH2)n-R3 [wherein, n is 1 to 5 integer. R3 are selected from hydrogen atom, halogen atom, lower alkoxycarbonyl group etc. and formula (II) and (III). {wherein, R4 is selected from lower alkyl group (1 to 5 carbon atom) etc. R5 and R6 are the same or different and are selected from hydrogen atom, halogen atom, lower alkyl group etc.}]] are reduced by sodium borohydride, chlorotrimethylsilane and optically active 2-[bis(4-methoxyphenyl)hydroxymethyl]pyrrolidine represented by formula (IV) to give optically active alcohol represented by formula (V) stereoselectively. (wherein, R1 and R2 are as defined above.)
    • 本发明涉及使用芳族酮不对称还原制备光学活性醇的方法。 该方法在大规模生产中提供高对映选择性的光学活性醇。 由式(I)表示的芳族酮[其中,R 1选自氢原子,卤素原子,低级烷基等。R 2为 - (CH 2)n -R 3 [其中,n为1〜5的整数。 R3选自氢原子,卤素原子,低级烷氧基羰基等和式(II)和(III)。 {其中,R4选自低级烷基(1〜5个碳原子)等。R5和R6相同或不同,选自氢原子,卤素原子,低级烷基等}]]由硼氢化钠还原 ,氯代三甲基硅烷和由式(IV)表示的光学活性的2- [双(4-甲氧基苯基)羟甲基]吡咯烷,由式(Ⅴ)代表的光学活性醇立体选择地得到。 (其中,R1和R2如上定义)
    • 19. 发明申请
    • Phosphonic Acid Derivatives and the Treating Agents of Diseases Related Hyperphosphatemia
    • 膦酸衍生物和相关高磷酸盐血症的治疗药物
    • US20080119441A1
    • 2008-05-22
    • US11664830
    • 2005-10-05
    • Hiroshi TomiyamaMasayuki YokotaKazuo TokuzakiRyoko Tomita
    • Hiroshi TomiyamaMasayuki YokotaKazuo TokuzakiRyoko Tomita
    • A61K31/675A61K31/66C07F9/06C07F9/22
    • C07F9/6541C07F9/3834C07F9/3882C07F9/3891C07F9/59C07F9/6539C07F9/65517C07F9/655345C07F9/655354C07F9/6558C07F9/65586
    • This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. (I)[wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or branched alkylene group. B ring and C ring are selected from benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle. D is —(CH2)(n+1)—, —(CH2)-O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— (wherein: D ring is connected with the carbon atom composing C ring.) E is selected from oxygen atom or sulfur atom. P is phosphine atom. R1˜R7 (wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle. R1, R2 and R3 are not hydrogen atom if B ring is benzene ring.) may be the same or different and are substituents. R8 and R9 are may be the same or different and are substituents. R10 is alkyl group. n and m are 0-10. o is 0-2.
    • 本发明涉及一系列具有抗高磷酸血症活性的新型膦酸衍生物。 (I)[其中:A选自 - (CH 2)n - , - CO - , - (CH 2 H 2) (CH 2)n - , - (CH 2)n - , - (CH 2 CH 2)n - -C( - ) - (CH 2 CH 2)m - 或支链亚烷基。 B环和C环选自苯环,萘环,薁环或杂环或稠合杂环。 D是 - (CH 2)2(n + 1) - , - (CH 2)-O-(CH 2 CH 2)m - (CH 2) - (CH 2)n - (CH 2)m - / > - , - CF 3 - 或 - (CH 2)n - NR 10 - (CH 3) 2)其中:D环与构成C环的碳原子连接。)E选自氧原子或硫原子。 P是膦原子。 (其中R 1和R 2,R 4,R 4,R 4, R 5与邻位的碳原子连接在一起形成5〜7元饱和或不饱和烃环,或5〜6元稠合杂环,R 1,R 2, > 2和R 3不是氢原子,如果B环是苯环)可以相同或不同,并且是取代基。 R 8和R 9可以相同或不同,并且是取代基。 R 10是烷基。 n和m为0-10。 o是0-2。