专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明授权

US5248777A Process and intermediates for preparing compounds having a disubstituted acetylene moiety and retinoic acid-like biological activity 失效
标题翻译：用于制备具有二取代乙炔部分和视黄酸样生物活性的化合物的方法和中间体
公开(公告)号：US5248777A
公开(公告)日：1993-09-28
申请号：US731161
申请日：1991-07-15
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： C07D215/06 , C07D215/14 , C07D311/58 , C07D335/06 , C07D401/06 , C07D405/06 , C07D409/06
CPC分类号： C07D335/06 , C07D215/06 , C07D215/14 , C07D311/58 , C07D401/06 , C07D405/06 , C07D409/06
摘要： A process is disclosed for the preparation of disubstituted acetylene derivatives having retinoic acid like biological activity, wherein 6-ethynyl-chroman, 6-ethynyl-thio chroman and 6-ethynyl-1,2,3,4-tetrahydroquinoline derivatives of the formula shown below are reacted in the presence of catalysts with halogenated phenyl or heteroaryl derivatives of the formula shown below to provide the disubstituted acetylenes.In the formulae the symbols have the following meanings. R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen or lower alkyl groups (of 1-6 carbons) where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be identical or different from one another) X is S, O or NR' where R' is hydrogen or lower alkyl, Z represents hydrogen, or a metal ion capable of forming a salt with the ethynyl moiety of the molecule, X' is a leaving group such as a halogen group, A is phenyl, or heteroaryl such as pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl, n is an integer between 0 to 5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons. ##STR1##
摘要翻译：公开了制备具有视黄酸类生物学活性的二取代乙炔衍生物的方法，其中所示的式为6-乙炔基 - 苯并二氢吡喃，6-乙炔基 - 硫代色满和6-乙炔基-1,2,3,4-四氢喹啉衍生物在催化剂存在下使下文所示的下式所示的卤代苯基或杂芳基衍生物反应，得到二取代的乙炔。在公式中，符号具有以下含义。 R 1，R 2，R 3，R 4和R 5是氢或低级烷基（1-6个碳），其中R 1，R 2，R 3，R 4和R 5可以相同或不同）X是S，O或NR' R'是氢或低级烷基，Z表示氢，或能够与分子的乙炔基部分形成盐的金属离子，X'是离去基团如卤素基团，A是苯基或杂芳基如吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基，吡嗪基，噻唑基或恶唑基，n是0-5之间的整数，B是H，-COOH或其药学上可接受的盐，酯或酰胺，-CH 2 OH或醚或酯衍生物或-CHO或缩醛衍生物，或-COR1或缩酮衍生物，其中R1是含有1至5个碳原子的烷基，环烷基或烯基。

32. 发明授权

US5045551A Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity 失效
标题翻译：具有类视黄醇样活性的杂芳基和2-取代的苯并二氢吡喃基或1,2,3,4-四氢喹啉基二取代的乙炔
公开(公告)号：US5045551A
公开(公告)日：1991-09-03
申请号：US409476
申请日：1989-09-19
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/38 , A61K31/41 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61P17/00 , C07D401/06 , C07D403/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06
CPC分类号： C07D401/06 , C07D405/06 , C07D409/06 , Y10S514/852 , Y10S514/861 , Y10S514/863
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.

33. 发明授权

US4923884A Ethynylheteroaromatic-acids having retinoic acid-like activity 失效
公开(公告)号：US4923884A
公开(公告)日：1990-05-08
申请号：US180649
申请日：1988-04-01
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/44 , C07D213/30 , C07D213/48 , C07D213/51 , C07D213/55 , C07D213/80 , C07D307/54 , C07D307/68 , C07D333/24 , C07D333/38
CPC分类号： C07D213/30 , C07C403/02 , C07D213/48 , C07D213/51 , C07D213/55 , C07D213/80 , C07D307/54 , C07D307/68 , C07D333/24 , C07D333/38 , C07C2101/16
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## wherein A is pyridyl, furyl, thienyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH and its esters, amides and pharmaceutically acceptable salts, --CHO and its acetal derivatives, --COR.sub.1 and its ketal derivatives where R.sub.1 is --(CH.sub.2).sub.n CH.sub.3 where n is defined above, or --CH.sub.2 OH and its ether and acyl ester derivatives; or a pharmaceutically acceptable salt.

