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1. 发明申请

WO2007089904A2 PYRIDYLPHENYL COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES 审中-公开
标题翻译：用于炎症和免疫相关用途的吡啶基苯酚化合物
公开(公告)号：WO2007089904A2
公开(公告)日：2007-08-09
申请号：PCT/US2007/002790
申请日：2007-01-31
申请人： SYNTA PHARMACEUTICALS CORP. , JIANG, Jun , XIA, Zhi-Qiang , ZHANG, Junyi , BOHNERT, Gary , CHEN, Shoujun , XIE, Yu
发明人： JIANG, Jun , XIA, Zhi-Qiang , ZHANG, Junyi , BOHNERT, Gary , CHEN, Shoujun , XIE, Yu
IPC分类号： A61K31/4439
CPC分类号： C07D417/14 , C07D211/70 , C07D211/72 , C07D213/72 , C07D213/75 , C07D213/81 , C07D401/12 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/12
摘要： The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, X 1 , X 2 , Z, R 3 , R 4 , and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译：本发明涉及结构式（I）的化合物或其药学上可接受的盐，溶剂合物，包合物或前药，其中Y，L，X 1，X 2，，Z，R 3，R 4和n如本文所定义。这些化合物可用作免疫抑制剂并用于治疗和预防炎性病症，过敏性疾病和免疫疾病。

2. 发明申请

WO2006081389A1 THIOPHENE COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES 审中-公开
标题翻译：用于炎症和免疫相关用途的噻吩化合物
公开(公告)号：WO2006081389A1
公开(公告)日：2006-08-03
申请号：PCT/US2006/002872
申请日：2006-01-25
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , CHEN, Shoujun , JIANG, Jun , XIA, Zhi-Qiang , XIE, Yu , YU, Chih-Yi
发明人： SUN, Lijun , CHEN, Shoujun , JIANG, Jun , XIA, Zhi-Qiang , XIE, Yu , YU, Chih-Yi
IPC分类号： C07D333/10
CPC分类号： C07D333/38 , A61K31/381 , A61K31/4427 , A61K31/4436 , A61K31/444 , C07D333/20 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/14 , Y02A50/422
摘要： The invention relates to compounds of structural formulas (I) and (XVI) or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X 1 , X 2 , Z, L, L 2 , R 1 , R 2 , R 3 , R 21 , n, q, and t are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译：本发明涉及结构式（I）和（XVI）的化合物或其药学上可接受的盐，溶剂化物，包合物或前药，其中X 1，X 2， Z，L，L 2，R 1，R 2，R 3，R 21， / SUB>，n，q和t在本文中定义。这些化合物可用作免疫抑制剂并用于治疗和预防炎性病症，过敏性疾病和免疫疾病。

3. 发明申请

WO2006065842A2 5,6,7,8-TETRAHYDROQUINOLINES AND RELATED COMPOUNDS AND USES THEREOF 审中-公开
标题翻译： 5,6,7,8-四氢喹啉和相关化合物及其用途
公开(公告)号：WO2006065842A2
公开(公告)日：2006-06-22
申请号：PCT/US2005/045136
申请日：2005-12-13
申请人： SYNTA PHARMACEUTICALS CORP. , BORELLA, Christopher , FOLEY, Kevin , SUN, Lijun , CHIMMANAMADA, Dinesh, U. , LI, Hao , XIA, Zhi-Qiang , VO, Nha, Huu , BOHNERT, Gary , CHEN, Shoujun , WU, Yaming
发明人： BORELLA, Christopher , FOLEY, Kevin , SUN, Lijun , CHIMMANAMADA, Dinesh, U. , LI, Hao , XIA, Zhi-Qiang , VO, Nha, Huu , BOHNERT, Gary , CHEN, Shoujun , WU, Yaming
CPC分类号： C07D215/38 , C07D215/20 , C07D215/24 , C07D215/54 , C07D219/06 , C07D221/20 , C07D401/04 , C07D401/06 , C07D405/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D471/04 , C07D491/04
摘要： This invention relates to substituted 5,6,7,8-tetrahydroquinoline compounds, substituted dihydropyridine compounds, and substituted tricyclic compounds. The invention also relates to methods of preventing or treating metabolic disorders, such as diabetes mellitus, and conditions and complications associated with diabetes mellitus, comprising administering to a subject in need thereof a compound of the invention or a composition comprising such a compound. The invention further relates to methods of treating inflammatory bowel disease, comprising administering to a subject in need thereof a compound of the invention or a composition comprising such a compound.
摘要翻译：本发明涉及取代的5,6,7,8-四氢喹啉化合物，取代的二氢吡啶化合物和取代的三环化合物。本发明还涉及预防或治疗诸如糖尿病的代谢疾病以及与糖尿病相关的病症和并发症的方法，其包括向有需要的受试者施用本发明的化合物或包含这种化合物的组合物。本发明进一步涉及治疗炎症性肠病的方法，包括向有需要的受试者施用本发明化合物或包含这种化合物的组合物。

