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61. 发明授权

US06730783B2 Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：制备氨基胍和烷氧基胍作为蛋白酶抑制剂的方法
公开(公告)号：US06730783B2
公开(公告)日：2004-05-04
申请号：US10419972
申请日：2003-04-22
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan
IPC分类号： A61K31255
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. 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, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。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，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

62. 发明授权

US06706765B2 Aminoguanidines and alkoxyguanidines as protease inhibitors 有权
标题翻译：氨基胍和烷氧基胍作为蛋白酶抑制剂
公开(公告)号：US06706765B2
公开(公告)日：2004-03-16
申请号：US10359078
申请日：2003-02-06
申请人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
发明人： Bruce E. Tomczuk , Richard M. Soll , Tianbao Lu , Cynthia L. Fedde , Carl R. Illig , Thomas P. Markotan , Thomas P. Stagnaro
IPC分类号： A61K3118
CPC分类号： C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07C311/16 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/21 , C07C317/14 , C07C323/66 , C07C2601/02 , C07C2601/14 , C07D211/96 , C07D213/42 , C07D213/74 , C07D215/36 , C07D217/02 , C07D217/22 , C07D239/42 , C07D295/13 , C07D295/26 , C07D307/66
摘要： Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. 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, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents.
摘要翻译：氨基胍和烷氧基胍化合物，包括下式的化合物：其中X是O或NR 9和R 1 -R 4，R 6 -R 9，R 11，R 12，说明书中列出的R a，R b，R c，Y，Z，n和m以及抑制蛋白水解酶如凝血酶的水合物，溶剂合物或其药学上可接受的盐是描述。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，凝血酶，纤溶酶和因子Xa。某些化合物通过直接，选择性抑制凝血酶表现出抗血栓形成活性，或者是用于形成具有抗血栓形成活性的化合物的中间体。本发明包括用于抑制血小板损失，抑制血小板聚集体形成，抑制纤维蛋白形成，抑制血栓形成和抑制哺乳动物栓塞形成的组合物，其包含本发明化合物在药学上可接受的载体中。本发明化合物的其它用途是作为凝血剂或者物理上连接于用于血液收集，血液循环和血液储存（例如导管，血液透析机，采血注射器和管）中使用的装置的制造中使用的材料的抗凝剂，血线和支架。

63. 发明授权

US5643552A Nanoparticulate diagnostic mixed carbonic anhydrides as x-ray contrast agents for blood pool and lymphatic system imaging 失效
标题翻译：纳米颗粒诊断混合碳酸酐作为血液和淋巴系统成像的x射线造影剂
公开(公告)号：US5643552A
公开(公告)日：1997-07-01
申请号：US524145
申请日：1995-08-22
申请人： Carl R. Illig
发明人： Carl R. Illig
IPC分类号： A61K49/04 , C07C271/02 , C07C69/96 , C07C63/68
CPC分类号： A61K49/0433 , Y10S977/773 , Y10S977/775 , Y10S977/927 , Y10S977/928
摘要： This invention relates to methods of x-ray diagnostic imaging the blood pool, liver, spleen, and/or lymph system of a mammal comprising administering a contrast effective amount of a mixed carbonic anhydride as a contrast agent having the structure ##STR1## X is H, NR.sup.1 R.sup.2 or CONR.sup.1 R.sup.3, R.sup.1 is H or alkylR.sup.2 is COR.sup.3R.sup.3 is H, alkyl, hydroxyl-substituted alkyl, aryl or a steroidially derived moietyY is NR.sup.1 R.sup.2 or CONR.sup.1 R.sup.3 and ##STR2## Z is OR.sup.3 or This invention further relates to novel mixed carbonic anhydride contrast agents having the above structure and to x-ray contrast compositions comprising such agents, and to methods of x-ray diagnostic imaging utilizing such agents.
摘要翻译：本发明涉及对哺乳动物的血液池，肝脏，脾脏和/或淋巴系统进行x射线诊断成像的方法，该方法包括施用对比有效量的具有结构kyl R2的造影剂的混合碳酸酐为COR3 R3 是H，烷基，羟基取代的烷基，芳基或类固醇衍生的部分Y是NR1R2或CONR1R3，并且Z是OR3，或本发明还涉及具有上述结构和x射线对比度的新型混合碳酸酐造影剂包含这些试剂的组合物以及利用这种试剂的X射线诊断成像方法。

64. 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。

65. 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。

66. 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。

67. 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。

68. 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.

69. 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。

70. 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.

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