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1. 发明申请

WO0187846A3 TRICYCLIC PYRAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的三聚吡唑衍生物
公开(公告)号：WO0187846A3
公开(公告)日：2002-03-21
申请号：PCT/US0116153
申请日：2001-05-17
申请人： KNOLL GMBH , DOYLE KEVIN J , RAFFERTY PAUL , STEELE ROBERT W , WILKINS DAVID J , ARNOLD LEE D , HOCKLEY MICHAEL , ERICSSON ANNA M , IWASAKI NOBUHIKO , OGAWA NOBUO
发明人： DOYLE KEVIN J , RAFFERTY PAUL , STEELE ROBERT W , WILKINS DAVID J , ARNOLD LEE D , HOCKLEY MICHAEL , ERICSSON ANNA M , IWASAKI NOBUHIKO , OGAWA NOBUO
IPC分类号： A61K31/416 , A61K31/4162 , A61K31/4178 , A61K31/4196 , A61K31/427 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/69 , A61P7/00 , A61P7/02 , A61P7/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/00 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P43/00 , C07D231/54 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D451/02 , C07D451/04 , C07D491/04 , C07D491/048 , C07D495/04
CPC分类号： C07D401/04 , C07D231/54 , C07D401/06 , C07D401/12 , C07D403/10 , C07D403/12 , C07D409/04 , C07D409/14 , C07D417/12 , C07D451/04 , C07D491/04 , C07D495/04
摘要： This invention relates to compounds of formula I which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
摘要翻译：本发明涉及作为蛋白激酶活性抑制剂的式I化合物，其中有些是新化合物，含有这些吡唑的药物组合物和制备这些吡唑的方法。

2. 发明申请

WO0027822A3 TRICYCLIC PYRAZOLE DERIVATIVES 审中-公开
标题翻译：三聚吡唑衍生物
公开(公告)号：WO0027822A3
公开(公告)日：2000-08-10
申请号：PCT/US9926105
申请日：1999-11-04
申请人： BASF AG , DOYLE KEVIN J , RAFFERTY PAUL , STEELE ROBERT W , WILKINS DAVID J , HOCKLEY MICHAEL , ARNOLD LEE D , ERICSSON ANNA M
发明人： DOYLE KEVIN J , RAFFERTY PAUL , STEELE ROBERT W , WILKINS DAVID J , HOCKLEY MICHAEL , ARNOLD LEE D , ERICSSON ANNA M
IPC分类号： A61K31/416 , A61K31/4162 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61P1/04 , A61P1/16 , A61P5/14 , A61P7/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P15/08 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P27/00 , A61P27/06 , A61P35/00 , A61P37/00 , A61P43/00 , C07D231/54 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D413/04 , C07D417/12 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/53 , A61P29/00
CPC分类号： C07D403/12 , C07D231/54 , C07D401/04 , C07D401/12 , C07D409/04 , C07D417/12 , C07D491/04 , C07D495/04
摘要： This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
摘要翻译：本发明涉及具有4,5（3,4） - 双环融合的某些3-芳基或3-杂芳基吡唑与蛋白激酶活性的抑制剂，其中一些是新化合物，含有这些吡唑的药物组合物和方法用于制备这些吡唑。

3. 发明申请

WO0119829A2 PYRAZOLOPYRIMIDINES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗剂的吡唑并嘧啶
公开(公告)号：WO0119829A2
公开(公告)日：2001-03-22
申请号：PCT/US0025468
申请日：2000-09-15
申请人： BASF AG , HIRST GAVIN C , CALDERWOOD DAVID , WISHART NEIL , RAFFERTY PAUL , RITTER KURT , ARNOLD LEE D , FRIEDMAN MICHAEL M
发明人： HIRST GAVIN C , CALDERWOOD DAVID , WISHART NEIL , RAFFERTY PAUL , RITTER KURT , ARNOLD LEE D , FRIEDMAN MICHAEL M
IPC分类号： A61K31/519 , A61K31/5377 , A61K38/22 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/12 , A61P15/16 , A61P17/02 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/22 , A61P33/02 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D487/04 , C07F9/6561
CPC分类号： C07D487/04 , C07F9/6561
摘要： The present invention provides compounds of Formula (I), including pharmaceutically acceptable salts and/or prodrugs thereof, where G, Ra, R2, R3 are defined as described herein.
摘要翻译：本发明提供式（I）化合物，包括其药学上可接受的盐和/或前药，其中G，R a，R 2，R 3如本文所述定义。

