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1. 发明专利

JP2012031198A Use of [3.2.0] heterocyclic compound and analog thereof for treatment of cancer, inflammation and infectious diseases 审中-公开
标题翻译： [3.2.0]杂环化合物及其类似物用于治疗癌症，炎症和感染性疾病的用途
公开(公告)号：JP2012031198A
公开(公告)日：2012-02-16
申请号：JP2011238014
申请日：2011-10-28
申请人： Nereus Pharmaceuticals Inc , ネレアスファーマシューティカルズインコーポレイテッド
发明人： PALLADINO MICHAEL , NEUTEBOOM SASKIA THEODORA CORNELIA , MACHERLA VENKATA RAMI REDDY , POTTS BARBARA CHRISTINE
IPC分类号： C07D491/044 , A61K31/407 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P31/04 , A61P31/10 , A61P33/00 , A61P33/02 , A61P33/06 , A61P35/00 , A61P35/02
CPC分类号： A61K31/407
摘要： PROBLEM TO BE SOLVED: To provide chemical compounds, including heterocyclic compounds and analogs thereof.SOLUTION: There are disclosed the compounds selected from a group comprising formulae I, II, III and IV to treat diseases in an animal; and a drug containing pharmaceutically acceptable salts thereof.
摘要翻译：待解决的问题：提供化合物，包括杂环化合物及其类似物。解决方案：公开了选自式I，II，III和IV组的化合物，以治疗动物的疾病; 和含有其药学上可接受的盐的药物。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2012211162A NOVEL INTERLEUKIN-1, TUMOR NECROSIS FACTOR-α MODULATOR, SYNTHESIS OF THE MODULATOR, AND METHOD OF USING THE MODULATOR 审中-公开
标题翻译：新一代白细胞介素-1，肿瘤坏死因子-α调节剂，调节剂的合成和使用调节剂的方法
公开(公告)号：JP2012211162A
公开(公告)日：2012-11-01
申请号：JP2012137825
申请日：2012-06-19
申请人： Nereus Pharmaceuticals Inc , Regents Of The Univ Of California , ザリージェンツオブザユニバーシティオブカリフォルニア , ネレアスファーマシューティカルズインコーポレーテッド
发明人： PALLADINO MICHAEL , THEODORAKIS EMMANUEL A
IPC分类号： A61P3/10 , C07C69/753 , A61K31/12 , A61K31/16 , A61K31/19 , A61K31/215 , A61P9/02 , A61P11/02 , A61P17/00 , A61P27/16 , A61P29/00 , A61P31/06 , A61P31/12 , A61P35/00 , A61P37/06 , C07C13/60 , C07C33/14 , C07C51/00 , C07C51/09 , C07C61/29 , C07C61/35 , C07C62/32 , C07C67/30 , C07C67/343 , C07C67/347 , C07C69/00
CPC分类号： C07C62/32 , A61K31/12 , A61K31/16 , A61K31/215 , C07B2200/05 , C07C61/29 , C07C61/35 , C07C69/753 , C07C2603/26
摘要： PROBLEM TO BE SOLVED: To provide compounds useful as Interleukin-1 and Tumor Necrosis Factor-α modulators, and thus useful in the treatment of various diseases.SOLUTION: Analogous compounds using an acanthoic acid of formula (I) has as a prototype the therapeutic effect.
摘要翻译：要解决的问题：提供可用作白介素-1和肿瘤坏死因子-α调节剂的化合物，因此可用于治疗各种疾病。解决方案：使用式（I）的棘皮酸的类似化合物具有治疗作用的原型。版权所有（C）2013，JPO＆INPIT

