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    Synthesis of anabaseine, salts and derivatives thereof
    1.
    发明授权
    Synthesis of anabaseine, salts and derivatives thereof 失效
    壬酰胺，其盐及其衍生物的合成

    公开(公告)号：US5530134A

    公开(公告)日：1996-06-25

    申请号：US301030

    申请日：1994-09-06

    申请人： Mohsen Daneshtalab ,  Dai Nguyen ,  Inderjit Sidhu ,  Ronald G. Micetich

    发明人： Mohsen Daneshtalab ,  Dai Nguyen ,  Inderjit Sidhu ,  Ronald G. Micetich

    IPC分类号： A61K31/44 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/443 ,  A61P25/28 ,  C07D213/50 ,  C07D401/04 ,  C07D405/06 ,  C07D211/68

    CPC分类号： C07D401/04 ,  C07D213/50

    摘要： A process for the synthesis of compounds of the formulas Ia and Ib below, wherein R.sub.1, R.sub.2, and R.sub.3, which are the same or different, are each selected from hydrogen and C.sub.1 -C.sub.4 alkyl, including the compound Anabaseine (Ia, wherein R.sub.1 =R.sub.2 R.sub.3 =H) (3,4,5,6-tetrahydro-2', 3'-bipyridine), the process comprising reacting sodium salt of .delta.-valerolactone with substituted ethyl nicotinate derivative to produce the Claisen product sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative, heating the sodium 3-nicotinoyl-2-tetrahydropyranone enolate derivative with concentrated HCl to produce 3-(5-chloro-1-pentanone-1-yl) pyridine derivative, dissolving the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol and then heating the 3-(5-chloro-1-pentanone-1-yl) pyridine derivative in ethanol with ethanolic ammonia solution in a sealed container to produce the compound Ia. Also, the process steps in the above process, and the products and intermediate products produced thereby. ##STR1##

    摘要翻译： 用于合成下式Ia和Ib化合物的方法，其中相同或不同的R 1，R 2和R 3各自选自氢和C 1 -C 4烷基，包括化合物Anabaseine（Ia，其中R1 = R2R3 = H）（3,4,5,6-四氢-2'，3'-联吡啶），该方法包括使δ-戊内酯的钠盐与取代的乙酸烟酸衍生物反应，生成Claisen产物3-烟酰基-3- 2-氯-4-羟基吡喃酮烯醇化物衍生物，用浓HCl加热3-烟酰基-2-四氢吡喃酮-3-烯醇钠衍生物，得到3-（5-氯-1-戊酮-1-基）吡啶衍生物，将3-（5-氯 - 1-戊酮-1-基）吡啶衍生物在乙醇中的溶液中，然后在密封容器中用乙醇氨溶液将3-（5-氯-1-戊酮-1-基）吡啶衍生物在乙醇中加热，得到化合物Ia。 而且，上述工艺中的工艺步骤以及由此生产的产品和中间产品。

    Penicillin derivatives
    3.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4529592A

    公开(公告)日：1985-07-16

    申请号：US501560

    申请日：1983-06-06

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Tomio Yamazaki ,  Naobumi Ishida ,  Takeshi Ishizawa

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Tomio Yamazaki ,  Naobumi Ishida ,  Takeshi Ishizawa

    IPC分类号： C07D499/87 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  A61P43/00 ,  C07D499/00 ,  C07D499/86 ,  C07D499/897 ,  C07F7/10

    CPC分类号： C07D499/00 ,  C07F7/10

    摘要： A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 and R.sub.2 are each the same or different and represent hydrogen, C.sub.1-18 alkyl, mononitro-substituted benzyl or group for forming a pharmaceutically acceptable salt and R.sub.3 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl and group for forming a pharmaceutically acceptable salt.

    摘要翻译： 由下式（IMAGE）表示的青霉素衍生物，其中R 1和R 2各自相同或不同，表示氢，C 1-18烷基，一硝基取代的苄基或用于形成药学上可接受的盐的基团，R 3选自 氢，C 1-6烷基，C 2-7烷氧基甲基，C 3-8烷基羰基氧基甲基，C 4-9烷基羰基氧基乙基，（C 5-7环烷​​基）羰基氧基甲基，C 9-14苄基羰氧基烷基，C 3-8烷氧基羰基甲基，C 4-9烷氧基羰基乙基， 吡啶-4-基，γ-丁内酯-4-基，被1至3个卤素原子取代的卤代C 1-6烷基，C 1-6烷氧基或硝基取代或未取代的苄基，二苯甲基，四氢吡喃基，二甲基氨基乙基，二甲基氯甲硅烷基，三氯硅烷基（5 取代的C 1-6烷基或苯基或未取代的-2-氧代-1,3-二氧杂环己烯-4-基）甲基，C 13-13苯甲酰氧基烷基和用于形成药学上可接受的盐的基团。

