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1. 发明申请

WO2004007481A2 SUBSTITUTED AMINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的胺衍生物和使用治疗血友病相关疾病的方法
公开(公告)号：WO2004007481A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/022275
申请日：2003-07-15
申请人： AMGEN INC.
发明人： PATEL, Vinod, F. , ASKEW, Benny , BOOKER, Shon , CHEN, Guoqing , DIPIETRO, Lucian, V. , GERMAIN, Julie , HABGOOD, Gregory, J. , HUANG, Qi , KIM, Tae-Seong , LI, Aiwen , NISHIMURA, Nobuko , NOMAK, Rana , RIAHI, Babak , YUAN, Chester, Chenguang , ELBAUM, Daniel
IPC分类号： C07D401/12
CPC分类号： C07D471/04 , A61K31/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：选择的胺对于预防和治疗疾病如血管生成介导的疾病是有效的。本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

2. 发明申请

WO2004007457A2 SUBSTITUTED BENZYLAMINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的苯甲酰胺衍生物及其使用方法
公开(公告)号：WO2004007457A2
公开(公告)日：2004-01-22
申请号：PCT/US2003/022276
申请日：2003-07-15
申请人： AMGEN INC.
发明人： ELBAUM, Daniel , ASKEW, Benny , BOOKER, Shon , GERMAIN, Julie , HABGOOD, Gregory , HANDLEY, Michael , KIM, Tae-Seong , LI, Aiwen , NISHIMURA, Nobuko , PATEL, Vinod, F. , YUAN, Chester, Chenguang , KIM, Joseph, L.
IPC分类号： C07D213/81
CPC分类号： C07D213/81 , C04B35/632 , C07D213/82 , C07D237/04 , C07D237/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： Selected compounds of formula IV are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as intermediates useful in such processes (IV).
摘要翻译：选择的式IV化合物可有效预防和治疗诸如血管生成介导的疾病之类的疾病。本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这种化合物的方法以及可用于这些方法（IV）的中间体。

3. 发明申请

WO2005009978A1 2-AMINOPYRIMIDINE AND 2-AMINOPYRIDINE-4-CARBAMATES FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES 审中-公开
标题翻译：用于治疗自身免疫性疾病的2-氨基嘧啶和2-氨基吡啶-4-羧酸酯
公开(公告)号：WO2005009978A1
公开(公告)日：2005-02-03
申请号：PCT/US2004/023233
申请日：2004-07-15
申请人： AMGEN INC. , BUCHANAN, John, L. , ELBAUM, Daniel , MARTIN, Matthew, W. , MCGOWAN, David, C. , NOVAK, Perry, M. , NUNES, Joseph, J.
发明人： BUCHANAN, John, L. , ELBAUM, Daniel , MARTIN, Matthew, W. , MCGOWAN, David, C. , NOVAK, Perry, M. , NUNES, Joseph, J.
IPC分类号： C07D239/48
CPC分类号： C04B35/632 , C07D213/75 , C07D239/48 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula (1) and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.
摘要翻译：本发明涉及具有通式（1）的嘧啶或吡啶氨基甲酸酯化合物及其药学上可接受的盐或衍生物。还包括治疗各种疾病和病症的方法，包括炎症，T细胞活化和增殖的抑制，关节炎，器官移植，缺血或再灌注损伤，心肌梗死，中风，多发性硬化，炎性肠病，克罗恩病，狼疮，超敏反应，1型糖尿病，牛皮癣，皮炎，桥本甲状腺炎，干燥综合征，自身免疫性甲状腺功能亢进，艾迪生病，自身免疫性疾病，肾小球性肾炎，过敏性疾病，哮喘，干草病，湿疹，癌症，结肠癌，胸腺瘤，仅举几例哺乳动物，所述方法包括给予治疗有效量的如上所述的式I化合物或其盐或衍生物形式。

