公开(公告)号：US3764616A

公开(公告)日：1973-10-09

申请号：US3764616D

申请日：1969-10-14

申请人： GLAXO LAB LTD

发明人： ELKS J ,  MAY P ,  PHILLIPPS G

IPC分类号： C07J51/00 ,  A61K31/573 ,  B23D33/00 ,  C07J5/00 ,  C07C169/30

CPC分类号： A61K31/573 ,  A61K9/0014 ,  A61K9/0043 ,  A61K9/0046 ,  A61K9/2018 ,  B23D33/00 ,  C07J5/00

摘要： This invention is concerned with novel 21-phosphate esters of 17 Alpha -acyloxy-21-hydroxy steroids of the pregane series and with methods of preparing such compounds. The compounds are useful as topical anti-inflamatory agents.

摘要翻译： 本发明涉及先天系列的17种α-酰氧基-21-羟基类固醇的新型21-磷酸酯及其制备方法。 该化合物可用作局部抗炎剂。

公开(公告)号：US3845085A

公开(公告)日：1974-10-29

申请号：US38748873

申请日：1973-08-10

申请人： GLAXO LAB LTD

发明人： PHILLIPPS G ,  MAY P

IPC分类号： C07J5/00 ,  A61K20060101 ,  A61K31/57 ,  C07C20060101 ,  C07J1/00 ,  C07J21/00 ,  C07C169/34

CPC分类号： C07J5/00 ,  Y10S514/825

摘要： 1. A COMPOUND OF THE GENERAL FORMULA

3-(O=),11-(HO-),16-(H3C-),17-(R1-O-),20-(O=),21-(R2-O-)-

PREGN-1,4,8-TRIENE

WHEREIN R1 REPRESENTS AN ALKANOYL GROUP CONTAINING 3 OR 4 CARBON ATOMS, AND R2 REPRESENTS A HYDROGEN ATOM OR AN ALKANOYL GROUP CONTAINING 2, 3 OR 4 CARBON ATOMS.

公开(公告)号：US3856828A

公开(公告)日：1974-12-24

申请号：US37947173

申请日：1973-07-16

申请人： GLAXO LAB LTD

发明人： PHILLIPPS G ,  WOOLLETT E ,  MAY P ,  MCDONALD B

IPC分类号： H05K13/02 ,  A61K20060101 ,  A61K31/56 ,  A61K31/565 ,  A61P29/00 ,  C07C20060101 ,  C07D20060101 ,  C07J20060101 ,  C07J1/00 ,  C07J3/00 ,  C07C169/24

CPC分类号： C07J75/00

摘要： The Specification describes compounds of the general formula WHEREIN X represents a hydrogen, chlorine or fluorine atom; R1 represents a Beta -hydroxy group, an oxo group or (when X is a chlorine atom) a Beta -chlorine atom; R2 represents a hydrogen atom, a methylene group or an Alpha or Beta -methyl group; R3 represents a hydrogen atom or C1-4alkyl or phenyl group; R4 represents a methyl group substituted by at least one halogen atom; an ethyl group substituted by at least one fluorine and/or iodine atom; or a propyl group substituted by at least one halogen atom; and represents a single or double bond. The Specification also describes processes for the preparation of compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I have good anti-inflammatory activity, particularly on topical application.

摘要翻译： 该说明书描述了通式的化合物，其中X表示氢，氯或氟原子; R1表示β-羟基，氧代基或（当X为氯原子时）β-氯原子; R2表示氢原子，亚甲基或α-或β-甲基; R3表示氢原子或C1-4烷基或苯基; R4表示被至少一个卤素原子取代的甲基; 被至少一个氟和/或碘原子取代的乙基; 或被至少一个卤素原子取代的丙基; 并且表示单键或双键。 本说明书还描述了制备式I化合物的方法以及含有这些化合物的药物组合物。 式I的化合物具有良好的抗炎活性，特别是局部应用。

公开(公告)号：US3828080A

公开(公告)日：1974-08-06

申请号：US21957472

申请日：1972-01-20

申请人： GLAXO LAB LTD

发明人： PHILLIPPS G ,  MAY P

IPC分类号： C07J3/00 ,  C07C169/52

CPC分类号： C07J3/00

摘要： THE SPECIFICATION DESCRIBES NEW ANDROSTANE COMPOUNDS HAVING ANTI-INFLAMMATORY ACTIVITY. THE NEW ANDROSTANCES DESCRIBED IN THE SPECIFICATION HAVE AN ESTERFIELD 17B-CARBOXYLICC ACID GROUPING WHEREIN THE ALCOHOL RESIDUE COMPRISES EITHER AT LEAST ONE HALOGEN ATOM OR A LOWER ALKOXYBY EITHER AT LEAST ONE HALOGEN ATOM OR A LOWER ALKOXYCARBONYL GROUP OR A (C2-4) LOWER ALKYL GROUP SUBSTITUTED BY A LOWER ACYLOXY GROUP. THE 17A-GROUPING OF THESE ANDROSTANCES IS AN ESTERIFIED HYDROXY GROUP COMPRISING A FORMLY, C2-4 ALKANOYL OR BENZOYL GROUP.

公开(公告)号：US3721687A

公开(公告)日：1973-03-20

申请号：US3721687D

申请日：1970-06-08

申请人： GLAXO LAB LTD

发明人： MAY P ,  ELKS J ,  PHILLIPPS G

IPC分类号： A61K31/573 ,  C07J5/00 ,  G02B7/22 ,  C07C169/34

CPC分类号： A61K31/573 ,  C07J5/00 ,  G02B7/22 ,  Y10S514/887

摘要： ANTI-INFLAMMATORY STERIODS OF THE FORMULA

9-Y,11-X,16-R3,17-(R2-O-),17-(R1-CH2-CO-)ANDROST-4-EN-

WHEREIN R1 IS A FLUORINE, CHLORINE, BROMINE OR IODINE ATOM, R2 IS AN ALKANOXY GROUP CONTAINING 1-4 CARBON ATOMS, R3 IS AN ALKYL GROUP CONTAINING 1-4 CARBON ATOMS OR A METHYLENE GROUP (=CH2), X IS A HYDROXY GROUP IN THE B-CONFIGURATION OR A KETO GROUP, Y IS A FLUORINE OR CHLORINE ATOM, AND = REPRESENTS A SINGLE OR DOUBLE BOND BETWEEN THE 1AND 2-POSITIONS OF THE MOLECULE.

3-ONE