34. 发明授权

US4895868A Thiochroman esters of phenols and terephthallates having retinoid-like activity 失效
标题翻译：具有类视黄醇样活性的苯酚和对苯二酸三乙酯的硫色满酯
公开(公告)号：US4895868A
公开(公告)日：1990-01-23
申请号：US212855
申请日：1988-06-29
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/38 , A61K31/382 , A61P17/00 , A61P31/00 , A61P35/00 , C07D335/06
CPC分类号： C07D335/06 , Y10S514/863
摘要： Compounds of formula I ##STR1## in which: the R groups are independently hydrogen or lower alkyl; one of A and B is O or S and the other is --C(O)--, A being attached to the thiochroman ring at the 6 or 7-position;n is 0-5; andZ is H, an acid or acid derivative, an alcohol or alcohol derivative, acetal or acetal derivative or ketone or ketone derivative, or a pharmaceutically acceptable salt, have retinoid-like activity.
摘要翻译：式I的化合物其中：R基团独立地为氢或低级烷基; A和B之一是O或S，另一个是-C（O） - ，A在6或7位连接到二氢苯并噻喃环上; n为0-5; Z为H，酸或酸衍生物，醇或醇衍生物，缩醛或缩醛衍生物或酮或酮衍生物或其药学上可接受的盐具有类视黄醇样活性。

35. 发明授权

US4739098A Ethynylphenyl-containing retinoic acid derivatives 失效
标题翻译：含乙炔基苯基的视黄酸衍生物
公开(公告)号：US4739098A
公开(公告)日：1988-04-19
申请号：US910096
申请日：1986-09-22
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/015 , A61K20060101 , A61K31/045 , A61K31/07 , A61K31/075 , A61K31/085 , A61K31/11 , A61K31/16 , A61K31/165 , A61K31/185 , A61K31/19 , A61K31/215 , A61K31/235 , A61P17/00 , A61P27/16 , A61P29/00 , A61P37/00 , C07C20060101 , C07C13/00 , C07C13/16 , C07C13/20 , C07C15/00 , C07C15/50 , C07C33/38 , C07C39/23 , C07C43/168 , C07C47/238 , C07C47/548 , C07C57/00 , C07C57/48 , C07C63/00 , C07C63/33 , C07C63/66 , C07C67/00 , C07C69/00 , C07C69/606 , C07C69/612 , C07C69/614 , C07C69/618 , C07C69/76 , C07C69/78 , C07C233/65 , C07C401/00 , C07C403/00 , C07C403/02 , C07C403/06 , C07C403/14 , C07C403/20 , C07C403/24
CPC分类号： C07C403/14 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/20 , C07C2101/16
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## where n is 0-5 and A is H, lower alkyl, or --COOH or ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or a pharmaceutically acceptable salt.

36. 发明授权

US06624188B1 Method of treatment with compounds having retinoid-like activity and reduced skin toxicity and lacking teratogenic effects 失效
标题翻译：使用具有类视黄醇样活性和降低皮肤毒性并缺乏致畸作用的化合物治疗方法
公开(公告)号：US06624188B1
公开(公告)日：2003-09-23
申请号：US08216990
申请日：1994-03-23
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31382
CPC分类号： C07D213/80 , C07D307/68 , C07D311/74 , C07D333/38
摘要： A process and pharmaceutical compositions for treating several diseases and conditions which are normally treatable with retinoid like compounds are disclosed where the compound used for the treatment are substantially non-teratogenic and not irritant to the skin. The process is useful for treating female mammals, including humans, who are pregnant or in the child bearing age. An important partial structural feature of the compounds which provides the non-teratogenic effect and lack of irritation of skin is shown by the formula where the partially drawn ring signifies an aromatic ring which may be carbocyclic or heteroaromatic, 6-membered or 5-membered, and may be condensed with another ring. R1 is lower alkyl, Cl, Br, or I, R2 is H, lower alkyl, Cl, Br, or I, and R3 is lower alkyl, Cl, Br, I, or is an ether, thioether, ester, thioester, amine or substituted amine group.
摘要翻译：公开了用于治疗通常用类视黄醇类化合物治疗的几种疾病和病症的方法和药物组合物，其中用于治疗的化合物基本上是非致畸性的并且不刺激皮肤。该过程可用于治疗怀孕或生育年龄的女性哺乳动物，包括人类。提供非致畸作用和缺乏皮肤刺激性的化合物的重要部分结构特征由下式示出：其中部分拉伸的环表示可以是碳环或杂芳族的芳族环，6元或5元，并且可以与另一个环稠合。 R1是低级烷基，C1，Br或I，R2是H，低级烷基，C1，Br或I，R3是低级烷基，C1，Br，I，或是醚，硫醚，酯，硫酯，胺或取代的胺基。