3. 发明专利

TW200744992A 介白素-1及腫瘤壞死因子-��調節劑,此等調節劑之合成及使用此等調節劑之方法 INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR-�� MODULATORS; SYNTHESES OF SUCH MODULATORS AND METHODS OF USING SUCH MODULATORS 审中-公开
简体标题：介白素-1及肿瘤坏死因子-��调节剂,此等调节剂之合成及使用此等调节剂之方法 INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR-�� MODULATORS; SYNTHESES OF SUCH MODULATORS AND METHODS OF USING SUCH MODULATORS
公开(公告)号：TW200744992A
公开(公告)日：2007-12-16
申请号：TW095126567
申请日：2006-07-20
申请人：納瑞斯製藥有限公司 NEREUS PHARMACEUTICALS, INC.
发明人：麥可A 派拉狄諾 PALLADINO, MICHAEL A. , 艾蒙A 瑟托雷金 THEODORAKIS, EMMANUEL A. , 維克雷米瑞迪馬夏拉 MACHERLA, VENKAT RAMI REDDY , 趙達興 CHAO, TA-HSIANG , 楊格松 SUH, YOUNG GER
IPC分类号： C07C , A61K , A61P
CPC分类号： C07C49/557 , C07C45/79 , C07C233/58 , C07C2601/14 , C07C2603/26 , C07C2603/86
摘要：本發明揭示具有式(II)、(IIA)及(IIB)之化學結構的化合物及其前藥酯及酸加成鹽,其可作為介白素-1及腫瘤壞死因子-��調節劑,因此可用於治療多種疾病,其中R基團係如申請專利範圍所定義。
095126567-p01.bmp
095126567-p02.bmp
095126567-p03.bmp
095126567-p04.bmp
095126567-p05.bmp
简体摘要：本发明揭示具有式(II)、(IIA)及(IIB)之化学结构的化合物及其前药酯及酸加成盐,其可作为介白素-1及肿瘤坏死因子-��调节剂,因此可用于治疗多种疾病,其中R基团系如申请专利范围所定义。 095126567-p01.bmp 095126567-p02.bmp 095126567-p03.bmp 095126567-p04.bmp 095126567-p05.bmp

4. 发明申请

WO2009134531A2 TOTAL SYNTHESIS OF SALINOSPORAMIDE A AND ANALOGS THEREOF 审中-公开
标题翻译：总的合成磺酰胺A及其类似物
公开(公告)号：WO2009134531A2
公开(公告)日：2009-11-05
申请号：PCT/US2009036376
申请日：2009-03-06
申请人： NEREUS PHARMACEUTICALS INC , TAOTAO LING , DANISHEFSKY SAMUEL
发明人： TAOTAO LING , DANISHEFSKY SAMUEL
IPC分类号： C07D487/14 , C07D487/04
CPC分类号： C07D487/14 , C07D487/04
摘要： The present application relates to certain compounds and to methods for the preparation of certain compounds that can be used in the fields of chemistry and medicine. Specifically, described herein are methods for the preparation of various compounds and intermediates, and the compounds and intermediates themselves. More specifically, described herein are methods for synthesizing Salinosporamide A and its analogs that includes forming a compound of formula (VIII).
摘要翻译：本申请涉及某些化合物和制备可用于化学和医学领域的某些化合物的方法。具体来说，本文描述了制备各种化合物和中间体以及化合物和中间体本身的方法。更具体地说，本文描述了合成Salinosporamide A及其类似物的方法，其包括形成式（VIII）化合物。

5. 发明申请

WO2008137780A3 USE OF [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR TREATING INFECTIOUS DISEASES 审中-公开
标题翻译： [3.2.0]杂环化合物及其类似物用于治疗感染性疾病的应用
公开(公告)号：WO2008137780A3
公开(公告)日：2009-03-26
申请号：PCT/US2008062553
申请日：2008-05-02
申请人： NEREUS PHARMACEUTICALS INC , PALLADINO MICHAEL
发明人： PALLADINO MICHAEL
IPC分类号： A61K31/133 , A61K31/407 , A61K31/4409 , A61K31/4965 , A61K31/65 , A61K31/7036 , A61K38/06 , A61K45/06 , A61P1/12 , A61P11/00 , A61P27/16 , A61P31/00 , A61P31/06 , A61P31/08 , A61P31/16
CPC分类号： A61K31/407 , A61K31/133 , A61K31/4409 , A61K31/4965 , A61K31/65 , A61K31/7036 , A61K38/06 , A61K45/06 , A61K2300/00
摘要： Disclosed is the use of [3.2.0] heterocyclic compounds, preferably salinosporamide A, for the manufacture of a medicament for treating infectious diseases in an animal. The animal is a mammal, preferably a human or a rodent.
摘要翻译：公开了使用[3.2.0]杂环化合物，优选盐酸胞苷酰胺A，用于制备用于治疗动物的感染性疾病的药物。动物是哺乳动物，优选人或啮齿动物。

