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1. 发明专利

JP2011079844A Receptor type kinase modulators and methods of use 审中-公开
标题翻译：受体型激酶调节剂及其使用方法
公开(公告)号：JP2011079844A
公开(公告)日：2011-04-21
申请号：JP2010259281
申请日：2010-11-19
申请人： Symphony Evolution Inc , シンフォニーエボルーション, インク.
发明人： RICE KENNETH D , ANAND NEEL KUMAR , BUSSENIUS JOERG , COSTANZA SIMONA , KENNEDY ABIGAIL R , KIM ANGIE I , PETO CSABA J , TSANG TSZE H , BLAZEY CHARLES M
IPC分类号： C07D239/94 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61K31/553 , A61K31/7064 , A61P1/04 , A61P9/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/06 , A61P43/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/04 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D493/20 , C07D495/04 , C07D498/04 , C07D513/04 , C07H17/02
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： PROBLEM TO BE SOLVED: To provide a compound having receptor kinase activity especially one for modulating ephrin and EGFR, and a method of treating the receptor kinase activity-mediated disorder utilizing the compound and drug composition. SOLUTION: This is a compound represented by chemical formula (I). The receptor kinase activity-mediated disorder includes, for example, cell growth of an abnormal level (that is tumor growth), programmed cell death (apotosis), migration and invasion of a cell and disorders having vascular formation relating to tumor growth as a part of characteristics. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供具有受体激酶活性的化合物，特别是用于调节ephrin和EGFR的化合物，以及利用该化合物和药物组合物治疗受体激酶活性介导的病症的方法。解决方案：这是由化学式（I）表示的化合物。受体激酶活性介导的病症包括例如细胞生长异常水平（即肿瘤生长），程序性细胞死亡（凋亡），细胞的迁移和侵袭以及与肿瘤生长相关的血管形成的疾病作为部分的特点。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2010265276A Human adam-10 inhibitor 审中-公开
标题翻译：人ADAM-10抑制剂
公开(公告)号：JP2010265276A
公开(公告)日：2010-11-25
申请号：JP2010142096
申请日：2010-06-22
申请人： Symphony Evolution Inc , シンフォニーエボルーション, インク.
发明人： BANNEN LYNNE CANNE , CO ERICK W , JAMMALAMADAKA VASU , NUSS JOHN M , KIM MOON HWAN , LE DONNA TRA , TSUHAKO AMY LEW , MAC MORRISON B , MAMO SHUMEYE , WEN ZHAOYANG , XU WEI , KHOURY RICHARD GEORGE
IPC分类号： C07C303/02 , A61K31/495 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P15/00 , A61P15/08 , A61P15/12 , A61P17/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07B61/00 , C07C309/87 , C07C309/88 , C07D213/70 , C07D241/04 , C07D401/06 , C07D401/12
CPC分类号： C07D241/04 , C07C309/87 , C07D213/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D413/06
摘要： PROBLEM TO BE SOLVED: To provide a compound useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1, and to provide an intermediate therefor. SOLUTION: The compound is useful for the in vitro study of the role of ADAM-10 (and inhibition thereof) in biological processes. There are included a pharmaceutical composition comprising one or a plurality of ADAM-10 inhibitors in combination with a pharmaceutically acceptable carrier, and a new sulfonyl halide exemplified by formula IX as the intermediate. The composition is useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, there is also included a method for treating forms of the cancer, arthritis, and diseases related to the angiogenesis in which the ADAM-10 plays a critical role. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供一种可用于抑制ADAM-10蛋白的化合物，具有对MMP-1的选择性，并提供其中间体。解决方案：该化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。包括一种药物组合物，其包含与药学上可接受的载体组合的一种或多种ADAM-10抑制剂和作为中间体的式IX示例的新的磺酰卤。该组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。相应地，还包括一种治疗癌症形式，关节炎和与其中ADAM-10起关键作用的血管发生相关的疾病的方法。版权所有（C）2011，JPO＆INPIT

3. 发明专利

TWI554502B 受體型激酶調節劑及治療多囊性腎疾病的方法有权
简体标题：受体型激酶调节剂及治疗多囊性肾疾病的方法
公开(公告)号：TWI554502B
公开(公告)日：2016-10-21
申请号：TW100130783
申请日：2011-08-26
申请人：交響演化公司 , SYMPHONY EVOLUTION, INC.
发明人：佛斯特菲利浦 , FROST, PHILIP , 廖威廉W N , LIAO, WILLIAM W. N. , 魯文斯基艾瑞克K , ROWINSKY, ERIC K.
IPC分类号： C07D239/94 , A61K31/517
CPC分类号： A61K31/517 , A61K9/08 , A61K9/20 , A61K9/2009 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054

