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1. 发明授权

US5120754A Thiazolidinedione hypoglycemic agents 失效
标题翻译：噻唑烷二酮降血糖药
公开(公告)号：US5120754A
公开(公告)日：1992-06-09
申请号：US679898
申请日：1991-04-03
申请人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
发明人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
IPC分类号： C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/06 , C07D417/10
CPC分类号： C07D417/06 , C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/10
摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and dB are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.
摘要翻译：式（I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键; A和dB各自独立地为CH或N，条件是当A或B为N时，另一个为CH; X是S，SO，SO 2，CH 2，CHOH或CO; n为0或1; Y是CHR1或NR2，条件是当n是1且Y是NR2时，X是SO2或CO; Z是CHR 3，CH 2 CH 2，CH = CH，CH 3，OCH 2，SCH 2，SOCH 2或SO 2 CH 2; R，R1，R2和R3各自独立地为氢或甲基; 苯基，苄基，羟基，甲氧基，苯氧基，苄氧基，溴，氯或氟; X 1和X 2各自独立地为氢，甲基，其药学上可接受的阳离子盐; 或当A或B为N时，其药学上可接受的酸加成盐。

2. 发明授权

US5061717A Thiazolidinedione hypoglycemic agents 失效
标题翻译：噻唑烷二酮降血糖药
公开(公告)号：US5061717A
公开(公告)日：1991-10-29
申请号：US566436
申请日：1990-08-14
申请人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
发明人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61P3/06 , A61P3/08 , C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/06 , C07D417/10
CPC分类号： C07D417/06 , C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/10
摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond; A and B are each independently CH or N, with the proviso that when A or B is N, the other is CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro; a pharmaceutically-acceptable cationic salt thereof; or a pharmaceutically-acceptable acid addition salt thereof when A or B is N.
摘要翻译： PCT No.PCT / US88 / 00744 Sec。 371日期1990年8月14日（I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键;（e）日本1990年8月14日PCT。 A和B各自独立地为CH或N，条件是当A或B为N时，另一个为CH; X是S，SO，SO 2，CH 2，CHOH或CO; n为0或1; Y是CHR1或NR2，条件是当n是1且Y是NR2时，X是SO2或CO; Z是CHR 3，CH 2 CH 2，CH = CH，CH 3，OCH 2，SCH 2，SOCH 2或SO 2 CH 2; R，R 1，R 2和R 3各自独立地为氢或甲基; 苯基，苄基，羟基，甲氧基，苯氧基，苄氧基，溴，氯或氟; X 1和X 2各自独立地为氢，甲基，其药学上可接受的阳离子盐; 或当A或B为N时，其药学上可接受的酸加成盐。

3. 发明授权

US5223522A Thiazolidinedione hypoglycemic agents 失效
标题翻译：噻唑烷二酮降血糖药
公开(公告)号：US5223522A
公开(公告)日：1993-06-29
申请号：US857039
申请日：1992-03-24
申请人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
发明人： David A. Clark , Steven W. Goldstein , Gerald F. Holland , Bernard Hulin , James P. Rizzi
IPC分类号： C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/06 , C07D417/10
CPC分类号： C07D417/06 , C07C311/21 , C07C323/22 , C07D213/50 , C07D277/34 , C07D417/10
摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;A and B are each independently CH;X is S, SO, SO.sub.2, CH.sub.2, CHOH or CO;n is 0 or 1;Y is CHR.sup.1 or NR.sup.2, with the proviso that when n is 1 and Y is NR.sup.2, X is SO.sub.2 or CO;Z is CHR.sup.3, CH.sub.2 CH.sub.2, CH.dbd.CH, ##STR2## OCH.sub.2, SCH.sub.2, SOCH.sub.2 or SO.sub.2 CH.sub.2 ; R, R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen or methyl; andX.sup.1 and X.sup.2 are each independently hydrogen, methyl, trifluoromethyl, phenyl, benzyl, hydroxy, methoxy, phenoxy, benzyloxy, bromo, chloro or fluoro;a pharmaceutically-acceptable cationic salt thereof; ora pharmaceutically-acceptable acid addition salt thereof.
摘要翻译：式（I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键; A和B各自独立地为CH; X是S，SO，SO 2，CH 2，CHOH或CO; n为0或1; Y是CHR1或NR2，条件是当n是1且Y是NR2时，X是SO2或CO; Z是CHR 3，CH 2 CH 2，CH = CH，CH 3，OCH 2，SCH 2，SOCH 2或SO 2 CH 2; R，R 1，R 2和R 3各自独立地为氢或甲基; 苯基，苄基，羟基，甲氧基，苯氧基，苄氧基，溴，氯或氟; X 1和X 2各自独立地为氢，甲基，其药学上可接受的阳离子盐; 或其药学上可接受的酸加成盐。