    Thioamides
    5.
    发明授权
    Thioamides 失效
    硫胺

    公开(公告)号：US4039530A

    公开(公告)日：1977-08-02

    申请号：US589560

    申请日：1975-06-23

    申请人： Ronald G. Micetich ,  Robert B. Morin

    发明人： Ronald G. Micetich ,  Robert B. Morin

    IPC分类号： C07D205/095 ,  C07D205/08

    CPC分类号： C07D205/095

    摘要： The invention relates to compounds of the formula: ##STR1## wherein R stands for lower alkyl, aryl, heteroaryl, benzyl, heteroarylloweralkyl, phenoxyloweralkyl, phenylthioloweralkyl, 4-amino-1-butyl and suitably protected derivatives, .alpha.-aminobenzyl and protected derivatives such as the carbamates (benzyl, trichloroethyl and methoxymethyl) and aldehyde and ketone adducts, .alpha.-hydroxybenzyl and protected derivatives, .alpha.-carboxybenzyl and protected derivatives, .alpha.-sulfobenzyl and protected derivatives, the radical R.sup.5 O--, R.sup.5 S--, or R.sup.5 R.sup.6 N--,wherein R.sup.5 and R.sup.6 may be the same or different and each be taken from the group lower alkyl, aryl, arylloweralkyl and heteroaryl and additionally, in the case of R.sup.5 R.sup.6 N--, R.sup.5 and/or R.sup.6 may be hydrogen;R.sup.1 is hydrogen or a cleavable radical such as loweralkoxymethyl, acyloxymethyl, loweralkylthiomethyl, loweralkyl, 2,2,2-trichloroethyl, benzyl, substituted (nitro, methoxy or halo) benzyl, benzhydryl, phenacyl or trialkylsilyl;R.sup.2 is hydrogen or methoxy;R.sup.3 stands for lower alkyl, aryl, arylloweralkyl, heteroaryl, and the radicals R.sup.5 O--, R.sup.5 S--, R.sup.5 R.sup.6 N--, or R.sup.5 R.sup.6 NR.sup.7 N-- wherein R.sup.5 and R.sup.6 have the same meaning set forth above; and R.sup.7 has the same meaning as R.sup.5 or R.sup.6 including hydrogen, andR.sup.4 has the same meaning as R.sup.5 or R.sup.6 including hydrogen.Broken lines at positions 3 and 4 in the formula indicate a double bond in either of the two positions;The novel compounds are useful intermediates in the preparation of cephalosporins and penicillins.

    摘要翻译： 本发明涉及下式的化合物：其中R代表低级烷基，芳基，杂芳基，苄基，杂芳基低级烷基，苯氧基低级烷基，苯基硫代低级烷基，4-氨基-1-丁基和适当保护的衍生物，α-氨基苄基和被保护的衍生物 例如氨基甲酸酯（苄基，三氯乙基和甲氧基甲基）和醛和酮加成物，α-羟基苄基和被保护的衍生物，α-羧基苄基和被保护的衍生物，α-磺基苄基和受保护的衍生物，基团R5O-，R5S-或R5R6N-， 其中R 5和R 6可以相同或不同，各自为低级烷基，芳基，芳基低级烷基和杂芳基，另外在R5R6N-的情况下，R5和/或R6可以是氢; R1是氢或可裂解的基团，例如低级烷氧基甲基，酰氧基甲基，低级烷硫基甲基，低级烷基，2,2,2-三氯乙基，苄基，取代的（硝基，甲氧基或卤代）苄基，二苯甲基，苯甲酰甲基或三烷基甲硅烷基。 R2是氢或甲氧基; R3代表低级烷基，芳基，芳基低级烷基，杂芳基和基团R5O-，R5S-，R5R6N-或R5R6NR7N-，其中R5和R6具有上述相同的含义; 并且R 7具有与包含氢的R 5或R 6相同的含义，并且R 4具有与包括氢的R 5或R 6相同的含义。

    Oligopeptide antiretroviral agents
    6.
    发明授权
    Oligopeptide antiretroviral agents 失效
    寡肽抗逆转录病毒药

    公开(公告)号：US5616606A

    公开(公告)日：1997-04-01

    申请号：US510333

    申请日：1995-08-02

    申请人： J. William Lown ,  Ronald G. Micetich

    发明人： J. William Lown ,  Ronald G. Micetich

    IPC分类号： A61K31/40 ,  A61K31/44 ,  C07D207/34 ,  C07D401/14 ,  A61K37/00 ,  C07K7/06 ,  C07C103/52

    CPC分类号： C07D401/14 ,  A61K31/40 ,  A61K31/44 ,  C07D207/34

    摘要： Oligopeptide antiretroviral agents are represented by formula (I), wherein A is a moiety bearing a positive charge and of a size which avoids steric inhibition of binding of said compound to nucleic acid sequences associated with the cellular activity of retroviruses; R.sub.1 is a moiety derived from a dicarboxylic acid; Hew is a five-membered heterocyclic moiety; y and z are independently 0, 1, 2 or 3; and x is 0 or 1. These compounds exhibit antiretroviral activity, especially against Human Immunodeficiency Virus (HIV). ##STR1##

