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1. 发明授权

US5767124A Polymorphic forms of a growth hormone secretagogue 失效
标题翻译：多形态的生长激素促分泌素
公开(公告)号：US5767124A
公开(公告)日：1998-06-16
申请号：US736170
申请日：1996-10-23
申请人： Jerome P. Draper , Michael J. Kaufman , David C. Dubost , James A. McCauley , Jennifer L. Vandrilla , Richard J. Varsolona
发明人： Jerome P. Draper , Michael J. Kaufman , David C. Dubost , James A. McCauley , Jennifer L. Vandrilla , Richard J. Varsolona
IPC分类号： A61K45/06 , C07D20060101 , C07D471/10 , A61K31/445 , C07D401/02
CPC分类号： A61K45/06 , C07D471/10
摘要： This invention is concerned with polymorphic forms of the compound N-�1(R)-�(1,2-dihydro-1-methanesulfonylspiro�3H-indole-3,4'-piperdin!-1'-yl)carbonyl!-2-(phenylmethyloxy)ethyl!-2-amino-2-methylpropanamide methanesulfonate which is a growth hormone secretagogue that is useful in food animals to promote their growth thereby rendering the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, and to treat medical conditions which are improved by the anabolic effects of growth hormone. The instant polymorphic forms have advantages over the other known forms of N-�1(R)-�(1,2-dihydro-1-methanesulfonylspiro�3H-indole-3,4'-piperdin!-1'-yl)carbonyl!-2-(phenylmethyloxy)-ethyl!-2-amino-2-methylpropanamide methanesulfonate in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations. The present invention is also concerned with processes for preparing these polymorphic forms, pharmaceutical formulations comprising these polymorphic forms as active ingredients and the use of the polymorphic form of the compound and their formulations in the treatment of certain disorders.
摘要翻译：本发明涉及化合物N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基] - 2-（苯基甲氧基）乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐，其是生物激素促分泌素，其可用于食用动物以促进其生长，从而使食用肉制品的生产更有效，并且在人类中，或以生长激素分泌不足为特征的医疗状况，以及治疗由生长激素的合成代谢作用改善的医疗状况。本发明的多晶型物质具有优于其他已知形式的N- [1（R） - [（1,2-二氢-1-甲磺酰基螺[3H-吲哚-3,4'-哌啶] -1'-基）羰基 ] -2-（苯基甲氧基） - 乙基] -2-氨基-2-甲基丙酰胺甲磺酸盐的热力学稳定性和药物制剂中的适用性。本发明还涉及制备这些多晶型形式的方法，包含这些多晶型形式作为活性成分的药物制剂以及化合物的多晶形式及其制剂在治疗某些疾病中的用途。

2. 发明授权

US5952323A Carbapenem antibiotic 失效
标题翻译：碳青霉烯类抗生素
公开(公告)号：US5952323A
公开(公告)日：1999-09-14
申请号：US64426
申请日：1998-04-22
申请人： Jeffrey A. Zimmerman , John M. Williams , Paul A. Bergquist , Lisa M. DiMichele , David C. DuBost , Michael J. Kaufman , Daniel R. Sidler , William A. Hunke
发明人： Jeffrey A. Zimmerman , John M. Williams , Paul A. Bergquist , Lisa M. DiMichele , David C. DuBost , Michael J. Kaufman , Daniel R. Sidler , William A. Hunke
IPC分类号： A61K31/40 , C07D20060101 , C07D477/20 , C07D207/16 , C07D403/12
CPC分类号： C07D477/20
摘要： A pharmaceutical composition is disclosed which contains a compound of formula I: ##STR1## or a pharmaceutically acceptable salt, prodrug or hydrate thereof, in the stabilized form and/or in combination with a carbon dioxide source.
摘要翻译：公开了一种药物组合物，其含有稳定形式的和/或与二氧化碳源组合的式I化合物或其药学上可接受的盐，前药或水合物。

