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1.发明授权Derivatives of .alpha.,D-glucofuranose or .alpha.,D-allofuranose and intermediates for preparing these derivatives 失效α，D-呋喃葡萄糖或α，D-异戊二醛的衍生物和制备这些衍生物的中间体
公开(公告)号：US4996195A
公开(公告)日：1991-02-26
申请号：US294838
申请日：1989-01-09
IPC分类号： A61K31/70 , A61K31/7028 , A61P29/00 , A61P37/06 , C07H9/04 , C07H13/04 , C07H15/04 , C07H15/12 , C07H15/14 , C07H15/26
CPC分类号： C07H9/04 , C07H13/04 , C07H15/04 , C07H15/12 , C07H15/14 , C07H15/26 , Y10S514/825 , Y10S514/861
摘要： Derivatives of -.alpha.,D-glucofuranose .alpha.,D-allanfuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as psoriasis, atopic dermatitus, rheumatoid arthritis, osterarthritis, scleroderma and systemic lupus erythematosus.
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2.发明授权3,5,6-substituted derivatives of 1,2-O-isopropylidene-.alpha.,D-glucofuranose and intermediates for preparing these derivatives 失效1,2-O-异亚丙基-α，D-葡萄糖呋喃糖的3,5,6-取代衍生物和制备这些衍生物的中间体
公开(公告)号：US5010058A
公开(公告)日：1991-04-23
申请号：US369932
申请日：1989-06-22
CPC分类号： C07H9/04 , C07H15/12 , C07H15/14 , Y10S514/825 , Y10S514/861
摘要： Derivatives of 1,2-O-isopropylidene-.alpha.,D-glucofuranose and intermediates for preparing these derivatives are described. These derivatives are useful for treating animals and mammals with inflammatory and/or autoimmune disorders such as autoimmune deficiency syndrome, psoriasis, atopic dermatitus, rheumatoid arthritis, osteoarthritis, scleroderma and systemic lupus erythematosus.
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3.发明授权
公开(公告)号：US5298494A
公开(公告)日：1994-03-29
申请号：US83879
申请日：1993-06-30
IPC分类号： C07H9/04 , C07H11/00 , C07H13/04 , C07H15/04 , C07H15/10 , C07H15/12 , C07H15/14 , C07H15/18 , C07H15/26 , C07H19/01 , A61K31/00 , A61K31/70 , C07H15/00
CPC分类号： C07H9/04 , C07H11/00 , C07H13/04 , C07H15/04 , C07H15/10 , C07H15/12 , C07H15/14 , C07H15/18 , C07H15/26 , C07H19/01 , Y10S514/825 , Y10S514/861
摘要： Derivatives of simple monosaccharides which exhibit anti-proliferative and/or anti-inflammatory activity and are useful for treating mammals having inflammatory disorders and/or autoimmune disorders. This invention also encompasses pharmaceutical compositions containing these compounds and methods of treating inflammatory and/or autoimmune disorders.
摘要翻译： 具有抗增殖和/或抗炎活性并且可用于治疗具有炎症性疾病和/或自身免疫性疾病的哺乳动物的简单单糖的衍生物。 本发明还包括含有这些化合物的药物组合物和治疗炎性和/或自身免疫性疾病的方法。
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">4.发明授权
公开(公告)号：US5922849A
公开(公告)日：1999-07-13
申请号：US754867
申请日：1996-11-22
CPC分类号： C07H17/08
摘要： A process for the preparation of N-demethyl-4"-deoxy-erythromycins A and B, having the formula: ##STR1## wherein R.sup.a is H or OH, by stepwise addition of iodine and base to the N-dimethyl-4"-deoxyerythromycin, preferably, accompanied by sparging with an inert gas.
