中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

52 records (took 0.018 seconds)

    Angiogenesis inhibitors
    22.
    发明申请
    Angiogenesis inhibitors 审中-公开
    血管生成抑制剂

    公开(公告)号：US20050107406A1

    公开(公告)日：2005-05-19

    申请号：US11009235

    申请日：2004-12-10

    Applicant: Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

    Inventor： Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

    IPC: C07D405/04 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4745 ,  A61K31/519 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00

    CPC classification number: A61K31/4162 ,  A61K31/416 ,  A61K31/4745 ,  A61K31/519

    Abstract: A method for treating an angiogenesis-related disorder. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: Each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

    Abstract translation: 一种治疗血管生成相关病症的方法。 该方法包括向有需要的受试者施用有效量的下式化合物：Ar 1，Ar 2和Ar 3中的每一个， 独立地是苯基，噻吩基，呋喃基，吡咯基，吡啶基或嘧啶基; R 1，R 2，R 3，R 4，R 5，和/或R 3中的每一个 >和R 6独立地是R，硝基，卤素，C（O）OR，C（O）SR，C（O）NRR'，（CH 2） （CH 2）m，或（CH 2）m SR，（CH 2 2）m， C（O）OR（CH 2 CH 2）m C（O）OR（CH 2） ，（CH 2 CH 2）m CHO，（CH 2 CH 2）m CH或NOR，或R 1， 1个和R 2个在一起，R 3和R 4一起，或者R 5和R 5 一起是O（CH 2 CH 2）m O，其中R和R'各自独立地是H或C 1 -C 6烷基， C 1 -C 6烷基; m为0,1,2,3,4,5或6，n为0,1,2或3。

    Piperazinedione compounds
    24.
    发明授权
    Piperazinedione compounds 失效
    哌嗪二酮化合物

    公开(公告)号：US06635649B2

    公开(公告)日：2003-10-21

    申请号：US09851077

    申请日：2001-05-08

    Applicant: Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

    Inventor： Che-Ming Teng ,  Hui-Po Wang ,  Eric I. C. Li ,  On Lee ,  Jih-Hwa Guh ,  Huei-Ting Chen ,  Ya-Bing Fan ,  Ya-Lan Chen

    IPC: A61K31496

    CPC classification number: C07D401/06 ,  C07D409/14

    Abstract: Piperazinedione compounds of the formula: Each of and and independently, is a single bond or a double bond; A is H or CH(RaRb) when is a single bond, or C(RaRb) when is a double bond; Z is R3O—(Ar)—B, in which B is CH(Rc) when is a single bond, or C(Rc) when is a double bond; Ar is heteroaryl; and R3 is H, alkyl, aryl, heteroaryl, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; each of R1 and R2, independently, is H, C(O)Rd, C(O)ORd, C(O)NRdRe, or SO2Rd; and each of Ra, Rb, Rc, Rd, and Re, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl. Optionally, Ra and Rb taken together are cyclyl or heterocyclyl; and, also optionally, R1 and Ra or R1 and Rb taken together are cyclyl or heterocyclyl. Also disclosed is a method for treating tumor with the above described piperazinedione compounds.

    Abstract translation: 哌嗪二酮化合物，分别为：＆lt; CUSTOM-CHARACTER FILE =“US06635649-20031021-P00900.TIF”ALT =“custom character”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00001”/ >和 或双键; 当是单键，或C（R a R b）当为双键时; 当是单键或C（R ）”ALT =“自定义字符”HE =“20”WI =“20”ID =“CUSTOM-CHARACTER-00005”/>是双键; Ar是杂芳基; 且R 3为H，烷基，芳基，杂芳基，C（O）R d，C（O）OR d，C（O）NR d R e或SO 2 R d; R 1和R 2各自独立地是H，C（O）R d，C（O）OR d，C（O）NR d R e或SO 2 R ; R a，R b，R c，R d和R e各自独立地是H，烷基，芳基，杂芳基，环基或杂环基。 任选地，R 5和R b一起是环基或杂环基; 并且还可任选地，R 1和R 5'或R 1和R b一起是环基或杂环基。 还公开了用上述哌嗪二酮化合物治疗肿瘤的方法。