37. 发明授权

US5663347A Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity 失效
标题翻译：具有异双环基团的二取代乙炔和具有类视黄醇样活性的杂芳族或苯基
公开(公告)号：US5663347A
公开(公告)日：1997-09-02
申请号：US466005
申请日：1995-06-06
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/35 , A61K31/352 , A61K31/38 , A61K31/382 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/50 , A61K31/505 , A61P9/10 , A61P13/02 , A61P15/00 , A61P17/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/06 , C07D215/12 , C07D215/14 , C07D311/58 , C07D335/06 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D215/00 , C07D215/38
CPC分类号： C07D335/06 , C07D215/12 , C07D311/58 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06
摘要： Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.8 is alkyl of 1 to 10 carbons, phenyl or lower alkylphenyl, R.sub.9 is lower alkyl, R.sub.10 is divalent alkyl radical of 2-5 carbons and R.sub.11 is alkyl, cycloalkyl or alkenyl containing 1 to 5 carbons, have retinoic acid like activity.
摘要翻译：其中R 1和R 2独立地为具有2至8个碳原子的烷基; R3是氢或低级烷基; X是S，O或N-R4，其中R4是氢或低级烷基; Y是苯基或吡啶基，噻吩基，呋喃基，哒嗪基，嘧啶基和吡嗪基; A为（CH 2）n，其中n为0-5，或低级支链烷基，具有2-6个碳原子和1或2个双键的烯基，具有2至6个碳原子的炔基和1或2个三键; B是氢，COOH或其盐，COOR5，CONR6R7，-CH2OH，CH2OR8，CH2OCOR8，CHO，CH（OR9）2，CHOR10O，-COR11，CR11（OR9）2或CR11OR10O，其中R5是1〜 10个碳原子或5至10个碳原子的环烷基，或R5为苯基或低级烷基苯基，R6和R7独立地为氢，1至10个碳原子的烷基或5至10个碳原子的环烷基，或苯基或低级烷基苯基，R8为烷基 1〜10个碳原子，苯基或低级烷基苯基，R9为低级烷基，R10为2-5个碳原子的二价烷基，R11为含1〜5个碳原子的烷基，环烷基或烯基，具有视黄酸类活性。

38. 发明授权

US5616597A Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4--tetrahydroquinolinyl group having retinoid-like activity 失效
标题翻译：具有类视黄醇样活性的杂芳基和2-取代的苯并二氢吡喃基或1,2,3,4-四氢喹啉基二取代的乙炔
公开(公告)号：US5616597A
公开(公告)日：1997-04-01
申请号：US460477
申请日：1995-06-02
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： C07D401/06 , C07D405/06 , C07D409/06 , A61K31/50
CPC分类号： C07D401/06 , C07D405/06 , C07D409/06
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is thiazolyl or oxazolyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
摘要翻译：类视黄醇样活性由式（I）的化合物表示，其中X是S，O; R1，R2和R3是氢或低级烷基; R4和R5是氢或低级烷基，条件是R4和R5不能都是氢，A是噻唑基或恶唑基; n为0-5，B为H，-COOH或其药学上可接受的盐，酯或酰胺，-CH 2 OH或醚或酯衍生物，或-CHO或缩醛衍生物，或-COR1或缩酮衍生物，其中R1 是 - （CH 2）m CH 3，其中m为0-4，或其药学上可接受的盐。

