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1. 发明申请

WO2008150426A1 PEPTIDE PHARMACEUTICAL FOR ORAL DELIVERY 审中-公开
标题翻译：口服药物用于口服
公开(公告)号：WO2008150426A1
公开(公告)日：2008-12-11
申请号：PCT/US2008/006804
申请日：2008-05-29
申请人： UNIGENE LABORATORIES INC. , STERN, William
发明人： STERN, William
IPC分类号： A61F2/00 , A01N25/34
CPC分类号： A61K38/2235 , A61K9/14 , A61K9/20 , A61K9/2013 , A61K9/2027 , A61K9/2846 , A61K9/48 , A61K9/4858 , A61K9/4866 , A61K9/50 , A61K38/23 , A61K38/29
摘要： Acid-containing oral pharmaceutical compositions are provided wherein the pharmaceutical active agents are peptide compounds (i.e., those that include a plurality of amino acids and at least one peptide bond in their molecular structures). Certain barrier layers and/or particulate coated acid are used to reduce any adverse interactions that might otherwise occur between the acid of the compositions and other components of the composition. Use of these barrier layers and/or use of particulate coated acid is believed to promote a more simultaneous release of the components of the composition than is achieved by prior art acid-protection techniques, thus enhancing, and making more consistent, the bioavailability of the active peptide compounds.
摘要翻译：提供含酸的口服药物组合物，其中药物活性剂是肽化合物（即，包括多个氨基酸和在其分子结构中至少一个肽键的那些）。使用某些阻隔层和/或颗粒涂覆的酸来减少组合物的酸和组合物的其它组分之间可能发生的任何不利相互作用。认为使用这些阻挡层和/或使用颗粒涂覆的酸可以促进组合物的组分比通过现有技术的酸保护技术实现的更多的同时释放，从而增强和更一致的生物利用度活性肽化合物。

2. 发明申请

WO2007070450A2 FAST-ACTING ORAL PEPTIDE PHARMACEUTICAL PRODUCTS 审中-公开
标题翻译：快速口服口服药物产品
公开(公告)号：WO2007070450A2
公开(公告)日：2007-06-21
申请号：PCT/US2006047108
申请日：2006-12-08
申请人： UNIGENE LAB INC , STERN WILLIAM
发明人： STERN WILLIAM
IPC分类号： A61K38/29 , A61K38/22 , A61K38/28
CPC分类号： A61K38/23 , A61K9/2086 , A61K9/4858 , A61K38/07 , A61K38/11 , A61K38/28 , A61K38/29
摘要： A finished pharmaceutical product adapted for oral delivery of a physiologically active peptide agent, wherein the product comprises a therapeutically effective amount of the active peptide agent; at least one pharmaceutically acceptable pH-lowering agent; and at least one absorption enhancer effective to promote bioavailability of the active agent, wherein the pH-lowering agent is present in the finished pharmaceutical product in a quantity which, if the product were added to 10 milliliters of 0.1M aqueous sodium bicarbonate solution, would be sufficient to lower the pH of the solution to no higher than 5.5, and wherein an outer surface of the product is substantially free of an acid-resistant protective vehicle. The product is adapted for use in a method for enhancing the bioavailability of a therapeutic peptide active agent delivered orally.
摘要翻译：适于口服递送生理活性肽剂的成品药物产品，其中所述产品包含治疗有效量的活性肽试剂; 至少一种药学上可接受的pH降低剂; 和至少一种有效促进活性剂的生物利用度的吸收促进剂，其中该降低pH值的药物存在于成品药物中，其量如果将产物加入到10毫升0.1M碳酸氢钠水溶液中，足以将溶液的pH降低至不高于5.5，并且其中产物的外表面基本上不含耐酸性保护载体。该产品适用于增加口服递送的治疗性肽活性剂的生物利用度的方法。

3. 发明申请

WO2005073581A1 UNIVERSAL JOINT WASHER BAFFLE 审中-公开
标题翻译：通用接头洗衣机
公开(公告)号：WO2005073581A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/001042
申请日：2005-01-11
申请人： FEDERAL-MOGUL CORPORATION , NELSON, David , STERN, William
发明人： NELSON, David , STERN, William
IPC分类号： F16D3/40
CPC分类号： F16D3/41 , F16D3/385
摘要： A combination of a thrust washer and lubrication baffle adapted for a press fitting installation into lubrication chamber of a universal joint cross-member journal. The thrust washer and lubrication baffle incorporate one or more lubrication grooves, facilitating the flow of lubricant between the surfaces of the cross-member and bearing cap. Elastomeric properties of the thrust washer eliminate the need for grinding of the journal surfaces to desired tolerances, while incorporation of lubrication grooves into the thrust washer surface eliminates the need for pressing of lubrication grooves directly into the journal ends prior to hardening or heat treating.
摘要翻译：止推垫圈和润滑挡板的组合，适用于压配件安装到万向节横向轴颈润滑室中。止推垫圈和润滑挡板包括一个或多个润滑槽，有利于润滑剂在横梁和轴承盖的表面之间的流动。止推垫圈的弹性特性消除了将轴颈表面磨削到所需公差的需要，同时将润滑槽结合到止推垫圈表面中消除了在硬化或热处理之前将润滑槽直接压入轴颈末端的需要。

