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    4-[4'-PIPERIDINYL OR 3'-PIRROLIDINYL] SUBSTITUTED IMIDAZOLES AS H3-RECEPTOR ANTAGONISTS AND THERAPEUTIC USES THEREOF
    1.
    发明申请
    4-[4'-PIPERIDINYL OR 3'-PIRROLIDINYL] SUBSTITUTED IMIDAZOLES AS H3-RECEPTOR ANTAGONISTS AND THERAPEUTIC USES THEREOF 审中-公开
    4- [4'-哌啶基或3'-吡啶二基]取代的咪唑烷作为H3-受体拮抗剂及其治疗用途

    公开(公告)号：WO1993020061A1

    公开(公告)日：1993-10-14

    申请号：PCT/US1993003104

    申请日：1993-03-31

    Applicant: THE UNIVERSITY OF TOLEDO ,  DURANT, Graham, J. ,  KHAN, Amin, M.

    Inventor： THE UNIVERSITY OF TOLEDO

    IPC: C07D401/04

    CPC classification number: C07D401/04 ,  A61K31/415 ,  A61K31/445 ,  C07D403/04

    Abstract: The present invention provides novel compounds having activity as histamine H3-receptor antagonists. In a preferred aspect, the compounds of the invention exhibit ready penetration of the blood-brain-barrier and reduced toxicity. The novel compounds of the invention include compounds of the formula (I) wherein D is CH2 or CH2-CH2, Z represents S or O, preferably O, x is 0 or 1, n is an integer from 0 to 6, R1 represents preferably hydrogen, or a hydrolysable group, but can be a lower alkyl or aryl group, and R2 represents a linear chain, branched chain or carbocyclic group or aryl group of up to about 20 carbon atoms, and salts thereof. If R2 is tert-butyl, cyclohexyl, or dicyclohexylmethyl, x or n must not be 0. If R2 is adamantane, the sum of x and n must be greater than 1. The various alkyl or aryl groups can have functional group substituents. Illustrative of the compounds of the invention is the molecule 4-(1-cyclohexylvaleryol-4-piperidyl)-1H-imidazole.

    Abstract translation: 本发明提供具有组胺H3受体拮抗剂活性的新化合物。 在优选的方面，本发明的化合物显示了血脑屏障的准备好的渗透和降低的毒性。 本发明的新化合物包括式（I）化合物，其中D是CH 2或CH 2 -CH 2，Z代表S或O，优选O，x是0或1，n是0至6的整数，R 1优选 氢或可水解基团，但可以是低级烷基或芳基，并且R 2表示具有至多约20个碳原子的直链，支链或碳环基或芳基及其盐。 如果R 2为叔丁基，环己基或二环己基甲基，则x或n不能为0.如果R 2为金刚烷，则x和n之和必须大于1.各种烷基或芳基可具有官能团取代基。 本发明化合物的实例是分子4-（1-环戊基-4-哌啶基）-1H-咪唑。

    BIOARTIFICIAL PANCREAS
    2.
    发明申请
    BIOARTIFICIAL PANCREAS 审中-公开
    生物谷

    公开(公告)号：WO1994003126A1

    公开(公告)日：1994-02-17

    申请号：PCT/US1993007078

    申请日：1993-07-28

    Applicant: THE UNIVERSITY OF TOLEDO

    Inventor： THE UNIVERSITY OF TOLEDO ,  FOURNIER, Ronald, L. ,  GOLDBLATT, Peter, J. ,  HORNER, James, M. ,  SARVER, Jeffrey, G.

    IPC: A61F02/02

    CPC classification number: A61F2/022

    Abstract: An implantable bioartificial pancreas device (1) having an islet chamber (5) containing glucose responsive and insulin-secreting islets of Langerhans or similar hormone secreting cells, the islet chamber (5) having baffle means (60) inside thereof to assist in even distribution of the islets in the chamber, one or more vascularizing chambers (10) open to surrounding tissue, a semi-permeable membrane (25) between the islet and vascularizing chambers that allows passage of small molecules including insulin, oxygen and glucose and does not allow passage of agents of the immune system such as white cells and antibodies, the vascularizing chambers containing a growth factor soaked fibrous or foam matrix (30) having a porosity of about 40 to 95 %, the matrix providing small capillary growth and preventing the blood from clotting in the lower chamber.

