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1. 发明申请

US20100160371A1 INHIBITION OF P38 KINASE ACTIVITY BY ARYL UREAS 审中-公开
标题翻译： ARYL URAAS对P38激酶活性的抑制作用
公开(公告)号：US20100160371A1
公开(公告)日：2010-06-24
申请号：US12619913
申请日：2009-11-17
申请人： Gerald RANGES , William Scott , Michael Bombara , Deborah Rauner , Aniko Redman , Roger Smith , Holger Paulsen , David Gunn , Jinshan Chen , Joel Renick
发明人： Gerald RANGES , William Scott , Michael Bombara , Deborah Rauner , Aniko Redman , Roger Smith , Holger Paulsen , David Gunn , Jinshan Chen , Joel Renick
IPC分类号： A61K31/381 , A61K31/341 , A61K31/40 , A61K31/433 , A61K31/47 , A61K31/404 , A61P29/00 , A61P37/00 , A61P19/10 , A61P11/06
CPC分类号： A61K31/4709 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/433 , Y02A50/401 , Y02A50/411 , Y02A50/414
摘要： This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.
摘要翻译：本发明涉及一组芳基脲在治疗癌症以外的细胞因子介导的疾病和除了癌症以外的蛋白水解酶介导的疾病以及用于这种治疗的药物组合物中的用途。

2. 发明授权

US07435739B2 Substituted pyrrolopyrimidines useful in the treatment of cancer 失效
标题翻译：可用于治疗癌症的取代吡咯并嘧啶
公开(公告)号：US07435739B2
公开(公告)日：2008-10-14
申请号：US10989842
申请日：2004-11-16
申请人： Jinshan Chen , Matthew A. Marx , Susan D. LaGreca , Matthew D. Wessel
发明人： Jinshan Chen , Matthew A. Marx , Susan D. LaGreca , Matthew D. Wessel
IPC分类号： C07D487/04 , A61K31/519 , A61K31/664 , C07F9/24 , A61P35/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，前药或水合物，其中X，L，R 1，R 2，R 3，＆lt; / SUP＆gt;和R 4＆gt;如本文所定义。本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗哺乳动物中过度增殖性疾病的方法。

3. 发明申请

US20050119489A1 4-Sulfide/sulfoxide/sulfonyl-1h-pyrazolyl derivative compounds, for use in diseases associated with the 5-ht2c receptor 审中-公开
标题翻译： 4-硫化物/亚砜/磺酰基-1h-吡唑基衍生物化合物，用于与5-ht2c受体相关的疾病
公开(公告)号：US20050119489A1
公开(公告)日：2005-06-02
申请号：US10499789
申请日：2002-12-28
申请人： Gaetan Ladouceur , Emil Velthuisen , Soongyu Choi , Zhonghua Zhang , Yamin Wang , Jeremy Baryza , Philip Coish , Roger Smith , Jinshan Chen
发明人： Gaetan Ladouceur , Emil Velthuisen , Soongyu Choi , Zhonghua Zhang , Yamin Wang , Jeremy Baryza , Philip Coish , Roger Smith , Jinshan Chen
IPC分类号： A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P15/12 , A61P25/00 , A61P43/00 , C07D231/18 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
CPC分类号： C07D231/18 , C07D401/12 , C07D403/04 , C07D403/12 , C07D413/12
摘要： Disclosed are 4-sulfide/sulfoxide/sulfonyl-1H-pyrazolyl derivative compounds of formulas (I) or (II): wherein the variables n, R, R1, R2, R3, R3′, R4, R4′, R5 and R6 are as defined in the specification. The compounds are useful for the treatment or prevention of diseases and/or behaviors involving the 5-HT2C receptor.
摘要翻译：公开了式（I）或（II）的4-硫化物/亚砜/磺酰基-1H-吡唑基衍生物化合物：其中变量n，R，R 1，R 2， R 3，R 3'，R 4，R 4'，R 5， / SUB和R 6如说明书中所定义。该化合物可用于治疗或预防涉及5-HT 2C受体的疾病和/或行为。

