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41. 发明授权

US07109191B2 Benzazepinone alpha vintegrin receptor antagonists 失效
标题翻译：苯扎西泮α整联蛋白受体拮抗剂
公开(公告)号：US07109191B2
公开(公告)日：2006-09-19
申请号：US10475697
申请日：2002-04-29
申请人： Robert S. Meissner , Paul J. Coleman , Mark E. Duggan , George D. Hartman , Jiabing Wang , John H. Hutchinson
发明人： Robert S. Meissner , Paul J. Coleman , Mark E. Duggan , George D. Hartman , Jiabing Wang , John H. Hutchinson
IPC分类号： C07D401/02 , A61K31/55 , A61P19/10
CPC分类号： C07D213/73 , A61K31/55 , A61K38/27 , A61K38/29 , A61K45/06 , C07D401/12 , C07D471/04 , C07D471/10 , A61K2300/00
摘要： The present invention relates to novel benzazepinone derivatives, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and αvβ5 and are therefore useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及新的苯并氮杂酮衍生物，它们的合成及其作为alphav整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体α1和α2β的拮抗剂，因此可用于抑制骨吸收，治疗和/或预防骨质疏松，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎性关节炎，癌症和转移性肿瘤生长。

42. 发明授权

US06693101B2 &agr;v integrin receptor antagonists 失效
标题翻译： alphav整合素受体拮抗剂
公开(公告)号：US06693101B2
公开(公告)日：2004-02-17
申请号：US09767471
申请日：2001-01-23
申请人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
发明人： Ben C. Askew , Michael J. Breslin , Mark E. Duggan , John H. Hutchinson , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Michael A. Patane
IPC分类号： A61K3144
CPC分类号： C07D213/73 , A61K45/06 , C07D239/26 , C07D239/42 , C07D239/48 , C07D401/06 , C07D403/06 , C07D405/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及其新的链烷酸衍生物，它们的合成及其作为αphav整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体alphavbeta3和/或alphavbeta5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎性关节炎，癌症和转移性肿瘤生长。

43. 发明授权

US06645974B2 Androgen receptor modulators and methods for use thereof 失效
标题翻译：雄激素受体调节剂及其使用方法
公开(公告)号：US06645974B2
公开(公告)日：2003-11-11
申请号：US10205634
申请日：2002-07-25
申请人： John H. Hutchinson , Michael J. Breslin , Gideon A. Rodan , Soumya P. Sahoo , Mark E. Duggan , Shun-Ichi Harada , Azriel Schmidt , Wasyl Halczenko , Dwight A. Towler
发明人： John H. Hutchinson , Michael J. Breslin , Gideon A. Rodan , Soumya P. Sahoo , Mark E. Duggan , Shun-Ichi Harada , Azriel Schmidt , Wasyl Halczenko , Dwight A. Towler
IPC分类号： A61K3158
CPC分类号： C07J73/005 , A61K31/435 , A61K31/473 , A61K31/58 , C07D221/18 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.
摘要翻译：公开了本文定义的结构式（I）的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法，以及在患者中激动雄激素受体的方法，特别是其中雄性受体在男性患者的前列腺或女性患者的子宫中被拮抗并在骨和/或肌肉组织中激动的方法。这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素施用而改善的病症，包括：骨质疏松症，牙周病，骨折，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老皮肤，男性性腺机能减退妇女的绝经症状，动脉粥样硬化，高胆固醇血症，高脂血症，再生障碍性贫血和其他造血障碍，胰腺癌，肾癌，关节炎和关节修复，单独或与其他活性剂组合。此外，这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。