4. 发明申请

WO2010065512A2 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
标题翻译：治疗增殖性疾病的化合物
公开(公告)号：WO2010065512A2
公开(公告)日：2010-06-10
申请号：PCT/US2009/066211
申请日：2009-12-01
申请人： SYNTA PHARMACEUTICALS CORP. , JIANG, Jun , KOWALCZYK-PRZEWLOKA, Teresa , SCHWEIZER, Stefan M. , XIA, Zhi-Qiang , CHEN, Shoujun , BORELLA, Christopher , SUN, Lijun
发明人： JIANG, Jun , KOWALCZYK-PRZEWLOKA, Teresa , SCHWEIZER, Stefan M. , XIA, Zhi-Qiang , CHEN, Shoujun , BORELLA, Christopher , SUN, Lijun
IPC分类号： C07C327/56 , C07D213/86 , C07D263/34 , C07D277/56 , C07D295/16 , C07D317/62 , A61K31/175 , A61K31/36 , A61K31/40 , A61K31/421 , A61K31/426 , A61K31/4402 , A61P35/00
CPC分类号： C07D295/195 , C07C327/56 , C07C333/12 , C07C335/40 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/04 , C07D211/72 , C07D213/86 , C07D213/87 , C07D241/24 , C07D277/56 , C07D295/155 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/68
摘要： The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
摘要翻译：本发明涉及由结构式（I）表示的化合物，或其药学上可接受的盐或过渡金属螯合物，其配位体或络合物或去质子化的过渡金属螯合物，配位体或络合物化合物的形式。还包括这些化合物的药物组合物和使用方法。

5. 发明申请

WO2008033494A3 PURIFICATION OF BIS(THIOHYDRAZIDE AMIDES) 审中-公开
公开(公告)号：WO2008033494A3
公开(公告)日：2008-03-20
申请号：PCT/US2007/019987
申请日：2007-09-14
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , XIA, Zhi-Qiang , KOSTIK, Elena , KOYA, Keizo , SUN, Lijun
发明人： CHEN, Shoujun , XIA, Zhi-Qiang , KOSTIK, Elena , KOYA, Keizo , SUN, Lijun
IPC分类号： C07C327/56
摘要： Disclosed herein is a method for the purification of bis(thiohydrazide amide) compounds of formula I, wherein R 1 , R 2 , R 3 , R 4 , R 7 , R 8 , Z and Y are defined herein, by dissolving the compound in a solvent selected from the group consisting of tetrahydrofuran-acetone, tetrahydrofuran-acetonitrile, tetrahydrofuran, acetone, acetonitrile, tetrahydrofuran-ethanol and acetone-ethanol and precipitating the compound with water.

