公开(公告)号：US20060194822A1

公开(公告)日：2006-08-31

申请号：US11262317

申请日：2005-10-28

申请人： Arnon Nagler ,  Israel Vlodavsky ,  Mark Pines ,  Shai Yarkoni

发明人： Arnon Nagler ,  Israel Vlodavsky ,  Mark Pines ,  Shai Yarkoni

IPC分类号： A61K31/517

CPC分类号： A61K31/495

摘要： The present invention relates to compositions containing quinazolinones. More particularly, the present invention relates to a composition for treatment renal fibrosis, comprising as active ingredient a quinazolinone derivative as herein defined. The currently preferred embodiment is halofuginone, which is now show to slow or prevent progression of renal fibrosis in vivo, thereby preventing end-stage renal failure.

摘要翻译： 本发明涉及含有喹唑啉酮的组合物。 更具体地，本发明涉及用于治疗肾纤维化的组合物，其包含作为本文定义的喹唑啉酮衍生物的活性成分。 目前优选的实施方案是卤夫酮，其现在显示为缓慢或预防体内肾纤维化的进展，从而防止终末期肾衰竭。

公开(公告)号：US20060009475A1

公开(公告)日：2006-01-12

申请号：US10500690

申请日：2002-12-30

申请人： Mark Pines ,  Israel Vlodavsky ,  Shai Yarkoni ,  Arnon Nagler

发明人： Mark Pines ,  Israel Vlodavsky ,  Shai Yarkoni ,  Arnon Nagler

IPC分类号： A61K31/517

CPC分类号： A61K45/06 ,  A61K31/517 ,  A61K2300/00

摘要： The present invention provides compositions and methods for improving the effectiveness of anti-tumor treatments. The compositions of the present invention comprise quinazolinones, specifically halofuginone. In currently preferred embodiments the compositions and methods of the present invention improve the effectiveness of radiation therapy and chemotherapy, and concomitantly alleviate or prevent the damage induced by radiation therapy.

摘要翻译： 本发明提供了用于提高抗肿瘤治疗效果的组合物和方法。 本发明的组合物包含喹唑啉酮，特别是卤夫酮。 在目前优选的实施方案中，本发明的组合物和方法提高了放射治疗和化疗的有效性，并且同时缓解或预防了由放射治疗引起的损伤。

公开(公告)号：US06420371B1

公开(公告)日：2002-07-16

申请号：US09479660

申请日：2000-01-10

申请人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

发明人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

IPC分类号： A61K31505

CPC分类号： A61K31/517

摘要： The invention provides a composition for attenuating neovascularization and treating malignancies, including a pharmaceutically effective amount of a compound having a formula: wherein: R1 is a number of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy, R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy carbonyl, as active ingredient therein, in combination with a pharmaceutically acceptable carrier.

摘要翻译： 本发明提供一种用于减毒新生血管形成和治疗恶性肿瘤的组合物，包括药学有效量的具有下式的化合物：其中：R1是氢，卤素，硝基，苯并，低级烷基，苯基和低级烷氧基 R2是羟基，乙酰氧基和低级烷氧基的成员，R 3是作为活性成分的氢和低级链烯氧基羰基的组成与药学上可接受的载体的组合。

公开(公告)号：US6028075A

公开(公告)日：2000-02-22

申请号：US797703

申请日：1997-02-11

申请人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler ,  Hua-Quan Miao

发明人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler ,  Hua-Quan Miao

IPC分类号： C07D401/06 ,  A61K31/517 ,  A61P35/00 ,  A61P43/00 ,  A61K31/505

CPC分类号： A61K31/517

摘要： The invention provides a composition for attenuating neovascularization and treating malignancies, including a pharmaceutically effective amount of a compound having a formula: ##STR1## wherein: R.sub.1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy;R.sub.2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, andR.sub.3 is a member of the group consisting of hydrogen and lower alkenoxy carbonyl;as active ingredient therein, in combination with a pharmaceutically acceptable carrier.

