公开(公告)号：US06710206B2

公开(公告)日：2004-03-23

申请号：US10414885

申请日：2003-04-16

申请人： John Clark Hubbs ,  Theresa Sims Barnette ,  Neil Warren Boaz

发明人： John Clark Hubbs ,  Theresa Sims Barnette ,  Neil Warren Boaz

IPC分类号： C07C6104

CPC分类号： C08G63/005 ,  C07C1/2078 ,  C07C1/213 ,  C07C13/04 ,  C07C17/02 ,  C07C51/09 ,  C07C51/363 ,  C07C51/367 ,  C07C51/377 ,  C07C51/412 ,  C07C67/03 ,  C07C67/313 ,  C07C69/708 ,  C07C2601/02 ,  C07D305/12 ,  C08G63/06 ,  C07C22/00 ,  C07C59/11 ,  C07C65/21 ,  C07C57/26 ,  C07C69/675 ,  C07C69/716

摘要： Poly(3-cyclopropyl-3-hydroxypropionates) (I) which are useful for the preparation of vinylcyclopropane and cyclopropylacetylene are disclosed. Methods for the preparation of a variety of intermediates obtained from (I) such as 3-cyclopropyl-3-hydroxypropionic acid and esters and salts thereof, 3-cyclopropylacrylic acids and vinylcyclopropane also are disclosed.

摘要翻译： 公开了可用于制备乙烯基环丙烷和环丙基乙炔的聚（3-环丙基-3-羟基丙酸酯）（I）。 还公开了制备从（I）得到的各种中间体如3-环丙基-3-羟基丙酸及其酯和盐，3-环丙基丙烯酸和乙烯基环丙烷的方法。

公开(公告)号：US06610878B1

公开(公告)日：2003-08-26

申请号：US09546817

申请日：2000-04-11

申请人： John Clark Hubbs ,  Theresa Sims Barnette ,  Neil Warren Boaz

发明人： John Clark Hubbs ,  Theresa Sims Barnette ,  Neil Warren Boaz

IPC分类号： C07C974

CPC分类号： C08G63/005 ,  C07C1/2078 ,  C07C1/213 ,  C07C13/04 ,  C07C17/02 ,  C07C51/09 ,  C07C51/363 ,  C07C51/367 ,  C07C51/377 ,  C07C51/412 ,  C07C67/03 ,  C07C67/313 ,  C07C69/708 ,  C07C2601/02 ,  C07D305/12 ,  C08G63/06 ,  C07C22/00 ,  C07C59/11 ,  C07C65/21 ,  C07C57/26 ,  C07C69/675 ,  C07C69/716

摘要： Poly(3-cyclopropyl-3-hydroxypropionates) (I) which are useful for the preparation of vinylcyclopropane and cyclopropylacetylene are disclosed. Methods for the preparation of a variety of intermediates obtained from (I) such as 3-cyclopropyl-3-hydroxypropionic acid and esters and salts thereof, 3-cyclopropylacrylic acid, and vinylcyclopropane also are disclosed.

摘要翻译： 公开了可用于制备乙烯基环丙烷和环丙基乙炔的聚（3-环丙基-3-羟基丙酸酯）（I）。 还公开了制备从（I）得到的各种中间体如3-环丙基-3-羟基丙酸及其酯和盐，3-环丙基丙烯酸和乙烯基环丙烷的方法。

公开(公告)号：US06552217B2

公开(公告)日：2003-04-22

申请号：US09897872

申请日：2001-07-02

申请人： John Clark Hubbs ,  David Carl Attride ,  Neil Warren Boaz ,  James Charles Ciula ,  John Thorton Maddox ,  Thomas Nabih ,  William Dell Nottingham ,  David Chris Spencer

发明人： John Clark Hubbs ,  David Carl Attride ,  Neil Warren Boaz ,  James Charles Ciula ,  John Thorton Maddox ,  Thomas Nabih ,  William Dell Nottingham ,  David Chris Spencer