4. 发明授权

US5130379A Hypoglycemic thiazolidinedione derivatives 失效
标题翻译：低血糖噻唑烷二酮衍生物
公开(公告)号：US5130379A
公开(公告)日：1992-07-14
申请号：US674833
申请日：1991-03-26
申请人： David A. Clark , Steven W. Goldstein , Bernard Hulin
发明人： David A. Clark , Steven W. Goldstein , Bernard Hulin
IPC分类号： C07D277/24 , C07D277/34 , C07D417/10 , C07D417/14 , C07F7/18
CPC分类号： C07D417/10 , C07D277/24 , C07D277/34 , C07D417/14 , C07F7/1856
摘要： Hypoglycemic thiazolidine-2,4-dione derivatives ##STR1## wherein the dotted line represents a bond or no bond;V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N-- or S;W is CH.sub.2, CHOH, CO, C.dbd.NOR or --CH.dbd.CH--;X is S, O, NR.sup.1, --CH.dbd.N-- or --N.dbd.CH--;Y is CH or N;Z is hydrogen, (C.sub.1 -C.sub.7)alkyl, (C.sub.3 -C.sub.7) cycloalkyl, phenyl, naphthyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, (C.sub.1 -C.sub.3)alkoxy, fluoro, chloro or bromo;Z.sup.1 is hydrogen or (C.sub.1 -C.sub.3)alkyl;R is hydrogen or methyl; andn is 1, 2 or 3;a pharmaceutically acceptble cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains a basic nitrogen.
摘要翻译：低血糖噻唑烷-2,4-二酮衍生物（I）其中虚线代表键或无键; V是-CH = CH-，-N = CH-，-CH = N-或S; W是CH 2，CHOH，CO，C = NOR或-CH = CH-; X是S，O，NR1，-CH = N-或-N = CH-; Y是CH或N; Z是氢，（C 1 -C 7）烷基，（C 3 -C 7）环烷基，苯基，萘基，吡啶基，呋喃基，噻吩基或被相同或不同的基团单独或二取代的苯基，（C 1 -C 3）烷氧基，氟，氯或溴; Z1是氢或（C1-C3）烷基; R是氢或甲基; n为1,2或3; 其药学上可接受的阳离子盐; 或其药学上可接受的酸加成盐时，该化合物含有碱性氮。