4. 发明申请

WO2005042518A2 SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：取代的杂环化合物和使用方法
公开(公告)号：WO2005042518A2
公开(公告)日：2005-05-12
申请号：PCT/US2004/034920
申请日：2004-10-21
申请人： AMGEN INC. , ELBAUM, Daniel , MARTIN, Matthew W. , NUNES, Joseph J.
发明人： ELBAUM, Daniel , MARTIN, Matthew W. , NUNES, Joseph J.
IPC分类号： C07D403/00
CPC分类号： C07D403/04
摘要： The present invention relates to hydroxybenzimidazole pyrimidines or pyridines or pharmaceutically-acceptable salts thereof. Also included is a method of treatment of inflammation, inhibition of T cell activation and proliferation, arthritis, rheumatoid arthritis, psoriatic arthritis, osteoarthritis, organ transplant, acute transplant or heterograft or homograft rejection, transplantation tolerance induction, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, including ulcerative colitis, Crohn's disease, lupus, contact hypersensitivity, delayed-type hypersensitivity, and gluten-sensitive enteropathy, type 1 diabetes, psoriasis, contact dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune polyglandular disease, autoimmune alopecia, pernicious anemia, vitiligo, autoimmune hypopituatarism, Guillain-Barre syndrome, glomerulonephritis, serum sickness, uticaria, allergic diseases, asthma, hayfever, allergic rhinitis, scleracielma, mycosis fungoides, dermatomyositis, alopecia areata, chronic actinic dermatitis, eczema, Behcet's disease, Pustulosis palmoplanteris, Pyoderma gangrenum, Sezary's syndrome, atopic dermatitis, systemic schlerosis, morphea, atopic dermatitis, colon carcinoma or thymoma in a mammal comprising administering a therapeutically-effective amount a compound as described above.
摘要翻译：本发明涉及羟基苯并咪唑嘧啶或其吡啶或其药学上可接受的盐。还包括治疗炎症，抑制T细胞活化和增殖，关节炎，类风湿性关节炎，牛皮癣性关节炎，骨关节炎，器官移植，急性移植或异体移植或同种移植排斥，移植耐受性诱导，局部缺血或再灌注损伤，心肌梗塞，中风，多发性硬化症，炎症性肠病，包括溃疡性结肠炎，克罗恩氏病，狼疮，接触性超敏反应，迟发型超敏反应和面筋敏感性肠病，1型糖尿病，牛皮癣，接触性皮炎，桥本氏甲状腺炎，舍格伦综合征，自身免疫性甲状腺机能亢进，艾迪生病，自身免疫性多腺疾病，自身免疫性脱发，恶性贫血，白癜风，自身免疫性垂体功能低下，格林巴利综合征，肾小球肾炎，血清病，乌氏病，过敏性疾病，哮喘，干燥症，过敏性鼻炎，巩膜炎，蕈样霉菌病，皮肌炎，，慢性ac 包括给予治疗有效量的如上所述的化合物，所述化合物包括但不限于：皮质类固醇，皮肤炎， p>

5. 发明申请

WO2004085425A1 FUSED AZOLES SUCH AS 2,5-DISUBSTITUTED BENZIMIDAZOLES, BENZOXAZOLES AND BENZOTHIAZOLES AS KINASE INHIBITORS 审中-公开
标题翻译：作为2,5-取代苯并咪唑，苯并噻唑和苯并噻唑的熔融偶氮化物作为激酶抑制剂
公开(公告)号：WO2004085425A1
公开(公告)日：2004-10-07
申请号：PCT/US2004/008809
申请日：2004-03-22
申请人： AMGEN INC
发明人： DIPIETRO, Lucian V. , HARMANGE, Jean-Christophe , ASKEW, JR., Benny C. , ELBAUM, Daniel , GERMAIN, Julie , HABGOOD, Gregory J. , KIM, Joseph L. , PATEL, Vinod F. , POTASHMAN, Michele , VAN DER PLAS, Simon
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D235/30 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The invention relates to compounds of the formulae (I) to (III) wherein the substituents are as defined in the specification. These compounds have kinase inhibitory activity, such as VEGFR/KDR inhibitory activity. Accordingly, the compounds of the formulae (I) to (III) would be useful in the prevention and treatment of angiogenesis related disorders, ophthalmological conditions, proliferative diseases, inflammatory diseases, and other pathological conditions as described in the specification.
摘要翻译：本发明涉及式（I）至（III）的化合物，其中取代基如说明书中所定义。这些化合物具有激酶抑制活性，例如VEGFR / KDR抑制活性。因此，式（I）至（III）的化合物可用于预防和治疗血管发生相关疾病，眼科病症，增殖性疾病，炎性疾病和其他病理状况，如本说明书所述。

6. 发明申请

WO2004007458A1 SUBSTITUTED 2-ALKYLAMINE NICOTINIC AMIDE DERIVATIVES AND USE THERE OF 审中-公开
标题翻译：取代的2-烷基胺丁基胺衍生物及其用途
公开(公告)号：WO2004007458A1
公开(公告)日：2004-01-22
申请号：PCT/US2003/022417
申请日：2003-07-15
申请人： AMGEN INC.
发明人： ASKEW, Benny , ADAMS, Jeffrey , BOOKER, Shon , CHEN, Guoqing , DIPIETRO, Lucian, V. , ELBAUM, Daniel , GERMAIN, Julie , GEUNS-MEYER, Stephanie, D. , HABGOOD, Gregory, J. , HANDLEY, Michael , HUANG, Qi , KIM, Tae-Seong , LI, Aiwen , NISHIMURA, Nobuko , NOMAK, Rana , PATEL, Vinod, F. , RIAHI, Babak , KIM, Joseph, L. , XI, Ning , YANG, Kevin , YUAN, Chester, Chenguang
IPC分类号： C07D213/82
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Selected amines of Formula XIII, which are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选择的式XIII的胺可有效预防和治疗诸如血管生成介导的疾病等疾病。本发明包括新的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