4. 发明申请

WO2002032235A3 PROCESS FOR MAKING MINERAL, FOOD OR PHARMACEUTICAL GRADE SALT PRODUCTS 审中-公开
公开(公告)号：WO2002032235A3
公开(公告)日：2002-04-25
申请号：PCT/US2001/032390
申请日：2001-10-18
申请人： NUTRAPURE, INC. , HAGER, Dennis, M. , STERN, William, E. , NIELSEN, Kim, R.
发明人： HAGER, Dennis, M. , STERN, William, E. , NIELSEN, Kim, R.
IPC分类号： A23L1/304
摘要： A process for forming a mineral, food or pharmaceutical grade salt product is described. The process comprises completing all the process steps in a single reactor vessel resulting in high yield and purity in shortened processing times on the order or 1/10 to 1/3 of the processing times required in prior processes.

5. 发明申请

WO1997033531A1 ORAL PEPTIDE PHARMACEUTICAL PRODUCTS 审中-公开
标题翻译：口服药物产品
公开(公告)号：WO1997033531A1
公开(公告)日：1997-09-18
申请号：PCT/US1997004024
申请日：1997-03-14
申请人： UNIGENE LABORATORIES, INC. , STERN, William , GILLIGAN, James, P.
发明人： UNIGENE LABORATORIES, INC.
IPC分类号： A61F02/00
CPC分类号： A61K9/4891 , A61K9/4858 , A61K38/23 , A61K47/186 , A61K47/28 , Y10S514/807 , Y10S514/808
摘要： Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by virtue of an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition includes an absorption enhancer and a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.
摘要翻译：口服给药的肽活性剂的生物利用度通过药物组合物增强，该药物组合物通过将本发明的成分通过胃输送的耐酸性保护载体向肽提供靶向释放。该组合物包括吸收增强剂和足量的降低pH的药物以降低局部肠道pH。所有组分与肽一起释放到肠内。

6. 发明申请

WO2010114830A1 PEPTIDE PHARMACEUTICALS FOR NASAL DELIVERY 审中-公开
标题翻译：用于NASAL递送的肽制剂
公开(公告)号：WO2010114830A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/029187
申请日：2010-03-30
申请人： Unigene Laboratories Inc. , STERN, William
发明人： STERN, William
IPC分类号： A61F13/00
CPC分类号： A61K38/29 , A61K9/0043 , A61K47/12 , A61K47/186 , A61K47/26
摘要： Pharmaceutical products for nasal administration contain peptide active agents and are formulated with compounds that enhance bioavailability of the peptide active agents. In particular, citrates, fatty acids, sugar esters of fatty acids or acyl carnitines are used. In some embodiments, a sugar ester of a fatty acid is used in combination with either a fatty acid, or alternatively, an acyl carnitine.
摘要翻译：用于鼻内给药的药物产品含有肽活性剂，并且与增强肽活性剂的生物利用度的化合物一起配制。特别地，使用柠檬酸盐，脂肪酸，脂肪酸的糖酯或酰基肉碱。在一些实施方案中，脂肪酸的糖酯与脂肪酸或酰基肉毒碱组合使用。

7. 发明申请

WO2010085700A3 TREATMENT FOR OBESITY 审中-公开
公开(公告)号：WO2010085700A3
公开(公告)日：2010-07-29
申请号：PCT/US2010/021872
申请日：2010-01-22
申请人： UNIGENE LABORATORIES INC. , MEHTA, Nozer M. , STURMER, Amy , STERN, William , GILLIGAN, James P.
发明人： MEHTA, Nozer M. , STURMER, Amy , STERN, William , GILLIGAN, James P.
IPC分类号： C07K14/585 , A61K38/00
摘要： The present invention provides peptides and pharmaceutical compositions thereof for appetite suppression and weight control. Preferred peptides are calcitonin analogs, preferably with specific amino acid changes to make the peptide more amylin-like.

