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1. 发明专利

AU2001277754B2 Proline derivatives and use thereof as drugs 未知
公开(公告)号：AU2001277754B2
公开(公告)日：2005-09-29
申请号：AU2001277754
申请日：2001-08-10
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： KITAJIMA HIROSHI , AKAHOSHI FUMIHIKO , SAKASHITA HIROSHI , HAYASHI YOSHIHARU
IPC分类号： A61P1/02 , A61P3/04 , A61P3/10 , A61P13/08 , A61P17/00 , A61P31/18 , A61P35/04 , A61P37/06 , A61P43/00 , C07D207/16 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04 , C07D498/04 , A61K031/438 , A61K031/427 , A61K031/506 , A61P031/18 , A61K031/401 , A61P035/04 , A61K031/454 , A61K031/5025 , A61P003/10 , A61K031/4439 , A61P043/00 , A61P013/08 , A61K031/551 , A61P001/02 , A61K031/4709 , A61P037/06 , A61K031/5377 , A61K031/496 , A61P017/00 , A61K031/517 , A61P003/04
摘要： The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the ³-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

2. 发明专利

AU2001294197C1 Aliphatic nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294197C1
公开(公告)日：2005-05-19
申请号：AU2001294197
申请日：2001-10-05
申请人： TANABE SEIYAKU CO LTD
发明人： ARAKAWA KENJI , MATSUMOTO TAKESHI , HIKOTA MASATAKA , KAWANAMI SABURO , MORIMOTO HIROSHI , YASUDA KOSUKE
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61P003/10 , A61P043/00 , C07D277/82 , C07D277/42 , C07D277/06 , A61K031/4155 , A61K031/41 , A61K031/4035 , A61K031/4365 , A61K031/4725 , A61K031/437 , A61K031/541 , A61K031/55 , A61K031/433 , A61K031/327 , A61K031/4025 , A61K031/454 , A61K031/4709 , A61K031/401 , A61K031/519 , A61K031/498 , A61K031/423 , A61K031/428 , A61K031/5377 , A61K031/497 , A61K031/501 , A61K031/506 , A61K031/4439 , C07D409/12 , C07D495/04 , C07D405/14
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

3. 发明专利

AU2001294196B2 Nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294196B2
公开(公告)日：2005-11-17
申请号：AU2001294196
申请日：2001-10-05
申请人： TANABE SEIYAKU CO LTD
发明人： YASUDA KOSUKE , KAWANAMI SABURO , ARAKAWA KENJI , MORIMOTO HIROSHI , HIKOTA MASATAKA , MATSUMOTO TAKESHI
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61K031/4709 , A61K031/496 , A61P003/10 , C07D403/14 , A61K031/4035 , A61P043/00 , A61K031/437 , A61K031/4545 , C07D413/04 , A61K031/427 , A61K031/5377 , A61K031/426 , A61K031/506 , A61K031/4439 , A61K031/454 , A61K031/4178 , A61K031/423 , A61K031/497 , A61K031/4025 , A61K031/422 , A61K031/501 , A61K031/517 , A61K031/401
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

4. 发明专利

AU2001233242B2 Tosylproline analogs as thymidylate synthase inhibitors 未知
公开(公告)号：AU2001233242B2
公开(公告)日：2004-11-18
申请号：AU2001233242
申请日：2001-02-02
申请人： SUNESIS PHARMACEUTICALS INC
发明人： ERLANSON DANIEL A
IPC分类号： A61K31/401 , A61P31/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07D207/48 , C07D211/96 , A61P033/00 , A61P031/12 , A61P031/04 , A61K031/401 , A61K031/445
摘要： Tosylproline analogs of formula I, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are thymidylate synthase inhibitors; and are useful as anti-tumor agents and as anti-parasitics, anti-bacterials, anti-fungals, and anti-virals.

5. 发明专利

AU2002319535B2 The treatment of lipodystrophy 未知
公开(公告)号：AU2002319535B2
公开(公告)日：2005-01-06
申请号：AU2002319535
申请日：2002-08-07
申请人： ARK THERAPEUTICS LTD
发明人： MARTIN JOHN FRANCIS , ERUSALIMSKY JORGE D , MONTGOMERY HUGH EDWARD
IPC分类号： A61K45/00 , A61K31/00 , A61K31/55 , A61K31/551 , A61K31/675 , A61K38/55 , A61P3/00 , A61P3/06 , A61P3/10 , A61K031/00 , A61K031/223 , A61K031/519 , A61K031/422 , A61P003/00 , A61K031/401 , A61K031/403 , A61K031/472 , A61K031/675 , A61K031/417 , A61K031/4178 , A61K031/4184 , A61K031/55 , A61K031/551 , A61K031/554
摘要： An inhibitor of the renin-angiotensin system is useful for the treatment or prevention of the lipodystrophy syndrome, e.g. in AIDS patients also receiving anti-retroviral therapy.

