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公开(公告)号:US06784190B2
公开(公告)日:2004-08-31
申请号:US09916977
申请日:2001-07-27
申请人: Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
发明人: Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
IPC分类号: A61K3147
CPC分类号: C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04
摘要: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
摘要翻译: 本发明涉及其化合物及其衍生物,其合成及其作为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,alphavbeta5和/或alphavbeta6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,伤口愈合,病毒性疾病,肿瘤生长和转移。
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公开(公告)号:US6048861A
公开(公告)日:2000-04-11
申请号:US212082
申请日:1998-12-15
申请人: Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
发明人: Ben C. Askew , Paul J. Coleman , Mark E. Duggan , Wasyl Halczenko , George D. Hartman , Cecilia A. Hunt , John H. Hutchinson , Robert S. Meissner , Michael A. Patane , Garry R. Smith , Jiabing Wang
IPC分类号: C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04 , C07D519/00 , A61K31/435 , A61K31/44
CPC分类号: C07D401/06 , C07D401/12 , C07D471/04 , C07D495/04
摘要: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5, and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
摘要翻译: 本发明涉及其化合物及其衍生物,其合成及其作为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αvβ3,αvβ5和/或αvβ6的拮抗剂,可用于抑制骨吸收,治疗和预防骨质疏松症,并抑制血管再狭窄, 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,伤口愈合,病毒性疾病,肿瘤生长和转移。
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公开(公告)号:US5665723A
公开(公告)日:1997-09-09
申请号:US460372
申请日:1995-06-02
IPC分类号: C07D217/04 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , C07D207/46 , C07D209/34 , C07D209/46 , C07D217/24 , C07D401/12 , A61K31/40 , C07D403/00 , C07D405/00
CPC分类号: C07D401/12 , C07D207/46 , C07D209/46 , C07D217/24
摘要: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
摘要翻译: 具有式
的纤维蛋白原受体拮抗剂例如 -
公开(公告)号:US5889023A
公开(公告)日:1999-03-30
申请号:US841884
申请日:1997-05-05
IPC分类号: C07D401/14 , A61K31/445
CPC分类号: C07D401/14
摘要: A fibrinogen receptor antagonist which is 3(R)-�2-(Piperidin-4-yl)ethyl!-2-piperidon-1-ylacetyl-3(S)-(3-pyridyl)-.beta.-alanine.
摘要翻译: 3(R) - [2-(哌啶-4-基)乙基] -2-哌啶-1-基乙酰基-3(S) - (3-吡啶基)-β-丙氨酸的纤维蛋白原受体拮抗剂。
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公开(公告)号:US5719144A
公开(公告)日:1998-02-17
申请号:US391851
申请日:1995-02-22
IPC分类号: C07D217/04 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , C07D207/46 , C07D209/34 , C07D209/46 , C07D217/24 , C07D401/12 , C07D217/22 , A61K31/55 , C07D215/12
CPC分类号: C07D401/12 , C07D207/46 , C07D209/46 , C07D217/24
摘要: Fibrinogen receptor antagonists having the formula ##STR1## where L is L is (CH.sub.2).sub.p, where p is 1 or 2; and Z is --CR.sup.1 .dbd.CR.sup.2 --; which are useful for inhibiting platelet aggregation for example ##STR2##
摘要翻译: 具有式(IMAGE)其中L为L的纤维蛋白原受体拮抗剂为(CH2)p,其中p为1或2; Z为-CR1 = CR2-; 其可用于抑制血小板聚集,例如
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公开(公告)号:US5852045A
公开(公告)日:1998-12-22
申请号:US729968
申请日:1996-10-15
申请人: Ben C. Askew , George D. Hartman , Mark E. Duggan , Steven D. Young , John H. Hutchinson , John S. Wai , Melissa S. Egbertson , Laura M. Vassallo , Laura A. Libby , Amy E. Krause , Wasyl Halczenko , Nathan C. Ihle
发明人: Ben C. Askew , George D. Hartman , Mark E. Duggan , Steven D. Young , John H. Hutchinson , John S. Wai , Melissa S. Egbertson , Laura M. Vassallo , Laura A. Libby , Amy E. Krause , Wasyl Halczenko , Nathan C. Ihle
IPC分类号: C07D401/06 , C07D401/14 , C07D405/14 , C07D453/04 , C07D521/00 , C07K5/06 , A61K31/445 , A61K31/495
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D405/14 , C07D453/04 , C07K5/06026
摘要: Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
摘要翻译: 具有例如
结构的纤维蛋白原受体拮抗剂,例如 -
公开(公告)号:US5719162A
公开(公告)日:1998-02-17
申请号:US459882
申请日:1995-06-02
IPC分类号: C07D217/04 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/47 , A61K31/472 , A61K31/495 , A61P7/02 , C07D207/46 , C07D209/34 , C07D209/46 , C07D217/24 , C07D401/12 , C07D217/22
CPC分类号: C07D401/12 , C07D207/46 , C07D209/46 , C07D217/24
摘要: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
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公开(公告)号:US5789421A
公开(公告)日:1998-08-04
申请号:US735844
申请日:1996-10-23
IPC分类号: C07D20060101 , C07D401/12 , A61K31/445
CPC分类号: C07D401/12
摘要: A fibrinogen receptor antagonist which is 5-�(4-Piperidinyl)methoxy!-2-indolecarbonyl-2(S)-phenylsulfonyl-amino-.beta.-alanine.
摘要翻译: 5 - [(4-哌啶基)甲氧基] -2-吲哚羰基-2(S) - 苯磺酰基 - 氨基-β-丙氨酸的纤维蛋白原受体拮抗剂。
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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。
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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。
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