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    3-ALKYL-3-PHENYL-PIPERIDINES
    4.
    发明申请
    3-ALKYL-3-PHENYL-PIPERIDINES 审中-公开
    3-烷基-3-苯基 - 哌啶

    公开(公告)号：WO1998011090A2

    公开(公告)日：1998-03-19

    申请号：PCT/US1997015443

    申请日：1997-09-02

    Applicant: WARNER-LAMBERT COMPANY ,  CHEN, Michael, Huai, Gu ,  CHUNG, Fu-Zon ,  LEE, Helen, Tsenwhei

    Inventor： WARNER-LAMBERT COMPANY

    IPC: C07D401/00

    CPC classification number: C07D401/14 ,  C07D211/22 ,  C07D211/26 ,  C07D211/48 ,  C07D211/52 ,  C07D309/12 ,  C07D405/06

    Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.

    Abstract translation: 本发明的小非肽是速激肽拮抗剂。 这些化合物是高度选择性和功能性的NK3拮抗剂，预期可用于治疗疼痛，抑郁症，焦虑症，恐慌症，精神分裂症，神经痛，成瘾症，炎性疾病，胃肠道疾病，血管疾病和神经病理学疾病。

    BUTYRIC ACID MATRIX METALLOPROTEINASE INHIBITORS
    5.
    发明申请
    BUTYRIC ACID MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
    丁酸基金属蛋白酶抑制剂

    公开(公告)号：WO1998006711A1

    公开(公告)日：1998-02-19

    申请号：PCT/US1997012389

    申请日：1997-07-16

    Applicant: WARNER-LAMBERT COMPANY ,  SLISKOVIC, Drago, Robert ,  PICARD, Joseph, Armand

    Inventor： WARNER-LAMBERT COMPANY

    IPC: C07D307/91

    CPC classification number: C07D307/91 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12

    Abstract: Compounds of formula (I) wherein R1 and R2 include hydrogen, alkyl, substituted alkyl, halo, and arylalkyl; R3 is hydroxy, alkoxy, or hydroxyamino; X is O, S, or NOH; and R4 and R5 include hydrogen, alkyl, and aryl, are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.

    Abstract translation: 其中R1和R2包括氢，烷基，取代的烷基，卤素和芳基烷基的式（Ⅰ）化合物; R3是羟基，烷氧基或羟基氨基; X是O，S或NOH; R4和R5包括氢，烷基和芳基，可用于抑制动物中的基质金属蛋白酶，从而预防和治疗由结缔组织破坏引起的疾病。

    2-PHENYL BENZIMIDAZOLE DERIVATIVES AS MCP-1 ANTAGONISTS
    6.
    发明申请
    2-PHENYL BENZIMIDAZOLE DERIVATIVES AS MCP-1 ANTAGONISTS 审中-公开
    作为MCP-1拮抗剂的2-苯基苯并咪唑衍生物

    公开(公告)号：WO1998006703A1

    公开(公告)日：1998-02-19

    申请号：PCT/US1997013870

    申请日：1997-08-06

    Applicant: WARNER-LAMBERT COMPANY ,  CONNOR, David, Thomas ,  GLASE, Shelly, Ann ,  PURCHASE, Terri, Stoeber ,  ROTH, Bruce, David ,  TRIVEDI, Bharat, Kalidas

    Inventor： WARNER-LAMBERT COMPANY

    IPC: C07D235/18

    CPC classification number: C07D235/02 ,  C07D235/18

    Abstract: Benzimidazole derivatives of formula (I) or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, artherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection wherein A is N or CH; where W, X, Y and Z can be independently C-R2, C-R3, C-R4, C-R5, or N; no more than two of W, X, Y and Z can be N in any one structure, R2, R3, R4 and R5 can be independently H, C1-20 alkyl, halogen, nitro, -SO2NR8R9, alkoxy of from 1-4 carbon atoms; -S(O)pR where p is an integer from 0 to 2; -(CH2)mOR, -(CH2)mCOOR, -(CH2)mNR8R9, -(CH2)mCONR8R9, -(CH2)mCOR, or -CF3; m is an integer of from 0 to 4, R is hydrogen, lower alkyl of from 1-4 carbon atoms, aryl of from 6-10 carbon atoms, or benzyl; R1 can be H, lower alkyl of from 1-4 carbon atoms, or -(CH2)m-Ph; R6 is alkyl of from 1-6 carbon atoms or R7; R7 is (CH2)nNR10R11; n is an integer from 2 to 6; R8 and R9 can be independently hydrogen, lower alkyl of from 1-4 carbon atoms, or can be taken together to form a ring of from 3-8 atoms having up to one additional heteroatom as O, S, SO2, or N-R12; R10 and R11 can independently be lower alkyl, -(CH2)mPh, unsubstituted or substituted with up to three R2 substituents, or R10 and R11 can be taken together to form a ring of from 3-8 atoms which may contain oxygen or NR12; R12 is hydrogen, lower alkyl, -(CH2)tPh, where Ph is phenyl unsubstituted or substituted with up to three R2 substituents; t is an integer of from 0 to 2.