5. 发明授权

US5330998A Thiazolidinedione derivatives as hypoglycemic agents 失效
标题翻译：噻唑烷二酮衍生物作为降血糖药
公开(公告)号：US5330998A
公开(公告)日：1994-07-19
申请号：US566437
申请日：1990-08-14
申请人： David A. Clark , Steven W. Goldstein , Bernard Hulin
发明人： David A. Clark , Steven W. Goldstein , Bernard Hulin
IPC分类号： C07D263/44 , C07D417/12 , A61K31/425
CPC分类号： C07D263/44 , C07D417/12
摘要： Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N--, S, O or NR;W is S, SO, SO.sub.2, SO.sub.2 NR.sup.1, NR.sup.1 SO.sub.2, CONR.sup.1 or NR.sup.1 CO;X is S, O, NR.sup.2, --CH.dbd.N-- or --N.dbd.CH;Y is CH or N;Z is hydrogen, (C.sub.1 -C.sub.7)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, (C.sub.1 -C.sub.3)alkoxy, fluoro, chloro or bromo;Z.sup.1 is hydrogen or (C.sub.1 -C.sub.3)alkyl;R, R.sup.1 and R.sup.2 are each independently hydrogen or (C.sub.1 -C.sub.4); andn is 1, 2 or 3;a pharmaceutically acceptable cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains a basic nitrogen.
摘要翻译： PCT No.PCT / US88 / 00745 Sec。 371日期1990年8月14日（I）的低血糖噻唑烷-2,4-二酮衍生物，其中虚线表示键或无键;（e）日本1990年8月14日PCT。 V是-CH = CH-，-N = CH-，-CH = N-，S，O或NR; W是S，SO，SO2，SO2NR1，NR1SO2，CONR1或NR1CO; X是S，O，NR2，-CH = N-或-N = CH; Y是CH或N; Z是氢，（C 1 -C 7）烷基，（C 3 -C 7）环烷基，苯基，吡啶基，呋喃基，噻吩基或被相同或不同的基团（C 1 -C 3）烷基，三氟甲基，（C 1 -C 3） -C 3）烷氧基，氟，氯或溴; Z1为氢或（C1-C3）烷基; R，R 1和R 2各自独立地为氢或（C 1 -C 4）; n为1,2或3; 其药学上可接受的阳离子盐; 或其药学上可接受的酸加成盐时，该化合物含有碱性氮。

6. 发明授权

US5036079A Hypoglycemic thiazolidinedione derivatives 失效
标题翻译：低血糖噻唑烷二酮衍生物
公开(公告)号：US5036079A
公开(公告)日：1991-07-30
申请号：US477261
申请日：1990-02-08
申请人： David A. Clark , Steven W. Goldstein , Bernard Hulin
发明人： David A. Clark , Steven W. Goldstein , Bernard Hulin
IPC分类号： C07D277/24 , C07D417/10 , C07D417/14
CPC分类号： C07D417/10 , C07D277/24 , C07D417/14
摘要： Hypoglycemic thiazolidine-2,4-derivatives ##STR1## wherein the dotted line represents a bond or no bond; V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N-- or S;W is CH.sub.2, CHOH, CO, C.dbd.NOR or --CH.dbd.CH--;X is S, O, NR.sup.1, --CH.dbd.N-- or --N.dbd.CH--;Y is CH or N;Z is hydrogen, (C.sub.1 -C.sub.7)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, naphtyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, (C.sub.1 -C.sub.3)alkoxy, fluoro, chloro or bromo;Z.sup.1 is hydrogen or (C.sub.1 -C.sub.3)alkyl;R is hydrogen or methyl; andn is 1, 2 or 3;a pharamceutically acceptable cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains basic nitrogen.
摘要翻译：低血糖噻唑烷-2,4-衍生物（I）其中虚线代表键或无键; V是-CH = CH-，-N = CH-，-CH = N-或S; W是CH 2，CHOH，CO，C = NOR或-CH = CH-; X是S，O，NR1，-CH = N-或-N = CH-; Y是CH或N; Z是氢，（C 1 -C 7）烷基，（C 3 -C 7）环烷基，苯基，萘基，吡啶基，呋喃基，噻吩基或被相同或不同的基团单独或二取代的苯基，（C 1 -C 3）烷氧基，氟，氯或溴; Z1是氢或（C1-C3）烷基; R是氢或甲基; n为1,2或3; 其药学上可接受的阳离子盐; 或其药学上可接受的酸加成盐时，该化合物含有碱性氮。

