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1. 发明申请

US20190177361A1 NOVEL PROCESS FOR PREPARATION OF CORTICOSTEROIDS 审中-公开
公开(公告)号：US20190177361A1
公开(公告)日：2019-06-13
申请号：US16327972
申请日：2017-08-14
申请人： CORAL DRUGS PVT. LTD.
发明人： Vinayak TRIPATHI , Rajesh KUMAR , Rohit BHUWANIA , Binay Kumar BHUWANIA
IPC分类号： C07J71/00 , C07J5/00 , C07J13/00
CPC分类号： C07J71/0031 , C07J5/0092 , C07J13/005 , C07J71/0015
摘要： The present invention discloses a process for the preparation of pregnadiene derivatives having formula I, their stereoisomer and intermediate thereof. Formula I wherein each substituent is independently, R1 and R2 is hydrogen or C1-C8 straight, branched alkyl chain, saturated or unsaturated cycloalkyl; R3 is hydrogen or wherein R5 represents C1-C8 straight, branched alkyl chain or cycloalkyl; R4 is hydrogen or halogen; R6 is hydrogen or halogen;

2. 发明申请

US20080090792A1 SELECTIVE GLUCOCORTICOID RECEPTOR AGONISTS 失效
标题翻译：选择性GLUCOCORTICOID受体激动剂
公开(公告)号：US20080090792A1
公开(公告)日：2008-04-17
申请号：US11737185
申请日：2007-04-19
申请人： Stephen Barr , Michael McKervey , Hughes Miel , David Ray , Andrew Brass
发明人： Stephen Barr , Michael McKervey , Hughes Miel , David Ray , Andrew Brass
IPC分类号： A61K31/56 , A61K31/58 , A61P29/00 , A61P37/06 , A61P7/00
CPC分类号： C07J5/0092 , C07J3/005 , C07J21/003 , C07J41/0011 , C07J41/0038
摘要： This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R═NH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1═C(1-4)alkyl, C(3-6)cycloalkyl, Cn, where n=1-3, R2=methyl, ethyl, R3=alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetrecoaryl; wherein R4, R5═C(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R5 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.
摘要翻译：本发明涉及治疗炎性病症，治疗血液学和其他恶性肿瘤，引起免疫抑制，或预防或治疗人或其他动物中的移植排斥的方法，其包括向患者施用具有式（I）结构的化合物，或下式定义的式（II）或其药学上可接受的衍生物或其前体药物，其中R-NH 2，NHR 1，NHOR 2，，NHNHR 2，NHCOR 2和R 1 -C 1-4烷基，（C 1 -C 4）烷基， C 3-6（C 3-6）环烷基，C n为N，其中n = 1-3，R 2 =甲基，乙基，烷基，环烷基，取代的烷基，取代的环烷基，芳基，杂芳基，取代的芳基或取代的hetrecoaryl; 其中R 4，R 5 -C（1-4） - 烷基）。根据式（III）的新型化合物，其中R 6和R 7是H，CH 3 CO，CH 3 CH 2 CO 2，CH 3 CH 2 CH 2 CO，条件是R 6 和/或R 7不同时为H或式（Ⅳ），其中R 5和R 9为H， CH 3 CO，CH 3 CH 2 CO或CH 3 CH 2 CH 2 也描述了在这些方法中使用的CO 2。

3. 发明授权

US07018995B2 Carbonate and carbamate modified forms of glucocorticoids 有权
公开(公告)号：US07018995B2
公开(公告)日：2006-03-28
申请号：US10369828
申请日：2003-02-20
申请人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
发明人： Mark G. Currie , Steve Jones , Paul Grover , Chris H. Senanayake , Q. Kevin Fang
IPC分类号： A61K31/573 , C07J5/00 , C07J71/00
CPC分类号： C07J71/0031 , A61K31/58 , C07J5/0076 , C07J5/0092 , C07J41/0033 , A61K2300/00
摘要： Carbonates and carbamates of the formula and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.

4. 发明授权

US5451690A Lambda-1,4-pregnadiene-3,20-diones 失效
标题翻译： λ-1,4-孕二烯-3,20-二酮
公开(公告)号：US5451690A
公开(公告)日：1995-09-19
申请号：US372647
申请日：1995-01-13
申请人： Luc Devocelle , Philippe Mackiewicz
发明人： Luc Devocelle , Philippe Mackiewicz
IPC分类号： A61K31/57 , B01J27/10 , C07B61/00 , C07J5/00 , C07J71/00 , C07J7/00
CPC分类号： C07J71/0031 , C07J5/0092
摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.
摘要翻译：式Ⅰ化合物，其中R选自氢，碳原子数1〜8的有机羧酸的酰基，高达8个碳原子的烷氧羰基和芳烷氧基羰基，烷基磺酰基和芳基磺酰基至8个碳原子，并用于制备取代的16,17-亚甲二氧基类固醇和新型中间体。