    .alpha.-methylene-.gamma.-butyrolactones: new inhibitors of platelet aggregation
    25.
    发明授权
    .alpha.-methylene-.gamma.-butyrolactones: new inhibitors of platelet aggregation 失效
    α-亚甲基γ-丁内酯：新型血小板聚集抑制剂

    公开(公告)号：US5646164A

    公开(公告)日：1997-07-08

    申请号：US557268

    申请日：1995-11-14

    Applicant: Cherng-Chyi Tzeng ,  Yeh-Long Chen ,  Tai-Chi Wang ,  Che-Ming Teng

    Inventor： Cherng-Chyi Tzeng ,  Yeh-Long Chen ,  Tai-Chi Wang ,  Che-Ming Teng

    IPC: C07D405/12 ,  C07D407/12 ,  A61K31/37 ,  A61K31/47

    CPC classification number: C07D405/12 ,  C07D407/12

    Abstract: The present inventors have discovered three classes of novel .alpha.-methylene-.gamma.-butyrolactones with excellent antiplatelet activity. As a result of intensive studies, it has been found that compounds represented by the formula I-III are potent inhibitors of platelet aggregation. ##STR1## For the formula I, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino.For the formula II, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.2 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino; R.sub.3 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino.For the formula III, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.4 represents hydrogen, hydroxy, (C.sub.1 -C.sub.4) alkyl.The present invention also provides a cost-efficient method for the preparation of formula I-III.Formula I-III may be administered orally or parenterly with an inert diluent or with a pharmaceutically acceptable carrier in the treatment or the prevention of cardiovascular disease.

    Abstract translation: 本发明人发现了三种具有优异抗血小板活性的新型α-亚甲基γ-丁内酯。 作为深入研究的结果，已经发现由式I-III表示的化合物是血小板聚集的有效抑制剂。 对于式I，R 1是甲基，任选被一个或两个选自卤素，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，苯基，硝基的基团取代的苯基 ，氨基。 对于式II，R 1是甲基，任选被一个或两个选自卤素，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，苯基，硝基，氨基的基团取代的苯基; R 2表示氢，卤素，（C 1 -C 4）烷基，苯基，硝基，氨基; R 3表示氢，卤素，（C 1 -C 4）烷基，苯基，硝基，氨基。 对于式III，R 1是甲基，任选被一个或两个选自卤素，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，苯基，硝基，氨基的基团取代的苯基; R4表示氢，羟基，（C1-C4）烷基。 本发明还提供了制备式I-III的成本有效的方法。 式I-III可以与惰性稀释剂或药学上可接受的载体口服或肠胃外给药以治疗或预防心血管疾病。

    1-(substituted benzyl)-3-(substituted aryl)-condensed pyrazole derivatives and processes of making the same
    26.
    发明授权
    1-(substituted benzyl)-3-(substituted aryl)-condensed pyrazole derivatives and processes of making the same 失效
    1-（取代的苄基）-3-（取代的芳基） - 缩合的吡唑衍生物及其制备方法

    公开(公告)号：US5574168A

    公开(公告)日：1996-11-12

    申请号：US237087

    申请日：1994-05-03

    Applicant: Sheng-Chu Kuo ,  Fang Yu Lee ,  Che-Ming Teng

    Inventor： Sheng-Chu Kuo ,  Fang Yu Lee ,  Che-Ming Teng

    IPC: C07D487/04 ,  A61K31/00 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4188 ,  A61P7/00 ,  A61P7/02 ,  C07D231/56 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