6. 发明申请

WO2007015757A3 INTERLEUKIN-1 AND TUMOR NECROSIS FACTOR-A MODULATORS; SYNTHESES OF SUCH MODULATORS AND METHODS OF USING SUCH MODULATORS 审中-公开
标题翻译：白细胞介素-1和肿瘤坏死因子-A调节剂; 这种调制器的合成和使用这种调制器的方法
公开(公告)号：WO2007015757A3
公开(公告)日：2007-06-21
申请号：PCT/US2006027385
申请日：2006-07-14
申请人： NEREUS PHARMACEUTICALS INC , PALLADINO MICHAEL A , THEODORAKIS EMMANUEL A , MACHERLA VENKAT RAMI REDDY , CHAO TA-HSIANG , SUH YOUNG GER
发明人： PALLADINO MICHAEL A , THEODORAKIS EMMANUEL A , MACHERLA VENKAT RAMI REDDY , CHAO TA-HSIANG , SUH YOUNG GER
IPC分类号： C07C233/58 , A61K31/16 , A61P35/00 , C07C49/557
CPC分类号： C07C49/557 , C07C45/79 , C07C233/58 , C07C2601/14 , C07C2603/26 , C07C2603/86
摘要： Compounds are disclosed that have the chemical structure of Formula (II), (IIA) and (IIB) and their prodrug esters and acid-addition salts, and that are useful as Interleukin-1 and Tumor Necrosis Factor-a modulators, and thus are useful in the treatment of various diseases, wherein the R groups are defined in the claims.
摘要翻译：公开了具有式（II），（IIA）和（IIB）的化学结构及其前药酯和酸加成盐并且可用作白细胞介素-1和肿瘤坏死因子-α调节剂的化合物，因此是用于治疗各种疾病，其中R基团在权利要求中定义。

7. 发明申请

WO2006060809A3 METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF 审中-公开
公开(公告)号：WO2006060809A3
公开(公告)日：2006-06-08
申请号：PCT/US2005/044091
申请日：2005-12-02
申请人： NEREUS PHARMACEUTICALS, INC. , PALLADINO, Michael , POTTS, Barbara Christine , MACHERLA, Venkata Rami Reddy , NEUTEBOOM, Saskia Theodora Cornelia
发明人： PALLADINO, Michael , POTTS, Barbara Christine , MACHERLA, Venkata Rami Reddy , NEUTEBOOM, Saskia Theodora Cornelia
IPC分类号： A61K31/407 , A61P35/00
摘要： Disclosed are methods of treating cancer, inflammatory conditions, and/or infectious disease in an animal comprising: administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.

8. 发明申请

WO2005011699A1 PHENYLAHISTIN AND THE PHENYLAHISTIN ANALOGS, A NEW CLASS OF ANTI-TUMOR COMPOUNDS 审中-公开
标题翻译：苯丙胺和苯丙胺类似物，一类新型抗肿瘤化合物
公开(公告)号：WO2005011699A1
公开(公告)日：2005-02-10
申请号：PCT/US2004/024940
申请日：2004-07-29
申请人： NEREUS PHARMACEUTICALS, INC. , HAYASHI, Yoshio , PALLADINO, Michael A., Jr. , GRODBERG, Jennifer
发明人： HAYASHI, Yoshio , PALLADINO, Michael A., Jr. , GRODBERG, Jennifer
IPC分类号： A61K31/496
CPC分类号： C07D403/06 , A61K31/496
摘要： Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the structure of Formula (I).
摘要翻译：使用分离形式的化合物，其药学上可接受的盐和/或其前药酯治疗癌症的方法，以及用于分配，用于配制和给予化合物，盐和/或前药的方法酯作为抗肿瘤剂，其中化合物，盐或前药酯具有式（I）的结构。