摘要翻译： 本发明提供用于减毒新生血管形成和治疗恶性肿瘤的组合物，包括药学有效量的具有下式的化合物：其中：R 1是氢，卤素，硝基，苯并，低级烷基，苯基和低级烷氧基 ; R2是由羟基，乙酰氧基和低级烷氧基组成的组的成员，R3是由氢和低级链烯氧基羰基组成的组的成员; 作为其中的活性成分，与药学上可接受的载体组合。

公开(公告)号：US20070010538A1

公开(公告)日：2007-01-11

申请号：US11402638

申请日：2006-04-11

申请人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

发明人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

IPC分类号： A61K31/517

CPC分类号： A61K31/517

摘要： According to the present invention compositions and methods are provided to prevent the pathogenic aspects of tissue trauma while preserving normal tissue repair mechanisms, based on the fact that these molecules abrogate the cascade of damage initiated by tissue trauma, while maintaining this the requisite healthy extracellular matrix economy. The composition for regulating the extracellular matrix economy, comprise a pharmaceutically effective amount of an effector in combination with a pharmaceutically acceptable carrier. Preferably, the effector is a quinazolinone derivative. More preferably, the quinazolinone derivative is a member of a group having formula (I), wherein R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl, and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy; and pharmaceutically acceptable salts thereof; and n is either 1 or 2. Most preferably, the effector is Halofuginone and pharmaceutically acceptable salts thereof.

摘要翻译： 根据本发明，提供了组合物和方法，以防止组织创伤的病态方面，同时保持正常组织修复机制，这是基于这些分子消除由组织创伤引起的损伤级联的事实，同时保持必需的健康细胞外基质 经济。 用于调节细胞外基质经济性的组合物包含与药学上可接受的载体组合的药学有效量的效应物。 优选地，效应子是喹唑啉酮衍生物。 更优选地，喹唑啉酮衍生物是具有式（I）的基团的成员，其中R 1是由氢，卤素，硝基，苯并，低级烷基，苯基和 低级烷氧基 R 2是由羟基，乙酰氧基和低级烷氧基组成的组中的成员，R 3 3是氢和低级链烯氧基的成员; 及其药学上可接受的盐; 并且n为1或2.最优选地，效应物是卤代酮及其药学上可接受的盐。

公开(公告)号：US20060293351A1

公开(公告)日：2006-12-28

申请号：US11433639

申请日：2006-05-12

申请人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

发明人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler

IPC分类号： A61K31/517

CPC分类号： A61K31/517

摘要： A promotor of wound healing and an inhibitor of formation of a urethral stricture, particularly following surgical intervention or infection in the area. Specifically, the most preferred compound of the present invention, Halofuginone, can be used to prevent collagen deposition from occurring within the lumen of the urethra after such trauma, thereby inhibiting urethral stricture formation. Halofuginone, and related compounds, are also useful for the promotion of wound healing after trauma, for example after surgery.

摘要翻译： 伤口愈合的促进剂和形成尿道狭窄的抑制剂，特别是在该区域的手术干预或感染后。 具体地说，本发明最优选的化合物Halofuginone可用于在这种创伤之后防止在尿道内腔内发生胶原沉积，由此抑制尿道狭窄形成。 卤夫酮和相关化合物也可用于促进创伤后的伤口愈合，例如手术后。

公开(公告)号：US5891879A

公开(公告)日：1999-04-06

申请号：US722046

申请日：1996-12-09

申请人： Arnon Nagler ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

发明人： Arnon Nagler ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

IPC分类号： A61K31/517 ,  A61K31/505

CPC分类号： A61K31/517

摘要： The invention provides a pharmaceutical composition for preventing restens by the inhibition of vascular smooth muscle cell proliferation, comprising a compound of formula I: ##STR1## wherein: n=1 or 2 R.sub.1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy;R.sub.2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, andR.sub.3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonylas active ingredient therein, and the physiologically acceptable salts thereof, in combination with a pharmaceutically acceptable carrier.