    摘要翻译： 寡肽抗逆转录病毒剂由式（I）表示，其中A是具有正电荷和大小的部分，其避免空间抑制所述化合物与逆转录病毒细胞活性相关的核酸序列的结合; R1是衍生自二羧酸的部分; Hew是五元杂环部分; y和z独立地为0,1,2或3; 这些化合物表现出抗逆转录病毒活性，特别是针对人类免疫缺陷病毒（HIV）。 （1）

    6.beta.-substituted penicillanic acids as beta-lactamase inhibitors
    7.
    发明授权
    6.beta.-substituted penicillanic acids as beta-lactamase inhibitors 失效
    6β-取代的青霉烷酸作为β-内酰胺酶抑制剂

    公开(公告)号：US5464616A

    公开(公告)日：1995-11-07

    申请号：US285670

    申请日：1994-08-04

    申请人： Kazuharu Noguchi ,  Ronald G. Micetich ,  Mohsen Daneshtalab

    发明人： Kazuharu Noguchi ,  Ronald G. Micetich ,  Mohsen Daneshtalab

    IPC分类号： C07D499/10 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/70 ,  C07D499/72 ,  C07D499/76 ,  A61K31/425

    CPC分类号： C07D499/00

    摘要： A 6.beta.-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, whereinA and B are each hydrogen wherein the carbon atoms to which A and B are attached are linked by a single bond, or A and B together form a bond, wherein the carbon atoms to which A and B are attached are linked by a double bond,R1 is selected from the group consisting of a) hydrogen, b) a pharmaceutically acceptable salt and c) a pharmaceutically acceptable group selected from the group consisting of C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, allyl, aryl, aralkyl, aralkenyl, aralkynyl, heterocyclyl, heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkynyl and alkylheterocyclyl; wherein said group c) is unsubstituted or substituted with a substituent selected from the group consisting of floro, chloro, bromo, iodo, azido, nitro, monoalkyl substituted amino, dialkyl substituted amino, aryl substituted amino, alkanoylamino, arylcarbonylamino, cyano, hydroxy, alkoxy, aryloxy, alkanoyloxy, arylcarbonyloxy, mercapto, alkylthio, arylthio, alkanoylthio, arylcarbonylthio, oxyimino, alkoxyimino and carboxy, andn is an integer between 0 and 2.

    摘要翻译： 式XII的6β-取代的青霉烷酸：其中A和B各自为氢，其中A和B所连接的碳原子通过单键连接，或 A和B一起形成键，其中A和B连接的碳原子通过双键连接，R 1选自a）氢，b）药学上可接受的盐，和c）药学上可接受的盐 选自C1-10烷基，C2-10烯基，C2-10炔基，C3-10环烷基，C3-10环烯基，烯丙基，芳基，芳烷基，芳烯基，芳炔基，杂环基，杂环基烷基，杂环基烯基，杂环基炔基和 烷基杂环基 其中所述基团c）未被取代或被选自以下的取代基取代：氟，氯，溴，碘，叠氮基，硝基，单烷基取代的氨基，二烷基取代的氨基，芳基取代的氨基，烷酰基氨基，芳基羰基氨基，氰基，羟基， 烷氧基，芳氧基，烷酰氧基，芳基羰氧基，巯基，烷硫基，芳硫基，烷酰硫基，芳基羰硫基，氧亚氨基，烷氧基亚氨基和羧基，n为0〜2的整数。

    3,4-Diarylisoxazol-5-acetic acids and process for making same
    10.
    发明授权
    3,4-Diarylisoxazol-5-acetic acids and process for making same 失效
    3,4-二芳基异恶唑-5-乙酸及其制备方法

    公开(公告)号：US4327222A

    公开(公告)日：1982-04-27

    申请号：US190060

    申请日：1980-09-23

    申请人： Ronald G. Micetich ,  Chia-Cheng Shaw ,  Ram B. Rastogi

    发明人： Ronald G. Micetich ,  Chia-Cheng Shaw ,  Ram B. Rastogi

    IPC分类号： A61K31/42 ,  A61P25/04 ,  A61P29/00 ,  C07D261/08

    CPC分类号： C07D261/08 ,  Y10S514/916

    摘要： 3,4-Diarylisoxazol-5-acetic acids of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are the same or different and are selected from phenyl and naphthyl, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are the same or different and are selected from hydrogen, halogen, trifluoromethyl, lower alkyl, and lower alkoxy, and R.sup.5 is selected from hydrogen, lower alkyl, and lower alkoxy. The compounds have anti-inflammatory, analgesic, and anti-pyretic activities and a low order of toxicity, and methods for their preparation and use are also disclosed.

    摘要翻译： 其中Ar1和Ar2相同或不同并且选自苯基和萘基的式“IMAGE”1的3,4-二芳基异恶唑-5-乙酸是相同的或不同的，并且是 选自氢，卤素，三氟甲基，低级烷基和低级烷氧基，R 5选自氢，低级烷基和低级烷氧基。 这些化合物具有抗炎，止痛和抗热解活性和低毒性，并且还公开了它们的制备和使用方法。