3. 发明申请

US20090325903A1 BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译：硼酸酯化合物及其药物组合物
公开(公告)号：US20090325903A1
公开(公告)日：2009-12-31
申请号：US12485344
申请日：2009-06-16
申请人： Eric L. Elliott , Abu J. Ferdous , Michael J. Kaufman , Sonja A. Komar , Debra L. Mazaik , Quentin J. McCubbin , Phuong Nguyen , Vaithianathan Palaniappan , Raymond D. Skwierczynski , Nobel T. Truong , Csanad M. Varga , Peter N. Zawaneh
发明人： Eric L. Elliott , Abu J. Ferdous , Michael J. Kaufman , Sonja A. Komar , Debra L. Mazaik , Quentin J. McCubbin , Phuong Nguyen , Vaithianathan Palaniappan , Raymond D. Skwierczynski , Nobel T. Truong , Csanad M. Varga , Peter N. Zawaneh
IPC分类号： A61K31/69 , C07F5/04 , A61P35/00
CPC分类号： C07F5/04 , A61K31/198 , A61K31/454 , A61K31/69 , C07C233/83 , C07F5/025 , C07K5/06139 , C07K5/06191
摘要： The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
摘要翻译：本发明提供了可用作蛋白酶体抑制剂的新化合物。本发明还提供包含本发明化合物的药物组合物和使用该组合物治疗各种疾病的方法。

4. 发明授权

US6029688A Water wheel for pumping chemical treatment into water stream 有权
标题翻译：用于将化学处理用于水流的水轮
公开(公告)号：US6029688A
公开(公告)日：2000-02-29
申请号：US140664
申请日：1998-08-26
申请人： Michael J. Kaufman
发明人： Michael J. Kaufman
IPC分类号： G05D11/00
CPC分类号： G05D11/008 , G05D11/006 , Y10T137/2516 , Y10T137/85994 , Y10T137/86171 , Y10T137/86871
摘要： The invention is a water wheel supplying energy to a pump. The pump will typically be used to apply chemical treatments to the water stream. Some examples of chemicals to be added are acids or bases to bring the pH to an acceptable level, precipitation aids for suspending metal out of water, coagulants to aid in filtering dissolved solids out of water, flocculants to aid in filtering dissolved ions out of water, chlorine, or coloring to prevent growth of algae.
摘要翻译：本发明是向泵供应能量的水轮。泵通常用于对水流进行化学处理。要添加的化学物质的一些实例是酸或碱，以使pH达到可接受的水平，沉淀助剂将金属从水中悬浮，凝结剂有助于从水中过滤溶解的固体，絮凝剂有助于将溶解的离子从水中过滤，氯或着色以防止藻类生长。

5. 发明授权

US5640666A Composite silicide/silicon carbide mechanical alloy 失效
标题翻译：复合硅化物/碳化硅机械合金
公开(公告)号：US5640666A
公开(公告)日：1997-06-17
申请号：US538004
申请日：1995-10-02
申请人： S. Jayashankar , Michael J. Kaufman
发明人： S. Jayashankar , Michael J. Kaufman
IPC分类号： C04B35/575 , C04B35/58 , C22C1/04 , B22F3/14 , B22F9/00 , C22C1/10
CPC分类号： C04B35/575 , C04B35/58092 , C04B35/645 , Y10S264/36
摘要： A method of producing a composite powder by providing particles of (I) tungsten, niobium, zirconium, titanium or mixtures thereof, (II) silicon and (III) carbon in a proportion relative to each other so as to possess an overall chemical composition in that segment of the ternary diagram of FIGS. 2(a), 2(b), 2(c) and 2(d) designated A, and subjecting the particles to a mechanical alloying process under conditions and for a time sufficient to produce the composite powder. Also disclosed is a method of forming a substantially oxygen-free composition of matter comprising a matrix substance of WSi.sub.2, NbSi.sub.2, ZrSi.sub.2, TiSi.sub.2 or alloys thereof having SiC dispersed therein, the method comprising consolidating the above-described composite powder. Also disclosed is a method of forming oxidation- and wear-resistant coatings by subjecting the composite powder whose composition lies in segment A to a metallurgical process such as plasma spraying. A method of forming a composite material of uniformly dispersed particles of silicon carbide in a silicide or an alloy silicide matrix is also disclosed. The matrix contains alloy silicides such as (Mo,W)Si.sub.2. The volume fraction of the silicon carbide may be varied from 10-90%. A method is also disclosed for producing hybrid composites consisting of a third phase of fibers or whiskers dispersed among a silicide/silicon carbide two-phase microstructure derived from the composite powder.
摘要翻译：通过以相对于彼此的比例提供（I）钨，铌，锆，钛或其混合物，（II）硅和（III）碳的颗粒来生产复合粉末的方法，以具有总体化学组成图3的三元图的该段。 2（a），2（b），2（c）和2（d）表示为A，并在足以产生复合粉末的条件下进行机械合金化处理。还公开了形成基本上无氧的物质组合物的方法，该组合物包含其中分散有SiC的WSi2，NbSi2，ZrSi2，TiSi2或其合金的基体物质，该方法包括固化上述复合粉末。还公开了一种通过使组分位于段A中的复合粉末经受诸如等离子体喷涂的冶金方法来形成氧化和耐磨涂层的方法。还公开了一种在硅化物或合金硅化物基质中形成均匀分散的碳化硅颗粒的复合材料的方法。该基质含有合金硅化物，如（Mo，W）Si 2。碳化硅的体积分数可以从10-90％变化。还公开了一种用于生产由分散在衍生自复合粉末的硅化物/碳化硅两相微结构中的纤维或晶须的第三相组成的混合复合材料的方法。