4. 发明申请

WO0075139A3 BENZOTHIAZINONE AND BENZOXAZINONE COMPOUNDS 审中-公开
标题翻译：苯并噻嗪酮和苯甲酸锌化合物
公开(公告)号：WO0075139A3
公开(公告)日：2001-03-29
申请号：PCT/US0015324
申请日：2000-06-02
申请人： BASF AG , RAFFERTY PAUL , CALDERWOOD DAVID , ARNOLD LEE D , GONZALEZ PASCUAL BEATRIZ , ORTEGO MATINEZ JOSE L , PEREZ DE VEGA MARIA J , FERNANDEZ ISABEL F
发明人： RAFFERTY PAUL , CALDERWOOD DAVID , ARNOLD LEE D , GONZALEZ PASCUAL BEATRIZ , ORTEGO MATINEZ JOSE L , PEREZ DE VEGA MARIA J , FERNANDEZ ISABEL F
IPC分类号： C07D265/36 , A61K31/42 , A61K31/425 , A61K31/437 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61P1/00 , A61P3/10 , A61P5/14 , A61P9/00 , A61P9/10 , A61P11/16 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D20060101 , C07D279/16 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/00 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
CPC分类号： C07D417/06 , C07D265/36 , C07D413/06 , C07D471/04
摘要： Q is - N=or CR ; X is S, O or NOR ; Y is-O-, -S-, -SO- or -SO2-; R and R are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl group R is H or a substituent; R is H, or -C(O)R ; R is a substituted or unsubstituted aliphatic or aromatic group; n is an integer from 0 to 1. Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.
摘要翻译： Q是-N =或CR <2>; X是S，O或NOR 3; Y是-O - ， - S - ， - SO-或-SO 2 - ; R和R 1各自独立地为H，取代或未取代的脂族，芳族，杂芳族或芳烷基R 2是H或取代基; R 3是H或-C（O）R 4; R 4是取代或未取代的脂族或芳族基团; n是0至1的整数。具有结构式（I）的化合物及其生理上可接受的盐是丝氨酸/苏氨酸和酪氨酸激酶活性的抑制剂。几种酪氨酸激酶（其活性被这些化合物抑制）参与血管发生过程。因此，这些化合物可以改善其中血管生成或内皮细胞过度增殖是一个因素的疾病状态。这些化合物可用于治疗癌症和过度增殖性疾病。

5. 发明申请

WO2007084667A3 FUSED HETEROBICYCLIC KINASE INHIBITORS 审中-公开
标题翻译：融合的杂环类激酶抑制剂
公开(公告)号：WO2007084667A3
公开(公告)日：2007-12-06
申请号：PCT/US2007001439
申请日：2007-01-18
申请人： OSI PHARMACEUTICAL INC , ARNOLD LEE D , CHEN XIN , DONG HANPING , GARTON ANDREW , MULVIHILL MARK JOSEPH , SMITH COLIN PETER SAMBROOK , THOMAS GERARD HUGH , KRULLE THOMAS MARTIN , WANG JING
发明人： ARNOLD LEE D , CHEN XIN , DONG HANPING , GARTON ANDREW , MULVIHILL MARK JOSEPH , SMITH COLIN PETER SAMBROOK , THOMAS GERARD HUGH , KRULLE THOMAS MARTIN , WANG JING
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中X 1，X 2，X 3，X 4， X SUB 5，SUB 6，SUB 7，SUB 1和SUP 1 本文定义为抑制激酶，并可用于治疗和/或预防过度增殖性疾病如癌症。这些化合物还可用于治疗炎症，变态反应，哮喘，疾病和免疫系统疾病和病症，神经系统疾病和病症，心血管疾病，眼睛疾病和病症，皮肤病，骨质疏松症，糖尿病，多发性硬化症和感染。