7. 发明申请

WO2002068406A2 SUBSTITUTED AMINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的胺衍生物及其用于治疗血液生成的用途
公开(公告)号：WO2002068406A2
公开(公告)日：2002-09-06
申请号：PCT/US2002/003064
申请日：2002-01-11
申请人： AMGEN INC.
发明人： CHEN, Guoqing , ADAMS, Jeffrey , BEMIS, Jean , CROGHAN, Michael , DIPIETRO, Lucian , DOMINGUEZ, Celia , ELBAUM, Daniel , GERMAIN, Julie , HUANG, Qi , KIM, Joseph, L. , OUYANG, Xiaohu , PATEL, Vinod, F. , SMITH, Leon, M. , TASKER, Andrew , XI, Ning , XU, Shimin , YUAN, Chester, Chenguang , KIM, Tae-Seong
IPC分类号： C07D401/00
CPC分类号： C07D401/14 , A61K31/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , Y02A50/401
摘要： Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：式（I）的选择的胺对预防和治疗诸如血管生成介导的疾病等疾病是有效的。本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

8. 发明申请

WO2005021532A1 SUBSTITUTED 2,3-DIHYDRO-1H-ISOINDOL-1-ONE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的2,3-二氢-1H-茚-1-酮衍生物及其使用方法
公开(公告)号：WO2005021532A1
公开(公告)日：2005-03-10
申请号：PCT/US2004/027595
申请日：2004-08-25
申请人： AMGEN INC
发明人： TEGLEY, Christopher , ADAMS, Jeffrey, A. , ASKEW, Benny C., Jr. , CROGHAN, Michael , ELBAUM, Daniel , GERMAIN, Julie , HABGOOD, Gregory, J. , HARRIED, Scott , LI, Aiwen , NISHIMURA, Nobuko , NOMAK, Rana , TASKER, Andrew , YANG, Kevin
IPC分类号： C07D401/12
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。本发明包括新的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

9. 发明申请

WO2002066470A1 SUBSTITUTED ALKYLAMINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：取代的烷基胺衍生物及其使用方法
公开(公告)号：WO2002066470A1
公开(公告)日：2002-08-29
申请号：PCT/US2002/000743
申请日：2002-01-11
申请人： AMGEN INC.
发明人： CHEN, Guoqing , ADAMS, Jeffrey , BEMIS, Jean , BOOKER, Shon , CAI, Guolin , CROGHAN, Michael , DIPIETRO, Lucian , DOMINGUEZ, Celia , ELBAUM, Daniel , GERMAIN, Julie , GEUNS-MEYER, Stephanie , HANDLEY, Michael , HUANG, Qi , KIM, Joseph, L. , KIM, Tae-Seong , KISELYOV, Alexander , OUYANG, Xiaohu , PATEL, Vinod, F. , SMITH, Leon, M. , STEC, Markian , TASKER, Andrew , XI, Ning , XU, Shimin , YUAN, Chester, Chenguang
IPC分类号： C07D409/12
CPC分类号： C07D213/82 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/00 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选择的杂环化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

10. 发明授权

EP1664027B1 SUBSTITUTED 2,3-DIHYDRO-1H-ISOINDOL-1-ONE DERIVATIVES AND METHODS OF USE 有权
标题翻译：取代的2,3-二氢-1H-异吲哚-1-酮衍生物及其使用方法
公开(公告)号：EP1664027B1
公开(公告)日：2009-12-30
申请号：EP04782152.5
申请日：2004-08-25
申请人： AMGEN INC.
发明人： TEGLEY, Christopher , ADAMS, Jeffrey, A. , ASKEW, Benny, C., Jr. , CROGHAN, Michael , ELBAUM, Daniel , GERMAIN, Julie , HABGOOD, Gregory, J. , HARRIED, Scott , LI, Aiwen , NISHIMURA, Nobuko , NOMAK, Rana Bogazici University , TASKER, Andrew , YANG, Kevin
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4427 , A61K31/4035 , A61K31/47 , A61P29/00 , A61P35/00
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

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