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21. 发明申请

US20060264425A1 Novel anthranilamide pyridinureas as vascular endothelial growth factor (VEGF) receptor kinase inhibitors 失效
标题翻译：新型邻氨基苯甲酰胺吡啶脲作为血管内皮生长因子（VEGF）受体激酶抑制剂
公开(公告)号：US20060264425A1
公开(公告)日：2006-11-23
申请号：US11265516
申请日：2005-11-03
申请人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp
发明人： Rolf Bohlmann , Martin Haberey , Andreas Huth , Stuart Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D213/75 , C07D401/12 , C07D401/14 , C07D491/10
摘要： The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.
摘要翻译：本发明涉及作为VEGF受体激酶抑制剂的新型邻氨基苯甲酰胺吡啶脲，其作为用于预防或治疗由持续血管生成引发的疾病的药剂的生产和用途。

22. 发明授权

US07081468B2 Ortho-substituted anthranilic acid amides and their use as medicaments 失效
标题翻译：邻氨基苯甲酸酰胺及其用作药物
公开(公告)号：US07081468B2
公开(公告)日：2006-07-25
申请号：US10275480
申请日：2001-05-08
申请人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
发明人： Martin Krueger , Andreas Huth , Orlin Petrov , Dieter Seidelmann , Karl-Heinz Thierauch , Martin Haberey , Andreas Menrad , Alexander Ernst
IPC分类号： A61K31/44
CPC分类号： C07D213/38
摘要： Ortho-substituted anthranilic acid amides and use thereof as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described.
摘要翻译：描述了邻位取代的邻氨基苯甲酸酰胺及其作为用于治疗由持续性血管生成触发的疾病的药物的用途。

23. 发明授权

US06448277B2 VEGF receptor tyrosine kinase inhibitors 失效
标题翻译： VEGF受体酪氨酸激酶抑制剂
公开(公告)号：US06448277B2
公开(公告)日：2002-09-10
申请号：US09850434
申请日：2001-05-07
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： A61K31166
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is S02; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述了式（I）的化合物，其中W是O或S; X为NR8; Y为CR 9 R 10 - （CH 2）n，其中R 9和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO2; R1是芳基; R2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二酰亚氨基，并且在Y = SO 2的情况下不能代表2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地为H或氢以外的取代基; 且R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

24. 发明授权

US5700791A Vitamin D derivatives modified in the 20-position and pharmaceutical compositions thereof 失效
标题翻译：在20位修饰的维生素D衍生物及其药物组合物
公开(公告)号：US5700791A
公开(公告)日：1997-12-23
申请号：US664121
申请日：1996-06-14
申请人： Andreas Steinmeyer , Gunter Neef , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
发明人： Andreas Steinmeyer , Gunter Neef , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
IPC分类号： A61K31/59 , A61P3/08 , A61P17/00 , A61P35/00 , A61P35/02 , A61P37/00 , C07C35/32 , C07C45/30 , C07C49/172 , C07C49/517 , C07C49/753 , C07C69/013 , C07C69/12 , C07C401/00 , C07F7/18
CPC分类号： C07F7/1856 , C07C401/00 , C07C45/30 , C07C45/305 , C07C49/517 , C07C49/753 , C07C69/013
摘要： The invention relates to vitamin D derivatives, modified in 20-position, of general formula I ##STR1## in which X, Y, Z, R.sub.1, R.sub.2 as well as R.sub.3 have the meaning indicated in the description, process for their production and their use as agents for treatment of hyperproliferative diseases of the skin.
摘要翻译：本发明涉及通式I的维生素D衍生物，其中X，Y，Z，R 1，R 2以及R 3具有说明书中指出的含义，其制备方法和它们用作治疗皮肤过度增生性疾病的药剂。