4. 发明申请

WO2014028334A1 SELECTIVE MMP INHIBITORS 审中-公开
标题翻译：选择性MMP抑制剂
公开(公告)号：WO2014028334A1
公开(公告)日：2014-02-20
申请号：PCT/US2013/054368
申请日：2013-08-09
申请人： SYMPHONY EVOLUTION, INC. , UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION
发明人： WOOD, Alastair, J.J. , DICHEK, David, Anthony
IPC分类号： A61K31/18 , A61K31/166 , A61K31/496
CPC分类号： A61K31/166 , A61K31/18 , A61K31/496
摘要： Described are methods for treating diseases by use of agents that selectively inhibit human metalloproteinases (MMP), such as MMP-9 and MMP-2, while optionally sparing MMP-1. Prevention of atherosclerotic plaque development and rupture and/or carotid arterial plaque development and rupture, by MMP inhibition can reduce the adverse consequences of plaque development and rupture including thromboembolism, stroke, myocardial infarction and acute coronary syndromes.
摘要翻译：描述了通过使用选择性抑制人金属蛋白酶（MMP）如MMP-9和MMP-2，同时可选择性地保护MMP-1的药物来治疗疾病的方法。通过MMP抑制预防动脉粥样硬化斑块发展和破裂和/或颈动脉斑块发育和破裂可以减少斑块发展和破裂的不良后果，包括血栓栓塞，中风，心肌梗死和急性冠状动脉综合征。

5. 发明申请

WO2011041545A1 METHODS OF TREATING ANEURYSMAL DILATATION, BLOOD VESSEL WALL WEAKNESS AND SPECIFICALLY ABDOMINAL AORTIC AND THORACIC ANEURYSM USING MATRIX METALLOPROTEASE-2 INHIBITORS 审中-公开
标题翻译：使用基质金属蛋白酶-2抑制剂治疗神经损伤，血管壁疲劳和特异性ABDOMINAL AORTIC和THORACIC ANEURYSYS的方法
公开(公告)号：WO2011041545A1
公开(公告)日：2011-04-07
申请号：PCT/US2010/050907
申请日：2010-09-30
申请人： SYMPHONY EVOLUTION, INC. , WOOD, Alastair, J.J.
发明人： WOOD, Alastair, J.J.
IPC分类号： A61K31/495 , A61P9/00
CPC分类号： A61K31/675 , A61K31/495 , A61K31/55 , A61K2300/00
摘要： The present invention provides methods of treating aneurysmal dilatation, blood vessel wall weakness, and specifically abdominal aortic aneurysm and thoracic aneurysm by inhibiting MMPs and ADAM-IO. Such compounds are useful in the in vitro study of the role of MMPs and ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more MMPs or ADAM- 10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm. The invention also comprises methods of treating aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm utilizing the compounds of the invention in conjunction with inhibitors of angiotensin II, including angiotensin II receptor blockers and angiotensin converting enzyme inhibitors, and cyclophillin inhibitors.
摘要翻译：本发明提供了通过抑制MMP和ADAM-10来治疗动脉瘤扩张，血管壁虚弱，特别是腹主动脉瘤和胸动脉瘤的方法。这些化合物可用于体外研究MMPs和ADAM-10（及其抑制）在生物过程中的作用。本发明还包括药物组合物，其包含根据本发明的一种或多种MMP或ADAM-10抑制剂与药学上可接受的载体的组合。这样的组合物可用于治疗动脉瘤扩张或血管壁无力，例如腹主动脉瘤和胸动脉瘤。本发明还包括利用本发明化合物与血管紧张素II抑制剂（包括血管紧张素II受体阻断剂和血管紧张素转换酶抑制剂）和环磷酰胺转移酶抑制剂联合治疗动脉瘤扩张或血管壁虚弱的方法，例如腹主动脉瘤和胸动脉瘤抑制剂。

6. 发明专利

CA2809633C RECEPTOR-TYPE KINASE MODULATOR AND METHODS OF TREATING POLYCYSTIC KIDNEY DISEASE 未知
公开(公告)号：CA2809633C
公开(公告)日：2020-04-28
申请号：CA2809633
申请日：2011-08-25
申请人： SYMPHONY EVOLUTION INC
发明人： FROST PHILIP , LIAO WILLIAM W N , ROWINSKY ERIC K
IPC分类号： A61K31/517 , A61P13/12
摘要： The invention comprises use of a therapeutically effective amount of the compound of the formula below for preparation of a medicament for treating polycystic kidney diseases (PKD) in a mammal, such as human or feline (e.g., Persian cat).Formula (I). Also provided are the above compound and compositions comprising it for treating PKD.

7. 发明专利

EA025451B1 МОДУЛЯТОР КИНАЗЫ РЕЦЕПТОРНОГО ТИПА И СПОСОБЫ ЛЕЧЕНИЯ ПОЛИКИСТОЗНОЙ БОЛЕЗНИ ПОЧЕК 未知
公开(公告)号：EA025451B1
公开(公告)日：2016-12-30
申请号：EA201390283
申请日：2011-08-25
申请人： SYMPHONY EVOLUTION INC
发明人： FROST PHILIP , LIAO WILLIAM W N , ROWINSKY ERIC K
IPC分类号： A61K31/517 , A61P13/12
摘要： Изобретениесодержитприменениетерапевтическиэффективногоколичествасоединенияформулынижедляполучениялекарственногопрепаратас цельюлеченияполикистознойболезнипочек (PKD) умлекопитающего, такогокакчеловекилиживотноеизсемействакошачьих (например, персидскийкот). Такжепредставляютсявышеуказанноесоединениеи композиции, егосодержащие, длялечения PKD.