6. 发明申请

WO2006009940A1 BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMIDE）用于治疗癌症的药物
公开(公告)号：WO2006009940A1
公开(公告)日：2006-01-26
申请号：PCT/US2005/021642
申请日：2005-06-20
申请人： SYNTA PHARMACEUTICALS CORP. , KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
发明人： KOSTIK, Elena , VAGHEFI, Farid , LIANG, Guiqing , KOYA, Keizo , SUN, Lijun , TATSUTA, Noriaki , CHEN, Shoujun , INOUE, Takayo , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07D305/14 , C07C327/56 , C07C2601/02
摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I) Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R 1 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is -O or -S. M + is a pharmaceutically acceptable monovalent cation and M 2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.
摘要翻译：公开了由结构式（I）表示的双（硫代酰肼酰胺）二盐，Y是共价键或取代或未取代的直链烃基。 [R <子

7. 发明申请

WO2006124736A2 SYNTHESIS OF BIS(THIO-HYDRAZIDE AMIDE) SALTS 审中-公开
标题翻译： BIS（THIO-HYDRAZIDE AMATE）SALTS的合成
公开(公告)号：WO2006124736A2
公开(公告)日：2006-11-23
申请号：PCT/US2006/018653
申请日：2006-05-11
申请人： SYNTA PHARMACEUTICALS CORP. , CHEN, Shoujun , XIA, Zhi-Qiang
发明人： CHEN, Shoujun , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： A method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide), an organic solvent and a base to form a bis(thio-hydrazide amide) solution; and combining the solution and methyl tert -butyl ether, thereby precipitating a disalt of the bis(thio-hydrazide amide). In some embodiments, a method of preparing a bis(thio-hydrazide amide) disalt includes the steps of combining a neutral bis(thio-hydrazide amide) and an organic solvent selected from methanol, ethanol, acetone, and methyl ethyl ketone to make a mixture; adding at least two equivalents of a base selected from sodium hydroxide, potassium hydroxide, sodium methoxide, potassium methoxide, sodium ethoxide and potassium ethoxide to the mixture, thereby forming a solution; and combining the solution and methyl tert -bvtyl ether to precipitate the disalt of the bis(thio-hydrazide amide). The disclosed methods do not require lyophylization and the solvents used in the process can be more readily removed to low levels consistent with pharmaceutically acceptable preparation.
摘要翻译：制备双（硫代 - 酰肼酰胺）二盐的方法包括将中性双（硫代酰肼）酰胺，有机溶剂和碱组合以形成双（硫代 - 酰肼酰胺）溶液的步骤; 并将该溶液与甲基叔丁基醚混合，从而沉淀出双（硫代 - 酰肼）酰胺的残留物。在一些实施方案中，制备双（硫代 - 酰肼酰胺）二盐的方法包括将中性双（硫代酰肼）酰胺和选自甲醇，乙醇，丙酮和甲基乙基酮的有机溶剂合并以制备混合物; 向混合物中加入至少两当量的选自氢氧化钠，氢氧化钾，甲醇钠，甲醇钾，乙醇钠和乙醇钾的碱，从而形成溶液; 并将该溶液与甲基叔丁基醚混合以沉淀双（硫代 - 酰肼）酰胺的混合物。所公开的方法不需要冻干，并且可以更容易地将该方法中使用的溶剂除去至与药学上可接受的制剂一致的低水平。

8. 发明申请

WO2004024727A2 SYNTHESIS OF INDOLIZINES 审中-公开
标题翻译：吲哚啉的合成
公开(公告)号：WO2004024727A2
公开(公告)日：2004-03-25
申请号：PCT/US2003/028252
申请日：2003-09-10
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , KOYA, Keizo , XIA, Zhi-Qiang , PRZEWLOKA, Teresa , ZHANG, Shijie , ONO, Mitsunori
发明人： SUN, Lijun , KOYA, Keizo , XIA, Zhi-Qiang , PRZEWLOKA, Teresa , ZHANG, Shijie , ONO, Mitsunori
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： Disclosed are methods of preparing substituted indolizines represented by the following formula: comprising reacting a substrate represented by the following formula: with either the cyclization reagent of the following formula: or, a reagent prepared by reacting the compound represented the formula below with an alkylating agent: The variables in the above formulas are defined herein.
摘要翻译：公开了制备由下式表示的取代的中氮茚的方法：包括使由下式表示的底物与下式的环化试剂反应：或通过使下式表示的化合物与烷基化剂反应制备的试剂：上述公式中的变量在此定义。

