公开(公告)号：US20080051402A1

公开(公告)日：2008-02-28

申请号：US11737517

申请日：2007-04-19

申请人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Molloy

发明人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Molloy

IPC分类号： A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00

CPC分类号： A61K31/5377 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D307/68 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C12N9/99

摘要： A method of reducing or inhibiting kinase activity of C-KIT 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 C-KIT 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C-KIT的激酶活性的方法，以及使用这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与C-KIT相关的病症的方法， 本发明：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。

公开(公告)号：US20060189623A1

公开(公告)日：2006-08-24

申请号：US11408096

申请日：2006-04-20

申请人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Flores ,  Christopher Molloy

发明人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Flores ,  Christopher Molloy

IPC分类号： A61K31/496 ,  C07D409/02 ,  A61K31/4545 ,  A61K31/454

CPC分类号： C07D307/71 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

摘要： The invention is directed to compounds of Formula I: wherein A, X, 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, 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.

公开(公告)号：US20060100201A1

公开(公告)日：2006-05-11

申请号：US11255043

申请日：2005-10-20

申请人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Jonathan Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee DesJarlais ,  Carl Manthey ,  Christopher Flores ,  Christopher Molloy

发明人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Jonathan Rudolph ,  Mark Wall ,  Kenneth Wilson ,  Renee DesJarlais ,  Carl Manthey ,  Christopher Flores ,  Christopher Molloy

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14

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 compounds of Formula I: wherein A, X, 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, 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化合物：其中A，X，R 2和W在本说明书中列出，以及其抑制蛋白酪氨酸的溶剂合物，水合物，互变异构体和药学上可接受的盐 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包括关节炎，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。

公开(公告)号：US20060148812A1

公开(公告)日：2006-07-06

申请号：US11254276

申请日：2005-10-20

申请人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolf ,  Mark Wall ,  Ken Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Flores ,  Chris Molloy

发明人： Carl Illig ,  Shelley Ballentine ,  Jinsheng Chen ,  Sanath Meegalla ,  M. Rudolf ,  Mark Wall ,  Ken Wilson ,  Renee Desjarlais ,  Carl Manthey ,  Christopher Flores ,  Chris Molloy

IPC分类号： A61K31/496 ,  A61K31/4545 ,  C07D409/14 ,  A61K31/4178

CPC分类号： C07D307/71 ,  C07D401/12 ,  C07D401/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14

摘要： The invention is directed to compounds of Formula I: wherein A, X, 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, 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化合物：其中A，X，R 2和W在本说明书中列出，以及其抑制蛋白质的溶剂合物，水合物，互变异构体和药学上可接受的盐 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包括关节炎，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。

公开(公告)号：US20070149572A1

公开(公告)日：2007-06-28

申请号：US11550077

申请日：2006-10-17

申请人： Shelley Ballentine ,  Christian Baumann ,  Jinsheng Chen ,  Carl Illig ,  Sanath Meegalla ,  M. Rudolph ,  Robert Tuman ,  Mark Wall ,  Kenneth Wilson ,  Dana Johnson

发明人： Shelley Ballentine ,  Christian Baumann ,  Jinsheng Chen ,  Carl Illig ,  Sanath Meegalla ,  M. Rudolph ,  Robert Tuman ,  Mark Wall ,  Kenneth Wilson ,  Dana Johnson

IPC分类号： A61K31/454

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 ompound 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： 一种减少或抑制细胞或受试者中FLT3的激酶活性的方法，以及使用本发明的方法使用这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3相关的病症：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。

公开(公告)号：US20050234081A1

公开(公告)日：2005-10-20

申请号：US10515554

申请日：2003-05-28

申请人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi Leonard ,  Farah Ali ,  Heather Hufnagel ,  Jeremy Travins ,  Shelley Ballentine ,  Kenneth Wilson ,  Maxwell Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen

发明人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi Leonard ,  Farah Ali ,  Heather Hufnagel ,  Jeremy Travins ,  Shelley Ballentine ,  Kenneth Wilson ,  Maxwell Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen

IPC分类号： C07D333/22 ,  A61K31/381 ,  A61K31/404 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/422 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4535 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/662 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P5/48 ,  A61P7/00 ,  A61P7/06 ,  A61P7/08 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/02 ,  A61P13/12 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/10 ,  A61P21/04 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P37/00 ,  A61P37/06 ,  A61P37/08 ,  A61P41/00 ,  A61P43/00 ,  C07D333/12 ,  C07D333/38 ,  C07D333/54 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04 ,  C07F7/08 ,  C07F7/10 ,  C07F9/6553 ,  C07D49/02

CPC分类号： C07D417/12 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D495/04 ,  C07F7/0812 ,  C07F9/655345

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 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.