8. 发明申请

WO2010085700A2 TREATMENT FOR OBESITY 审中-公开
标题翻译：治疗肥胖
公开(公告)号：WO2010085700A2
公开(公告)日：2010-07-29
申请号：PCT/US2010021872
申请日：2010-01-22
申请人： UNIGENE LAB INC , MEHTA NOZER M , STURMER AMY , STERN WILLIAM , GILLIGAN JAMES P
发明人： MEHTA NOZER M , STURMER AMY , STERN WILLIAM , GILLIGAN JAMES P
IPC分类号： H04L12/56
CPC分类号： A61K38/1706 , A61K9/0053 , A61K9/28 , A61K9/4891 , A61K38/00 , C07K14/00 , C07K14/585
摘要： The present invention provides peptides and pharmaceutical compositions thereof for appetite suppression and weight control. Preferred peptides are calcitonin analogs, preferably with specific amino acid changes to make the peptide more amylin-like.
摘要翻译：本发明提供了用于食欲抑制和体重控制的肽及其药物组合物。优选的肽是降钙素类似物，优选具有特定的氨基酸改变以使肽更像胰岛淀粉样多肽。

9. 发明申请

WO2006058225A8 ENZYMATIC REACTIONS IN THE PRESENCE OF KETO ACIDS 审中-公开
标题翻译：凯特酸存在下的酶促反应
公开(公告)号：WO2006058225A8
公开(公告)日：2007-06-28
申请号：PCT/US2005042765
申请日：2005-11-23
申请人： UNIGENE LAB INC , CONSALVO ANGELO P , MEHTA NOZER M , STERN WILLIAM , GILLIGAN JAMES P
发明人： CONSALVO ANGELO P , MEHTA NOZER M , STERN WILLIAM , GILLIGAN JAMES P
IPC分类号： C12P13/02 , C12P21/06
CPC分类号： C12Y114/17003 , C12P13/02 , C12P21/02 , C12Y403/02005
摘要： Conversion in vitro of X-Gly to X-alpha-hydroxy-Gly or X-NH 2 (X being a peptide or any other compound having a carbonyl group capable of forming a covalent bond with glycine) is accomplished enzymatically in the presence of keto acids, or salts or esters thereof, to provide a good yield without the necessity of catalase or similar enzymatic reaction enhancers. Peptidylglycine a-amidating monooxygenase (PAM) is a preferred enzyme for catalyzing the conversion. Alternatively, peptidylglycine a-hydroxylating monooxygenase (PHM) is utilized to convert X-Gly to X-alpha-hdroxy-Gly which may be recovered, or optionally may be simultaneously or sequentially converted to an amid by either a Lewis base or action of the enzyme peptidyl a-hydroxyglycine A-amidating lyase (PAL). Both PHM and PAL are functional domains of PAM.
摘要翻译： X-Gly转化为X-α-羟基-Gly或X-NH 2（X为肽或具有能够与甘氨酸形成共价键的羰基的任何其它化合物）为在酮酸或其盐或酯的存在下酶促完成，以提供良好的产率而不需要过氧化氢酶或类似的酶促反应增强剂。酰基甘氨酸α-酰胺化单加氧酶（PAM）是催化转化的优选酶。或者，使用肽基甘氨酸α-羟化化单加氧酶（PHM）将X-Gly转化为可以回收的X-α-羟基-Gly，或者可选地可以通过路易斯碱或通过路易斯碱的作用同时或顺序地转化为酰胺 β-肽酰基β-羟基甘氨酸A-酰胺化裂解酶（PAL）。 PHM和PAL都是PAM的功能域。

10. 发明申请

WO2006058225A3 ENZYMATIC REACTIONS IN THE PRESENCE OF KETO ACIDS 审中-公开
公开(公告)号：WO2006058225A3
公开(公告)日：2006-06-01
申请号：PCT/US2005/042765
申请日：2005-11-23
申请人： UNIGENE LABORATORIES, INC. , CONSALVO, Angelo, P. , MEHTA, Nozer, M. , STERN, William , GILLIGAN, James, P.
发明人： CONSALVO, Angelo, P. , MEHTA, Nozer, M. , STERN, William , GILLIGAN, James, P.
IPC分类号： C12P13/02 , C12P21/06
摘要： Conversion in vitro of X-Gly to X-alpha-hydroxy-Gly or X-NH 2 (X being a peptide or any other compound having a carbonyl group capable of forming a covalent bond with glycine) is accomplished enzymatically in the presence of keto acids, or salts or esters thereof, to provide a good yield without the necessity of catalase or similar enzymatic reaction enhancers. Peptidylglycine α-amidating monooxygenase (PAM) is a preferred enzyme for catalyzing the conversion. Alternatively, peptidylglycine α-hydroxylating monooxygenase (PHM) is utilized to convert X-Gly to X-alpha-hdroxy-Gly which may be recovered, or optionally may be simultaneously or sequentially converted to an amid by either a Lewis base or action of the enzyme peptidyl α-hydroxyglycine A-amidating lyase (PAL). Both PHM and PAL are functional domains of PAM.

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