6. 发明申请

WO2005074603A2 AMINOBENZOXAZOLES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：氨苄青霉素作为治疗剂
公开(公告)号：WO2005074603A2
公开(公告)日：2005-08-18
申请号：PCT/US2005003196
申请日：2005-02-03
申请人： ABBOTT LAB , WISHART NEIL , FRIEDMAN MICHAEL , ARNOLD LEE D , YANG BRYANT , FIX-STENZEL SHANNON R , ERICSSON ANNA , MICHAELIDES MICHAEL R , QIAN XIAO-DONG , HOLMES JAMES H , STEINMAN DOUGLAS H , TIAN ZHENGPING , WITTENBERGER STEVEN J
发明人： WISHART NEIL , FRIEDMAN MICHAEL , ARNOLD LEE D , YANG BRYANT , FIX-STENZEL SHANNON R , ERICSSON ANNA , MICHAELIDES MICHAEL R , QIAN XIAO-DONG , HOLMES JAMES H , STEINMAN DOUGLAS H , TIAN ZHENGPING , WITTENBERGER STEVEN J
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A compound of Formula (I), wherein the substituents are as defined herein, which are useful as kinase inhibitors.
摘要翻译：式（I）的化合物，其中取代基如本文所定义，其可用作激酶抑制剂。

7. 发明申请

WO2007075554A2 COMBINED TREATMENT WITH AND COMPOSITION OF 6,6-BICYCLIC RING SUBSTITUTED HETEROBICYCLIC PROTEIN KINASE INHIBITOR AND ANTI-CANCER AGENTS 审中-公开
标题翻译：联合治疗6,6-双环环取代的异环蛋白激酶抑制剂和抗癌剂的组合
公开(公告)号：WO2007075554A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048222
申请日：2006-12-18
申请人： OSI PHARM INC , JI QUN-SHENG , ARNOLD LEE D , MULVIHILL MARK JOSEPH
发明人： JI QUN-SHENG , ARNOLD LEE D , MULVIHILL MARK JOSEPH
IPC分类号： A61K45/06 , A61K31/4985 , A61K31/519 , A61K31/53 , A61P35/00 , A61P35/04
CPC分类号： A61K45/06 , A61K31/4985 , A61K31/519 , A61K31/53 , A61K2300/00
摘要： The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an EGFR kinase inhibitor and an IGFlR inhibitor compound of Formula I combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also encompasses a pharmaceutical composition that is comprised of an EGFR kinase inhibitor and IGFlR inhibitor compound of Formula I combination with a pharmaceutically acceptable carrier. The IGFlR inhibitor is represented by Formula I. wherein X 1 X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein.
摘要翻译：本发明提供了一种用于治疗患者的肿瘤或肿瘤转移的方法，其包括向所述患者同时或依次施用治疗有效量的EGFR激酶抑制剂和式I化合物的IGF1R抑制剂化合物，其具有或不具有另外的试剂或治疗，如其他抗癌药物或放射治疗。本发明还包括由EGFR激酶抑制剂和式I的IGF1R抑制剂化合物与药学上可接受的载体组合的药物组合物。 IGF1R抑制剂由式I表示。其中X 1，X 2，X 3，X 4，X X 6，X 6，X 7，R 1和Q 1都是本文定义。

