ACTIVATED MACROLACTAMS HAVING IMMUNOMODULATORY ACTIVITIES
    351.
    发明申请
    ACTIVATED MACROLACTAMS HAVING IMMUNOMODULATORY ACTIVITIES 审中-公开
    具有免疫调节活性的活化大肠杆菌

    公开(公告)号:WO1995004061A1

    公开(公告)日:1995-02-09

    申请号:PCT/US1994008646

    申请日:1994-07-29

    CPC classification number: C07D498/18 C07F7/1804

    Abstract: Activated macrolactam compounds having immunomodulatory activity and having formula (I), wherein n is zero or one, R is selected from the group consisting of methyl, ethyl, allyl, propyl and cyclopropylmethyl; R is hydrogen, and R is selected from the group consisting of hydrogen, hydroxy and a protected hydroxy group or, taken together, R and R form a bond; R and R are chosen such that one is hydrogen while the other is -OS(O)2F; and R is selected from the group consisting of hydrogen, a protected hydroxy group, lower alkyl, alkenyl, cycloalkyl, aryl and arylalkyl, as well as processes for making such compounds and methods for their use in the preparation of C-32-modified derivatives of ascomycin or the congeners or analogs thereof.

    Abstract translation: 具有免疫调节活性并具有式(I)的活性大分子内酰胺化合物,其中n为0或1,R 101选自甲基,乙基,烯丙基,丙基和环丙基甲基; R 102是氢,R 103选自氢,羟基和被保护的羟基,或者R 102和R 103一起形成一个键; R 104和R 105选自一个为氢,另一个为-OS(O)2 F; R 106选自氢,被保护的羟基,低级烷基,烯基,环烷基,芳基和芳基烷基,以及制备这些化合物的方法及其用于制备C-32的方法 修饰的子囊霉素衍生物或其同系物或类似物。

    ERYTHROMYCIN DERIVATIVES
    352.
    发明申请
    ERYTHROMYCIN DERIVATIVES 审中-公开
    红霉素衍生物

    公开(公告)号:WO1995001794A1

    公开(公告)日:1995-01-19

    申请号:PCT/US1994007575

    申请日:1994-07-06

    CPC classification number: C07H17/08

    Abstract: Antibacterial compounds having formula (II) and pharmaceutically acceptable salts thereof, wherein Y is selected form (a), (b), and (c) and X is selected from the group consisting of -C(O)-, -C(S)-, CH2-, -CH2CH2- and -C(CH3)2-; also disclosed are processes and intermediates useful in the preparation of the above compounds, as well as compositions containing the same and methods for their use.

    Abstract translation: 具有式(II)的抗菌化合物及其药学上可接受的盐,其中Y选自(a),(b)和(c)形式,X选自-C(O) - , - C ) - ,CH 2 - , - CH 2 CH 2 - 和-C(CH 3)2 - ; 还公开了可用于制备上述化合物的方法和中间体,以及含有该化合物的组合物及其使用方法。

    LOW PROFILE GASTROSTOMY DEVICE WITH DOME
    354.
    发明申请
    LOW PROFILE GASTROSTOMY DEVICE WITH DOME 审中-公开
    具有DOME的低剖面气体装置

    公开(公告)号:WO1994027655A1

    公开(公告)日:1994-12-08

    申请号:PCT/US1994004214

    申请日:1994-04-12

    Abstract: A gastrostomy device (30) for easier insertion into an established stoma is provided with an apertured dome (34) connected at its bottom wall to a tubular shaft (31), wherein the dome is particularly characterized by having the sidewall (38) thinned from apex to bottom wall whereby the dome, when elongated with an obturator, stretches smoothly and readily to very close to the diameter of the tubular shaft. The device is ordinarily provided with a one-way valve (42) mounted in the dome as well as with a retention flange (32) at the outer end of the tubular shaft. Preferably the one-way valve is a cross-slit duckbill valve of novel design.