6. 发明专利

AU2001294197B2 Aliphatic nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294197B2
公开(公告)日：2004-09-16
申请号：AU2001294197
申请日：2001-10-05
申请人： TANABE SEIYAKU CO
发明人： ARAKAWA KENJI , MATSUMOTO TAKESHI , HIKOTA MASATAKA , KAWANAMI SABURO , MORIMOTO HIROSHI , YASUDA KOSUKE
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61P003/10 , A61P043/00 , C07D277/82 , C07D277/42 , C07D277/06 , A61K031/4155 , A61K031/41 , A61K031/4035 , A61K031/4365 , A61K031/4725 , A61K031/437 , A61K031/541 , A61K031/55 , A61K031/433 , A61K031/327 , A61K031/4025 , A61K031/454 , A61K031/4709 , A61K031/401 , A61K031/519 , A61K031/498 , A61K031/423 , A61K031/428 , A61K031/5377 , A61K031/497 , A61K031/501 , A61K031/506 , A61K031/4439 , C07D409/12 , C07D495/04 , C07D405/14
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

7. 发明申请

WO2003004068A1 HYPERTENSION TREATMENT 审中-公开
标题翻译：高血压治疗
公开(公告)号：WO2003004068A1
公开(公告)日：2003-01-16
申请号：PCT/NZ2002/000118
申请日：2002-07-04
申请人： AUCKLAND UNISERVICES LIMITED , VICKERS, Mark, Hedley , BREIER, Bernhard, Hermann, Heinrich , GLUCKMAN, Peter, David
发明人： VICKERS, Mark, Hedley , BREIER, Bernhard, Hermann, Heinrich , GLUCKMAN, Peter, David
IPC分类号： A61K031/401
CPC分类号： A61K31/5025 , A61K31/401 , A61K31/405 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/472 , A61K38/27 , A61K2300/00
摘要： A method of delaying or preventing the onset of hypertension in mammals, including predisposed mammals, is disclosed. The method includes the administering of an effective amount of or increasing the effective concentration of growth hormone, an analog thereof or a functionally equivalent ligand.
摘要翻译：公开了延迟或预防哺乳动物（包括易感哺乳动物）中高血压发作的方法。该方法包括施用有效量或增加生长激素的有效浓度，其类似物或功能等同的配体。

8. 发明申请

US20040259925A1 Pharmaceutical compositions and methds for the prevention or treatment of cardiovascular, cardiopulmonary, pulmonary or renal diseases 审中-公开
标题翻译：用于预防或治疗心血管，心肺，肺或肾脏疾病的药物组合物和方法
公开(公告)号：US20040259925A1
公开(公告)日：2004-12-23
申请号：US10757295
申请日：2004-01-14
申请人： Boehringer Ingelheim Pharma GmbH & Co. KG
发明人： Axel Riedel , Josep-Maria Sendra , Josef M.E. Leiter , Stefan Kauschke , Michael Mark
IPC分类号： A61K031/4178 , A61K031/401
CPC分类号： A61K31/416 , A61K31/40 , A61K2300/00
摘要： The present invention relates to a process for the prevention or treatment of cardiovascular, cardiopulmonary, pulmonary or renal diseases by improving endothelial function and achieving protection of organs, tissues and blood vessels in indications in which control of blood pressure and lipid levels are necessary, particularly in people in whom type 2 diabetes mellitus has been diagnosed or who are suspected of prediabetes, for preventing diabetes and prediabetes, or for the treatment of Metabolic Syndrome and insulin resistance in patients with normal blood pressure. The process comprises generally administering effective amounts of telmisartan or a polymorph or salt thereof and atorvastatin. The invention further relates to suitable pharmaceutical compositions which contain telmisartan or a polymorph or salt thereof and atorvastatin, as a combined preparation for simultaneous, separate or sequential use in the prevention or treatment of these diseases.
摘要翻译：本发明涉及一种预防或治疗心血管，心肺，肺或肾脏疾病的方法，该方法通过改善内皮功能并实现对需要控制血压和脂质水平的适应症的器官，组织和血管的保护，特别是在2型糖尿病诊断或怀疑患有糖尿病前期的人群中，用于预防糖尿病和糖尿病前期，或用于治疗正常血压患者的代谢综合征和胰岛素抵抗。该方法通常施用有效量的替米沙坦或其多晶型物或盐和阿托伐他汀。本发明还涉及包含替米沙坦或其多晶型物或盐和阿托伐他汀的合适的药物组合物，作为用于同时，分开或顺序用于预防或治疗这些疾病的组合制剂。