25. 发明授权

US5446035A 20-methyl-substituted vitamin D derivatives 失效
标题翻译： 20-甲基取代的维生素D衍生物
公开(公告)号：US5446035A
公开(公告)日：1995-08-29
申请号：US307081
申请日：1994-09-16
申请人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
发明人： Gunter Neef , Andreas Steinmeyer , Gerald Kirsch , Katica Schwarz , Ruth Thieroff-Ekerdt , Herbert Wiesinger , Martin Haberey
IPC分类号： A61K31/59 , A61P3/02 , A61P3/14 , A61P17/00 , A61P35/02 , A61P37/00 , A61P43/00 , C07C401/00
CPC分类号： C07C401/00
摘要： New 20-methyl-substituted vitamin D derivatives of general formula I ##STR1## are described in whichR.sup.1 means a hydrogen atom, a hydroxy group or an alkanoyloxy group with 1 to 12 carbon atoms or a benzoyloxy group,R.sup.2 means a hydrogen atom or an alkanoyl group with 1 to 12 carbon atoms or a benzoyl group andR.sup.3 means a saturated or unsaturated, straight-chain or branched hydrocarbon radical with up to 18 C atoms, which optionally contains carbocyclic structures, optionally substituted with one or more hydroxy, oxo, amino group(s) and/or one or more halogen atom(s) as well as optionally exhibits one or more oxygen, sulfur and/or nitrogen atom(s) as a bridging link or links in the hydrocarbon radical, and a process for their production.Relative to calcitriol, the new compounds exhibit a greatly improved induction of cell differentiation (HL-60) and are suitable for the production of pharmaceutical agents.
摘要翻译：描述了通式I的新的20-甲基取代的维生素D衍生物（I），其中R 1表示氢原子，羟基或具有1至12个碳原子的烷酰氧基或苯甲酰氧基，R2表示氢原子或具有1至12个碳原子的烷酰基或苯甲酰基，R 3表示具有至多18个C原子的饱和或不饱和的直链或支链烃基，其任选地含有碳环结构，任选地被一个或多个羟基，氧代，氨基和/或一个或多个卤素原子，以及任选地表现出一个或多个氧，硫和/或氮原子作为烃基中的桥连或连接，及其生产过程。相对于骨化三醇，新化合物表现出极大改善的细胞分化诱导（HL-60），适用于制药。

26. 发明授权

US4868166A 2,2:6,6-diethylen-3-oxo-17alpha-pregn-4-ene-21,17alpha-carbolactones, process for their production & pharmaceutical preparations containing them 失效
标题翻译： 2,2,6,6-二乙基-3-氧代-17α-孕-4-烯-21,17α-卡宾内酯，其制备方法和含有它们的药物制剂
公开(公告)号：US4868166A
公开(公告)日：1989-09-19
申请号：US150413
申请日：1988-02-05
申请人： Dieter Bittler , Klaus Nickisch , Henry Laurent , Rudolf Wiechert , Martin Haberey
发明人： Dieter Bittler , Klaus Nickisch , Henry Laurent , Rudolf Wiechert , Martin Haberey
IPC分类号： A61K31/57 , C07J1/00 , C07J53/00
CPC分类号： C07J53/001 , C07J53/008
摘要： 2,2;6,6-diethylene-3-oxo-17alpha-pregn-4-ene-21,17-carbolactones of general formula I, ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group,R.sub.2 represents a methyl or ethyl group and ##STR2## process for their production and their pharmaceutical use.
摘要翻译： PCT No.PCT / DE87 / 00208 Sec。 371日期1988年2月5日 102（e）日期1988年2月5日PCT提交1987年5月5日PCT公布。出版物WO87 / 06937 1987年11月19日2.2.1通式I的6,6-二亚乙基-3-氧代-17α-孕-4-烯-21,17-碳内酯，其中R1表示氢原子或甲基，R2代表甲基或乙基和它们的制备方法及其药物用途。

27. 发明申请

US20110124680A1 NOVEL ANTHRANILAMIDE PYRIDINUREAS AS VASCULAR ENDOTHELIAL GROWTH FACTOR (VEGF) RECEPTOR KINASE INHIBITORS 审中-公开
标题翻译：新型ANTHRANILAMIDE PYRIDINUREAS作为血管内皮生长因子（VEGF）受体激酶抑制剂
公开(公告)号：US20110124680A1
公开(公告)日：2011-05-26
申请号：US13019530
申请日：2011-02-02
申请人： Rolf BOHLMANN , Martin Haberey , Andreas Huth , Stuart James Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp , Andreas Reichel
发明人： Rolf BOHLMANN , Martin Haberey , Andreas Huth , Stuart James Ince , Martin Krueger , Karl-Heinz Thierauch , Holger Hess-Stumpp , Andreas Reichel
IPC分类号： A61K31/4439 , A61K31/4725 , A61K31/4709 , A61K31/44 , A61P35/00 , A61P17/06 , A61P27/02 , A61P9/10 , A61P11/06 , A61P13/12 , A61P1/16 , A61P29/00
CPC分类号： C07D401/12
摘要： The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.
摘要翻译：本发明涉及作为VEGF受体激酶抑制剂的新型邻氨基苯甲酰胺吡啶脲，其作为用于预防或治疗由持续血管生成引发的疾病的药剂的生产和用途。