    Abstract translation: 一种具有胰岛室（5）的可植入生物人造胰腺装置（1），所述胰岛室（5）含有葡萄糖反应性胰岛素分泌胰岛或类胰激素分泌细胞，所述胰岛室（5）在其内部具有挡板装置（60）以辅助均匀分布 的胰岛，一个或多个向周围组织开放的血管化室（10），胰岛和血管化室之间的半透膜（25），允许小分子包括胰岛素，氧和葡萄糖通过，并且不允许 免疫系统的药物如白细胞和抗体的通过，血管化腔含有生长因子浸泡的纤维状或泡沫基质（30），孔隙率为约40至95％，所述基质提供较小的毛细血管生长并防止血液 凝结在下腔室。

    PRODUCTION AND USE OF IMINES OF PORPHYRINS
    5.
    发明申请
    PRODUCTION AND USE OF IMINES OF PORPHYRINS 审中-公开
    生产和使用吡啶的方法

    公开(公告)号：WO1994000118A1

    公开(公告)日：1994-01-06

    申请号：PCT/US1993005727

    申请日：1993-06-16

    Applicant: THE UNIVERSITY OF TOLEDO ,  MEDICAL COLLEGE OF OHIO

    Inventor： THE UNIVERSITY OF TOLEDO ,  MEDICAL COLLEGE OF OHIO ,  SKALKOS, Dimitris ,  SELMAN, Steven, H. ,  HAMPTON, James, A.

    IPC: A61K31/40

    CPC classification number: C07D487/22 ,  A61K31/40 ,  A61K31/555

    Abstract: Purified imines of porphyrins, chlorins, bacteriochlorins, chlorophylls, bacteriochlorophylls, purpurins, reduced purpurins, verdins, Diels Alder adducts, benzochlorins and metal complexes of the foregoing imines are disclosed. The formulas of the benzochlorinimines and of the benzochlorinimine metal complexes are set forth (1) and (2). In specific examples, M in the metal complexes is a copper cation that is complexed with two of the nitrogens of the benzochlorinimine R' and R"" are methyl, and R1 through R8 are ethyl.

    Abstract translation: 公开了卟啉，二氢卟酚，细菌二氢卟酚，叶绿素，细菌叶绿素，紫草素，还原紫草素，葡蛋白，狄尔斯lder木加合物，苯并二氢卟酚和前述亚胺的金属络合物的亚胺。 （1）和（2）列出了苯并氯嘧啶和苯并氯亚胺金属络合物的配方。 在具体实例中，金属络合物中的M是与两个苯并氯嘧啶R'的氮络合的铜阳离子，R“”是甲基，R 1至R 8是乙基。

    MUSCARINIC AGONISTS
    6.
    发明申请
    MUSCARINIC AGONISTS 审中-公开
    肌肉激素

    公开(公告)号：WO1998046232A1

    公开(公告)日：1998-10-22

    申请号：PCT/US1997006218

    申请日：1997-04-15

    Applicant: THE UNIVERSITY OF TOLEDO

    Inventor： THE UNIVERSITY OF TOLEDO ,  MESSER, William, S., Jr. ,  OJO, Babatunde

    IPC: A61K31/505

    CPC classification number: C07D239/06 ,  C07D413/04

    Abstract: A muscarinic agonist compound having formula (I) or (II) or a pharmaceutically acceptable salt thereof. In formula (I) R is (trans) 3-methyl-2-penten-4-ynyl, (cis) 3-methyl-2-penten-4-ynyl, 2-butynyl, 2-methylbutenyl, 3-methylpropynyl, phenylpropynyl, butynyl. In formula (II) R' is butynyl.

    Abstract translation: 具有式（I）或（II）的毒蕈碱激动剂化合物或其药学上可接受的盐。 在式（I）中，R是（反式）3-甲基-2-戊烯-4-炔基，（顺式）3-甲基-2-戊烯-4-炔基，2-丁炔基，2-甲基丁烯基，3-甲基丙炔基，苯基丙炔基 ，丁炔基。 在式（II）中，R'是丁炔基。

    HISTAMINE H3-RECEPTOR ANTAGONISTS AND THERAPEUTIC USES THEREOF
    7.
    发明申请
    HISTAMINE H3-RECEPTOR ANTAGONISTS AND THERAPEUTIC USES THEREOF 审中-公开
    组胺H3受体拮抗剂及其治疗用途

    公开(公告)号：WO1995011894A1

    公开(公告)日：1995-05-04

    申请号：PCT/US1994011790

    申请日：1994-10-18

    Applicant: THE UNIVERSITY OF TOLEDO ,  GLIATECH, INC.

    Inventor： THE UNIVERSITY OF TOLEDO ,  GLIATECH, INC. ,  DURANT, Graham, J. ,  KHAN, Amin, M. ,  TEDFORD, Clark, E.