6. 发明授权

US5457107A Polymorphic form of a tachykinin receptor antagonist 失效
标题翻译：速激肽受体拮抗剂的多形态
公开(公告)号：US5457107A
公开(公告)日：1995-10-10
申请号：US307962
申请日：1994-09-16
申请人： Michael J. Kaufman
发明人： Michael J. Kaufman
IPC分类号： C07D413/06 , A61K31/535
CPC分类号： C07D413/06
摘要： This invention is concerned with a novel polymorphic form of the compound 2-(S)-(3,5-bis(trifluoromethyl)benzyloxy)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-3-(S)-phenyl-morpholine which is a tachykinin receptor antagonist useful in the treatment of inflammatory diseases, pain or migraine, asthma, and emesis.The instant polymorphic form has advantages over the other known forms of 2-(S)-(3,5-bis(trifluoromethyl)benzyloxy)-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methyl)-3-(S)-phenyl-morpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
摘要翻译：本发明涉及新的多晶型形式的化合物2-（S） - （3,5-双（三氟甲基）苄氧基）-4-（3-（5-氧代-1H，4H- 三唑并）甲基）-3-（S） - 苯基 - 吗啉，其是用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐的速激肽受体拮抗剂。本发明的多晶型物质具有优于其它已知形式的2-（S） - （3,5-双（三氟甲基）苄氧基）-4-（3-（5-氧代-1H，4H- 三唑并）甲基）-3-（S） - 苯基 - 吗啉在热力学稳定性和药物制剂中的适用性方面。

7. 发明授权

US07029821B2 Photoresist and organic antireflective coating compositions 失效
标题翻译：光致抗蚀剂和有机抗反射涂料组合物
公开(公告)号：US07029821B2
公开(公告)日：2006-04-18
申请号：US10777997
申请日：2004-02-11
申请人： Richard J. Carey , Peter Trefonas, III , Michael J. Kaufman
发明人： Richard J. Carey , Peter Trefonas, III , Michael J. Kaufman
IPC分类号： G03F7/00 , G03F7/004
CPC分类号： G03F7/0392 , G03F7/0382 , G03F7/091 , Y10S430/151
摘要： Methods are provides methods are provided to prepare photoresist and organic antireflective coating composition with a filter having a mean pore size of less than about 0.4 microns. Photoresist compositions and antireflective coatings produced by such methods can provide manufactured microelectronic devices that have significantly reduced defects. Photoresist and antireflective compositions obtainable by such methods also are provided.
摘要翻译：提供了提供用于制备具有平均孔径小于约0.4微米的过滤器的光致抗蚀剂和有机抗反射涂料组合物的方法。通过这种方法制备的光致抗蚀剂组合物和抗反射涂层可以提供具有显着降低的缺陷的制造的微电子器件。还提供通过这些方法获得的光致抗蚀剂和抗反射组合物。

