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1. 发明授权

US07973035B2 Inhibitors of C-FMS kinase 有权
标题翻译： C-FMS激酶抑制剂
公开(公告)号：US07973035B2
公开(公告)日：2011-07-05
申请号：US12139876
申请日：2008-06-16
申请人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
发明人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
IPC分类号： A61K31/54 , A61K31/505 , C07D285/16 , C07D239/02
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
摘要翻译：本发明涉及式I化合物：其中Z，X，J，R 2和W在本说明书中列出，以及其抑制蛋白酪氨酸激酶，特别是c-型的溶剂化物，水合物，互变异构体和药学上可接受的盐， fms激酶。治疗自身免疫性疾病的方法和具有炎症成分的疾病; 治疗卵巢癌，子宫癌，乳腺癌，前列腺癌，肺癌，结肠癌，胃癌，毛细胞白血病的转移; 并治疗疼痛，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏，炎症和神经源性疼痛; 骨质疏松症，佩吉特氏病和其他疾病，其中骨吸收介导包括类风湿性关节炎和其它形式的炎症性关节炎，骨关节炎，假体衰竭，溶骨性肉瘤，骨髓瘤和肿瘤转移至骨骼的发病率与式I化合物，也提供。

2. 发明授权

US07795279B2 Method of inhibiting FLT3 kinase 有权
标题翻译：抑制FLT3激酶的方法
公开(公告)号：US07795279B2
公开(公告)日：2010-09-14
申请号：US11550077
申请日：2006-10-17
申请人： Shelley K. Ballentine , Christian Andrew Baumann , Jinsheng Chen , Carl R. Illig , Sanath K. Meegalla , M. Jonathan Rudolph , Robert W. Tuman , Mark J. Wall , Kenneth Wilson , Dana L. Johnson
发明人： Shelley K. Ballentine , Christian Andrew Baumann , Jinsheng Chen , Carl R. Illig , Sanath K. Meegalla , M. Jonathan Rudolph , Robert W. Tuman , Mark J. Wall , Kenneth Wilson , Dana L. Johnson
IPC分类号： A61K31/445 , C07D293/10
CPC分类号： A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/5355 , Y10S514/908
摘要： A method of reducing or inhibiting kinase activity of FLT3 in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：降低或抑制细胞或受试者中FLT3的激酶活性的方法，以及使用本发明的化合物，在受试者中预防或治疗细胞增殖性病症和/或与FLT3有关的病症的用途：或其溶剂合物，水合物，互变异构体或其药学上可接受的盐。本发明还涉及治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

3. 发明申请

US20080275031A1 Inhibitors of C-FMS Kinase 有权
标题翻译： C-FMS激酶抑制剂
公开(公告)号：US20080275031A1
公开(公告)日：2008-11-06
申请号：US12139876
申请日：2008-06-16
申请人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
发明人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
IPC分类号： A61K31/549 , C07D401/12 , C07D285/16 , A61K31/506 , A61P35/00 , A61P25/00 , A61P37/00 , A61P35/04 , A61P9/00 , A61P29/00 , C07D239/04 , A61K31/454
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
摘要翻译：本发明涉及式I化合物：其中Z，X，J，R 2和W在本说明书中列出，以及溶剂合物，水合物，互变异构体及其药学上可接受的盐，其中抑制蛋白酪氨酸激酶，特别是c-fms激酶。治疗自身免疫性疾病的方法和具有炎症成分的疾病; 治疗卵巢癌，子宫癌，乳腺癌，前列腺癌，肺癌，结肠癌，胃癌，毛细胞白血病的转移; 并治疗疼痛，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏，炎症和神经源性疼痛; 骨质疏松症，佩吉特氏病和其他疾病，其中骨吸收介导包括类风湿性关节炎和其它形式的炎症性关节炎，骨关节炎，假体衰竭，溶骨性肉瘤，骨髓瘤和肿瘤转移至骨骼的发病率与式I化合物，也提供。