4. 发明授权

US5968795A Biaryl acetylenes as inhibitors of matrix metalloproteases 失效
标题翻译：作为基质金属蛋白酶抑制剂的二芳基乙炔
公开(公告)号：US5968795A
公开(公告)日：1999-10-19
申请号：US856694
申请日：1997-05-15
申请人： Brian R. Dixon , Jinshan Chen
发明人： Brian R. Dixon , Jinshan Chen
IPC分类号： C07C59/84 , C07D209/48 , C12N9/99 , A01N37/10 , C07C63/00 , C12N9/50
CPC分类号： C07D209/48 , C07C59/84
摘要： Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## where R.sup.15 is selected from the group comprising: HOCH.sub.2, (n--Pr).sub.2 NCH.sub.2, CH.sub.3 CO.sub.2 CH.sub.2, EtOCO.sub.2 CH.sub.2, HO(CH.sub.2).sub.2, CH.sub.3 CO.sub.2 (CH.sub.2).sub.2, HO.sub.2 C(CH.sub.2).sub.2, OHC(CH.sub.2).sub.3, HO(CH.sub.2).sub.4, 3--HO--Ph, and PhCH.sub.2 OCH.sub.2 ; and R.sup.16 is ##STR2## These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.
摘要翻译：提出了基质金属蛋白酶抑制化合物，其药物组合物和使用这些化合物的疾病治疗方法。本发明的化合物具有以下通式：其中R 15选自HOCH 2，（n-Pr）2 NCH 2，CH 3 CO 2 CH 2，EtOCO 2 CH 2，HO（CH 2）2，CH 3 CO 2（CH 2）2，HO 2 C（CH 2）2， OHC（CH 2）3，HO（CH 2）4，3-HO-Ph和PhCH 2 OCH 2; R16是这些化合物可用于抑制基质金属蛋白酶，因此可用于抑制MMP的贡献，如骨关节炎，类风湿性关节炎，脓毒性关节炎，牙周病，角膜溃疡，蛋白尿，动脉瘤性主动脉疾病，疏水性表皮松解症，大疱性病变导致炎症反应，由MMP活性介导的骨质减少，颞下颌关节疾病，神经系统脱髓鞘疾病，创伤性关节损伤后的肿瘤转移或退行性软骨损失以及来自动脉粥样硬化斑块破裂的冠状动脉血栓形成。本发明还提供了用于治疗这些病症的药物组合物和方法。

5. 发明授权

US5932577A Substituted oxobutyric acids as matrix metalloprotease inhibitors 失效
标题翻译：取代的氧代丁酸作为基质金属蛋白酶抑制剂
公开(公告)号：US5932577A
公开(公告)日：1999-08-03
申请号：US857053
申请日：1997-05-15
申请人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
发明人： Brian R. Dixon , Jinshan Chen , Michael C. VanZandt , David R. Brittelli
IPC分类号： C07C59/90 , C07D209/48 , C07D253/08 , A61K31/53 , C07C65/32 , C07D251/00
CPC分类号： C07D209/48 , C07C59/90 , C07D253/08
摘要： The present invention provides pharmaceutical compositions and methods for treating certain conditions associated with matrix metalloproteases comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are either of the generalized formula: ##STR1## wherein y is 0, 2, or, 3, r is 0-6, Z is (CH.sub.2).sub.7 or (CH.sub.2).sub.e --C.sub.6 H.sub.4 --(CH.sub.2).sub.f, wherein e is 0-1 and f is 0-5, and R.sup.15 is --H, --Cl, --OMe or ##STR2## wherein n is 0-4, R.sup.17 is C.sub.2 H.sub.5, alkyl, benzyl, and R.sup.16 is ##STR3## wherein t is 0-2, x is 0-4, and R.sup.4 is one of the following: halide, alkyl of 1-6 carbons, OR, NR.sub.2, NO.sub.2 (R=H or alkyl of 1-6 carbons).
摘要翻译：本发明提供用于治疗与基质金属蛋白酶相关的某些病症的药物组合物和方法，其包括给予一定量的有效抑制至少一种基质金属蛋白酶活性的本发明化合物或组合物，从而达到预期的效果。本发明的化合物是以下通式：其中y是0,1或3，r是0-6，Z是（CH2）7或（CH2）e-C6H4-（CH2）f，其中 e为0-1，f为0-5，R15为-H，-Cl，-OMe或其中n为0-4，R17为C2H5，烷基，苄基，R16为其中t为0-2，x 是0-4，R4是以下之一：卤化物，1-6个碳的烷基，OR，NR2，NO2（R = H或1-6个碳原子的烷基）。

6. 发明授权

US07585869B2 Substituted heterocylces for the treatment of abnormal cell growth 失效
标题翻译：用于治疗异常细胞生长的取代杂环
公开(公告)号：US07585869B2
公开(公告)日：2009-09-08
申请号：US10849707
申请日：2004-05-20
申请人： Samit Kumar Bhattacharya , Jinshan Chen , Richard Damian Connell , John Charles Kath , Goss S. Kauffman , Blaise S. Lippa , Joel Morris
发明人： Samit Kumar Bhattacharya , Jinshan Chen , Richard Damian Connell , John Charles Kath , Goss S. Kauffman , Blaise S. Lippa , Joel Morris
IPC分类号： A61K31/517 , C07D239/94
CPC分类号： C07D401/12 , C07D239/94 , C07D405/14 , C07D471/04
摘要： The invention relates to compounds of formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R11, N, Z, A, m and p are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
摘要翻译：本发明涉及式1化合物及其药学上可接受的盐，前药和溶剂合物，其中R1，R3，R4，R11，N，Z，A，m和p如本文所定义。本发明还涉及通过施用式1的化合物和用于治疗含有式1化合物的这种病症的药物组合物来治疗哺乳动物异常细胞生长的方法。本发明还涉及制备式1化合物的方法。