9. 发明申请

US20040259860A1 Substituted piperidines and pyrrolidines as calcium sensing receptor modulators and method 有权
标题翻译：取代的哌啶和吡咯烷作为钙敏感受体调节剂和方法
公开(公告)号：US20040259860A1
公开(公告)日：2004-12-23
申请号：US10854689
申请日：2004-05-26
发明人： John K. Dickson , R. Michael Lawrence , Jacques Y. Roberge , David P. Rotella , Wu Yang
IPC分类号： C07D43/02 , C07D41/02 , A61K031/55 , A61K031/454 , A61K031/4025 , A61K031/401
CPC分类号： C07D207/06 , C07D207/08 , C07D207/10 , C07D211/18 , C07D211/22 , C07D333/28
摘要： Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula 1 wherein m is 0, 1, 2, 3 or 4; each X is independently selected from the group consisting of hydrogen, halo, cyano, nitro, OCF3, hydroxy, amino, carboxyl, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, haloalkyl, alkoxy, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkylalkyl, R1O, R1R2N, R1OCO, R1CO, R1R2NCO, R1R2NCONR2a, R1OCONR2a, R1CONR2a, R1S, R1SO, R1SO2, R1R2NSO2, R1R2NSO2NR2a, and R1SO2NR2a; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; R2 and R2a are the same or different and are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloheteroalkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; n is 1, 2, or 3; W is O or H,R3; R3 is hydrogen or hydroxyl; Ar is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group; Q is hydrogen, F, or hydroxyl. In addition, a method for using these compounds to treat diseases associated with abnormal or mineral homeostasis is also provided.
摘要翻译：提供了作为钙感应受体的拮抗剂的化合物，并具有通式，其中m为0,1,2,3或4; 每个X独立地选自氢，卤素，氰基，硝基，OCF 3，羟基，氨基，羧基，烷基，烯基，炔基，环烷基，环杂烷基，卤代烷基，烷氧基，烷氧基羰基烷基，羟基羰基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基烷基，R 1 O，R 1 R 2 N，R 1 OCO，R 1 CO，R 1 R 2 NCO，R 1 R 2， NCONR 2a，R 1 OCONR 2a，R 1 CONR 2a，R 1 S，R 1 SO，R 1 SO 2，R 1 R 2 NSO 2 R 1 R 2 NSO 2 NR 2a和R 1 SO 2 NR 2a; R 1是烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; R 2和R 2a相同或不同并且独立地选自氢，烷基，烯基，炔基，环烷基，环杂烷基，芳基，杂芳基，芳基烷基或杂芳基烷基; n为1,2或3; W是O或H，R 3; R 3是氢或羟基; Ar是取代或未取代的芳基或取代或未取代的杂芳基; Q是氢，F或羟基。此外，还提供了使用这些化合物治疗与异常或矿物质内稳态相关疾病的方法。

10. 发明申请

US20040220112A1 Kappa agonist compounds, pharmaceutical formulations and method of prevention and treatment of pruritus therewith 失效
标题翻译：卡帕激动剂化合物，药物制剂和预防和治疗瘙痒的方法
公开(公告)号：US20040220112A1
公开(公告)日：2004-11-04
申请号：US10455687
申请日：2003-06-05
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： A61K038/04 , A61K031/675 , A61K031/4015 , A61K031/401
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04 , Y02A50/422
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and pruritic agents are provided. The compounds of formulae I, II, III and IV have the structure: 1 wherein X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification
摘要翻译：提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和瘙痒剂的方法。式I，II，III和IV的化合物具有以下结构：其中X，X4，X5，X7，X9; R1，R2，R3，R4; Y，Z和n如说明书所述

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