5. 发明授权

US3919421A Pregnanoic acid derivatives and process for the preparation thereof 失效
标题翻译：孕酸衍生物及其制备方法
公开(公告)号：US3919421A
公开(公告)日：1975-11-11
申请号：US42670273
申请日：1973-12-20
申请人： SCHERING AG
发明人： LAURENT HENRY , WIECHERT RUDOLF , HOFMEISTER HELMUT , MENGEL KLAUS , WENDT HANS , ANNEN KLAUS
IPC分类号： C07J5/00 , C07J71/00 , C01B7/00
CPC分类号： C07J5/0092 , C07J71/0031
摘要： Pharmacologically active pregnanoic acid derivatives of the Formula I

wherein -A-B- is -CH2-CH2-, -CH CH-, or -CCl CH-; X is a hydrogen atom, a halogen atom, or methyl; -Y-Z- is -CH-CH2-, C CH-, -CV-CHOU-, -CV-CO-, -CW-CHW''-, wherein U is a hydrogen atom or acyl, V is a hydrogen atom or a halogen atom, and W and W'' each are a halogen atom; R1 is alkyl; R2 is alkyl or aryl; or, R1 and R2 together represent a tetramethylene group or pentamethylene group; R3 is a hydrogen atom, an alkali metal atom, or a hydrocarbon. The invention also comprises the process of producing the compounds by various procedures.
摘要翻译：其中-A-B-是-CH 2 -CH 2 - ， - CH = CH-或-CCl = CH-的式I的药理学活性孕酸衍生物; X是氢原子，卤素原子或甲基; -YZ-是-CH-CH2-，-C = CH-，-CV-CHOU-，-CV-CO-，-CW-CHW'-，其中U是氢原子或酰基，V是氢原子或卤素原子，W和W'各自为卤素原子; R1是烷基; R2是烷基或芳基; 或者R1和R2一起表示四亚甲基或五亚甲基; R3是氢原子，碱金属原子或烃。

6. 发明申请

US20040102425A1 Selective glucocorticoid receptor agonists 审中-公开
标题翻译：选择性糖皮质激素受体激动剂
公开(公告)号：US20040102425A1
公开(公告)日：2004-05-27
申请号：US10415711
申请日：2003-12-05
发明人： Alexander Stephen Barr , Michael Anthony McKervey , Hughes Jean-Pierre Miel , David William Ray , Andrew Michael Brass
IPC分类号： A61K031/58 , A61K031/573
CPC分类号： C07J5/0092 , C07J3/005 , C07J21/003 , C07J41/0011 , C07J41/0038
摘要： This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein RnullNH2, NHR1, NHOR2, NHNHR2, NHCOR2, and R1nullC(1-4)alkyl, C(3-6)cycloalkyl, Cn, where nnull1-3, R2nullmethyl, ethyl, R3nullalkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetreoaryl; wherein R4, R5nullC(1-4)alkyl. Novel compounds according to Formula (III), wherein R6 and R7 are any of H, CH3CO, CH3CH2CO, CH3CH2CH2CO provided that R6 and R7 are not both H, or Formula (IV), wherein R8 and R9 are any of H, CH3CO, CH3CH2CO or CH3CH2CH2CO, having use in such methods, are also described.
摘要翻译：本发明涉及治疗炎性病症，治疗血液学和其他恶性肿瘤，引起免疫抑制，或预防或治疗人或其他动物中的移植排斥的方法，其包括向患者施用具有式（I）结构的化合物，或下式定义的式（II）或其药学上可接受的衍生物或其前体药物，其中R = NH 2，NHR 1，NHOR 2，NHNHR 2，NHCOR 2和R 1 = C（1-4）烷基，C（3-6）环烷基，Cn，其中n = 1-3，R2 =甲基，乙基，R3 =烷基，环烷基，取代的烷基，取代的环烷基，芳基，芳基或取代的杂芳基; 其中R 4，R 5 = C（1-4）烷基。根据式（III）的新化合物，其中R 6和R 7是H，CH 3 CO，CH 3 CH 2 CO，CH 3 CH 2 CH 2 CO 2中的任何一个，条件是R 6和R 7不同时为H或式（IV）其中R 8和R 9是在这些方法中使用的H，CH 3 CO，CH 3 CH 2 CO或CH 3 CH 2 CH 2 CO中的任何一种。

