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    SUSTAINED RELEASE OF MICROCRYSTALLINE PEPTIDE SUSPENSIONS
    11.
    发明申请
    SUSTAINED RELEASE OF MICROCRYSTALLINE PEPTIDE SUSPENSIONS 审中-公开
    持续释放微晶蛋白酶悬浮液

    公开(公告)号：US20100239683A1

    公开(公告)日：2010-09-23

    申请号：US12795246

    申请日：2010-06-07

    申请人： Romano Deghenghi ,  Francois Boutignon

    发明人： Romano Deghenghi ,  Francois Boutignon

    IPC分类号： A61K9/19 ,  A61K9/14 ,  A61P5/04 ,  A61K38/02 ,  A61K38/24 ,  A61K38/31 ,  A61P5/02

    CPC分类号： A61K9/0024 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/19 ,  A61K38/09 ,  A61K38/31 ,  A61K47/02 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26

    摘要： The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

    摘要翻译： 本发明涉及肽或肽模拟物的流体，乳状微晶水悬浮液和水中强质子供体的抗衡离子，其中肽或拟肽和抗衡离子以足以形成的量和摩尔比存在 混合后的悬浮液，而不形成凝胶。 本发明还涉及包含干燥悬浮液，制备冻干组合物的方法，制备悬浮液的方法和通过该方法制备的持续释放制剂的冻干组合物。

    Pseudopeptides growth hormone secretagogues
    12.
    发明授权
    Pseudopeptides growth hormone secretagogues 失效
    假肽生长激素促分泌素

    公开(公告)号：US07034050B2

    公开(公告)日：2006-04-25

    申请号：US10835563

    申请日：2004-04-28

    申请人： Romano Deghenghi

    发明人： Romano Deghenghi

    IPC分类号： A61K31/405 ,  C07D209/04

    CPC分类号： C07K5/06026 ,  A61K38/00

    摘要： The present invention relates to novel growth hormone releasing pseudopeptides capable of stimulating the release of growth hormone from the pituitary and of promoting growth in mammals. The invention also provides pharmaceutical compositions comprising the pseudopeptides growth hormone secretagogues and a method for promoting the release of growth hormone in mammals. If continuously administered, the present pseudopeptides may also inhibit the release of growth hormone by down-regulating the growth response. An exemplary pseudopeptide compound of this invention is Aib-D-Trp-D-Trpψ[CH2—NH—O]Gly-NH2:

    摘要翻译： 本发明涉及能够刺激生长激素从垂体中释放并促进哺乳动物生长的新型生长激素释放假肽。 本发明还提供包含假多肽生长激素促分泌素的药物组合物和促进哺乳动物中生长激素释放的方法。 如果连续施用，本发明的假肽也可以通过下调生长反应来抑制生长激素的释放。 本发明的示例性假肽化合物是Aib-D-Trp-D-Trppsi [CH 2 -NH-O] Gly-NH 2：

    Pseudopeptides growth hormone secretagogues
    13.
    发明申请
    Pseudopeptides growth hormone secretagogues 失效
    假肽生长激素促分泌素

    公开(公告)号：US20050245457A1

    公开(公告)日：2005-11-03

    申请号：US10835563

    申请日：2004-04-28

    申请人： Romano Deghenghi

    发明人： Romano Deghenghi

    IPC分类号： A61K38/00 ,  C07K5/06 ,  A61K38/04 ,  A61K31/405 ,  C07D43/02

    CPC分类号： C07K5/06026 ,  A61K38/00

    摘要： The present invention relates to novel growth hormone releasing pseudopeptides capable of stimulating the release of growth hormone from the pituitary and of promoting growth in mammals. The invention also provides pharmaceutical compositions comprising the pseudopeptides growth hormone secretagogues and a method for promoting the release of growth hormone in mammals. If continuously administered, the present pseudopeptides may also inhibit the release of growth hormone by down-regulating the growth response. An exemplary pseudopeptide compound of this invention is Aib-D-Trp-D-Trpψ[CH2—NH—O]Gly-NH2:

    摘要翻译： 本发明涉及能够刺激生长激素从垂体中释放并促进哺乳动物生长的新型生长激素释放假肽。 本发明还提供包含假多肽生长激素促分泌素的药物组合物和促进哺乳动物中生长激素释放的方法。 如果连续施用，本发明的假肽也可以通过下调生长反应来抑制生长激素的释放。 本发明的示例性假肽化合物是Aib-D-Trp-D-Trppsi [CH 2 -NH-O] Gly-NH 2：

    Process to manufacture implants containing bioactive peptides
    15.
    发明授权
    Process to manufacture implants containing bioactive peptides 失效
    制造含有生物活性肽的植入物的方法

    公开(公告)号：US5945128A

    公开(公告)日：1999-08-31

    申请号：US897942

    申请日：1997-07-21

    申请人： Romano Deghenghi

    发明人： Romano Deghenghi

    IPC分类号： A61K9/00 ,  A61K9/20 ,  A61K38/00 ,  A61K47/34 ,  A61K9/50 ,  B01J13/02

    CPC分类号： A61K9/0024 ,  A61K9/204 ,  A61K9/2095

    摘要： A process for manufacturing a pharmaceutical composition for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This process includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.; aseptically extruding the dried mixture at a temperature between about 70 and 110.degree. C.; and aseptically cutting cylindrical rods of about 1 to 2 mm diameter and between about 10 and 25 mm in length from the extruded mixture to form the pharmaceutical implants.

    摘要翻译： 1到12个月的时间内制备用于递送有效量的生物活性肽或肽类似物的药物组合物的方法。 该方法包括以下步骤：将具有约0至5：1的乙交酯与丙交酯单元的比例的乳酸和乙醇酸的共聚物研磨至约50至150μm的粒度; 以约1至2.5Mrad的电离γ辐射剂量灭菌研磨共聚物; 用生物活性肽或肽类似物的无菌水性浆液润湿研磨和灭菌的共聚物; 无菌混合共聚物和浆料以获得共聚物的均匀混合物和约10至50％的生物活性肽或肽类似物; 在减压和不超过25℃的温度下干燥混合物。 在约70至110℃的温度下无菌挤出干燥的混合物; 以及无菌切割直径为1至2mm直径的长度为约10至25mm的长圆柱形棒，从而形成药物植入物。

    SUSTAINED RELEASE OF MICROCRYSTALLINE PEPTIDE SUSPENSIONS
    18.
    发明申请
    SUSTAINED RELEASE OF MICROCRYSTALLINE PEPTIDE SUSPENSIONS 有权
    持续释放微晶蛋白酶悬浮液

    公开(公告)号：US20110312889A1

    公开(公告)日：2011-12-22

    申请号：US13224105

    申请日：2011-09-01

    申请人： Romano Deghenghi ,  Francois Boutignon

    发明人： Romano Deghenghi ,  Francois Boutignon

    IPC分类号： A61K38/09 ,  A61P43/00 ,  A61K38/00 ,  A61K38/08 ,  C07K2/00 ,  C07K7/06

    CPC分类号： A61K9/0024 ,  A61K9/0019 ,  A61K9/10 ,  A61K9/19 ,  A61K38/09 ,  A61K38/31 ,  A61K47/02 ,  A61K47/12 ,  A61K47/20 ,  A61K47/26

    摘要： The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

    摘要翻译： 本发明涉及肽或肽模拟物的流体，乳状微晶水悬浮液和水中强质子供体的抗衡离子，其中肽或拟肽和抗衡离子以足以形成的量和摩尔比存在 混合后的悬浮液，而不形成凝胶。 本发明还涉及包含干燥悬浮液，制备冻干组合物的方法，制备悬浮液的方法和通过该方法制备的持续释放制剂的冻干组合物。

    Diazaspiro, azepino and azabicyclo therapeutic peptides
    19.
    发明授权
    Diazaspiro, azepino and azabicyclo therapeutic peptides 失效
    Diazaspiro，azepino和azabicyclo治疗肽

    公开(公告)号：US6025471A

    公开(公告)日：2000-02-15

    申请号：US89954

    申请日：1998-06-03

    申请人： Romano Deghenghi

    发明人： Romano Deghenghi

    IPC分类号： A61K38/00 ,  C07K7/06 ,  C07K7/00

    CPC分类号： C07K7/06 ,  A61K38/00

    摘要： The present invention relates a number of novel peptide sequences which include a spirolactam, bicyclic or tricyclic peptidomimetic unit. The peptides disclosed herein exhibit binding to cardiac tissue and normalize cardiac pressure after administration, as well as diagnostic and therapeutic properties for certain neoplastic tissues. Importantly, these peptides do not release pituitary hormones such as corticotropin (ACTH) and growth hormone (GH), and are therefore devoid of certain unwanted side-effects. These peptides preferably have at least one lysine unit and at least one D-2-alkyl-trptophan unit.