    CPC classification number: C07D495/04 ,  C07D231/56 ,  C07D405/04 ,  C07D491/04

    Abstract: The invention pertains to a process for preparing (1-substituted benzyl)-3-(hydroxy-carbonyl aryl) condensed pyrazoles or (1-substituted benzyl)-3-(hydroxymethyl aryl) condensed pyrazoles comprising the steps of: (a) reacting compound I and compound II, or compound III and compound IV, to produce compound V, which is a substituted aryl ketone, as follows: ##STR1## wherein Ar.sub.2 and At.sub.3 can be, independently, ##STR2## R.sub.1 is H, C.sub.1-3 alkyl, or X (halogen), R.sub.3 is H, C.sub.1-3 alkyl, X (halogen), or --OR radical, and R is H or C.sub.1-3 alkyl; the process comprising the following steps of: R.sub.2 represents CH.sub.2 OR, H, COOR, C.sub.1-3 alkyl, or X (halogen); (b) reacting the compound V with a hydrazine compound to form a hydrazone compound; (c) reacting the hydrazone compound compound with trifluoride etherate (BF.sub.3 .cndot.Et.sub.2 O) to form a 1-(substituted benzyl) 3-(substituted aryl) condensed pyraxzole, which is represented by the following formula of ##STR3## Compound X can be further hydrolyzed or reduced to form corresponding carboxylic acids or alcohols.

    Abstract translation: 本发明涉及制备（1-取代苄基）-3-（羟基 - 羰基芳基）缩合吡唑或（1-取代苄基）-3-（羟基甲基芳基）稠合吡唑的方法，包括以下步骤：（a） 化合物I和化合物II或化合物III和化合物IV，以产生作为取代的芳基酮的化合物V，其如下：其中Ar 2和At 3可以独立地是， H，C 1-3烷基或X（卤素），R 3是H，C 1-3烷基，X（卤素）或-OR基，R是H或C 1-3烷基; 该方法包括以下步骤：R 2表示CH 2 OR，H，COOR，C 1-3烷基或X（卤素）; （b）使化合物V与肼化合物反应以形成腙化合物; （c）使腙化合物与三氟化醚（BF 3·Et 2 O）反应以形成1-（取代的苄基）3-（取代的芳基）缩合吡唑，其由下式表示，其水解或还原形成相应的羧酸 或醇类。

    Fused pyrazolyl compounds having an aminoalkylcarbonyl group
    30.
    发明授权
    Fused pyrazolyl compounds having an aminoalkylcarbonyl group 有权
    具有氨基烷基羰基的稠合的吡唑基化合物

    公开(公告)号：US07767707B2

    公开(公告)日：2010-08-03

    申请号：US12292160

    申请日：2008-11-13

    Applicant: Sheng-Chu Kuo ,  Che-Ming Teng ,  Fang-Yu Lee

    Inventor： Sheng-Chu Kuo ,  Che-Ming Teng ,  Fang-Yu Lee

    IPC: A61K31/416 ,  C07D231/56

    CPC classification number: C07D405/04

    Abstract: A fused pyrazolyl compound having an anti-tumor potency of the following formula is synthesized: wherein A is in which n is 0, 1, 2, or 3; Ar1 is benzene, thiophene or furan; Ar2 is furyl; and Ar3 is phenyl; R1 and R2 independently are hydrogen, halogen or —(CH2)mORe; R3 is hydrogen or alkyl; R4 is —(CH2)r-A1, wherein r is an integer of 1-5, and A1 has a formula of —O—C(O)—(CRcH)q—NRc′Rd′; R5 and R6 independently are hydrogen, halogen, or alkyl, or R5 and R6 together are —O(CH2)mO—; Rc is H, halogen, nitro, cyano, alkyl, or aryl; Re is H, alkyl, or aryl; Rc′ and Rd′ independently are H, alkyl, or aryl; m is 0, 1, 2, 3, 4, 5, or 6; and q is 1, 2, 3, 4, 5, or 6; or a salt thereof.

    Abstract translation: 合成具有下式的抗肿瘤效力的稠合吡唑基化合物：其中A为n为0,1,2或3; Ar1为苯，噻吩或呋喃; Ar2是呋喃基; 和Ar 3是苯基; R1和R2独立地是氢，卤素或 - （CH2）mORe; R3是氢或烷基; R4是 - （CH2）r-A1，其中r是1-5的整数，并且A1具有下式的-O-C（O） - （CRcH）q-NRc'Rd'; R5和R6独立地是氢，卤素或烷基，或R5和R6一起是-O（CH2）mO-; Rc是H，卤素，硝基，氰基，烷基或芳基; Re为H，烷基或芳基; Rc'和Rd'独立地是H，烷基或芳基; m为0,1,2,3,4,5或6; q为1,2,3,4,5或6; 或其盐。

Patent Agency Ranking