39. 发明授权

US5599819A Acetylenes disubstituted with a thienyl or furyl group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4 - tetrahydroquinolinyl group having retinoid-like activity 失效
标题翻译：用噻吩基或呋喃基二取代的乙酰基和具有类视黄醇样活性的2-取代的1,2,3,4-四氢喹啉基
公开(公告)号：US5599819A
公开(公告)日：1997-02-04
申请号：US458389
申请日：1995-06-02
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： C07D401/06 , C07D405/06 , C07D409/06 , A61K31/50
CPC分类号： C07D401/06 , C07D405/06 , C07D409/06
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is NR'; where R' is hydrogen or lower alkyl; R.sub.1, R.sub.2 and R.sub.3 are hydrogen or lower alkyl; R.sub.4 and R.sub.5 are hydrogen or lower alkyl with the proviso that R.sub.4 and R.sub.5 cannot both be hydrogen, A is thienyl, furyl; n is 0-5, and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.
摘要翻译：类视黄醇样活性由式（I）的化合物表示，其中X是NR'; 其中R'是氢或低级烷基; R1，R2和R3是氢或低级烷基; R4和R5是氢或低级烷基，条件是R4和R5不能都是氢，A是噻吩基，呋喃基; n为0-5，B为H，-COOH或其药学上可接受的盐，酯或酰胺，-CH 2 OH或醚或酯衍生物，或-CHO或缩醛衍生物，或-COR1或缩酮衍生物，其中R1 是 - （CH 2）m CH 3，其中m为0-4，或其药学上可接受的盐。

40. 发明授权

US5516904A Acetylenes disubstituted with a heteroaromatic group and a substituted phenyl group having retinoid like activity 失效
标题翻译：用杂芳基取代的乙炔和具有类视黄醇样活性的取代苯基
公开(公告)号：US5516904A
公开(公告)日：1996-05-14
申请号：US384886
申请日：1995-02-07
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： C07D213/80 , A61K31/425
CPC分类号： C07D213/80
摘要： Retinoid like activity is exhibited by compounds of the formula ##STR1## where R.sub.1 -R.sub.3 independently are hydrogen, lower alkyl, cycloalkyl or lower alkenyl, A and B independently are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, SR.sub.4 or OR.sub.4 where R.sub.4 is lower alkyl, cycloalkyl or lower alkenyl; Y is selected from a group consisting of pyridazinyl, pyrimidinyl, pyrazinyl or oxazolyl; E is lower alkenyl, lower alkynyl, lower cycloalkyl, lower branched chain alkyl, or is characterized by the formula (CH.sub.2).sub.n where n is 0-5, and Z is H, OH, OR.sub.5, OCOR.sub.5, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH, CH.sub.2 OR.sub.6, CH.sub.2 OCOR.sub.6, or --CHO, CH(OR.sub.7).sub.2, CHOR.sub.8 O, or COR.sub.9, CR.sub.9 (OR.sub.7).sub.2, CR.sub.9 OR.sub.8 O where R.sub.5 is lower alkyl, phenyl or lower alkylphenyl, R.sub.6 is lower alkyl, phenyl or lower alkylphenyl, R.sub.7 is lower alkyl, R.sub.8 is a divalent alkyl radical of 2-5 carbons, and R.sub.9 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons.
摘要翻译：其中R 1 -R 3独立地是氢，低级烷基，环烷基或低级链烯基，A和B独立地是氢，低级烷基，环烷基，低级烯基，SR4或OR4，其中R4是低级烷基，环烷基或低级烯基; Y选自哒嗪基，嘧啶基，吡嗪基或恶唑基; E为低级链烯基，低级炔基，低级环烷基，低级支链烷基，或其特征为式（CH2）n，其中n为0-5，Z为H，OH，OR5，OCOR5，-COOH或药学上可接受的其盐，酯或酰胺，-CH 2 OH，CH 2 OR 6，CH 2 OCOR 6或-CHO，CH（OR 7）2，CHOR 8 O或COR 9，CR 9（OR 7）2，CR 9OR 8 O，其中R 5为低级烷基，苯基或低级烷基苯基，烷基，苯基或低级烷基苯基，R7为低级烷基，R8为2-5个碳原子的二价烷基，R9为含有1至5个碳原子的烷基，环烷基或链烯基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式