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61. 发明授权

US5525327A Polymeric x-ray contrast compositions containing iodinated polymeric beads and microcrystaline cellulose 失效
标题翻译：含有碘化聚合物珠粒和微晶纤维素的聚合X射线对比组合物
公开(公告)号：US5525327A
公开(公告)日：1996-06-11
申请号：US227415
申请日：1994-04-14
申请人： Edward J. Baker , Robert W. Lee , Carl R. Illig , John L. Toner
发明人： Edward J. Baker , Robert W. Lee , Carl R. Illig , John L. Toner
IPC分类号： A61K49/04
CPC分类号： A61K49/0409 , A61K49/04 , A61K49/0404 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodinated polymeric, water-insoluble beads having a particle size of from about 0.01 to about 1000.mu. wherein said iodinated polymeric beads comprise a polymer containing repeating units of the formula (I) ##STR1## wherein A is a repeating organic unit in the backbone chain of the polymer; and X is an organic moiety containing or iodinated eromatic group and a hydrophilic group, said moiety having an iodine content within the range of from about 40 to about 80 weight percent based or the molecular weight of X, in a pharmaceutically acceptable carrier comprising a cellulose derivative.
摘要翻译：公开了用于口腔或逆行检查胃肠道的X射线造影剂组合物，其包含粒径为约0.01至约1000μm的碘化聚合物，水不溶性珠粒，其中所述碘化聚合物珠粒包含含有式（I）其中A是聚合物的主链中的重复有机单元; 并且X是含有或碘化的丙烯酸基团和亲水基团的有机部分，所述部分在药学上可接受的载体中具有在约40至约80重量％的范围内或基于X的分子量的碘含量，其包含纤维素衍生物。

62. 发明授权

US5476644A Cyclic triamine chelating agents 失效
标题翻译：环状三胺螯合剂
公开(公告)号：US5476644A
公开(公告)日：1995-12-19
申请号：US227161
申请日：1994-04-13
申请人： Carl R. Illig , Thomas J. Caulfield , John L. Toner , Peng Guo , David L. Ladd
发明人： Carl R. Illig , Thomas J. Caulfield , John L. Toner , Peng Guo , David L. Ladd
IPC分类号： A61K49/00 , A61K49/06 , C07C227/02 , C07C229/16 , C07C229/76 , C07C237/06 , C07C237/08 , C07C265/12 , C07C327/38 , C07C331/28 , C07F5/00 , C07F9/00 , C07F11/00 , C07F13/00 , C07F15/02 , C07F15/04 , C07F15/06 , C09K3/00 , A61K51/00 , A61K31/28
CPC分类号： A61K49/06 , C07C229/16 , C07C2101/14
摘要： The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.20);n is 1 or 2;m is 1 to 15;X is a targeting moiety; andAr is phenyl optionally substituted with one, two or three substituents selected from the group consisting of amino, acylamino, hydroxy, alkyl (C1-C5) and halogen.
摘要翻译：本发明提供了与顺磁金属离子螯合的式“IMAGE”化合物，其中Z 1和Z 2各自表示完成单环或多环碳环或杂环系统所必需的原子，所述Z 1和Z 2独立地任选地被R6和R7取代，分别; R1，R2，R3和R4独立地是羧基烷基（C1-C2）， - （CH2）nC（= O）-NH-R8或 - （CH2）nC（= O）-O-R8 R5是羧基烷基 C2）; R6和R7独立地是氢，苄基或苄氧基，所述苄基或苄氧基任选地被一个，两个或三个选自氨基，异氰酸酯基（-N = C = O），异硫氰酸酯（-N = C = S），-NH-C（= O）-X或-NH-C（= S）-X; R8是烷基（C1-C20）， - （CH2）m-Ar或多羟基烷基（C1-C20）; n为1或2; m为1〜15; X是靶向部分; 并且Ar是任选地被一个，两个或三个选自氨基，酰基氨基，羟基，烷基（C 1 -C 5）和卤素的取代基取代的苯基。

63. 发明授权

US5360604A X-ray contrast compositions containing an organic crystalline X-ray contrast agent in combination with pharmaceutically acceptable clays 失效
标题翻译：含有有机结晶X射线造影剂与药学上可接受的粘土组合的X射线造影剂组合物
公开(公告)号：US5360604A
公开(公告)日：1994-11-01
申请号：US247424
申请日：1994-05-23
申请人： Stephen B. Ruddy , Mary E. Roberts , Gregory L. McIntire , Eugene R. Cooper , Carl R. Illig
发明人： Stephen B. Ruddy , Mary E. Roberts , Gregory L. McIntire , Eugene R. Cooper , Carl R. Illig
IPC分类号： A61K49/04
CPC分类号： A61K49/0404 , A61K49/0409 , A61K49/0433 , A61K49/0461 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a crystalline organic constrast agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
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，其包含与药学上可接受的载体中的药学上可接受的粘土结合的结晶有机对比剂; 以及它们用于胃肠道诊断放射学的方法。

64. 发明授权

US5312616A Compositions of iodobenzoic acid derivatives in film-forming materials for visualization of the gastrointestinal tract 失效
标题翻译：碘苯甲酸衍生物在用于胃肠道可视化的成膜材料中的组合物
公开(公告)号：US5312616A
公开(公告)日：1994-05-17
申请号：US29756
申请日：1993-03-11
申请人： Carl R. Illig , Brent D. Douty
发明人： Carl R. Illig , Brent D. Douty
IPC分类号： A61K47/30 , A61K49/04 , C08K5/07 , A61K31/075 , A61K31/235 , A61K31/715
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## wherein Z=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=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxycarbonyloxy, (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 lower-alkyl, optionally substituted with halo;x is 1-3y is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
摘要翻译：公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物，其包含能够在胃肠道上形成涂层的聚合物材料和下式的X射线产生剂，其中Z = H，卤素，C1 -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; 任选被卤素，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 - 烷氧基羰基氧基取代的C 1 -C 25烷基，环烷基或卤代低级烷基，（CR 1 R 2）p - （CR3 = CR4）mQ，或（CR1R2）pC 3BOND CQ; R 1，R 2，R 3和R 4独立地为低级烷基，任选被卤素取代; x为1-3 y为1-4; n为1-5; m为1-15; p为1-10; 并且Q是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。