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病症症状的方法，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， 水合物或其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7， 在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。

公开(公告)号：US20050049274A1

公开(公告)日：2005-03-03

申请号：US10894940

申请日：2004-07-20

申请人： Mark Wall ,  Mark Player ,  Raymond Patch ,  Sanath Meegalla ,  Jian Liu ,  Carl Illig ,  Wing Cheung ,  Jinsheng Chen ,  Davoud Asgari

发明人： Mark Wall ,  Mark Player ,  Raymond Patch ,  Sanath Meegalla ,  Jian Liu ,  Carl Illig ,  Wing Cheung ,  Jinsheng Chen ,  Davoud Asgari

IPC分类号： A61P35/00 ,  C07D215/22 ,  C07D215/227 ,  C07D401/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D471/02 ,  A61K31/47 ,  C07D215/36

CPC分类号： C07D215/227 ,  C07D401/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  Y02P20/582

摘要： The invention is directed to compounds of Formulae I and II: wherein R1, R2, R3, R5, R6, Y1, Y2, Y3, Y4 and X are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.

摘要翻译： 本发明涉及式I和II的化合物：其中R 1，R 2，R 3，R 5，R 6，Y 1，Y 2， 3>，Y 4和X在说明书中列出，以及其抑制蛋白酪氨酸激酶，特别是c-fms激酶的溶剂合物，水合物，互变异构体或其药学上可接受的盐。

公开(公告)号：US07138530B2

公开(公告)日：2006-11-21

申请号：US10515554

申请日：2003-05-28

申请人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi A. Leonard ,  Farah Ali ,  Heather Hufnagel ,  Jeremy M. Travins ,  Shelley K. Ballentine ,  Kenneth T. Wilson ,  Maxwell D. Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen ,  Jonathan M. Rudolph ,  Hui Huang

发明人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi A. Leonard ,  Farah Ali ,  Heather Hufnagel ,  Jeremy M. Travins ,  Shelley K. Ballentine ,  Kenneth T. Wilson ,  Maxwell D. Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen ,  Jonathan M. Rudolph ,  Hui Huang

IPC分类号： C07D333/32 ,  A61K31/38

CPC分类号： C07D417/12 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D495/04 ,  C07F7/0812 ,  C07F9/655345

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 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.

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病症症状的方法，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， 水合物或其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7， 在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。

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。

公开(公告)号：US07109354B2

公开(公告)日：2006-09-19

申请号：US10445817

申请日：2003-05-28

申请人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi Leonard ,  Farah Ali ,  Heather Rae Hufnagel ,  Jeremy M. Travins ,  Shelley K. Ballentine ,  Kenneth T. Wilson ,  Maxwell D. Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen ,  M. Jonathan Rudolph ,  Hui Huang

发明人： Nalin Subasinghe ,  Ehab Khalil ,  Kristi Leonard ,  Farah Ali ,  Heather Rae Hufnagel ,  Jeremy M. Travins ,  Shelley K. Ballentine ,  Kenneth T. Wilson ,  Maxwell D. Cummings ,  Wenxi Pan ,  Joan Gushue ,  Sanath Meegalla ,  Mark Wall ,  Jinsheng Chen ,  M. Jonathan Rudolph ,  Hui Huang

IPC分类号： C07D333/02 ,  C07D333/32

CPC分类号： C07D417/12 ,  C07D333/38 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D495/04 ,  C07F7/0812 ,  C07F9/655345

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 and R7 are defined in the specification, Z is SO or SO2, and Ar is an aromatic or heteroaromatic group as defined herein.

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病症症状的方法，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 其药学上可接受的盐; 其中R 1，R 2，R 3，R 4和R 7， 在本说明书中定义，Z是SO或SO 2，Ar是如本文所定义的芳族或杂芳族基团。