7. 发明授权

US5801165A Antiinflammatory, immunosuppressive and antialleric 16, 17-alkylidioxy-steroids 失效
标题翻译：抗炎，免疫抑制和抗过敏的16,17-亚烷基氧基类固醇
公开(公告)号：US5801165A
公开(公告)日：1998-09-01
申请号：US459954
申请日：1995-06-02
申请人： Michael John Ashton , Sven Jan-Anders Karlsson , Bernard Yvon Jack Vacher , Michael Thomas Withnall
发明人： Michael John Ashton , Sven Jan-Anders Karlsson , Bernard Yvon Jack Vacher , Michael Thomas Withnall
IPC分类号： A61K31/56 , A61P29/00 , C07J3/00 , C07J5/00 , C07J71/00 , A61K31/58 , C07J75/00
CPC分类号： C07J71/0031 , C07J3/005 , C07J5/0092
摘要： Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.
摘要翻译：式I的化合物其中R 1，R 2，R 3，R 4，R 5，R 6，n和+ Z如本文所定义，其用作抗炎，免疫抑制和抗过敏剂，包含它们的药物组合物和方法在其存在或不存在式R3-SS（O）m -R8的化合物的情况下，在惰性气氛下照射式II化合物II的化合物，其中R 7，R 8和m如本文所定义公开了其制备方法，包括氧化，还原，卤化或烷基化式I化合物。

8. 发明授权

US5482934A Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions 失效
标题翻译：前草-1,4-二烯-3,20-二酮-16-17-乙缩醛-21酯，其制备方法，组合物和治疗炎性病症的方法
公开(公告)号：US5482934A
公开(公告)日：1996-01-09
申请号：US278112
申请日：1994-07-20
申请人： Jose Calatayud , Jose R. Conde , Manuel Luna
发明人： Jose Calatayud , Jose R. Conde , Manuel Luna
IPC分类号： A61K31/58 , A61P29/00 , C07J5/00 , C07J71/00
CPC分类号： C07J5/0092 , C07J71/0031
摘要： The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.
摘要翻译：本发明涉及下式的化合物：其中X1和X2不区分对应于H或F; R1表示以下基团：R 1和R 2分别代表取代基的R取代基的取代基的R差向异构体，S差向异构体或立体异构体混合物的形式的基团在22位的碳原子上，新的中间体及其通过水解缩醛化制备的方法，以及使用这些化合物作为药物和/或治疗剂。

9. 发明授权

US5200518A Anti-inflammatory carboxycyclic acetal pregnane derivatives 失效
标题翻译：抗炎性羧基环缩醛孕烷衍生物
公开(公告)号：US5200518A
公开(公告)日：1993-04-06
申请号：US658542
申请日：1991-02-21
申请人： Hyun P. Kim , Kwan S. Sin , Chang M. Kim , Moon Y. Heo , Henry J. Lee
发明人： Hyun P. Kim , Kwan S. Sin , Chang M. Kim , Moon Y. Heo , Henry J. Lee
IPC分类号： C07J5/00 , C07J7/00 , C07J13/00 , C07J21/00 , C07J41/00 , C07J71/00
CPC分类号： C07J13/005 , C07J21/00 , C07J41/005 , C07J5/0092 , C07J7/0095 , C07J71/0031
摘要： Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH.sub.3and Y is ##STR2## wherein R.sub.1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl;R.sub.2 is COOR.sub.6, R.sub.5 COOR.sub.6, or R.sub.5 CONHR.sub.6 ;R.sub.3 is H, F, OH, or CH.sub.3 ;R.sub.4 is CH.sub.2 OH, CH.sub.2 OCOR.sub.6, COOR.sub.6, or CONHR.sub.6 ;R.sub.5 is alkyl of 1-3 carbon atoms;R.sub.6 is alkyl of 1-5 carbon atoms, or benzyl; represents a single or double bond;.about. represents .alpha.-position, .beta.-position, or a mixture of both .alpha.- and .beta.-positions; and-- represents .alpha.-position;and methods for preparing the same.
摘要翻译：其中X是H，F，Cl或CH 3，Y是下式的化合物：其中R 1是H，1-5个碳原子的烷基，苯基或苄基; R2是COOR6，R5 COOR6或R5CONHR6; R3是H，F，OH或CH3; R4是CH2OH，CH2OCOR6，COOR6或CONHR6; R5是1-3个碳原子的烷基; R6是1-5个碳原子的烷基，或苄基; 代表单键或双键; 差异表示α位，β位，或α和β位的混合物; 和 - 表示α位; 及其制备方法。

10. 发明授权

US4226862A Steroids and process for preparing the same 失效
标题翻译：类固醇及其制备方法
公开(公告)号：US4226862A
公开(公告)日：1980-10-07
申请号：US553124
申请日：1975-02-26
申请人： Mario Riva , Gaetano Palladino , Lucian Toscano
发明人： Mario Riva , Gaetano Palladino , Lucian Toscano
IPC分类号： C07J5/00 , C07J71/00 , A61K31/56
CPC分类号： C07J5/0046 , C07J5/0053 , C07J5/0076 , C07J5/0092 , C07J71/0026 , C07J71/0031
摘要： Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially anti-inflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.
摘要翻译：新型类固醇与其制备方法和含有它们的药物组合物一起描述。类固醇具有药物活性，特别是抗炎活性。它们都是2-溴-6β-氟 - 前 - 己二烯-3,20-二酮。

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