8. 发明申请

WO0172778A2 METHOD OF IDENTIFYING INHIBITORS OF TIE-2 审中-公开
标题翻译：识别TIE-2抑制剂的方法
公开(公告)号：WO0172778A2
公开(公告)日：2001-10-04
申请号：PCT/US0108853
申请日：2001-03-20
申请人： BASF AG , BUMP NANCY J , ARNOLD LEE D , DIXON RICHARD W , HOEFFKEN HANS WOLFGANG , ALLEN KAREN , BELLAMACINA CORNELIA
发明人： BUMP NANCY J , ARNOLD LEE D , DIXON RICHARD W , HOEFFKEN HANS WOLFGANG , ALLEN KAREN , BELLAMACINA CORNELIA
IPC分类号： G01N33/48 , A61K38/00 , A61K45/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P43/00 , C07K14/71 , C12N9/12 , C12N9/99 , C12N15/09 , G01N33/15 , G01N33/50 , G01N33/68 , C07K14/00
CPC分类号： C07K14/71 , A61K38/00 , C07K2299/00
摘要： The present invention relates to polypeptides which comprise the ligand binding domain of Tie-2, crystalline forms of these polypeptides and the use of these crystalline forms to determine the three dimensional structure of the catalytic domain of Tie-2. The invention also relates to the use of the three dimensional structure of the Tie-2 catalytic domain both alone, or in complex with inhibitors, in methods of designing and/or identifying potential inhibitors of Tie-2 activity, for example, compounds which inhibit the binding of a native substrate to the Tie-2 catalytic domain.
摘要翻译：本发明涉及包含Tie-2的配体结合结构域，这些多肽的结晶形式以及这些结晶形式用于确定Tie-2催化结构域的三维结构的多肽。本发明还涉及在设计和/或鉴定Tie-2活性的潜在抑制剂的方法中单独或与抑制剂复合的Tie-2催化结构域的三维结构的用途，例如抑制天然底物与Tie-2催化结构域的结合。