9. 发明申请

WO2005025507A2 DIHYDROPYRIDINE COMPOUNDS FOR TREATING OR PREVENTING METABOLIC DISORDERS 审中-公开
标题翻译：用于治疗或预防代谢性疾病的二氢吡啶化合物
公开(公告)号：WO2005025507A2
公开(公告)日：2005-03-24
申请号：PCT/US2004/029636
申请日：2004-09-10
申请人： SYNTA PHAMACEUTICALS CORP. , ONO, Mitsunori , WADA, Yumiko , SUN, Lijun , CHEN, Shoujun , PRZEWLOKA, Teresa , ZHANG, Shijie , BORELLA, Christopher , KOYA, Keizo , FOLEY, Kevin , XIA, Zhi-Qiang , LI, Hao , ZHOU, Dan
发明人： ONO, Mitsunori , WADA, Yumiko , SUN, Lijun , CHEN, Shoujun , PRZEWLOKA, Teresa , ZHANG, Shijie , BORELLA, Christopher , KOYA, Keizo , FOLEY, Kevin , XIA, Zhi-Qiang , LI, Hao , ZHOU, Dan
IPC分类号： A61K
CPC分类号： C04B35/632 , C07D215/54 , C07D221/20 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D491/04
摘要： This invention relates to dihydropyridine compounds of formula: (I) or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein A 2 , R 12, R 13 , R 14 , R 15 , R 16 , R 17 , R 18 , R 19 , R 20 , R 21 , R 22 , and m are defined herein, and compositions comprising such compounds. The invention also relates to methods of preventing or treating metabolic disorders, such as diabetes mellitus, and conditions and complications associated with diabetes mellitus, comprising administering to a subject in need thereof a compound of formula (I) or a composition comprising such a compound. The invention further relates to kits comprising a compound of formula (I).
摘要翻译：本发明涉及式（I）的二氢吡啶化合物或其药学上可接受的盐，溶剂合物，包合物或前药，其中A 2，R 12， R 13，R 14，R 15，R 16，R 17，R 16， R 18，R 19，R 20，R 21，R 22，R 21，R 22，本文定义了m和包含这些化合物的组合物。本发明还涉及预防或治疗代谢病症例如糖尿病以及与糖尿病有关的病症和并发症的方法，其包括向有需要的受试者给药式（I）的化合物或包含该化合物的组合物。本发明进一步涉及包含式（I）化合物的试剂盒。

10. 发明申请

WO2003006428A1 TAXOL ENHANCER COMPOUNDS 审中-公开
标题翻译： TAXOL增强剂化合物
公开(公告)号：WO2003006428A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/021714
申请日：2002-07-10
申请人： SBR PHARMACEUTICALS CORP. , KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
发明人： KOYA, Keizo , SUN, Lijun , CHEN, Shoujun , TATSUTA, Noriaki , WU, Yaming , ONO, Mitsunori , XIA, Zhi-Qiang
IPC分类号： C07C327/56
CPC分类号： C07D307/68 , A45D2008/006 , A61K31/337 , A61K31/505 , A61K31/53 , A61K31/5377 , A61K47/58 , C07C327/56 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D209/44 , C07D213/83 , C07D261/18 , C07D333/38 , C07D333/68
摘要： One embodiment of the present invention is a compound represented by Structural Formula (I) wherein Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R 7 R 8 )-. R 1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R 2 -R 4 are independently -H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R 1 and R 3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R 2 and R 4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R 5 -R 6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R 7 and R 8 are each independently -H, an aliphatic or substituted aliphatic group, or R 7 is -H and R 8 is a substituted or unsubstituted aryl group, or, R 7 and R 8 , taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =0 or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.
摘要翻译：本发明的一个实施方案是由结构式（I）表示的化合物，其中Y是取代或未取代的直链烃基的共价键。此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。优选Y为共价键或-C（R 7 R 8） - 。 R1是脂肪族基团，取代脂肪族基团，非芳香族杂环基团或取代的非芳香族杂环基团，R2-R4独立地是-H，脂肪族基团，取代的脂肪族基团，非芳香族的杂环基团，取代的非芳香族杂环基团，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4与碳和氮原子一起形成与芳环稠合的非芳族杂环。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基。 Z = 0或= S。还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

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