7. 发明授权

US06541495B1 Carboxylic acid derivatives as inhibitors of hyperproliferation diseases 失效
标题翻译：羧酸衍生物作为过度增生疾病的抑制剂
公开(公告)号：US06541495B1
公开(公告)日：2003-04-01
申请号：US09548937
申请日：2000-04-13
申请人： Steven W. Goldstein , Kelly P. Longo , Bernard Hulin
发明人： Steven W. Goldstein , Kelly P. Longo , Bernard Hulin
IPC分类号： A61K3142
CPC分类号： A61K31/343
摘要： A method of treating hyperproliferation diseases in mammals in need of such treatment, which method includes administering to said mammal a therapeutically effective amount of a compound of the formula: or a pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein R1, R2, R3, R4, W, X, Y, Z and t are as defined herein.
摘要翻译：一种在需要这种治疗的哺乳动物中治疗过度增生疾病的方法，该方法包括向所述哺乳动物施用治疗有效量的下式化合物或其药学上可接受的盐，水合物或前药，其中R1，R2，R3， R4，W，X，Y，Z和t如本文所定义。

8. 发明授权

US5401761A Thiazolidinedione hypoglycemic agents 失效
标题翻译：噻唑烷二酮降血糖药
公开(公告)号：US5401761A
公开(公告)日：1995-03-28
申请号：US162075
申请日：1993-12-09
申请人： Steven W. Goldstein , Bernard Hulin
发明人： Steven W. Goldstein , Bernard Hulin
IPC分类号： C07D417/14 , A61K31/425
CPC分类号： C07D417/14
摘要： Compounds of the formula ##STR1## where R is alkyl, cycloalkyl, phenyl or substituted phenyl are useful as hypoglycemic agents.
摘要翻译：其中R是烷基，环烷基，苯基或取代的苯基的式“IMAGE”的化合物可用作降血糖剂。

9. 发明授权

US5498621A Oxazolidinedione hypoglycemic agents 失效
标题翻译：恶唑烷二酮降血糖药
公开(公告)号：US5498621A
公开(公告)日：1996-03-12
申请号：US289612
申请日：1994-08-12
申请人： Robert L. Dow , Bernard Hulin , David A. Clark
发明人： Robert L. Dow , Bernard Hulin , David A. Clark
IPC分类号： C07D263/44 , C07D413/14 , C07D417/12 , A61K31/42
CPC分类号： C07D263/44 , C07D413/14 , C07D417/12
摘要： Compounds of the formulae ##STR1## where R is cycloalkyl or aryl; R.sub.1 is alkyl, X is O or C.dbd.O; A is O or S; and B is N or CH are useful as hypoglycemic agents.
摘要翻译：其中R是环烷基或芳基的式和的化合物; R1是烷基，X是O或C = O; A是O或S; B是N或CH可用作降血糖药。

10. 发明授权

US06812350B2 Synthesis of 3,3,4,4-tetrafluoropyrrolidine and novel dipeptidyl peptidase-IV inhibitor compounds 失效
标题翻译：合成3,3,4,4-四氟吡咯烷和新型二肽基肽酶-IV抑制剂化合物
公开(公告)号：US06812350B2
公开(公告)日：2004-11-02
申请号：US10455747
申请日：2003-06-03
申请人： Bernard Hulin
发明人： Bernard Hulin
IPC分类号： C07D20504
CPC分类号： C07D207/10
摘要： The present invention relates to a method of making novel dipeptidyl peptidase-IV (“DPP-IV’) inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.
摘要翻译：本发明涉及一种制备新的二肽基肽酶-IV（“DPP-IV”）抑制剂化合物的方法，其用于治疗特别是与DPP-IV进行加工的蛋白质相关的疾病，例如2型糖尿病，代谢综合征（X综合征或胰岛素抵抗综合征），高血糖症，糖耐量异常，糖尿病，代谢性酸中毒，白内障，糖尿病性神经病变，糖尿病性肾病，糖尿病性视网膜病变，糖尿病性心肌病，1型糖尿病，肥胖症，高血压，高脂血症，动脉粥样硬化骨质疏松症，骨质疏松症，骨质疏松症，骨折，急性冠状动脉综合征，多囊卵巢综合症不育症，短肠综合征，预防2型糖尿病等疾病进展，本发明还涉及一种制备3,3， 4,4-四氟吡咯烷，用于上述制备DPP-IV化合物的方法中的原料。

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