    摘要翻译： 本发明涉及许多新的肽序列，其包括螺内酰胺，双环或三环肽模拟单元。 本文公开的肽表现出与心脏组织结合并且在给药后使心脏压力标准化，以及某些肿瘤组织的诊断和治疗性质。 重要的是，这些肽不释放垂体激素，如促肾上腺皮质激素（ACTH）和生长激素（GH），因此没有某些不必要的副作用。 这些肽优选具有至少一个赖氨酸单元和至少一个D-2-烷基 - 萜类单元。

    Oligopeptide compounds containing D-2-alkyltryptophan capable of promoting the release of growth hormone
    20.
    发明授权
    Oligopeptide compounds containing D-2-alkyltryptophan capable of promoting the release of growth hormone 失效
    含有能够促进生长激素释放的D-2-烷基色氨酸的寡肽化合物

    公开(公告)号：US5807985A

    公开(公告)日：1998-09-15

    申请号：US871415

    申请日：1997-06-09

    申请人： Romano Deghenghi

    发明人： Romano Deghenghi

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/078 ,  C07K5/083 ,  C07K5/097 ,  C07K7/02 ,  C07K5/00

    CPC分类号： C07K7/02 ,  C07K5/0205 ,  C07K5/06156 ,  C07K5/0806 ,  C07K5/0821 ,  A61K38/00

    摘要： A peptide of formula: A--D--X--D--Mrp--B (I) A--D--X--D-.beta.Nal--B (II) E--D--X--Mrp--NH.sub.2 (III) wherein A is hydrogen, 2-aminoisobutyryl, or 4-aminobutyryl; D relates to the dextro isomer; X is Mrp, wherein Mrp is a 2-alkyltryptophan of formula (IV): ##STR1## wherein R is hydrogen, CHO, SO.sub.2 CH.sub.3, mesitylene-2-sulfonyl, PO.sub.3 (CH.sub.3).sub.2, PO.sub.3 H.sub.2, wherein R.sub.1 is a C.sub.1 -C.sub.3 alkyl group, or wherein X is a residue of protected serine, Ser (Y), wherein Y is benzyl, p-chlorobenzyl, 4-methoxybenzyl, 2,4,6-trimethoxybenzyl, or tert-butyl; B is NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3, may be the same or different, are hydrogen, a C.sub.1 -C.sub.3 alkyl group, an OR.sub.4 group, wherein R.sub.4 is hydrogen, a C.sub.1 -C.sub.3 alkyl group or the C--Lys--NH.sub.2 group, wherein C is Phe, Mrp or D--Mrp; E is hydrogen, GAB or D--Mrp, and addition salts with pharmaceutically acceptable organic or inorganic acids of the peptide.

    摘要翻译： A-D-X-D-Mrp-B（I）A-D-X-D-Nal-B（II）E-D-X-Mrp-NH 2（III）的肽，其中A是氢，2-氨基异丁酰基或4-氨基丁酰基; D涉及右旋异构体; X是Mrp，其中Mrp是式（Ⅳ）的2-烷基色氨酸：其中R是氢，CHO，SO2CH3，均三甲基-2-磺酰基，PO3（CH3）2，PO3H2，其中R1是C1-C3 烷基，或其中X是被保护的丝氨酸残基，Ser（Y），其中Y是苄基，对氯苄基，4-甲氧基苄基，2,4,6-三甲氧基苄基或叔丁基; B是NR2R3，其中R2和R3可以相同或不同，是氢，C1-C3烷基，OR4基，其中R4是氢，C1-C3烷基或C-Lys-NH2基， 其中C是Phe，Mrp或D-Mrp; E是氢，GAB或D-Mrp，以及与肽的药学上可接受的有机酸或无机酸的加成盐。