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1. 发明授权

US07098305B2 Sustained release of microcrystalline peptide suspensions 有权
公开(公告)号：US07098305B2
公开(公告)日：2006-08-29
申请号：US10080130
申请日：2002-02-19
申请人： Romano Deghenghi , Francois Boutignon
发明人： Romano Deghenghi , Francois Boutignon
IPC分类号： A61K38/00 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00
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 method of preventing gel formation of a hydrophobic peptides by contacting the hydrophobic peptide with a counter-ion in an amount and at a molar ratio with the peptide that are sufficient to provide a fluid, milky microcrystalline aqueous suspension of the peptide without formation of a gel. The invention also relates to a fluid, milky microcrystalline aqueous suspension of a hydrophobic peptide and a counter-ion in water, wherein the peptide and counter-ion are present in amounts and at a molar ratio sufficient to form, upon mixing, the suspension without formation of a gel.

2. 发明授权

US06211156B1 Peptides for treatment of erectile dysfunction 失效
标题翻译：用于治疗勃起功能障碍的肽
公开(公告)号：US06211156B1
公开(公告)日：2001-04-03
申请号：US09437147
申请日：1999-11-10
申请人： Antonio Argiolas , Romano Deghenghi
发明人： Antonio Argiolas , Romano Deghenghi
IPC分类号： A61K3805
CPC分类号： C07K7/06 , A61K38/07 , A61K38/08 , C07K5/0205 , C07K7/02
摘要： The present invention relates to small peptides that cause penile erections in male animals when injected into the paraventricular nucleus of the hypothalamus or when given systemically (intravenously or subcutaneously) to such animals. These peptides are useful in the treatment of erectile dysfunction.
摘要翻译：本发明涉及当注射到下丘脑的室旁核中时或当全身（静脉内或皮下）给予这些动物时，引起雄性动物阴茎勃起的小肽。这些肽可用于治疗勃起功能障碍。

3. 发明授权

US5962409A Somatostatin-analogous cyclic peptides with inhibitory activity on growth hormone 失效
标题翻译：具有生长激素抑制活性的生长抑素类似环肽
公开(公告)号：US5962409A
公开(公告)日：1999-10-05
申请号：US983363
申请日：1998-01-14
申请人： Romano Deghenghi
发明人： Romano Deghenghi
IPC分类号： A61K38/00 , A61K31/00 , A61K51/00 , A61P5/00 , A61P5/08 , A61P35/00 , C07K14/655 , A61K38/31
CPC分类号： C07K14/6555 , A61K38/00
摘要： Cyclic peptides of general formula (I), wherein the groups are as described in the disclosure, having inhibitory activity on growth hormone. The peptides of formula (I) have also anticancer activity. ##STR1##
摘要翻译： PCT No.PCT / EP96 / 03149 371日期：1998年1月14日 102（e）1998年1月14日PCT PCT 1996年7月17日PCT公布。第WO97 / 05167号公报日期1997年2月13日通式（I）的环肽，其中基团如本公开所述，对生长激素具有抑制活性。式（I）的肽也具有抗癌活性。

4. 发明授权

US08415300B2 Sustained release of microcrystalline peptide suspensions 有权
标题翻译：微晶肽悬浮液的持续释放
公开(公告)号：US08415300B2
公开(公告)日：2013-04-09
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 , A61K38/00 , A61K38/08 , A61P43/00 , 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： 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. Also, 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：肽或肽模拟物的流体，乳状微晶水悬浮液和强质子供体在水中的抗衡离子，其中肽或拟肽和抗衡离子以足以在混合时形成悬浮液的量和摩尔比存在并且不形成凝胶。此外，包括干燥悬浮液的冻干组合物，制备冻干组合物的方法，制备悬浮液的方法以及通过该方法制备的缓释制剂。

5. 发明授权

US6159490A Implants containing bioactive peptides 失效
标题翻译：植入物含有生物活性肽
公开(公告)号：US6159490A
公开(公告)日：2000-12-12
申请号：US543707
申请日：2000-04-05
申请人： Romano Deghenghi
发明人： Romano Deghenghi
IPC分类号： A61K9/00 , A61K9/20 , A61K38/00 , A61K47/34 , A61F2/02 , B01J13/02 , B01J13/04 , A61F9/50
CPC分类号： A61K9/0024 , A61K9/204 , A61K9/2095
摘要： A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which 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 a cylindrical rod from the extruded mixture to form the pharmaceutical implant.
摘要翻译：用于在1至12个月的时间内递送有效量的生物活性肽或肽类似物的药物植入物。该植入物的直径为约1-2mm，长度在约10-25mm之间，可通过以下步骤获得，该方法包括以下步骤：将具有乙交酯与丙交酯单元的比例的乳酸和乙醇酸的共聚物约0至5:1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; 并从挤出的混合物无菌切割圆柱形杆以形成药物植入物。

6. 发明授权

US6077523A Process to manufacture implants containing bioactive peptides 失效
标题翻译：制造含有生物活性肽的植入物的方法
公开(公告)号：US6077523A
公开(公告)日：2000-06-20
申请号：US311744
申请日：1999-05-14
申请人： Romano Deghenghi
发明人： Romano Deghenghi
IPC分类号： A61K9/00 , A61K9/20 , A61K38/00 , A61K47/34 , A61F2/02 , A61K9/50 , B01J13/02
CPC分类号： A61K9/0024 , A61K9/204 , A61K9/2095
摘要： A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which 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 a cylindrical rod from the extruded mixture to form the pharmaceutical implant.
摘要翻译：用于在1至12个月的时间内递送有效量的生物活性肽或肽类似物的药物植入物。该植入物的直径为约1-2mm，长度在约10-25mm之间，可通过以下步骤获得，该方法包括以下步骤：将具有乙交酯与丙交酯单元的比例的乳酸和乙醇酸的共聚物约0至5:1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; 并从挤出的混合物无菌切割圆柱形杆以形成药物植入物。