    Abstract translation: 用于更容易地插入建立的造口的胃造口术装置(30)设置有在其底壁处连接到管状轴(31)的有孔圆顶(34),其中,圆顶的特征在于使侧壁(38)从 顶端到底壁,由此,当用闭孔器细长时,圆顶平滑且容易地伸展到非常接近管状轴的直径。 该装置通常设置有安装在圆顶中的单向阀(42)以及在管状轴的外端具有保持凸缘(32)。 优选地,单向阀是新颖设计的十字切口鸭嘴阀。

    SECURING COLLAR FOR CANNULA CONNECTOR
    356.
    发明申请
    SECURING COLLAR FOR CANNULA CONNECTOR 审中-公开
    保护肛门连接器

    公开(公告)号:WO1994023775A1

    公开(公告)日:1994-10-27

    申请号:PCT/US1994003077

    申请日:1994-03-22

    Abstract: A securing collar (10) is used in combination with two tubular flow connectors (12, 14) to prevent the inadvertent disconnection of I.V. tubing sets. The securing collar (10) includes a housing (26) supported by one of the connectors, a radial flange (42) extending from the housing (26), a tubular collar (44) having an outwardly splayed end, at least two notches (52) that separate the splayed collar (44) into at least two elongated segments, a transition portion (54) on the exterior of the collar, and a sliding annular locking ring (60). The locking ring (60) slides on the collar (44) from the proximal end over the transition portion to the distal segments so that the annular locking ring (60) forces the splayed and segmented distal portions radially inward to grip the second connector.

    Abstract translation: 固定环(10)与两个管状流动连接器(12,14)组合使用,以防止IV的意外断开。 管套。 所述固定环(10)包括由所述连接器之一支撑的壳体(26),从所述壳体(26)延伸的径向凸缘(42),具有向外张开的端部的管状套环(44),至少两个凹口 将所述凸出的轴环(44)分成至少两个细长段,所述轴环的外部上的过渡部分(54)和滑动环形锁定环(60)。 锁定环(60)在过渡部分上的近端处在轴环(44)上滑动到远侧段,使得环形锁定环(60)径向向内迫使张开的和分段的远端部分夹持第二连接器。

    TETRACYCLIC COMPOUNDS AS DOPAMINE AGONISTS
    357.
    发明申请
    TETRACYCLIC COMPOUNDS AS DOPAMINE AGONISTS 审中-公开
    四氢化合物作为DOPAMINE AGONISTS

    公开(公告)号:WO1994022858A1

    公开(公告)日:1994-10-13

    申请号:PCT/US1994002894

    申请日:1994-03-18

    CPC classification number: C07D491/04 C07D495/04 C07D513/04

    Abstract: A tetracyclic compound of formula (I) wherein A and the atoms to which it is attached and the optional double bond represent a mono- or di-heterocyclic ring selected from formulas (a), (b), (c), (d) and (e) wherein R , R , R , R and X are specifically defined, which compounds are useful in the treatment of dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of substance abuse and other addictive behavior disorders, cognitive impairment and attention deficit disorder.

    Abstract translation: 式(I)的四环化合物,其中A及其所连接的原子和任选的双键表示选自式(a),(b),(c),(d)的单 - 或二 - 杂环, 和(e)其中R 1,R 2,R 3,R 4和X是具体定义的,哪些化合物可用于治疗多巴胺相关的神经,心理和心血管疾病以及 在治疗药物滥用和其他成瘾行为障碍,认知障碍和注意力缺陷障碍。

    PACKAGING FOR T-SHAPED TENSION DEVICES
    358.
    发明申请
    PACKAGING FOR T-SHAPED TENSION DEVICES 审中-公开
    T形夹紧装置的包装

    公开(公告)号:WO1994022381A1

    公开(公告)日:1994-10-13

    申请号:PCT/US1994002728

    申请日:1994-03-14

    Abstract: A T-fastener installation kit (10) includes a packaging device (13) for loading a T-fastener (19) into a slotted needle (18) without requiring the hands of the surgeon to touch the sharp end of the needle. T-fasteners may be commonly used, for example, in surgical procedures in which the T-fasteners are used to secure a patient's stomach or bowel in apposition to the abdominal wall. The packaging device (13) includes a housing (15) having a cylindrical recess (26) into which the "T" head (45) of the T-fastener (19) is loaded. The surgeon can slide the open end of the slotted needle (18) into the cylindrical recess and over the "T" head of the T-fastener, thereby effectively loading the T-fastener into the slotted needle without requiring the surgeon to touch the sharp point of the needle.