IPC分类号： C07C6974

CPC分类号： C07C209/56 ,  C07C67/00 ,  C07C67/307 ,  C07C67/317 ,  C07C2601/02 ,  C07C69/74 ,  C07C69/63 ,  C07C211/35

摘要： Disclosed is a 4-step process for the preparation of alkyl esters of 1-methylcyclopropanecarboxylic acid which comprises the steps of (1) converting &ggr;-butyrolactone to &agr;-methyl-&ggr;-butyrolactone; (2) converting the &agr;-methyl-&ggr;-butyrolactone from step (1) to an alkyl 4-halo-2-methylbutyrate; (3) producing a xylene solution of the alkyl 4-halo-2-methylbutyrate; and (4) contacting the xylene solution of an alkyl 4-halo-2-methylbutyrate from step (3) with an alkali metal alkoxide under conditions of temperature and pressure which causes vaporization of (i) an alkanol as it is formed and (ii) an alkyl 1-methylcyclopropanecarboxylate as it is formed from the alkyl 4-halo-2-methylbutyrate. Also disclosed are processes whereby the alkyl 1-methylcyclopropanecarboxylate, prepared as described above, is converted to 1-methylcyclopropylamine.

公开(公告)号：US20130273183A1

公开(公告)日：2013-10-17

申请号：US13446240

申请日：2012-04-13

申请人： Stephanie Kay Clendennen ,  Liu Deng ,  Neil Warren Boaz

发明人： Stephanie Kay Clendennen ,  Liu Deng ,  Neil Warren Boaz

IPC分类号： A61K8/49 ,  A61K8/58 ,  A61Q19/02 ,  A61K8/97 ,  A61K8/92 ,  A61K8/67

CPC分类号： A61Q19/02 ,  A61K8/4926 ,  A61K2800/782

摘要： 2-Pyrimidine thioesters and thiocarbonates are disclosed as effective skin brightening agents. These compounds may be formulated with dermatologically acceptable carriers to form skin brightening compositions. Methods for brightening skin and for inhibiting melanogenesis using these agents are also disclosed.

摘要翻译： 公开了2-嘧啶硫酯和硫代碳酸酯作为有效的皮肤增亮剂。 这些化合物可以与皮肤病学上可接受的载体配制以形成皮肤增亮组合物。 还公开了使用这些试剂增亮皮肤和抑制黑素生成的方法。

公开(公告)号：US08263094B2

公开(公告)日：2012-09-11

申请号：US12236171

申请日：2008-09-23

申请人： Michael Fitzpatrick Wempe ,  Liu Deng ,  Stephanie Kay Clendennen ,  Neil Warren Boaz

发明人： Michael Fitzpatrick Wempe ,  Liu Deng ,  Stephanie Kay Clendennen ,  Neil Warren Boaz

IPC分类号： A61K8/02 ,  C12P33/20 ,  C07D487/00

CPC分类号： A61K31/22 ,  A61K31/23 ,  C07C67/08 ,  C07C69/95 ,  C07C2601/16

摘要： Esters of 4,5-disubstituted-oxy-2-methyl-3,6-dioxo-cyclohexa-1,4-dienyl alkyl acids were prepared chemically and/or enzymatically. Depending upon the ester, improved melanocyte cytotoxicity was achieved. Improved cytotoxicity characteristics are consistent with ester analogs being more physiologically compatible and less irritating to skin than their corresponding acids.

摘要翻译： 化学和/或酶促制备4,5-二取代 - 氧基-2-甲基-3,6-二氧代 - 环己-1,4-二烯基烷基酯的酯。 取决于酯，实现了改善的黑素细胞细胞毒性。 改进的细胞毒性特征与酯类似物与其相应的酸相比更具生理学相容性并且对皮肤刺激性较低。

公开(公告)号：US06939981B1

公开(公告)日：2005-09-06

申请号：US10876392

申请日：2004-06-25

申请人： Neil Warren Boaz

发明人： Neil Warren Boaz

IPC分类号： B01J31/00 ,  C07B53/00 ,  C07C29/00 ,  C07C29/145 ,  C07C67/31 ,  C07F15/00 ,  C07F17/00 ,  C07C31/18

CPC分类号： B01J31/2495 ,  B01J31/188 ,  B01J31/2295 ,  B01J31/24 ,  B01J31/2404 ,  B01J2231/643 ,  B01J2531/0205 ,  B01J2531/821 ,  B01J2531/825 ,  B01J2531/842 ,  C07B53/00 ,  C07B2200/07 ,  C07B2200/09 ,  C07C29/145 ,  C07C67/31 ,  C07F15/0053 ,  C07C69/732 ,  C07C69/675 ,  C07C31/205 ,  C07C31/207 ,  C07C31/20