摘要翻译： 制备N-脱甲基-4'-脱氧 - 红霉素A和B的方法，具有下式：其中Ra为H或OH，通过逐步加入碘和碱至N-二甲基-4'-脱氧红霉素 ，优选伴随着用惰性气体喷射。
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公开(公告)号：US5760198A
公开(公告)日：1998-06-02
申请号：US785451
申请日：1997-01-17
申请人： Shyamal I. Parekh , Alexandra E. Graham , Michael John Dipierro , Albert V. Thomas , David A. Riley
发明人： Shyamal I. Parekh , Alexandra E. Graham , Michael John Dipierro , Albert V. Thomas , David A. Riley
CPC分类号： C07H17/08
摘要： A process for the preparation of 4"-deoxyerythromycins, having the formula: ##STR1## wherein R is H or OH, and R.sup.1 is H or loweralkyl by treatment of the 2'-O-acetyl-4"-imidazolylthionocarbonyl-erythromycin starting material with the radical initiator 4,4'-azobis-(4-cyanovaleric acid), H.sub.3 PO.sub.2 and an organic base in a water-miscible solvent and optionally eliminating the 2'-O-acetyl group. In a preferred embodiment, the water-miscible solvent is an alcohol and the deoxygenation and deacetylation is carried out in one step.
摘要翻译： 一种制备4'-脱氧红霉素的方法，具有下式：其中R为H或OH，R1为H或低级烷基，通过处理2'-O-乙酰基-4“ - 咪唑硫代羰基 - 红霉素 起始材料与自由基引发剂4,4'-偶氮双（4-氰基戊酸），H 3 PO 2和有机碱在水混溶性溶剂中并任选除去2'-O-乙酰基。 在优选的实施方案中，水混溶性溶剂是醇，脱氧和脱乙酰化在一个步骤中进行。
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公开(公告)号：US06084079A
公开(公告)日：2000-07-04
申请号：US80340
申请日：1998-05-15
摘要： The claimed invention relates to a novel process of preparing N-demethyl-N-alkyl-4"-deoxy erythromycin A and B. The process comprises protecting the 2'-hydroxy or the 2'- and 11-hydroxy of a N-demethyl-4"-deoxy erythromycin derivative having the formula: ##STR1## where R.sub.b is H or OH, with a silyl protecting group and alkylating the N-position of the desosamine sugar.
摘要翻译： 所要求保护的发明涉及制备N-去甲基-N-烷基-4'-脱氧红霉素A和B的新方法。该方法包括保护N-甲基-N-烷基-4'-脱氧红霉素A和B的2'-羟基或2'-和11-羟基。 具有下式的脱甲基-4'-脱氧红霉素衍生物：其中Rb是H或OH，具有甲硅烷基保护基团并烷基化脱氨基糖的N-位。
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7.发明授权
公开(公告)号：US06040440A
公开(公告)日：2000-03-21
申请号：US36186
申请日：1998-03-06
CPC分类号： C07H17/08
摘要： A process for the preparation of 4"-deoxyerythromycins, having the formula: ##STR1## wherein R is H or OH, R.sup.1 is H or loweralkyl, and R.sup.2 is H or CH.sub.3 by treatment of the starting material, 2'-O-acetyl-4"-imidazolylthiocarbamoyl-erythromycin, with a hypophosphite reagent, in a water-miscible protic solvent optionally comprising a phase transfer agent. In a preferred embodiment, the water-miscible solvent is an alcohol and the starting material is reacted with sodium hypophosphite, ACVA and tetra-n-butylammonium hydroxide.
摘要翻译： 一种制备4'-脱氧红霉素的方法，具有下式：其中R是H或OH，R1是H或低级烷基，R2是H或CH3，通过处理原料2'-O-乙酰基-4 “ - 咪唑基硫代氨基甲酰基 - 红霉素与次亚磷酸酯试剂在任选包含相转移剂的水混溶性质子溶剂中。 在优选的实施方案中，水混溶性溶剂是醇，起始原料与次磷酸钠，ACVA和氢氧化四正丁基铵反应。
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8.发明授权Process for the preparation of arylalkynyl-N-hydroxyurea derivatives having lipoxygenase inhibitory activity 失效制备具有脂氧合酶抑制活性的芳基炔基-N-羟基脲衍生物的方法
公开(公告)号：US5714633A
公开(公告)日：1998-02-03
申请号：US698674
申请日：1996-08-16
IPC分类号： C07C43/29 , C07C43/295 , C07C273/18 , C07C275/64 , C07C275/04 , C07C275/18
CPC分类号： C07C43/29 , C07C273/1827 , C07C43/295
摘要： The present invention provides a process for the preparation of a compound of formula ##STR1## wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.
摘要翻译： 本发明提供一种制备式（Ⅰa）化合物的方法，其中R是具有1至12个碳原子的直链或支链烷基; M表示氢或药学上可接受的阳离子; 并且A选自任选取代的碳环苯基。
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