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1. 发明授权

US5118678A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5118678A
公开(公告)日：1992-06-02
申请号：US686728
申请日：1991-04-17
申请人： Wenling Kao , Robert L. Vogel , John H. Musser
发明人： Wenling Kao , Robert L. Vogel , John H. Musser
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONH(CR.sup.3 R.sup.4).sub.n --X;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl;X ix hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y;Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio;n=0-5;with the proviso that R.sup.1 and R.sup.2 are not both hydrogen and when n=0, X is lower alkyl, cycloalkyl, aralkyl, or Y;or a pharmaceutically acceptable salt thereof when X is dialkylamino, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.
摘要翻译：结构的化合物，其中R 1和R 2各自独立地为氢或-CONH（CR 3 R 4）n -X; R 3和R 4各自独立地为氢，烷基，芳烷基，环烷基，卤素或三氟甲基; 硝基，烷氧基，烷氧基，芳烷基，卤素，二烷基氨基，硫代烷基或Y; Y是可以任选被选自烷基，芳烷基，烷氧基，氰基，卤素，硝基，烷氧基，三氟甲基，二烷基氨基或烷硫基中的基团单，二或三取代的苯基。 n = 0-5; 条件是R1和R2不同时为氢，当n = 0时，X为低级烷基，环烷基，芳烷基或Y; 当X是二烷基氨基时，或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病; 由于其抗肿瘤活性可用于治疗实体瘤; 并且由于其抗真菌活性可用于治疗真菌感染。

2. 发明授权

US5120727A Rapamycin dimers 失效
标题翻译：雷帕霉素二聚体
公开(公告)号：US5120727A
公开(公告)日：1992-06-09
申请号：US706821
申请日：1991-05-29
申请人： Wenling Kao , Robert L. Vogel , John H. Musser
发明人： Wenling Kao , Robert L. Vogel , John H. Musser
IPC分类号： A61K31/445 , A61K31/395 , A61K31/435 , A61P29/00 , A61P31/04 , A61P31/10 , A61P35/00 , A61P37/06 , C07D498/12 , C07D498/18 , C07D519/00
CPC分类号： C07D498/18 , C07D519/00
摘要： A rapamycin dimer of general formula (1) ##STR1## wherein A is --(CH.sub.2).sub.n --, --(CH.sub.2)n--(CH.dbd.CH)--(CH.sub.2).sub.m --, --(CH.sub.2)n--(--C.tbd.C--)--(CH.sub.2).sub.m --, ##STR2## substituted alkyl, substituted alkenyl, substituted alkynyl, and substituted aromatic; n=1-10, m=1-10 and n=m or n .noteq.mor a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：其中A为 - （CH 2）n - ， - （CH 2）n - （CH = CH） - （CH 2）m - ， - （CH 2）取代的烷基，被取代的烯基，被取代的炔基和被取代的芳族; n - （ - C 3 O） - （CH 2）m - ， - n = 1-10，m = 1-10，n = m或n由于其免疫抑制活性而引起的或其药学上可接受的盐可用于治疗移植排斥宿主与移植物疾病，自身免疫疾病和炎症疾病

3. 发明授权

US5120725A Bicyclic rapamycins 失效
标题翻译：双环雷帕霉素
公开(公告)号：US5120725A
公开(公告)日：1992-06-09
申请号：US706811
申请日：1991-05-29
申请人： Wenling Kao , Robert L. Vogel , John H. Musser
发明人： Wenling Kao , Robert L. Vogel , John H. Musser
IPC分类号： A61K31/445 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , C07D491/22 , C07D498/22 , C07D519/00
CPC分类号： C07D498/22 , C07D519/00
摘要： A bicyclic derivative of rapamycin of general formula (1) ##STR1## wherein ##STR2## n=2 to 10, m=2 to 10 andn=m or n.noteq.mor a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：其中A为（CH 2）n或（CH 2）n（CHCH）（CH 2）m或n = CH 3）的雷帕霉素的双环衍生物， 2〜10，m = 2〜10，n = m或n。其等同于其免疫抑制活性的药学上可接受的盐可用于治疗移植排斥宿主与移植物疾病，自身免疫疾病和疾病炎。

4. 发明授权

US5530121A Carbamates of rapamycin 失效
公开(公告)号：US5530121A
公开(公告)日：1996-06-25
申请号：US451104
申请日：1995-05-25
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

5. 发明授权

US5349060A Rapamycin 31-ester with N,N-dimethylglycine derivatives useful as immunosuppressive agents 失效
标题翻译：雷帕霉素31-酯与可用作免疫抑制剂的N，N-二甲基甘氨酸衍生物
公开(公告)号：US5349060A
公开(公告)日：1994-09-20
申请号：US58918
申请日：1993-05-06
申请人： Wenling Kao , Robert L. Vogel
发明人： Wenling Kao , Robert L. Vogel
IPC分类号： C07D498/18 , C07D491/16 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## or hydrogen; R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen; R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y-=halide, methanesulfonate, toluene sulfonate or maleate; andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：（1）和（2）的雷帕霉素的衍生物其中图像或氢; R2 =氢或具有1至6个碳原子的低级烷基; 其中X =氢，具有1至6个碳原子的低级烷基，-CF 3，-NO 2，-OR 2，NR 2，SR 2或卤素; R4 =具有1至6个碳原子的低级烷基，烯基或炔基或选自苯基，萘基，噻吩基和喹啉基的芳族或杂环部分; Y- =卤化物，甲磺酸盐，甲苯磺酸盐或马来酸盐; Z =氧或OH和H.由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫性疾病和炎症疾病。