9. 发明申请

WO0027414A3 INHIBITION OF THE FORMATION OF VASCULAR HYPERPERMEABILITY 审中-公开
标题翻译：抑制血管超敏反应性的形成
公开(公告)号：WO0027414A3
公开(公告)日：2000-09-08
申请号：PCT/US9925903
申请日：1999-11-03
申请人： BASF AG , ARNOLD LEE D , BOUSQUET PETER F
发明人： ARNOLD LEE D , BOUSQUET PETER F
IPC分类号： A61K45/00 , A61K31/7105 , A61K38/00 , A61K38/17 , A61K38/19 , A61K39/395 , A61K48/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/10 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/06 , A61P11/16 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/02 , A61P19/00 , A61P27/00 , A61P27/06 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07K14/71 , A61K31/415
CPC分类号： C07K14/71 , A61K38/00 , A61K39/39533 , A61K45/06 , A61K2039/505 , C12N15/1137 , C12N15/1138 , C12N2310/11 , C12N2310/12 , A61K2300/00
摘要： Vascular hyperpermeability and the subsequent events such as macular edema, retinoblastoma, ocular ischemia, ocular inflammatory disease or infection, choroidal melanoma, edematous side-effects induced by iron chelation therapy, pulmonary edema, myocardial infarction, rheumatoid diseases, anaphylaxis, allergies, hypersensitive reactions, cerebral edema, brain tumor fluid-filled cysts, communicating hydrocephalus, carpal tunnel syndrome, organ damage resulting from a burn, irritation or infection, erythema multiforme, edematous macules and other disorders, brain tumors, tumor effusions, lung or breast carcinomas, ascites, pleural effusions, pericardial effusions, high altitude "sickness", radioanaphylaxis, radiodermatitis, glaucoma, conjunctivitis, choroidal melanoma, adult respiratory distress syndrome, asthma, bronchitis, ovarian hyperstimulation syndrome, polycystic ovary syndrome, menstrual swelling, menstrual cramps, stroke, head trauma, cerebral infarct or occlusion, hyotension, ulcerations, sprains, fractures, effusions associated with synovitis, diabetic complications, hyperviscosity syndrome, liver cirrhosis, microalbuminuria, proteinuria, oliguria, electrolyte imbalance, nephrotic syndrome, exudates, fibroses, keloid, can be inhibited by the administration of a compound that inhibits the enzyme activity of the VEGF tyrosine kinase receptor known as KDR tyrosine kinase. The preferred compound 4,5-dihydro-3-pyridin-4-yl-1(2)H-benzo[g]indazole selectively inhibits the function of KDR tyrosine kinase but do not block the activity of Flt-1 tyrosine kinase which is another VEGE tyrosine kinase receptor.
摘要翻译：血管渗透性过高以及随后的事件，如黄斑水肿，视网膜母细胞瘤，眼部缺血，眼部炎性疾病或感染，脉络膜黑色素瘤，铁螯合疗法引起的水肿副作用，肺水肿，心肌梗塞，类风湿性疾病，过敏反应，过敏，过敏反应，脑水肿，脑肿瘤充满液体的囊肿，交通性脑积水，腕管综合征，由烧伤，刺激或感染引起的器官损伤，多形性红斑，水肿性斑疹和其他疾病，脑肿瘤，肿瘤积液，肺癌或乳腺癌，腹水，胸膜积液，心包积液，高原“疾病”，放射性过敏反应，放射性皮炎，青光眼，结膜炎，脉络膜黑素瘤，成人呼吸窘迫综合征，哮喘，支气管炎，卵巢过度刺激综合征，多囊卵巢综合征，月经肿胀，月经来潮，外伤，脑梗塞或闭塞，高血压，可以通过施用抑制滑膜炎的化合物来抑制与滑膜炎，糖尿病并发症，高粘滞综合征，肝硬化，微量白蛋白尿，蛋白尿，少尿，电解质失衡，肾病综合征，渗出物，纤维化，瘢痕瘤相关的炎症，损伤，扭伤，骨折，被称为KDR酪氨酸激酶的VEGF酪氨酸激酶受体的酶活性。优选的化合物4,5-二氢-3-吡啶-4-基-1（2）H-苯并[g]吲唑选择性地抑制KDR酪氨酸激酶的功能，但不阻断Flt-1酪氨酸激酶的活性，另一种VEGE酪氨酸激酶受体。

10. 发明申请

WO2007061737A3 FUSED BICYCLIC mTOR INHIBITORS 审中-公开
标题翻译：融合的自行车mTOR抑制剂
公开(公告)号：WO2007061737A3
公开(公告)日：2007-12-06
申请号：PCT/US2006044461
申请日：2006-11-15
申请人： OSI PHARM INC , CHEN XIN , COATE HEATHER , CREW ANDREW-PHILIP , DONG HAN-QING , HONDA AYAKO , MULVIHILL MARK JOSEPH , TAVARES PAULA A R , WANG JING , WERNER DOUGLAS S , MULVIHILL KRISTEN MICHELLE , SIU KAM W , PANICKER BIJOY , BHARADWAJ APOORBA , ARNOLD LEE D , JIN MEIZHONG , VOLK BRIAN , WENG QINGHUA , BEARD JAMES DAVID
发明人： CHEN XIN , COATE HEATHER , CREW ANDREW-PHILIP , DONG HAN-QING , HONDA AYAKO , MULVIHILL MARK JOSEPH , TAVARES PAULA A R , WANG JING , WERNER DOUGLAS S , MULVIHILL KRISTEN MICHELLE , SIU KAM W , PANICKER BIJOY , BHARADWAJ APOORBA , ARNOLD LEE D , JIN MEIZHONG , VOLK BRIAN , WENG QINGHUA , BEARD JAMES DAVID
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00 , C07D519/00
CPC分类号： C07D487/04 , A61K31/5025 , C07D253/07 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐是mTOR的抑制剂并且可用于治疗癌症。

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