9. 发明申请

WO2004054498A2 DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF AND THE SYNTHESIS OF DEHYDROPHENYLAHISTINS AND ANALOGS THEREOF 审中-公开
标题翻译：脱氢鞣质及其类似物的合成及脱氢鞣质及其类似物的合成
公开(公告)号：WO2004054498A2
公开(公告)日：2004-07-01
申请号：PCT/US2003/024232
申请日：2003-08-01
申请人： NEREUS PHARMACEUTICALS, INC.
发明人： HAYASHI, Yoshio , GRODBERG, Jennifer , PALLADINO, Michael
IPC分类号： A61K
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04
摘要： Compounds represented by structure (I) are disclosed, as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an intermediate compound; and reacting the intermediate compound with a second aldehyde to produce the class of compounds with the generic structure, where the first aldehyde and the second aldehydes are selected from the group consisting of an oxazolecarboxaldeyhyde, imidazolecarboxaldehyde, a benzaldehyde, imidazolecarboxaldehyde derivatives, and benzaldehyde derivatives, thereby forming the above compound wherein R 1 , R 1 ', R 1 '', R 2 , R 3 , R 4 , R 5 , and R 6 , X 1 and X 2 , Y, Z, Z 1 , Z 2 , Z 3 , and Z 4 may each be separately defined in a manner consistent with the accompanying description. Compositions and methods for treating cancer and fungal infection are also disclosed.
摘要翻译：公开了由结构（I）表示的化合物以及用于制备此类化合物的方法，其中所述方法包括使二酰基二酮哌嗪与第一醛反应以产生中间体化合物; 并使该中间体化合物与第二醛反应以制备具有通式结构的一类化合物，其中第一醛和第二醛选自恶唑甲醛，咪唑甲醛，苯甲醛，咪唑甲醛衍生物和苯甲醛衍生物，从而形成上述化合物，其中R 1，R 1，R 1，R 2，R 1，R 2，R 3， 3，R 4，R 5和R 6，X 1和 X 2，Y，Z，Z 1，Z 2，Z 3和Z 4 每个可以以与所附描述一致的方式分别定义。还公开了治疗癌症和真菌感染的组合物和方法。

10. 发明申请

WO2009140287A1 SALINOSPORAMIDE DERIVATIVES AS PROTEASOME INHIBITORS 审中-公开
标题翻译：作为缓释抑制剂的盐酸吡哆醛衍生物
公开(公告)号：WO2009140287A1
公开(公告)日：2009-11-19
申请号：PCT/US2009/043644
申请日：2009-05-12
申请人： NEREUS PHARMACEUTICALS, INC. , MACHERLA, Venkat, Rami Reddy , POTTS, Barbara, Christine , MANAM, Rama, Rao , MCARTHUR, Katherine, A. , CHAO, Ta-Hsiang , NEUTEBOOM, Saskia, Theodora Cornelia
发明人： MACHERLA, Venkat, Rami Reddy , POTTS, Barbara, Christine , MANAM, Rama, Rao , MCARTHUR, Katherine, A. , CHAO, Ta-Hsiang , NEUTEBOOM, Saskia, Theodora Cornelia
IPC分类号： C07D491/044 , A61K31/655 , A61P31/04 , A61K31/407 , A61P29/00 , A61P35/00
CPC分类号： C07D491/04
摘要： Disclosed herein are 6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione or heterobicyclic γ-lactam-β-lactone derivatives of formula (I) that include a sulfonate ester, ester or ether group in the substituent at the 4-position as proteasome inhibitors. These Salinosporamide derivatives of formula (I) can be included in pharmaceutical compositions and can be used for treating or ameliorating a disease or condition such as cancer, a microbial disease or inflammation.
摘要翻译：本文公开了式（I）的6-氧杂-2-氮杂双环[3.2.0]庚烷-3,7-二酮或杂双环β-内酰胺-β-内酯衍生物，其在取代基中包括磺酸酯，酯或醚基团在4位作为蛋白酶体抑制剂。式（I）的这些Salinosporamide衍生物可以包括在药物组合物中，并且可以用于治疗或改善诸如癌症，微生物疾病或炎症的疾病或病症。

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