摘要翻译： PCT No.PCT / US95 / 11186 Sec。 371日期1996年12月9日第 102（e）日期1996年12月9日PCT提交1995年8月29日PCT公布。 出版物WO96 / 06616 日期：1996年3月7日本发明提供了一种用于通过抑制血管平滑肌细胞增殖来预防再狭窄的药物组合物，其包含式I化合物：其中：n = 1或2 R 1为下列成员： 的氢，卤素，硝基，苯并，低级烷基，苯基和低级烷氧基; R2是由羟基，乙酰氧基和低级烷氧基组成的组的成员，R3是作为其中作为活性成分的氢和低级链烯氧基 - 羰基的成员，其生理上可接受的盐与药学上可接受的盐组合 可接受的载体

公开(公告)号：USRE39574E1

公开(公告)日：2007-04-17

申请号：US09742993

申请日：2000-12-20

申请人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler ,  Hua-Quan Mian

发明人： Mark Pines ,  Israel Vlodavsky ,  Arnon Nagler ,  Hua-Quan Mian

IPC分类号： A61K31/519

CPC分类号： A61K31/517

摘要： The invention provides a composition for attenuating neovascularization and treating malignancies, including a pharmaceutically effective amount of a compound having a formula: wherein: R1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy; R2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy carbonyl; as active ingredient therein, in combination with a pharmaceutically acceptable carrier.

摘要翻译： 本发明提供了用于减毒新生血管形成和治疗恶性肿瘤的组合物，包括药学有效量的具有甲醛的化合物

公开(公告)号：US6159488A

公开(公告)日：2000-12-12

申请号：US325198

申请日：1999-06-03

申请人： Arnon Nagler ,  Eli Hazum ,  Ehud Geller ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

发明人： Arnon Nagler ,  Eli Hazum ,  Ehud Geller ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

IPC分类号： A61F2/82 ,  A61K31/517 ,  A61K31/505

CPC分类号： A61K31/517 ,  A61F2/82

摘要： The invention provides an intracoronary stent coated with a quinazolinone derivative of formula (I), wherein n is 1 or 2, R.sub.1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy; R.sub.2 is a member of the group consisting of hydroxy, acetoxy and lower alkoxy, and R3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl, and physiologically acceptable salts thereof, for preventing restenosis after angioplasty.

摘要翻译： 本发明提供涂覆有式（I）的喹唑啉酮衍生物的冠状动脉内支架，其中n为1或2，R 1为氢，卤素，硝基，苯并，低级烷基，苯基和低级烷氧基的成员; R2是由羟基，乙酰氧基和低级烷氧基组成的组的成员，R3是由氢和低级链烯氧基 - 羰基组成的组的成员及其生理上可接受的盐，用于防止血管成形术后的再狭窄。

公开(公告)号：US6090814A

公开(公告)日：2000-07-18

申请号：US11696

申请日：1998-05-26

申请人： Arnon Nagler ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

发明人： Arnon Nagler ,  Shimon Slavin ,  Israel Vlodavsky ,  Mark Pines

IPC分类号： A61K31/517

CPC分类号： A61K31/517

摘要： The invention provides a composition for attenuating neovascularization crising administering a pharmaceutically effective amount of a compound of formula I: ##STR1## wherein: n=1 or 2; R.sub.1 is a member of the group consisting of hydrogen, halogen, nitro, benzo, lower alkyl, phenyl and lower alkoxy;R.sub.2 is a member of the group consisting of hydroxy, acetoxy, and lower alkoxy, andR.sub.3 is a member of the group consisting of hydrogen and lower alkenoxy-carbonyl;as an active ingredient therein, in combination with a pharmaceutically acceptable carrier.

摘要翻译： PCT No.PCT / US96 / 13210 Sec。 371日期：1998年5月26日 102（e）日期1998年5月26日PCT提交1996年8月12日PCT公布。 出版物WO97 / 06805 日本1997年2月27日本发明提供了一种用于减弱新生血管形成的组合物，其包括给予药学有效量的式I化合物：其中：n = 1或2; R1是由氢，卤素，硝基，苯并，低级烷基，苯基和低级烷氧基组成的组的成员; R2是由羟基，乙酰氧基和低级烷氧基组成的组的成员，R3是氢和低级链烯氧羰基的成员; 作为其中的活性成分，与药学上可接受的载体组合。