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1. 发明授权

US08957074B2 Pyrrolopyrimidine compounds as inhibitors of CDK4/6 有权
标题翻译：吡咯并嘧啶化合物作为CDK4 / 6的抑制剂
公开(公告)号：US08957074B2
公开(公告)日：2015-02-17
申请号：US13579359
申请日：2011-02-17
申请人： Christopher Thomas Brain , Young Shin Cho , John William Giraldes , Bharat Lagu , Julian Roy Levell , Michael J. Luzzio , Lawrence Blas Perez , Yaping Wang , Fan Yang
发明人： Christopher Thomas Brain , Young Shin Cho , John William Giraldes , Bharat Lagu , Julian Roy Levell , Michael J. Luzzio , Lawrence Blas Perez , Yaping Wang , Fan Yang
IPC分类号： A61K31/50 , A61K31/501 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , A01N43/90 , A61K31/519 , C07D487/00 , C07D498/20 , C07D487/04 , C07D519/00 , C07D471/08 , C07D471/10 , C07D487/08 , C07D498/08
CPC分类号： C07D487/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D498/08 , C07D498/10 , C07D498/20 , C07D519/00
摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的式（I）吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌癌症和乳腺癌。本发明还涉及包含本发明化合物的药物组合物。本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

2. 发明授权

US5126351A Antitumor compounds 失效
标题翻译：抗菌化合物
公开(公告)号：US5126351A
公开(公告)日：1992-06-30
申请号：US645373
申请日：1991-01-24
申请人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson
发明人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson
IPC分类号： C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.4 substituents are hydrogen,intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

3. 发明授权

US07071217B2 Substituted oxindole derivatives as tyrosine kinase inhibitors 失效
标题翻译：取代的羟吲哚衍生物作为酪氨酸激酶抑制剂
公开(公告)号：US07071217B2
公开(公告)日：2006-07-04
申请号：US10362743
申请日：2001-08-23
申请人： Scott Howard Dickerson , Robert N Hunter , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael J. Luzzio , Edgar Raymond Wood, III
发明人： Scott Howard Dickerson , Robert N Hunter , Lee Frederick Kuyper , Karen Elizabeth Lackey , Michael J. Luzzio , Edgar Raymond Wood, III
IPC分类号： A61K31/44 , C07D401/02
CPC分类号： C07D401/12 , C07D209/34 , C07D209/40 , C07D417/12
摘要： The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
摘要翻译：本发明涉及结构（I）的羟吲哚衍生物，含有它们的组合物及其使用和制造方法。这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用，特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。这种疾病状态包括肿瘤生长，再狭窄，动脉粥样硬化，疼痛和血栓形成。特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出Trk家族蛋白酪氨酸激酶抑制，并且其可用于癌症治疗和慢性疼痛适应症。

4. 发明授权

US5223506A Cyclic antitumor compounds 失效
标题翻译：循环抗体化合物
公开(公告)号：US5223506A
公开(公告)日：1993-06-29
申请号：US710230
申请日：1991-06-04
申请人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
发明人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
IPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/14 , C07D491/147 , C07D491/153
CPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/14
摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.3 is hydrogen or methoxy and R.sup.4 is hydrogen;iii) when R.sup.2 is hydroxy, methoxy or amino, R.sup.3 is hydrogen, hydroxy or methoxy, and R.sup.4 is hydrogen;iv) when R.sup.4 is hydroxy or amino, R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is hydroxy or amino; and.v) when R.sup.1 is fluoro, chloro, iodo or amino, R.sup.2 is hydrogen, hydroxy or methoxy, R.sup.3 is hydrogen, hydroxy or methoxy and R.sup.4 is hydrogenand the use of these compounds as topoisomerase inhibitors and antitumor agents.

5. 发明授权

US5559235A Water soluble camptothecin derivatives 失效
标题翻译：水溶性喜树碱衍生物
公开(公告)号：US5559235A
公开(公告)日：1996-09-24
申请号：US258136
申请日：1994-06-10
申请人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , Peter L. Myers
发明人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , Peter L. Myers
IPC分类号： C07D317/66 , C07D319/18 , C07D491/22 , A61K31/47
CPC分类号： C07D319/18 , C07D317/66
摘要： The present invention relates to water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: 1) R.sup.1 and R.sup.2 represent independently, hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl;ii) R.sup.1 represents hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R.sup.2 represents --COR.sup.3,wherein:R.sup.3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; oriii) R.sup.1 and R.sup.2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) ##STR2## wherein: Y represents O, S, SO, SO.sub.2, CH.sub.2 or NR.sup.4wherein:R.sup.4 represents hydrogen, lower alkyl, perhalo lower alkyl, aryl, aryl substituted with one or more lower alkyl, lower alkoxy, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;--COR.sup.5,wherein:R.sup.5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.
摘要翻译：本发明涉及式（I）的水溶性喜树碱衍生物，其中：1）R1和R2独立地表示氢，低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基低级烯基，羟基低级烷基，低级烷氧基低级烷基; ii）R1表示氢，低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基，低级烯基，羟基低级烷基或低级烷氧基低级烷基，R2表示-COR3，其中：R3表示氢，低级烷基，全卤代低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基，低级烯基，羟基低级烷基，低级烷氧基或低级烷氧基低级烷基; 或（iii）R 1和R 2与连接氮一起形成式（IA）的饱和3至7个原子的杂环基（IA）其中：Y表示O，S，SO，SO 2，CH 2或NR 4，其中：R 4 代表氢，低级烷基，全卤代低级烷基，芳基，被一个或多个低级烷基，低级烷氧基，卤素，硝基，氨基，低级烷基氨基，全卤代低级烷基，羟基低级烷基，低级烷氧基低级烷基取代的芳基。 -COR 5，其中：R 5表示氢，低级烷基，全卤代低级烷基，低级烷氧基，芳基，被一个或多个低级烷基，全卤代低级烷基，羟基低级烷基，低级烷氧基低级烷基取代的芳基。其药学上可接受的盐; 其用于治疗肿瘤及其制备方法。