    Abstract translation: T型紧固件安装套件(10)包括用于将T型紧固件(19)装载到开槽针(18)中的包装装置(13),而不需要外科医生的手接触针的尖端。 T型紧固件可以通常用于例如外科手术中,其中T型紧固件用于固定患者的胃或排便于腹壁的肠。 包装装置(13)包括具有圆柱形凹部(26)的壳体(15),T形紧固件(19)的“T”头(45)被装载到该圆柱形凹部中。 外科医生可以将开槽针(18)的开口端滑入圆柱形凹槽中并在T型紧固件的“T”头之上,从而有效地将T型紧固件装载到开缝针中,而不需要外科医生接触尖锐的 针点。

    MACROCYCLIC CARBAMATE IMMUNOMODULATORS
    359.
    发明申请
    MACROCYCLIC CARBAMATE IMMUNOMODULATORS 审中-公开
    大环碳酸盐免疫调节剂

    公开(公告)号:WO1994021643A1

    公开(公告)日:1994-09-29

    申请号:PCT/US1994002729

    申请日:1994-03-14

    CPC classification number: C07D498/18

    Abstract: Immunomodulatory macrocyclic compounds having formula (I) and the pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein R and R are selected such that one of R and R is hydrogen, and the other is chosen from the group consisting of: (1) -OC(=NR )-NHR ; (2) -OC(=O)-R ; and (3) -OC(=O)-NR R , (4) -OC(=O)-N(OR )R ; (5) -OC(=O)-NHNR R ; (6) -OC(=O)-NH-NHC(=O)-NR R ; (7) -OC(=O)-NH-NHS(O)2-NR R ; and (8) -OC(=O)-NH-NHC(=NR )-NR R as well as pharmaceutical compositions containing such compounds and methods for their use in immunosuppressive, antimicrobial, antifungal, antiviral, antiinflammatory and antiproliferative therapy.

    Abstract translation: 具有式(I)的免疫调节大环化合物及其药学上可接受的盐,酯,酰胺和前药,其中R 8和R 9被选择为使得R 8和R 9之一是氢,和 另一个选自:(1)-OC(= NR 10) - NHR 10; (2)-OC(= O)-R 11; 和(3)-OC(= O)-NR 12 R 13,(4)-OC(= O)-N(OR 14)R 12; (5)-OC(= O)-NHNR 12 R 13; (6)-OC(= O)-NH-NHC(= O)-NR 12 R 13; (7)-OC(= O)-NH-NHS(O)2 -NR 12 R 13; 和(8)-OC(= O)-NH-NHC(= NR 21)-NR 12 R 13以及含有这些化合物的药物组合物及其用于免疫抑制,抗微生物,抗真菌, 抗病毒,抗炎和抗增生治疗。

    MACROCYCLIC AMIDE AND UREA IMMUNOMODULATORS
    360.
    发明申请
    MACROCYCLIC AMIDE AND UREA IMMUNOMODULATORS 审中-公开
    大环酰胺和尿素免疫调节剂

    公开(公告)号:WO1994021642A1

    公开(公告)日:1994-09-29

    申请号:PCT/US1994002692

    申请日:1994-03-11

    CPC classification number: C07D498/18

    Abstract: Immunomodulatory macrocyclic compounds having formula (I) and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, as well as pharmaceutical compositions containing the same, which possess immunosuppressive, antimicrobial, antifungal, antiviral, antiinflammatory and antiproliferative activity, as well as the ability to reverse chemotherapeutic drug resistance.

    Abstract translation: 具有式(I)的免疫调节大环化合物及其药学上可接受的盐,酯,酰胺和前药,以及含有它们的药物组合物,其具有免疫抑制,抗微生物,抗真菌,抗病毒,抗炎和抗增殖活性,以及 逆转化疗药物耐药。

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