    IPC: C07D401/04

    CPC classification number: C07D401/04 ,  A61K31/415 ,  A61K31/445 ,  C07D403/04

    Abstract: The present invention is directed to compounds of the class of piperidyl-imidazole derivative histamine H3-receptor antagonist. Such compounds have affinity for histamine H3-receptor, and preferably penetrate the blood-brain barrier. The compounds can block the soporific effect of an H3-receptor agonist. Illustrative of the compounds of the invention is the molecule 4-(1-cyclohexylvaleroyl-4-piperidyl)-1H-imidazole. These compounds have been found to have utility in treating cognitive disorders and have been found to be useful as appetite suppressants.

    Abstract translation: 本发明涉及哌啶 - 咪唑衍生物组胺H3受体拮抗剂类的化合物。 这些化合物对组胺H3受体具有亲和力，优选渗透血脑屏障。 这些化合物可以阻止H3受体激动剂的发挥作用。 本发明化合物的实例是分子4-（1-环己基戊酰基-4-哌啶基）-1H-咪唑。 已经发现这些化合物在治疗认知障碍中具有用途，并且已被发现可用作食欲抑制剂。

    DELIVERY OF A CYTOTOXIC COMPOUND TO A CANCER CELL USING A PATHWAY OF PLASMINOGEN ACTIVATOR MATERIAL
    8.
    发明申请
    DELIVERY OF A CYTOTOXIC COMPOUND TO A CANCER CELL USING A PATHWAY OF PLASMINOGEN ACTIVATOR MATERIAL 审中-公开
    将细胞毒素化合物递送至使用PLASMINOGEN ACTIVATOR材料途径的癌细胞

    公开(公告)号：WO1993024141A1

    公开(公告)日：1993-12-09

    申请号：PCT/US1993005034

    申请日：1993-05-27

    Applicant: THE UNIVERSITY OF TOLEDO

    Inventor： THE UNIVERSITY OF TOLEDO ,  JANKUN, Jerzy ,  HART, Richard

    IPC: A61K37/36

    CPC classification number: C07K14/81 ,  A61K47/62

    Abstract: A method of delivering a cytotoxic compound to a cancer cell and getting the compound inside the cancer cell using a plasminogen material such as a plasminogen activator inhibitor (PAI-1). The toxic compound is coupled to PAI-1 to form a reaction product that is coupled with urokinase plasminogen activator (uPA) that is bound to the cell surface by uPA receptors (uPAR). The resultant complex is internalized to enter the cancer cell to deliver the cytotxic compound within the cell.

    Abstract translation: 使用纤溶酶原物质如纤溶酶原激活物抑制剂（PAI-1）将细胞毒性化合物递送至癌细胞并使化合物进入癌细胞内的方法。 有毒化合物与PAI-1偶联以形成与uPA受体（uPAR）结合于细胞表面的尿激酶纤溶酶原激活物（uPA）结合的反应产物。 所得的复合物被内化以进入癌细胞以将细胞毒化合物递送到细胞内。

    ELECTROLESS PLATING OF A METAL LAYER ON AN ACTIVATED SUBSTRATE
    9.
    发明申请
    ELECTROLESS PLATING OF A METAL LAYER ON AN ACTIVATED SUBSTRATE 审中-公开
    金属层在活性基体上的电镀

    公开(公告)号：WO1997046326A1

    公开(公告)日：1997-12-11

    申请号：PCT/US1997009247

    申请日：1997-05-30

    Applicant: THE UNIVERSITY OF TOLEDO

    Inventor： THE UNIVERSITY OF TOLEDO ,  FRY, James, L. ,  UHLENBROCK, Stephen ,  KLEIN, Rita

    IPC: B05D03/04

    CPC classification number: C23C18/1893 ,  C23C18/1658

    Abstract: A method of electroless plating at least one homogeneous metal coating in a predetermined pattern on a solid substrate surface having pendant hydroxy groups. The method includes the steps of providing a first monatomic metal layer in a predetermined pattern on the solid substrate surface having pendant hydroxy groups and then immersing the solid substrate surface in a bath containing a chemical reducing agent to build up the at least one homogeneous metal coating only on the monatomic metal layer.

    Abstract translation: 在具有侧羟基的固体基材表面上以预定图案化学镀至少一种均匀金属涂层的方法。 该方法包括以下步骤：在具有侧羟基的固体基材表面上以预定图案提供第一单原子金属层，然后将固体基材表面浸入含有化学还原剂的浴中，以形成至少一种均质金属涂层 仅在单原子金属层上。

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