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1. 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。

2. 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。

3. 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。

4. 发明授权

US07291618B2 Therapeutic compounds 有权
标题翻译：治疗化合物
公开(公告)号：US07291618B2
公开(公告)日：2007-11-06
申请号：US11129277
申请日：2005-05-12
申请人： Bernard Hulin , David W. Piotrowski
发明人： Bernard Hulin , David W. Piotrowski
IPC分类号： A61K31/497 , C07D403/14
CPC分类号： C07D207/14 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
摘要翻译：本发明提供式（I）化合物，其前体药物和立体异构体，以及化合物，前药和立体异构体的药学上可接受的盐，其中R 1，R 2， R 3，HET，n，Q，X，Y和Z如本文所述; 组合物; 及其用于治疗糖尿病性神经病变，糖尿病性肾病，糖尿病性微血管病变等糖尿病并发症的用途。

5. 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。

6. 发明授权

US5998463A Glycogen phosphorylase inhibitors 失效
标题翻译：糖原磷酸化酶抑制剂
公开(公告)号：US5998463A
公开(公告)日：1999-12-07
申请号：US251141
申请日：1999-02-16
申请人： Bernard Hulin , Reinhard Sarges
发明人： Bernard Hulin , Reinhard Sarges
IPC分类号： A61K45/06 , C07D209/34 , A01N43/38
CPC分类号： A61K45/06 , C07D209/34
摘要： This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.
摘要翻译：本发明涉及可用作糖原磷酸化酶抑制剂的某些5-酰基-2-氧代 - 吲哚-3-甲酰胺，用这些化合物治疗糖原磷酸化酶依赖性疾病或病症的方法和包含这些化合物的药物组合物。本发明还涉及包含5-酰基-2-氧代 - 吲哚-3-甲酰胺与抗糖尿病药物的组合物的药物组合物以及用这些组合物治疗糖原磷酸化酶依赖性疾病或病症的方法。

7. 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。

8. 发明授权

US5306726A 3-aryl-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents 失效
标题翻译： 3-芳基-2-羟基丙酸衍生物和类似物作为降血糖剂
公开(公告)号：US5306726A
公开(公告)日：1994-04-26
申请号：US980404
申请日：1992-11-24
申请人： Bernard Hulin
发明人： Bernard Hulin
IPC分类号： A61K31/34 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/496 , A61K31/50 , A61K31/505 , A61P3/06 , A61P3/08 , C07C59/48 , C07C235/04 , C07C235/32 , C07C317/44 , C07C323/50 , C07D20060101 , C07D207/333 , C07D211/22 , C07D231/12 , C07D239/10 , C07D241/06 , C07D263/24 , C07D263/32 , C07D263/36 , C07D263/56 , C07D277/20 , C07D277/30 , C07D277/32 , C07D307/79 , C07D307/80 , C07D307/81 , C07D311/02 , C07D311/04 , C07D311/58 , C07D311/60 , C07D405/04 , C07D407/04 , C07D407/06 , C07D409/04 , C07D409/06 , C07D413/04 , C07D413/06 , C07D417/06
CPC分类号： C07D413/06 , C07D263/32 , C07D311/04
摘要： Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.
摘要翻译：某些3-（苯基，苯并二氢吡喃-2-基，苯并呋喃-5-基或苯并恶唑-5-基）-2-（羟基或巯基）丙酸衍生物和类似物可用作低血糖和低胆固醇血症药。

9. 发明申请

US20070161664A1 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：US20070161664A1
公开(公告)日：2007-07-12
申请号：US11682945
申请日：2007-03-07
申请人： Bernard Hulin , David Piotrowski
发明人： Bernard Hulin , David Piotrowski
IPC分类号： A61K31/519 , C07D487/02
CPC分类号： C07D207/14 , C07D275/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The invention provides compounds of formula (I), or a pharmaceutically acceptable salt of said compound, or a solvate of said compound or salt, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof including treating Type 2 diabetes.
摘要翻译：本发明提供式（I）化合物或所述化合物的药学上可接受的盐或所述化合物或盐的溶剂合物，其中R 1，R 2，R 2，R 2， HET，n，Q，X，Y和Z如本文所述; 组合物; 及其用途，包括治疗2型糖尿病。

10. 发明授权

US06846820B2 Substituted N-(indole-2-carbonyl) -amides and derivatives as glycogen phosphorylase inhibitors 失效
标题翻译：取代的N-（吲哚-2-羰基） - 酰胺和衍生物作为糖原磷酸化酶抑制剂
公开(公告)号：US06846820B2
公开(公告)日：2005-01-25
申请号：US10464728
申请日：2003-06-17
申请人： Dennis J. Hoover , Bernard Hulin , William H. Martin , Judith L. Treadway
发明人： Dennis J. Hoover , Bernard Hulin , William H. Martin , Judith L. Treadway
IPC分类号： A61K31/405 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , C07D209/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D237/02 , A61K31/50
CPC分类号： A61K31/405 , A61K31/416 , A61K31/4178 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , C07D209/42 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： This invention relates to certain indole-2-carboxamides of formula (I) and the pharmaceutically acceptable salts and prodrugs thereof, wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, C(O)NR8R9 or C(O)R12, useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds.
摘要翻译：本发明涉及式（I）的某些吲哚-2-甲酰胺及其药学上可接受的盐和前药，其中R6是羧基，（C1-C8）烷氧基羰基，C（O）NR8R9或C（O）糖原磷酸化酶抑制剂，用此类化合物治疗糖原磷酸化酶依赖性疾病或病症的方法和包含这些化合物的药物组合物。

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