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1. 发明公开

EP0767789A2 A METHOD FOR THE PREPARATION OF A NOVEL C-RING PRECURSOR FOR TAXOIDS AND NOVEL INTERMEDIATES 失效
标题翻译：产生输出连接对于紫杉烷类化合物及其中间体的C环的方法
公开(公告)号：EP0767789A2
公开(公告)日：1997-04-16
申请号：EP95920915.0
申请日：1995-06-06
申请人： Xia, Zhi-Qiang , Karvinen, Esko , Koskinen, Ari
发明人： Xia, Zhi-Qiang , Karvinen, Esko , Koskinen, Ari
IPC分类号： C07D317 , C07D493
CPC分类号： C07D317/72 , C07D493/10
摘要： The present invention relates to a process for the preparation of a compound of formula (VIII) or (IX) useful as precursor for the C-ring in taxanes, wherein R' is a C1-C6-alkyl. The invention further relates to the novel compounds (VIII) and (IX) and to novel intermediates in said process.

2. 发明专利

AU2617695A A method for the preparation of a novel c-ring precursor for taxoids and novel intermediates 未知
公开(公告)号：AU2617695A
公开(公告)日：1996-01-25
申请号：AU2617695
申请日：1995-06-06
申请人： KARVINEN ESKO , KOSKINEN ARI , XIA ZHI QIANG
发明人： XIA ZHI-QIANG , KARVINEN ESKO , KOSKINEN ARI
IPC分类号： C07D317/72 , C07D493/10 , C07D305/14
摘要： The present invention relates to a process for the preparation of a compound of the formula (VIII) or (IX) useful as precursor for the C-ring in taxanes (VIII) (IX) wherein R' is a C1-C6-alkyl. The invention further relates to the novel compounds (VIII) and (IX) and to novel intermediates in said process.

3. 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。

4. 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.

5. 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

6. 发明申请

WO2004082606A8 FUSED PYRROLE COMPOUNDS 审中-公开
标题翻译：稠合吡咯化合物
公开(公告)号：WO2004082606A8
公开(公告)日：2005-03-03
申请号：PCT/US2004007469
申请日：2004-03-11
申请人： SYNTA PHARMACEUTICALS CORP , ONO MITSUNORI , SUN LIJUN , XIA ZHI QIANG , KOSTIK ELENA , KOYA KEIZO , WU YAMING , NAGAI MASAZUMI
发明人： ONO MITSUNORI , SUN LIJUN , XIA ZHI QIANG , KOSTIK ELENA , KOYA KEIZO , WU YAMING , NAGAI MASAZUMI
IPC分类号： A61K20060101 , A61K31/429 , A61K31/5025 , A61K31/519 , A61K31/53 , C07D455/02 , C07D487/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： This invention relates to fused pyrrole compounds of Formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein V1, V2, V3, V4, R1, R2, R3, W1 and W2 are as defined herein. The compounds of this invention may be used to prevent or treat cancer, inflammatory disorders, autoimmune diseases and other conditions involving PDE4 or elevated levels of cytokines. The invention also provides methods of using the compounds to treat or prevent such disorders and pharmaceutical compositions containing the compounds.
摘要翻译：本发明涉及式（I）的稠合吡咯化合物及其药学上可接受的盐和前药，其中V 1，V 2，V 3，V 4，R 1，R 2，R 3，W 1和W 2如本文所定义。本发明的化合物可用于预防或治疗癌症，炎性病症，自身免疫性疾病和其他涉及PDE4或细胞因子水平升高的病症。本发明还提供了使用这些化合物治疗或预防这些疾病的方法和含有这些化合物的药物组合物。

7. 发明申请

WO2008024302A8 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
标题翻译：用于治疗增生性疾病的化合物
公开(公告)号：WO2008024302A8
公开(公告)日：2008-05-08
申请号：PCT/US2007018362
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP , SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
发明人： SUN LIJUN , KOYA KEIZO , CHEN SHOUJUN , DEMKO ZACHARY , XIA ZHI-QIANG
IPC分类号： C07D213/86 , A61K31/16 , A61K31/165 , C07C243/24 , C07C327/00 , C07D207/416 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/30 , C07D333/36 , C07D333/38
CPC分类号： C07C327/56 , C07C243/24 , C07C255/56 , C07C255/58 , C07C337/02 , C07C337/06 , C07C2601/02 , C07C2601/14 , C07D207/34 , C07D213/81 , C07D213/86 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/38 , C07D333/36 , C07D333/38
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了使用本发明化合物治疗患有增殖性疾病如癌症的受试者的化合物和方法，以及用于治疗响应于Hsp70诱导和/或自然杀伤诱导的病症的方法。此外，公开了包含本发明化合物和药学上可接受的载体的药物组合物。

8. 发明申请

WO2008024302A3 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS 审中-公开
公开(公告)号：WO2008024302A3
公开(公告)日：2008-02-28
申请号：PCT/US2007/018362
申请日：2007-08-20
申请人： SYNTA PHARMACEUTICALS CORP. , SUN, Lijun , KOYA, Keizo , CHEN, Shoujun , DEMKO, Zachary , XIA, Zhi-qiang
发明人： SUN, Lijun , KOYA, Keizo , CHEN, Shoujun , DEMKO, Zachary , XIA, Zhi-qiang
IPC分类号： C07D213/86 , C07D231/08 , C07D237/04 , C07D277/50 , C07D303/48 , C07D307/66 , C07D307/68 , C07D309/30 , C07D333/36 , C07D333/38 , C07D207/416 , C07C243/24 , C07C327/00 , A61K31/16 , A61K31/165
摘要： Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.

9. 发明申请

WO2007089904A3 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：WO2007089904A3
公开(公告)日：2008-01-03
申请号：PCT/US2007002790
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： C07D213/44 , A61K31/44
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。

10. 发明申请

WO2006124736A3 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：WO2006124736A3
公开(公告)日：2007-03-29
申请号：PCT/US2006018653
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。

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