摘要： Disclosed are ruthenium complexes of phosphine-aminophosphine ligands that may be used to catalyze large number of reactions of a wide variety of substrates such as asymmetric hydrogenations, asymmetric reductions, asymmetric hydroborations, asymmetric olefin isomerizations, asymmetric hydrosilations, asymmetric allylations, and asymmetric organometallic additions. Also disclosed is a process for the preparation of the ruthenium complexes and processes for the enantioselective asymmetric hydrogenations of 1,3-dicarbonyl, α-hydroxycarbonyl, and β-hydroxycarbonyl compounds to produce the corresponding hydroxycarbonyl, 1,2-diol, and 1,3-diol compounds, respectively, using the ruthenium complexes to catalyze the hydrogenation.

摘要翻译： 公开了可用于催化多种底物的大量反应的膦 - 氨基膦配体的钌络合物，例如不对称氢化，不对称还原，不对称氢化，不对称烯烃异构化，不对称氢化硅，不对称烯丙基化和不对称有机金属添加 。 还公开了制备钌络合物的方法和1,3-二羰基，α-羟基羰基和β-羟基羰基化合物的对映选择性不对称氢化的方法，以产生相应的羟基羰基，1,2-二醇和1， 分别使用钌配合物来催化氢化。

公开(公告)号：US06635784B2

公开(公告)日：2003-10-21

申请号：US09957549

申请日：2001-09-20

申请人： Sheryl Davis Debenham ,  Neil Warren Boaz

发明人： Sheryl Davis Debenham ,  Neil Warren Boaz

IPC分类号： C07C6974

CPC分类号： C07D263/42 ,  C07B2200/07 ,  C07C231/10 ,  C07C231/18 ,  C07C233/47 ,  C07C233/86 ,  C07C269/00 ,  C07C269/06 ,  C07C271/22 ,  C07F9/4006 ,  C07C233/84 ,  C07C233/87

摘要： Disclosed are processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives by the hydrogenation of certain enamides in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst and certain novel enamide ester compounds which are intermediates in the processes. The processes include novel 2-step and 3-step processes for the preparation of enantiomerically-enriched cyclopropylalanine derivatives. The two-step process comprises the steps of reacting cyclopropanecarboxaldehyde with a substituted phosphorylglycine to afford an enamide ester which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst. The three-step process comprises the steps of forming an azlactone from an N-acylglycine and cyclopropanecarboxaldehyde, converting the azlactone to the aforesaid enamide which then is hydrogenated in the presence of a catalyst comprising a transition metal and a substantially enantiomerically-pure bis-phosphine catalyst.

公开(公告)号：US5650422A

公开(公告)日：1997-07-22

申请号：US270964

申请日：1994-07-05

申请人： Richard Paul Dunlap ,  Neil Warren Boaz ,  Albert Joseph Mura ,  Dennis John Hlasta ,  Ranjit Chimanlal Desai ,  Chakrapani Subramanyam ,  Lee Hamilton Latimer ,  Eric Piatt Lodge

发明人： Richard Paul Dunlap ,  Neil Warren Boaz ,  Albert Joseph Mura ,  Dennis John Hlasta ,  Ranjit Chimanlal Desai ,  Chakrapani Subramanyam ,  Lee Hamilton Latimer ,  Eric Piatt Lodge

IPC分类号： A61K31/425 ,  A61K31/415 ,  A61K31/428 ,  A61K31/47 ,  A61P29/00 ,  A61P43/00 ,  C07D275/04 ,  C07D275/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  C07F9/6541 ,  A61K31/535

CPC分类号： C07D275/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D513/04 ,  C07F9/6541

摘要： Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula ##STR1## wherein: L is --O--, --S--, --SO-- or --SO.sub.2 --;m and n are each independently 0 or 1;R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, whenL is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl;R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; andR.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.