4. 发明授权

US07414050B2 Inhibitors of c-fms kinase 有权
标题翻译： c-fms激酶抑制剂
公开(公告)号：US07414050B2
公开(公告)日：2008-08-19
申请号：US11736617
申请日：2007-04-18
申请人： Carl R. Illig , Shelly K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
发明人： Carl R. Illig , Shelly K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Mark Wall , Kenneth Wilson
IPC分类号： C07D417/04 , C07D417/14 , A61K31/541
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
摘要翻译：本发明涉及式I化合物：其中Z，X，J，R 2和W在本说明书中列出，以及溶剂合物，水合物，互变异构体及其药学上可接受的盐，其中抑制蛋白酪氨酸激酶，特别是c-fms激酶。治疗自身免疫性疾病的方法和具有炎症成分的疾病; 治疗卵巢癌，子宫癌，乳腺癌，前列腺癌，肺癌，结肠癌，胃癌，毛细胞白血病的转移; 并治疗疼痛，包括由肿瘤转移或骨关节炎引起的骨骼疼痛，或内脏，炎症和神经源性疼痛; 骨质疏松症，佩吉特氏病和其他疾病，其中骨吸收介导包括类风湿性关节炎和其它形式的炎症性关节炎，骨关节炎，假体衰竭，溶骨性肉瘤，骨髓瘤和肿瘤转移至骨骼的发病率与式I化合物，也提供。

5. 发明授权

US06562840B1 Heteroaryl amidines, methylamidines and guanidines, and the use thereof as protease inhibitors 失效
标题翻译：杂芳基脒，甲脒和胍，以及其作为蛋白酶抑制剂的用途
公开(公告)号：US06562840B1
公开(公告)日：2003-05-13
申请号：US10082127
申请日：2002-02-26
申请人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
发明人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
IPC分类号： A61K3147
CPC分类号： C07D409/04 , C07D333/38 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1—R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
摘要翻译：本发明涉及式I化合物：其中X是O，S或NR 7，R 1 -R 7，Y和Z在说明书中列出，以及其水合物，溶剂合物或其药学上可接受的盐。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，纤溶酶和尿激酶。某些化合物表现出对尿激酶的直接选择性抑制，或者是用于形成具有这种活性的化合物的中间体。

6. 发明授权

US06515002B2 Compounds and compositions for treating C1s-mediated diseases and conditions 有权
标题翻译：用于治疗C1s介导的疾病和病症的化合物和组合物
公开(公告)号：US06515002B2
公开(公告)日：2003-02-04
申请号：US09962304
申请日：2001-09-26
申请人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Roger F. Bone , Scott L. Klein , Troy L. Randle
发明人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Roger F. Bone , Scott L. Klein , Troy L. Randle
IPC分类号： C07D41718
CPC分类号： C07D409/04 , A61K31/427 , C07D333/38 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of Formula I or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R1, R2, R3, R4, X, Y and Z are defined in the specification.
摘要翻译：公开了一种治疗由补体级联的经典途径介导的急性或慢性障碍的症状的方法，其包括向需要这种治疗的哺乳动物施用治疗有效量的式I化合物或溶剂合物，水合物或药学上其可接受的盐; 其中R1，R2，R3，R4，X，Y和Z在说明书中定义。

7. 发明授权

US06403633B2 Heteroaryl amidines, methylamidines and guanidines, and use thereof as protease inhibitors 失效
标题翻译：杂芳基脒，甲脒和胍，以及其作为蛋白酶抑制剂的用途
公开(公告)号：US06403633B2
公开(公告)日：2002-06-11
申请号：US09828783
申请日：2001-04-10
申请人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
发明人： Carl R. Illig , Nalin L. Subasinghe , James B. Hoffman , Kenneth J. Wilson , M. Jonathan Rudolph , Juan José Marugán
IPC分类号： A61K3138
CPC分类号： C07D409/04 , C07D333/38 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention is directed to compounds of Formula I: wherein X is O, S or NR7 and R1-R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
摘要翻译：本发明涉及式I化合物：其中X是O，S或NR 7，R 1 -R 7，Y和Z在说明书中列出，以及其水合物，溶剂合物或其药学上可接受的盐。还描述了制备式I化合物的方法。本发明的新化合物是蛋白酶的有效抑制剂，特别是胰蛋白酶样丝氨酸蛋白酶，例如胰凝乳蛋白酶，胰蛋白酶，纤溶酶和尿激酶。某些化合物表现出对尿激酶的直接选择性抑制，或者是用于形成具有这种活性的化合物的中间体。

8. 发明授权

US06281206B1 Amidino protease inhibitors 有权
公开(公告)号：US06281206B1
公开(公告)日：2001-08-28
申请号：US09502005
申请日：2000-02-11
申请人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
发明人： Tianbao Lu , Bruce E. Tomczuk , Carl R. Illig , Richard M. Soll
IPC分类号： A61K31445
CPC分类号： C07D295/195 , C07C309/73 , C07C311/21 , C07D211/22 , C07D211/26
摘要： Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.