8. 发明授权

US06534505B2 Therapeutic polymorphs of a GABA-A alpha-5 inverse agonist and pamoate formulations of the same 失效
标题翻译： GABA-Aα-5反向激动剂和双羟萘酸盐配方的治疗多晶型物
公开(公告)号：US06534505B2
公开(公告)日：2003-03-18
申请号：US09728497
申请日：2000-11-30
申请人： Michael J. Kaufman , Daniel J. Rush
发明人： Michael J. Kaufman , Daniel J. Rush
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
摘要翻译：公开了3-（5-甲基异恶唑-3-基）-6-（1-甲基-1,2,3-三唑-4-基）甲氧基-1,2,4-三唑并[3,4-a] 二水合物形式的酞嗪，二水合物和五水合物的脱水剂，包含形式的药物组合物，用于增强认知的形式的使用，用于制备形式的方法，它们掺入包含双羟萘酸盐离子的药物组合物中的用途以及使用这种离子用于溶解中性分子。

9. 发明授权

US06297231B1 Stabilized carbapenem antibiotic compositions and method of making 失效
标题翻译：稳定的碳青霉烯类抗生素组合物及其制备方法
公开(公告)号：US06297231B1
公开(公告)日：2001-10-02
申请号：US09284321
申请日：1999-04-06
申请人： Orn Almarsson , Michael J. Kaufman , John D. Stong , John M. Williams
发明人： Orn Almarsson , Michael J. Kaufman , John D. Stong , John M. Williams
IPC分类号： C07D47720
CPC分类号： C07D477/20 , C07D477/02
摘要： The present invention relates to a novel stabilized form of carbapenem antibiotics of formula II: compositions and methods thereof wherein the antibiotics and compositions are stabilized degradation and dimer formation. The compounds can be used in the treatment of infectious diseases, including gram positive and negative, aerobic and anaerobic bacteria. The compounds provide good stability against beta-lactamases, and a favorable duration of action. The compounds of this invention are represented structural formula I: or a pharmaceutically acceptable or hydrate thereof.
摘要翻译：本发明涉及式II的碳青霉烯类抗生素的新型稳定化形式：组合物及其方法，其中抗生素和组合物是稳定的降解和二聚体形成。该化合物可用于治疗感染性疾病，包括革兰氏阳性和阴性，需氧和厌氧细菌。这些化合物对β-内酰胺酶提供良好的稳定性和有利的作用持续时间。本发明的化合物表示结构式I：或其药学上可接受的或水合物。

10. 发明授权

US6136783A Antifungal compositions 失效
标题翻译：抗真菌组合物
公开(公告)号：US6136783A
公开(公告)日：2000-10-24
申请号：US333245
申请日：1999-06-15
申请人： Maneesh J. Neururkar , Michael J. Kaufman , William A. Hunke
发明人： Maneesh J. Neururkar , Michael J. Kaufman , William A. Hunke
IPC分类号： A61K38/12 , A61K9/00 , A61K9/19 , A61K47/12 , A61K47/26 , C07K20060101 , A61K38/00
CPC分类号： A61K9/19 , A61K38/12 , A61K9/0019 , A61K47/12 , A61K47/26
摘要： The invention is a pharmaceutical composition for intravenous administration to a patient comprisinga) a pharmaceutically effective amount of a compound having the formula ##STR1## and the pharmaceutically acceptable salts thereof; b) a pharmaceutically acceptable amount of an excipient such as a bulking agent effective to form a lyophilized cake; andc) a pharmaceutically acceptable amount of acetate buffer effective to provide a pH of between about 4 and 7.
摘要翻译：本发明是用于静脉内施用于患者的药物组合物，其包含：a）药学有效量的具有下式的化合物及其药学上可接受的盐; b）药学上可接受量的赋形剂，例如有效形成冻干饼的填充剂; 和c）药学上可接受量的乙酸盐缓冲剂，其有效提供约4至7的pH。

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