7. 发明授权

US5720977A Oral water soluble pharmaceutical compositions containing estrone compound and calcium salt 失效
标题翻译：含有雌酮化合物和钙盐的口服水溶性药物组合物
公开(公告)号：US5720977A
公开(公告)日：1998-02-24
申请号：US592377
申请日：1996-02-01
申请人： Romano Deghenghi
发明人： Romano Deghenghi
IPC分类号： A61K9/08 , A61K9/20 , A61K9/46 , A61K31/565 , A61K31/66 , A61K33/06 , A61K33/10 , A61P3/02 , A61P3/14 , A61P19/10 , A61P43/00 , A61K9/16
CPC分类号： A61K31/565 , A61K33/10 , Y10S514/874
摘要： Oral water-soluble pharmaceutical compositions containing a therapeutically effective amount of a water-soluble and stable estrogen compound such as estropipate (piperazine estrone sulfate), and at least one water-soluble, pharmaceutically acceptable calcium salt in the presence of a suitable, pharmaceutically acceptable excipient. Compositions which include an organic acid and a calcium carbonate or bicarbonate compound which reacts with the organic acid when the composition is added to water to provide effervescence are preferred.
摘要翻译： PCT No.PCT / EP94 / 02465 Sec。 371日期：1996年2月1日 102（e）日期1996年2月1日PCT PCT 1994年7月26日PCT公布。 WO95 / 07701 PCT出版物日期1995年3月23日含有治疗有效量的水溶性和稳定的雌激素化合物如雌激素（硫酸哌嗪雌酮）和至少一种水溶性药学上可接受的钙盐的口服水溶性药物组合物在合适的药学上可接受的赋形剂。优选包含有机酸和碳酸钙或碳酸氢盐化合物的组合物，当将组合物加入到水中以产生泡腾时，其与有机酸反应。

8. 发明授权

US5286637A Biologically active drug polymer derivatives and method for preparing same 失效
标题翻译：生物活性药物聚合物衍生物及其制备方法
公开(公告)号：US5286637A
公开(公告)日：1994-02-15
申请号：US1434
申请日：1993-01-07
申请人： Francesco Veronese , Luciana Sartore , Piero Orsolini , Romano Deghenghi
发明人： Francesco Veronese , Luciana Sartore , Piero Orsolini , Romano Deghenghi
IPC分类号： A61K47/48 , C12P21/04 , C12N9/00 , A01N37/18 , C12P21/06
CPC分类号： A61K47/48215 , Y10S435/832
摘要： New biologically active drug polymer derivatives, namely peptides or protein derivatives, are useful medicaments and are represented by the generic formula:RO--(CH.sub.2 --CH.sub.2 O).sub.n --(CO)--NH--X--(CO)--NH--Z (I)whereinR represents a lower alkyl group,n is an integer comprised between 25 and 250,X when combined with adjacent NH and CO groups represents an amino acid or a dipeptide or tripeptide residue, andZ when combined with the adjacent NH group represents a biologically active peptide or protein or NH or NH.sub.2 containing drug residue.
摘要翻译： PCT No.PCT / EP90 / 01261 Sec。 371日期1991年6月3日 102（e）1991年6月3日PCT PCT 1990年7月26日PCT公布。公开号WO91 / 01758 日期：1991年2月21日。新的生物活性药物聚合物衍生物，即肽或蛋白质衍生物，是有用的药物，由以下通式表示：RO-（CH 2 -CH 2 O）n-（CO）-NH-X-（CO ）-NH-Z（I）其中R表示低级烷基，n是25至250之间的整数，当与相邻的NH和CO基团组合时，X代表氨基酸或二肽或三肽残基，当组合时，Z 相邻的NH基团代表生物活性肽或蛋白质或含NH或NH 2的药物残留物。

9. 发明授权

US4595686A Niflumic acid morpholinoethyl ester diniflumate, use as analgesic and anti-inflammatory agents and compositions 失效
标题翻译：尼氟酸吗啉代乙酯二氟酸盐，用作镇痛和抗炎剂及组合物
公开(公告)号：US4595686A
公开(公告)日：1986-06-17
申请号：US597808
申请日：1984-04-09
申请人： Nicole Bru-Magniez , Jean-Marie Teulon , Romano Deghenghi
发明人： Nicole Bru-Magniez , Jean-Marie Teulon , Romano Deghenghi
IPC分类号： C07D413/12 , A61K31/455 , A61P25/04 , A61P29/00 , C07D213/80 , C07D295/14 , A61K31/535
CPC分类号： C07D213/80
摘要： A novel compound of formula: ##STR1## useful as analgesic and anti-inflammatory drug, with very interesting therapeutic index.
摘要翻译：一种新型的化合物：具有非常有趣的治疗指标的有用的镇痛和抗炎药物。

10. 发明申请

US20100239683A1 SUSTAINED RELEASE OF MICROCRYSTALLINE PEPTIDE SUSPENSIONS 审中-公开
标题翻译：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。

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