44. 发明授权

US06472403B2 &agr;V integrin receptor antagonists 失效
标题翻译： αV整联蛋白受体拮抗剂
公开(公告)号：US06472403B2
公开(公告)日：2002-10-29
申请号：US09766148
申请日：2001-01-19
申请人： Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Aiwen Li , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Jiabing Wang , Michael A. Patane
发明人： Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Aiwen Li , Robert S. Meissner , James J. Perkins , Thomas G. Steele , Jiabing Wang , Michael A. Patane
IPC分类号： A61K3144
CPC分类号： C07D213/73 , A61K45/06 , C07D401/14 , C07D405/14 , C07D471/04 , C07D471/10
摘要： The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及其新颖的咪唑啉酮衍生物，其合成及其作为αphav整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体α2和/或阿尔巴博5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症，炎症性关节炎，病毒性疾病，癌症和转移性肿瘤生长。

45. 发明授权

US06426353B1 &agr; v integrin receptor antagonists 失效
标题翻译： αv整联蛋白受体拮抗剂
公开(公告)号：US06426353B1
公开(公告)日：2002-07-30
申请号：US09952084
申请日：2001-09-14
申请人： Byron H. Arison , Donghui Cui , Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Thomayant Prueksaritanont , Raju Subramanian , Xiaojun Fang
发明人： Byron H. Arison , Donghui Cui , Mark E. Duggan , Wasyl Halczenko , John H. Hutchinson , Thomayant Prueksaritanont , Raju Subramanian , Xiaojun Fang
IPC分类号： A61K31435
CPC分类号： C07D471/04
摘要： The present invention relates to novel compounds formed by metabolic conversion of compounds of structural formula (1), pharmaceutical compositions containing such compounds, and their use as &agr;v&bgr;3 integrin receptor antagonists. The compounds of the present invention are useful for inhibiting bone resorption, restenosis, angiogenesis, diabetic retinopathy, macular degeneration, inflammatory arthritis, cancer, and metastatic tumor growth. They are particularly useful for inhibiting bone resorption and for the treatment and prevention of osteoporosis.
摘要翻译：本发明涉及由结构式（1）的化合物，含有这些化合物的药物组合物的代谢转化形成的新化合物，以及它们作为α-角蛋白3整联蛋白受体拮抗剂的用途。本发明的化合物可用于抑制骨吸收，再狭窄，血管生成，糖尿病性视网膜病变，黄斑变性，炎症性关节炎，癌症和转移性肿瘤生长。它们对抑制骨吸收和治疗和预防骨质疏松症尤其有用。

46. 发明授权

US6017925A Integrin antagonists 失效
标题翻译：整合素拮抗剂
公开(公告)号：US6017925A
公开(公告)日：2000-01-25
申请号：US6626
申请日：1998-01-13
申请人： Mark E. Duggan
发明人： Mark E. Duggan
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为玻连蛋白受体拮抗剂的用途。本发明的玻连蛋白受体拮抗剂化合物是可用于抑制骨吸收，治疗和预防骨质疏松症以及抑制再狭窄的糖尿病性视网膜病变的αvβ3拮抗剂，αvβ5拮抗剂或双重αvβ3 /αvβ5拮抗剂，黄斑变性，血管生成，动脉粥样硬化，炎症，病毒性疾病和肿瘤生长。

47. 发明授权

US5925655A .alpha..sub.v .beta..sub.3 antagonists 失效
标题翻译： αvβ3拮抗剂
公开(公告)号：US5925655A
公开(公告)日：1999-07-20
申请号：US841979
申请日：1997-04-08
申请人： Mark E. Duggan , George D. Hartman , William F. Hoffman
发明人： Mark E. Duggan , George D. Hartman , William F. Hoffman
IPC分类号： C07D401/12 , C07D403/12 , C07D401/14 , A61K31/40 , C07D209/46
CPC分类号： C07D401/12 , C07D403/12
摘要： This invention relates to certain novel isoindolone compounds and derivatives thereof, their synthesis, and their use as .alpha.v.beta.3 receptor antagonists. The .alpha.v.beta.3 receptor antagonist compounds of this invention are useful for inhibiting bone resorption, treating and preventing osteoporosis and cancer, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
摘要翻译：本发明涉及某些新颖的异吲哚酮化合物及其衍生物，其合成及其作为αvβ3受体拮抗剂的用途。本发明的αvβ3受体拮抗剂化合物可用于抑制骨吸收，治疗和预防骨质疏松症和癌症，以及抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症和肿瘤生长。