摘要翻译： 抑制蛋白水解酶的酶活性的新型2-取代糖精可用于治疗退行性疾病，并具有下式：其中：L是-O - ， - S - ， - SO-或-SO 2 - ; m和n各自独立地为0或1; R 1为卤素，低级烷酰基，1-氧代对苯二烯基，苯基或取代的苯基，杂环基或取代的杂环基，或当L为-O-并且n为1时，环庚三烯-2-基或当L为-S-且n为 1，氰基或低级烷氧基硫代羰基，或当L为-SO 2 - 且n为1时，为低级烷基或三氟甲基; R2是氢，低级烷氧基羰基，苯基或苯硫基; 并且R 3和R 4各自为氢或各种取代基和制备方法，并且公开了药物组合物及其使用方法。

公开(公告)号：US08846723B2

公开(公告)日：2014-09-30

申请号：US12975572

申请日：2010-12-22

申请人： Liu Deng ,  Neil Warren Boaz ,  Sabine Delaire

发明人： Liu Deng ,  Neil Warren Boaz ,  Sabine Delaire

IPC分类号： A61K31/4406 ,  A61K31/221 ,  A61K31/235 ,  C07C69/76 ,  C07C69/734 ,  C07C403/20 ,  C07C403/12 ,  C07C67/11 ,  A61Q19/08 ,  A61K8/67 ,  A61Q19/00 ,  C12P7/62 ,  C07C67/03 ,  C07D309/40 ,  A61Q19/02

CPC分类号： A61K8/671 ,  A61Q19/00 ,  A61Q19/002 ,  A61Q19/02 ,  A61Q19/08 ,  C07C67/03 ,  C07C67/10 ,  C07C67/11 ,  C07C69/734 ,  C07C403/12 ,  C07C403/20 ,  C07C2601/16 ,  C07D213/80 ,  C07D213/803 ,  C07D309/38 ,  C07D309/40 ,  C12P7/62 ,  C07C69/63

摘要： Esters of O-substituted hydroxy carboxylic acids are provided having Formula 1, or 2, or both Formulas 1 and 2: wherein R and R1 are independently selected from the group consisting of substituted and unsubstituted, branched- and straight-chain, saturated, unsaturated, and polyunsaturated C1-C22 alkyl, substituted and unsubstituted C3-C8 cycloalkyl, substituted and unsubstituted C6-C20 carbocyclic aryl, and substituted and unsubstituted C4-C20 heterocyclic; wherein the heteroatoms are selected from sulfur, nitrogen, and oxygen; and wherein n is 1-6. Process of producing esters of O-substituted hydroxy carboxylic acids are also provided.

摘要翻译： 提供O-取代的羟基羧酸的酯，其具有式1或2或两者或式2或其两者：其中R和R 1独立地选自取代和未取代的，支链和直链的饱和不饱和的 和多不饱和C 1 -C 22烷基，取代和未取代的C 3 -C 8环烷基，取代和未取代的C 6 -C 20碳环芳基和取代和未取代的C 4 -C 20杂环; 其中所述杂原子选自硫，氮和氧; 并且其中n为1-6。 还提供了生产O-取代羟基羧酸酯的方法。

公开(公告)号：US20120215024A1

公开(公告)日：2012-08-23

申请号：US13031375

申请日：2011-02-21

申请人： Neil Warren Boaz

发明人： Neil Warren Boaz

IPC分类号： C07C69/732 ,  C12P7/62 ,  C07C69/675

CPC分类号： C07C403/12 ,  A61K8/85 ,  A61Q19/00 ,  C07C2601/16 ,  C12P7/62 ,  C12P23/00

摘要： Retinyl hydroxyesters and retinyl oligo-hydroxyesters were prepared using a chemoenzymatic process from retinol and short chain esters of hydroxycarboxylic acids or short chain esters of hydroxycarboxylic acids. The presence of the hydroxyl group on the acid can result in a mixture of esters from various oligomers of the hydroxycarboxylic acid. The retinyl ester products are readily enzymatically hydrolyzed in vitro, which indicates that application to the skin should result in release of the anti-aging ingredient retinol (without the inherent instability and irritation) along with the acid, which, if chosen appropriately, should also have desirable biological effects. This combination should be effective as an anti-aging skin care ingredient.

摘要翻译： 使用视黄醇和羟基羧酸的短链酯或羟基羧酸的短链酯的化学酶法制备视黄基羟基酯和视黄酯低聚羟基酯。 酸上的羟基的存在可以产生来自羟基羧酸的各种低聚物的酯的混合物。 视黄酯产物在体外容易地酶水解，这表明施用于皮肤应该导致抗老化成分视黄醇的释放（没有固有的不稳定性和刺激性）以及酸，如果适当选择，也应当 具有理想的生物效应。 该组合应作为抗衰老护肤成分有效。