28. 发明授权

US07517894B2 VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines 失效
标题翻译： VEGFR-2和VEGFR-3抑制性邻氨基苯甲酰胺吡啶
公开(公告)号：US07517894B2
公开(公告)日：2009-04-14
申请号：US10870491
申请日：2004-06-18
申请人： Andreas Huth , Ludwig Zorn , Martin Krueger , Stuart Ince , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
发明人： Andreas Huth , Ludwig Zorn , Martin Krueger , Stuart Ince , Karl Heinz Thierauch , Andreas Menrad , Martin Haberey , Holger Hess-Stumpp
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D213/61 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04
摘要： VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver; mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
摘要翻译：描述了VEGFR-2和VEGFR-3抑制性邻氨基苯酰胺吡啶酰胺，其作为用于治疗由持续血管发生引起的疾病的药物的制备和用途，以及用于制备化合物的中间产物。根据本发明的化合物可用于或在肿瘤或转移生长的情况下，牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位，克罗恩病，霍奇金病，白血病; 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化; 肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管假体中或使用机械装置用于保持血管开放（例如，支架）作为免疫抑制剂的抑制，作为免疫抑制剂无疤痕愈合，老年角化病和接触性皮炎的支持。在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。

29. 发明授权

US07479491B2 Azanthranylalkyl and -cycloalkyl amides and their use as VEGF receptor inhibitors 失效
标题翻译：蒽醌基烷基和环烷基酰胺及其作为VEGF受体抑制剂的用途
公开(公告)号：US07479491B2
公开(公告)日：2009-01-20
申请号：US10945690
申请日：2004-09-21
申请人： Dieter Seidelmann , Martin Krueger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
发明人： Dieter Seidelmann , Martin Krueger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
IPC分类号： A61K31/535 , A61K31/44 , A61K31/445 , C07D265/30 , C07D211/70
CPC分类号： C07D213/38
摘要： The invention relates to substituted anthranylalkyl and -cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.
摘要翻译：本发明涉及通式（I）的取代的苯甲酰基烷基和 - 环烷基酰胺及其用作治疗由持续性血管发生引起的疾病的药物。

30. 发明授权

US07429592B2 Cyanoanthranilamide derivatives and the use thereof as medicaments 失效
标题翻译：氰基脒酰胺衍生物及其作为药物的用途
公开(公告)号：US07429592B2
公开(公告)日：2008-09-30
申请号：US10476761
申请日：2002-05-03
申请人： Alexander Ernst , Andreas Huth , Martin Krueger , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
发明人： Alexander Ernst , Andreas Huth , Martin Krueger , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
IPC分类号： C07D401/12 , A61K31/44 , A61K31/47
CPC分类号： C04B35/632 , C07D401/12
摘要： Substituted cyanoanthranilamide derivatives, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are described. The compounds according to the invention can be used as or in the case of psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.
摘要翻译：取代的氰基邻氨基苯甲酰胺衍生物，其制备和用作治疗由持续血管发生引发的疾病的药物。根据本发明的化合物可以用作牛皮癣，卡波西肉瘤，再狭窄，例如支架诱导的再狭窄，子宫内膜异位症，克罗恩病，霍奇金病，白血病; 关节炎，如类风湿关节炎，血管瘤，血管纤维瘤; 眼睛疾病如糖尿病性视网膜病变，新生血管性青光眼; 肾脏疾病如肾小球性肾炎，糖尿病肾病，恶性肾硬化，血栓性微血管病综合征，移植排斥反应和肾小球病; 纤维化疾病，如肝硬化，肾小球膜细胞增生性疾病，动脉硬化，神经组织损伤，以及球囊导管治疗后血管再狭窄的抑制，血管修复术或机械装置用于保持血管开放的诸如例如作为免疫抑制剂的支架，作为无疤痕愈合的支持，老年角化病和接触性皮炎。在淋巴管生成的情况下，根据本发明的化合物也可以用作VEGFR-3抑制剂。

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