65. 发明授权

US5068345A Oxazolidinone aldol adduct 失效
标题翻译：恶唑烷酮醛醇加合物
公开(公告)号：US5068345A
公开(公告)日：1991-11-26
申请号：US428800
申请日：1989-10-30
申请人： Carl R. Illig , Alexander L. Weis
发明人： Carl R. Illig , Alexander L. Weis
IPC分类号： C07D263/26
CPC分类号： C07D263/26
摘要： A oxazolidinone aldol adduct having the formula: ##STR1## wherein R is alkyl having 6 or more carbons or aryl; R.sup.1 is alkyl or aryl; R.sup.2 is alkyl, aryl or hydrogen; and X is a halogen atom or an azide. This aldol adduct is useful in a process for making 2-amino-1,3 diols.
摘要翻译：具有下式的恶唑烷酮醛醇加合物：其中R是具有6个或更多个碳原子的烷基或芳基; R1是烷基或芳基; R2是烷基，芳基或氢; X是卤素原子或叠氮化物。该醛醇加合物可用于制备2-氨基-1,3-二醇的方法。

66. 发明授权

US08859602B2 Inhibitors of c-fms kinase 有权
公开(公告)号：US08859602B2
公开(公告)日：2014-10-14
申请号：US11736644
申请日：2007-04-18
申请人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Bruce E. Tomczuk , Mark Wall , Kenneth Wilson
发明人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Renee Louise DesJarlais , Sanath K. Meegalla , Bruce E. Tomczuk , Mark Wall , Kenneth Wilson
IPC分类号： A61K31/4178 , C07D405/12 , C07D207/34 , C07D413/14 , C07D401/12 , C07D233/90 , C07D405/14 , C07D401/14 , C07D493/08 , C07D413/12 , C07D409/12
CPC分类号： C07D409/12 , C07D207/34 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D493/08 , C12N9/99
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.

67. 发明授权

US08722718B2 Inhibitors of C-FMS kinase 有权
标题翻译： C-FMS激酶抑制剂
公开(公告)号：US08722718B2
公开(公告)日：2014-05-13
申请号：US11736650
申请日：2007-04-18
申请人： Carl R. Illig , Jinsheng Chen , Renee Louise DesJarlais , Kenneth Wilson
发明人： Carl R. Illig , Jinsheng Chen , Renee Louise DesJarlais , Kenneth Wilson
IPC分类号： A61K31/4178 , C07D407/12
CPC分类号： C07D409/12 , C07D207/34 , C07D233/90 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D493/08 , C12N9/99
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。

68. 发明授权

US08481564B2 Inhibitors of c-fms kinase 有权
公开(公告)号：US08481564B2
公开(公告)日：2013-07-09
申请号：US13080861
申请日：2011-04-06
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： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/549 , A61K31/506 , A61K31/4545 , A61K31/444
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.

69. 发明申请

US20110195960A1 INHIBITORS OF C-FMS KINASE 有权
标题翻译： C-FMS激酶抑制剂
公开(公告)号：US20110195960A1
公开(公告)日：2011-08-11
申请号：US13080861
申请日：2011-04-06
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 , C07D403/12 , A61K31/506 , C07D417/14 , C07D401/14 , A61K31/4545 , A61K31/444 , C07D401/12 , A61K31/443 , A61K31/4178 , A61P35/00 , A61P29/00 , A61P9/00 , A61P1/00 , A61P11/00 , A61P25/28 , A61P25/18 , A61P19/00 , C12N9/99
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。

70. 发明授权

US07705042B2 Class of arylamide compounds useful as inhibitors of c-fms kinase 有权
标题翻译：可用作c-fms激酶抑制剂的芳酰胺化合物类
公开(公告)号：US07705042B2
公开(公告)日：2010-04-27
申请号：US11255043
申请日：2005-10-20
申请人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Sanath Meegalla , Jonathan Rudolph , Mark J. Wall , Kenneth J. Wilson , Renee DesJarlais , Carl L. Manthey , Christopher M. Flores , Christopher J. Molloy
发明人： Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Sanath Meegalla , Jonathan Rudolph , Mark J. Wall , Kenneth J. Wilson , Renee DesJarlais , Carl L. Manthey , Christopher M. Flores , Christopher J. Molloy
IPC分类号： A61K31/34
CPC分类号： C07D263/34 , C07D207/34 , C07D233/90 , C07D307/68 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12
摘要： The invention relates to arylamide and hetereoarylamide compounds of Formula I: wherein A, X, R2 and W are set forth in the specification, as well as 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, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; 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 arthritis, 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的芳基酰胺和hetereoarylamide化合物：其中A，X，R 2和W在说明书中列出，以及其互变异构体和药学上可接受的盐，其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，结肠癌，胃癌，毛细胞白血病和非小细胞肺癌的转移; 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; 还提供了骨质疏松症，佩吉特氏病和其它骨吸收介导关节炎，假体失败，溶骨性骨肉瘤，骨髓瘤以及与式I化合物对骨的肿瘤转移的其它疾病。

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