9. 发明授权

US5422114A Compositions of iodoaniline derivatives and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：用于可视化胃肠道的碘苯胺衍生物和纤维素衍生物的组合物
公开(公告)号：US5422114A
公开(公告)日：1995-06-06
申请号：US201731
申请日：1994-02-25
申请人： Carl R. Illig , Thomas J. Caulfield , Robert W. Lee , Edward J. Baker
发明人： Carl R. Illig , Thomas J. Caulfield , Robert W. Lee , Edward J. Baker
IPC分类号： A61K9/107 , A61K49/04 , C08K5/315 , C08L101/00 , C08L101/06 , G01N21/00
CPC分类号： A61K49/0404 , A61K49/0409 , A61K49/0461
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract, whereinZ is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl and halo lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy and said acetyl is optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;n is 1-4;y is 1-4; andx is 1 or 2in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了用于胃肠道口服或逆行检查的x射线造影剂组合物，其包含下式的x射线产生剂或其药学上可接受的盐及其用于胃肠道诊断放射学的方法，其中Z 是H，卤素，C 1 -C 20烷基，环烷基，低级烷氧基，氰基，其中烷基和环烷基可被卤素或卤代低级烷基取代; R 1和R 2独立地为H，C 1 -C 25烷基，环烷基，乙酰基或卤代低级烷基，其中所述C 1 -C 25烷基，环烷基和卤代低级烷基任选被氟 - 低级 - 烷基，芳基，低级 - 烷氧基，羟基，羧基，低级烷氧基羰基或低级烷氧基 - 羰氧基，所述乙酰基任选被氟 - 低级 - 烷基，芳基，低级 - 烷氧基，羟基，低级 - 烷氧基羰基或低级 - 烷氧基 - 羰氧基取代; n为1-4; y为1-4; 并且在包含纤维素衍生物的药学上可接受的载体中x为1或2。

10. 发明授权

US5385721A Compositions of alkylbenzenes and cellulose derivatives for visualization of the gastrointestinal tract 失效
标题翻译：用于胃肠道可视化的烷基苯和纤维素衍生物的组合物
公开(公告)号：US5385721A
公开(公告)日：1995-01-31
申请号：US217138
申请日：1994-03-22
申请人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
发明人： Edward J. Baker , Kurt A. Josef , Edward R. Bacon , Kimberly G. Estep , Carl R. Illig , Brent D. Douty , John L. Toner , Robert W. Lee
IPC分类号： A61K49/00 , A61K49/04 , C07C17/00 , C07C17/12 , C07C17/26 , C07C25/02 , C07C25/13 , C07C25/24 , C07C33/46 , C07C43/225 , C07C69/65 , C07C69/76 , C07C69/92 , A61K31/715 , A61K31/02
CPC分类号： C07C17/354 , A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0433 , C07C17/12 , C07C17/2635 , C07C25/02 , C07C25/24 , C07C69/65
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## wherein R is methyl, ethyl, n-propyl, C.sub.4 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 2-5;m is 2-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含下式的x射线产生剂或其药学上可接受的盐，其中R是甲基，乙基，正丙基，C 4 -C 25烷基，环烷基，不饱和烯丙基或卤代低级烷基，其各自可以任选被卤素，氟代低级烷基，芳基，低级烷氧基，羟基，羧基或低级烷氧基羰基取代; （CR 1 R 2）p - （CR 3 = CR 4）m Q或（CR 1 R 2）p -C 3OND C-Q; R 1，R 2，R 3和R 4独立地为H，低级烷基，任选被卤素取代; n为2-5; m为2-5; p为1-10; Q为H，低级烷基，低级烯基，低级炔基，低级亚烷基，芳基或芳基 - 低级烷基; 在包含纤维素衍生物的可药用载体中。

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