6. 发明授权

US5508399A Carbamates of rapamycin 失效
公开(公告)号：US5508399A
公开(公告)日：1996-04-16
申请号：US450835
申请日：1995-05-25
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloallcyl;R.sup.9 and R.sup.10 are each, independently, alkyl , alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl,, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, or Ar;A is --CH.sub.2 --, --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 --, --PR.sup.7 --, --CO--, --NHCO--, --NHSO--, or --P(O)(R.sup.7)--;Ar is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, indolyl, thiazolyl, isoxazolyl, pyrimidinyl, pyrazinyl, imidazolyl, benzopyranyl, benz[b]thiophenolyl, benzimidazolyl, benzthiazolyl, benzodioxolyl, piperidinyl, morpholinyl, piperazinyl, tetrahydrofuranyl, or pyrrolidinyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; ##STR3## is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;m=0-6;n=0-6;p=0-1;q=0-1;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

7. 发明授权

US5260299A Rapamycin 42-sulfonates and 42-(N-Carboalkoxy)Sulfamates Useful as Immunosuppressive Agents 失效
标题翻译：雷帕霉素42-磺酸盐和42-（N-羧基烷氧基）磺酸盐可用作免疫抑制剂
公开(公告)号：US5260299A
公开(公告)日：1993-11-09
申请号：US917555
申请日：1992-07-21
申请人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
发明人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
IPC分类号： C07D498/18 , A61K31/395
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

8. 发明授权

US5177203A Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents 失效
标题翻译：雷帕霉素42-磺酸盐和42-（N-烷氧羰基）氨基磺酸盐可用作免疫抑制剂
公开(公告)号：US5177203A
公开(公告)日：1993-01-05
申请号：US846637
申请日：1992-03-05
申请人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
发明人： Amedeo A. Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.
摘要翻译：通式（I）的雷帕霉素的衍生物其中R 1是含有1至6个碳原子的烷基，烯基或炔基; 或选自苯基和萘基的芳族部分或选自噻吩基和喹啉基或NHCO 2 R 2的杂环部分，其中R 2是含有1至6个碳原子的低级烷基或其药学上可接受的盐，其由于其免疫抑制活性可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

9. 发明授权

US5559120A Carbamates of rapamycin 失效
标题翻译：雷帕霉素的氨基甲酸酯
公开(公告)号：US5559120A
公开(公告)日：1996-09-24
申请号：US402571
申请日：1995-03-13
申请人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
发明人： Wenling Kao , Magid A. Abou-Gharbia , Robert L. Vogel
IPC分类号： A61K31/395 , A61K31/44 , A61K31/675 , C07D491/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/70
摘要： A compound of the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, A, B and Ar are all defined in the body of the specification or a pharmaceutically acceptable salt thereof which is useful as an immuno-suppressive, antiinflammatory, antifungal, antiprliferative and antitumor agent.
摘要翻译：结构的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，A，B和Ar均在本说明书的主体或其药学上可接受的盐中定义，可用作免疫抑制，抗炎，抗真菌，抗增殖和抗肿瘤剂。

10. 发明授权

US5346893A Rapamycin 42-sulfonates and 42-(N-carbalkoxy) sulfamates useful as immunosuppressive agents 失效
标题翻译：雷帕霉素42-磺酸盐和42-（N-烷烃氧基）氨基磺酸盐可用作免疫抑制剂
公开(公告)号：US5346893A
公开(公告)日：1994-09-13
申请号：US65107
申请日：1993-05-19
申请人： Amedeo Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
发明人： Amedeo Failli , Wenling Kao , Robert J. Steffan , Robert L. Vogel
IPC分类号： C07D498/18 , A61K31/395 , C07D491/06
CPC分类号： C07D498/18
摘要： The invention concerns compounds of formula (I) ##STR1## where R.sup.1 is alkyl, haloalkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from phenyl, naphthyl and 4-(phenylaza) phenyl wherein said aromatic group is optionally substituted by one or more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifuluoromethyl, trifluoromethoxy or R.sup.1 is a heteroaromatic group of 5 to 10 ring atoms containing oxygen, nitrogen and/or sulfur as heteroatom(s) wherein said heteroaromatic group is optionally substituted by one or more substituents selected form C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy or R.sup.1 is NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which compounds are useful in the treatment of transplantation rejection, host versus graft disease, autoimmune diseases and diseases of inflammation.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是含有1至6个碳原子的烷基，卤代烷基，烯基或炔基; 或选自苯基，萘基和4-（苯基苯基）苯基的芳族部分，其中所述芳族基团任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，氨基，单 - 或二 - C1-C6）烷基氨基，羧基，（C1-C6烷氧基）羰基，C2-C7烷酰基，（C1-C6）硫代烷基，卤素，氰基，硝基，三氟甲基，三氟甲氧基或R1是含有5-10个环原子的杂芳族基团氧，氮和/或硫作为杂原子，其中所述杂芳基任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，氨基，单 - 或二 - （C 1 -C 6）烷基氨基，羧基，（C1-C6烷氧基）羰基，C2-C7烷酰基，（C1-C6）硫代烷基，卤素，氰基，硝基，三氟甲基，三氟甲氧基或R1是NHCO2R2，其中R2是含有1至6个碳原子的低级烷基; 或其药学上可接受的盐，该化合物可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

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