6. 发明申请

US20130150342A1 PYRROLOPYRIMIDINE COMPOUNDS AS INHIBITORS OF CDK4/6 有权
标题翻译：作为CDK4 / 6的抑制剂的吡咯烷酮化合物
公开(公告)号：US20130150342A1
公开(公告)日：2013-06-13
申请号：US13579359
申请日：2011-02-17
申请人： Christopher Thomas Brain , Young Shin Cho , John William Giraldes , Bharat Lagu , Julian Roy Levell , Michael J. Luzzio , Lawrence Blas Perez , Yaping Wang , Fan Yang
发明人： Christopher Thomas Brain , Young Shin Cho , John William Giraldes , Bharat Lagu , Julian Roy Levell , Michael J. Luzzio , Lawrence Blas Perez , Yaping Wang , Fan Yang
IPC分类号： C07D498/20 , C07D498/08 , C07D471/10 , C07D487/04 , C07D471/08 , C07D487/08
CPC分类号： C07D487/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D498/08 , C07D498/10 , C07D498/20 , C07D519/00
摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译：本发明涉及新的式（I）吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌癌症和乳腺癌。本发明还涉及包含本发明化合物的药物组合物。本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

7. 发明申请

US20090118316A1 Methods for Augmenting Bone 审中-公开
标题翻译：增强骨的方法
公开(公告)号：US20090118316A1
公开(公告)日：2009-05-07
申请号：US11570815
申请日：2005-06-10
申请人： Lisa M. Olson , Thomas A. Brown , Leonard Buckbinder , Angel Guzman-Perez , John C. Kath , Hua Zhu Ke , Michael J. Luzzio
发明人： Lisa M. Olson , Thomas A. Brown , Leonard Buckbinder , Angel Guzman-Perez , John C. Kath , Hua Zhu Ke , Michael J. Luzzio
IPC分类号： A61K31/506 , A61K31/405 , A61K31/40
CPC分类号： A61K31/506 , A61K31/00
摘要： The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.
摘要翻译：本发明涉及在具有骨质疏松症，骨折，非联合，假性关节炎，牙周病或其他骨代谢紊乱的受试者中用PYK2抑制剂刺激成骨细胞功能的方法。任选地，所述方法还包括施用第二治疗骨剂。本发明还涉及鉴定有效作为治疗性骨质的PYK2抑制剂的方法，其包括向成骨细胞样细胞施用测试试剂并确定是否刺激成骨细胞功能。任选地，识别方法还包括使测试试剂与PYK2接触并确定PYK2活性是否被抑制。

8. 发明授权

US07019147B1 Benzimidazole derivatives useful as antiproliferative agents 有权
标题翻译：可用作抗增殖剂的苯并咪唑衍生物
公开(公告)号：US07019147B1
公开(公告)日：2006-03-28
申请号：US10148335
申请日：2000-11-10
申请人： Wayne E. Barth , Michael J. Luzzio , Joseph P. Lyssikatos
发明人： Wayne E. Barth , Michael J. Luzzio , Joseph P. Lyssikatos
IPC分类号： C07D27/02 , C07D401/00 , C07D215/20 , A61K31/47 , A01N43/50
CPC分类号： C07D401/14 , C07D401/04 , C07D413/14 , C07D417/14 , C07D491/04 , C07D491/10
摘要： The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, 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）的化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 7，R 8， >，R 9，R 10和R 11如本文所定义。本发明还涉及通过施用式1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中异常细胞生长如癌症的方法。本发明还涉及制备式（1）化合物的方法。

9. 发明授权

US06995171B2 Bicyclic pyrimidine and pyrimidine derivatives useful as anticancer agents 失效
标题翻译：用作抗癌剂的双环嘧啶和嘧啶衍生物
公开(公告)号：US06995171B2
公开(公告)日：2006-02-07
申请号：US10479655
申请日：2002-06-20
申请人： Christopher Autry , Michael J. Luzzio , Matthew A. Marx
发明人： Christopher Autry , Michael J. Luzzio , Matthew A. Marx
IPC分类号： A61K31/4365 , C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to compounds of the formulas 1 and 2 and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R1 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1 and 2 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formulas 1 and 2.
摘要翻译：本发明涉及式1和化合物2化学式=“CHEM-US-00001”num =“000”

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