48. 发明授权

US5854245A Fibrinogen receptor antagonists 失效
标题翻译：纤维蛋白原受体拮抗剂
公开(公告)号：US5854245A
公开(公告)日：1998-12-29
申请号：US883108
申请日：1997-06-26
申请人： Mark E. Duggan , Melissa S. Egbertson , George D. Hartman , Steven D. Young , Nathan C. Ihle
发明人： Mark E. Duggan , Melissa S. Egbertson , George D. Hartman , Steven D. Young , Nathan C. Ihle
IPC分类号： C07D471/04 , C07D493/04 , A61K31/495 , A61K31/435 , C07D241/04 , C07D241/38
CPC分类号： C07D471/04 , C07D493/04
摘要： Fibrinogen receptor antagonists having the structure X--Y--Z--A--B and pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g., ##STR1##
摘要翻译：具有结构X-Y-Z-A-Band药学上可接受的盐的纤维蛋白原受体拮抗剂，其中X是5,6或7元芳族或非芳族环，Y是5或6元芳族环，例如，

49. 发明授权

US5338723A Fibrinogen receptor antagonists 失效
标题翻译：纤维蛋白原受体拮抗剂
公开(公告)号：US5338723A
公开(公告)日：1994-08-16
申请号：US948331
申请日：1992-09-21
申请人： Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber , Mark E. Duggan
发明人： Ruth F. Nutt , Stephen F. Brady , Daniel F. Veber , Mark E. Duggan
IPC分类号： C07K5/10 , C07K5/107 , C07K14/75 , C07K7/00 , A61K37/02 , C07K7/64
CPC分类号： C07K14/75 , C07K5/1016
摘要： A fibrinogen receptor antagonist of the formula ##STR1## wherein XX represents a synthetic alpha-amino acid containing a linear side chain and ZZ represents a sequence of 1, 2, 3 or 4 amino acids.
摘要翻译：一种下式的纤维蛋白原受体拮抗剂，其中XX代表含有线性侧链的合成α-氨基酸，ZZ代表1,2,3或4个氨基酸的序列。

50. 发明授权

US5294616A Fibrinogen receptor antagonists 失效
标题翻译：纤维蛋白原受体拮抗剂
公开(公告)号：US5294616A
公开(公告)日：1994-03-15
申请号：US857528
申请日：1992-03-25
申请人： Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , Laura M. Turchi , William L. Laswell
发明人： Mark E. Duggan , Melissa S. Egbertson , Wasyl Halczenko , George D. Hartman , Laura M. Turchi , William L. Laswell
IPC分类号： A61K31/155 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/215 , A61K31/265 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/435 , A61K31/495 , A61K31/496 , A61P7/02 , C07C229/34 , C07C233/47 , C07C233/51 , C07C233/83 , C07C237/12 , C07C271/10 , C07C271/22 , C07C279/04 , C07C317/28 , C07C317/32 , C07C325/02 , C07C327/22 , C07C327/30 , C07C327/48 , C07D205/04 , C07D207/08 , C07D211/22 , C07D215/12 , C07D233/22 , C07D241/04 , C07D263/48 , C07D295/08 , C07D295/088 , C07D307/66 , C07D333/20 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07F9/38 , C07F9/58 , C07F9/60 , C07F9/6509 , C07F9/6558 , A61K31/675 , A61K31/445 , C07D295/00 , C07D211/30 , C07D277/62 , C07D307/02
CPC分类号： C07D295/088 , C07C271/22 , C07C317/28 , C07C325/02 , C07C327/22 , C07C327/48 , C07D211/22 , C07F9/3882 , C07F9/60 , C07F9/650958 , C07F9/65583 , C07F9/65586 , C07C2101/08 , C07C2101/14
摘要： A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
摘要翻译：作为纤维蛋白原IIb / IIIa受体的拮抗剂的一系列非肽衍生物，因此是可用于预防和治疗由血栓形成引起的疾病的血小板聚集化合物。

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