8. 发明专利

ES2425013T3 Inhibidores de ADAM-10 humana 未知
公开(公告)号：ES2425013T3
公开(公告)日：2013-10-10
申请号：ES03736979
申请日：2003-06-11
申请人： SYMPHONY EVOLUTION INC
发明人： BANNEN LYNNE CANNE , CO ERICK W , JAMMALAMADAKA VASU , NUSS JOHN M , KIM MOON HWAN , LE DONNA TRA , LEW AMY , MAC MORRISON B , MAMO SHUMEYE , WEN ZHAOYANG , XU WEI , KHOURY RICHARD GEORGE
IPC分类号： C07D241/04 , A61K31/495 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P15/00 , A61P15/12 , A61P17/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C309/87 , C07D213/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D413/06 , C07D413/12
摘要： Un compuesto según la fórmula IV,**Fórmula** y una de sus sales farmacéuticamente aceptables, en los que, Z es -C(R15)>=, -C(H)>= o -N>=; Ar es arilo o heteroarilo, cada uno opcionalmente sustituido con hasta 3 sustituyentes independientementeseleccionados entre alquilo, alcoxi, amino, carboxi, ciano, halógeno e hidroxi; R15 es fluoro; p es 0, 1, 2, o 3; L1 es -C(O)-, -S(O)2- o -(CH2)n-; L4 es -O-; R1 es -H, -OR11, -(CH2)nR11, -C(O)R11 o -NR12R13; R11, R12 y R13 son independientemente a) R50; b) hidrocarbilo C5-C14 -mono- o poli-cíclico condensado, saturado o mono- o poli-insaturado, que contieneopcionalmente uno o dos heteroátomos anulares por anillo y opcionalmente sustituido con uno odos sustituyentes R50; c) alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, o -C(O)H, cada uno de los cuales está opcionalmentesustituido con uno, dos o tres sustituyentes seleccionados independientemente de R50 e hidrocarbilo C5-C14-mono- o poli-cíclico condensado, saturado o mono- o poli-insaturado, que contiene opcionalmente uno o dosheteroátomos anulares por anillo y opcionalmente sustituido con uno, dos o tres sustituyentes R50;o R12 y R13 junto con el N al que están unidos por enlace covalente, un heterociclo C5-C6 que contieneopcionalmente un segundo heteroátomo anular y opcionalmente sustituido con uno o dos sustituyentes R50; yR50 es R51-L3-(CH2)n-; L3 es -O-, -NH-, -S(O)0-2, -C(O)-, -C(O)O-, -C(O)NH-, -OC(O)-, -NHC(O)-, -C6H4-, o un enlace directo;R51 es -H, alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, halo, -CF3 ,-OCF3, -OH, -NH2, mono-alquil C1-C6 amino,di-alquil C1C6 amino, -SH, -CO2H, -CN, -NO2, -SO3H, o un hidrocarbilo C5-C14-mono- o poli-cíclico condensado,saturado o mono- o poli-insaturado, que contiene opcionalmente uno o dos heteroátomos anulares por anillo yopcionalmente sustituido con uno, dos o tres sustituyentes independientemente seleccionados entre alquilo,alcoxi, amino, carboxi, ciano, halógeno e hidroxi; en el que n es 0, 1, 2, o 3; siempre que un O o S no estén individualmente unidos a otro O o S.

9. 发明专利

AU2003249212C1 Receptor-type kinase modulators and methods of use 未知
公开(公告)号：AU2003249212C1
公开(公告)日：2011-10-27
申请号：AU2003249212
申请日：2003-07-14
申请人： SYMPHONY EVOLUTION INC
发明人： SIMONA COSTANZO , KIM ANGIE I , KUMAR ANAND NEEL , BLAZEY CHARLES M , PETO CSABA J , RICE KENNETH D , JOERG BUSSENIUS , KENNEDY ABIGAIL R , TSANG TSZE H
IPC分类号： C07D239/94 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D498/04
摘要： The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death ( apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include "spectrum selective" kinase modulators, compounds that inhibit, regulate and/or mo dulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

10. 发明专利

AU2003237532B2 Human ADAM-10 inhibitors 未知
公开(公告)号：AU2003237532B2
公开(公告)日：2009-07-30
申请号：AU2003237532
申请日：2003-06-11
申请人： SYMPHONY EVOLUTION INC
发明人： JAMMALAMADAKA VASU , BANNEN LYNNE CANNE , NUSS JOHN M , MAC MORRISON B , XU WEI , LEW AMY , WEN ZHAOYANG , LE DONNA TRA , CO ERICK W , MAMO SHUMEYE , KHOURY RICHARD GEORGE , KIM MOON HWAN
IPC分类号： A61K31/495 , A61K31/496 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P15/00 , A61P15/12 , A61P17/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07C309/87 , C07D213/70 , C07D241/04 , C07D401/06 , C07D401/12
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.

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