7. 发明申请

US20050130994A1 Pyrrolopyre compounds useful in treatment of cancer 失效
标题翻译：用于治疗癌症的吡咯类化合物
公开(公告)号：US20050130994A1
公开(公告)日：2005-06-16
申请号：US10989842
申请日：2004-11-16
申请人： Jinshan Chen , Matthew Marx , Susan LaGreca , Matthew Wessel
发明人： Jinshan Chen , Matthew Marx , Susan LaGreca , Matthew Wessel
IPC分类号： A61K31/519 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，前药或水合物，其中X，L，R 1，R 2，R 3，＆lt; / SUP＆gt;和R 4＆gt;如本文所定义。本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗哺乳动物中过度增殖性疾病的方法。

8. 发明申请

US20050037999A1 Pyrrolopyrimidine derivatives 失效
标题翻译：吡咯并嘧啶衍生物
公开(公告)号：US20050037999A1
公开(公告)日：2005-02-17
申请号：US10732509
申请日：2003-12-10
申请人： Susan La Greca , Joel Arcari , Jinshan Chen , Matthew Marx , Matthew Wessel
发明人： Susan La Greca , Joel Arcari , Jinshan Chen , Matthew Marx , Matthew Wessel
IPC分类号： A61K31/505 , A61P35/00 , C07D487/04 , A61K31/675 , A61K31/519 , C07D487/02
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein Q, A, L, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，前药或水合物，其中Q，A，L，R 1，R 2和R 3如本文所定义。本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗哺乳动物中过度增殖性疾病的方法。

9. 发明授权

US06353006B1 Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents 有权
标题翻译：取代的2-芳基亚氨基杂环和含有它们的组合物，用作孕激素受体结合剂
公开(公告)号：US06353006B1
公开(公告)日：2002-03-05
申请号：US09453613
申请日：1999-12-03
申请人： Brian R. Dixon , Cedo M. Bagi , Catherine R. Brennan , David R. Brittelli , William H. Bullock , Jinshan Chen , William L. Collibee , Robert Dally , Jeffrey S. Johnson , Harold C. E. Kluender , William F. Lathrop , Peiying Liu , Carol Ann Mase , Anikó M. Redman , William J. Scott , Klaus Urbahns , Donald J. Wolanin
发明人： Brian R. Dixon , Cedo M. Bagi , Catherine R. Brennan , David R. Brittelli , William H. Bullock , Jinshan Chen , William L. Collibee , Robert Dally , Jeffrey S. Johnson , Harold C. E. Kluender , William F. Lathrop , Peiying Liu , Carol Ann Mase , Anikó M. Redman , William J. Scott , Klaus Urbahns , Donald J. Wolanin
IPC分类号： A01N4340
CPC分类号： C07D263/28 , C07D263/58 , C07D277/18 , C07D277/60 , C07D279/06 , C07D281/02 , C07D417/06 , C07D417/12 , C07D513/04 , C07D513/10
摘要： This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
摘要翻译：本发明涉及2-芳基亚氨基杂环，包括2-芳基亚氨基-1,3-噻唑烷，2-芳基亚氨基-2,3,4,5-四氢-1,3-噻嗪，2-芳基亚氨基-1,3-噻唑烷-2-酮， 4-芳基亚氨基-1,3-噻唑烷-5-酮和2-芳基亚氨基-1,3-恶唑烷，以及它们在调节孕酮受体介导的过程中的用途，以及用于这些疗法的药物组合物。

10. 发明授权

US07595325B2 Substituted pyrrolo[2,3-d]pyrimidine derivatives useful in cancer treatment 失效
标题翻译：用于癌症治疗的取代的吡咯并[2,3-d]嘧啶衍生物
公开(公告)号：US07595325B2
公开(公告)日：2009-09-29
申请号：US11140411
申请日：2005-05-27
申请人： Matthew A. Marx , Jinshan Chen , Susan LaGreca
发明人： Matthew A. Marx , Jinshan Chen , Susan LaGreca
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula 1 or a pharmaceutically acceptable salt, prodrug, solvate or hydrate thereof, wherein L, R1, R2, R3 and R4 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating abnormal cell growth, such as cancer in a mammal by administering the compounds of formula 1.
摘要翻译：本发明涉及式1化合物或其药学上可接受的盐，前药，溶剂合物或水合物，其中L，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物治疗哺乳动物异常细胞生长如癌症的方法。

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