    Abstract translation: 式（I）的苯并咪唑衍生物或其药学上可接受的盐是MCP-1拮抗剂，因此可用于治疗炎症，动脉粥样硬化，再狭窄和免疫疾病如关节炎和移植排斥，其中A是N或CH; 其中W，X，Y和Z可以独立地为C-R2，C-R3，C-R4，C-R5或N; 不超过两个W，X，Y和Z可以是任何一个结构中的N，R2，R3，R4和R5可以独立地是H，C1-20烷基，卤素，硝基，-SO2NR8R9，1-4的烷氧基 碳原子 -S（O）p R，其中p是0至2的整数; - （CH 2）m COOR， - （CH 2）m COOR， - （CH 2）m NR 8 R 9， - （CH 2）m CONR 8 R 9， - （CH 2）m -COR或-CF 3; m为0-4的整数，R为氢，1-4个碳原子的低级烷基，6-10个碳原子的芳基或苄基; R1可以是H，1-4个碳原子的低级烷基，或 - （CH2）m-Ph; R6是1-6个碳原子的烷基或R7; R7是（CH2）nNR10R11; n为2-6的整数; R 8和R 9可以独立地为氢，1-4个碳原子的低级烷基，或者可以一起形成具有至多一个另外的杂原子的3-8个原子的环作为O，S，SO2或N-R12 ; R 10和R 11可以独立地为低级烷基， - （CH 2）m Ph，未被取代或被至多三个R 2取代基取代，或者R 10和R 11可以一起形成可含有氧或NR 12的3-8个原子的环; R 12是氢，低级烷基， - （CH 2）t Ph，其中Ph是未被取代或被至多三个R 2取代基取代的苯基; t是0到2的整数。

    AMIDE DERIVATIVES OF SUBSTITUTED QUINOXALINE 2,3-DIONES AS GLUTAMATE RECEPTOR ANTAGONISTS
    8.
    发明申请
    AMIDE DERIVATIVES OF SUBSTITUTED QUINOXALINE 2,3-DIONES AS GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
    取代的喹喔啉2,3-二酮作为谷氨酸受体拮抗剂的酰胺衍生物

    公开(公告)号：WO1997046539A1

    公开(公告)日：1997-12-11

    申请号：PCT/US1997008525

    申请日：1997-05-20

    Applicant: WARNER-LAMBERT COMPANY ,  NIKAM, Sham, S.

    Inventor： WARNER-LAMBERT COMPANY

    IPC: C07D241/44

    CPC classification number: C07D405/12 ,  C07D241/44 ,  C07D409/12

    Abstract: A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate receptor antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, seizure disorders, pain, Alzheimer's, Parkinson's, and Huntington's Diseases.

    Abstract translation: 教导了一系列用作神经保护剂的取代喹喔啉2,3-二酮。 还教导了新的中间体，制备方法和含有这些化合物的药物组合物。 这些化合物是谷氨酸受体拮抗剂，可用于治疗由血栓栓塞或出血性脑卒中，脑血管痉挛，低血糖症，心脏骤停，癫痫持续状态，围产期窒息，缺氧，癫痫发作，疼痛，阿尔茨海默氏症等引起的脑卒中，脑缺血或脑梗塞。 ，帕金森病和亨廷顿疾病。

    N-ACYL SULFAMIC ACID ESTERS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS
    10.
    发明申请
    N-ACYL SULFAMIC ACID ESTERS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS 审中-公开
    N-乙酰基硫酸酯有机物作为高效液相色谱

    公开(公告)号：WO1997044314A1

    公开(公告)日：1997-11-27

    申请号：PCT/US1997006725

    申请日：1997-04-21

    Applicant: WARNER-LAMBERT COMPANY ,  LEE, Helen, Tsenwhei ,  PICARD, Joseph, Armand ,  ROARK, William, Howard ,  ROTH, Bruce, David ,  SLISKOVIC, Drago, Robert

    Inventor： WARNER-LAMBERT COMPANY

    IPC: C07C307/02

    CPC classification number: C07C307/02 ,  C07C311/08 ,  C07C311/44 ,  C07C323/60 ,  C07D209/20

    Abstract: The instant invention is new compounds of formula (I), wherein R is -CN, -(CH2)0-1-NR R , -O-(CH2)1-10-Z wherein Z is -NR R , OR , or CO2R , -OC(=O)R , -SR , -SCN, -S(CH2)1-10Z, -S(O)1-2R wherein R is hydroxy, alkoxy, alkyl, (CH2)1-10Z or NR R , -C(=O)XR , -CH2-R wherein R is (CH2)0-5-Y-(CH2)0-5Z, or alkyl with from 1-3 double bonds, which alkyl is optionally substituted by one or more selected from -CN, NO2, halogen, OR , NR R , and CO2R ; their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.

    Abstract translation: 本发明是新的式（I）化合物，其中R 6是-CN， - （CH 2）0-1 -NR 7 R 8，-O-（CH 2）1-10 -Z，其中 Z是-NR 9 R 10，OR 1或CO 2 R 1，-OC（= O）R 11，-SR 11，-SCN，-S（CH 2） 10Z，-S（O）1-2R 12其中R 12是羟基，烷氧基，烷基，（CH 2）1-10Z或NR 7 R 8，-C（= O）X R 11 其中R 13为（CH 2）0-5-Y-（CH 2）0-5Z，或具有1-3个双键的烷基，该烷基任选被一个或多个 选自-CN，NO 2，卤素，OR 1，NR 9 R 10和CO 2 R 1; 它们用作中风，外周血管疾病，再狭窄等疾病中的脑血管因子，以及用于调节血浆胆固醇浓度的药剂，用于治疗高胆固醇血症和动脉粥样硬化，以及降低Lp（a）的血清或血浆水平。 还要求药物组合物。

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