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公开(公告)号:US09101635B2
公开(公告)日:2015-08-11
申请号:US13383345
申请日:2010-07-10
申请人: Arnab Basu , Debra M. Mills , Norton P. Peet , John D. Williams
发明人: Arnab Basu , Debra M. Mills , Norton P. Peet , John D. Williams
IPC分类号: A61K31/18 , A61K31/5513 , C07D213/74 , C07D215/40 , C07D243/12 , C07D249/10 , C07D307/71 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D471/04 , C07D491/22
CPC分类号: A61K31/5513 , A61K31/18 , C07D213/74 , C07D215/40 , C07D243/12 , C07D249/10 , C07D307/71 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D471/04 , C07D491/22 , A61K2300/00
摘要: Organic compounds showing the ability to inhibit viral glycoprotein (GP)-mediated entry of a filovirus into a host cell are disclosed. The disclosed filovirus entry inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by filovirus including the type species Marburg virus (MARV) and Ebola virus (EBOV). Preferred inhibitors of the invention provide therapeutic agents for combating the Ivory Coast, Sudan, Zaire, Bundibugyo, and Reston Ebola virus strains.
摘要翻译: 公开了显示抑制病毒糖蛋白(GP)介导的病毒入宿主细胞的能力的有机化合物。 所公开的叶病毒入侵抑制剂化合物可用于治疗,预防或减少包括类型物种马尔堡病毒(MARV)和埃博拉病毒(EBOV)的病毒感染的扩散。 本发明优选的抑制剂提供用于对抗科特迪瓦海岸,苏丹,扎伊尔,Bundibugyo和Reston埃博拉病毒毒株的治疗剂。
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公开(公告)号:US07645755B2
公开(公告)日:2010-01-12
申请号:US11408096
申请日:2006-04-20
申请人: Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Sanath K. Meegalla , M. Jonathan Rudolph , Mark J. Wall , Kenneth J. Wilson , Renee L. Desjarlais , Carl L. Manthey , Christopher Flores , Christopher J. Molloy
发明人: Carl R. Illig , Shelley K. Ballentine , Jinsheng Chen , Sanath K. Meegalla , M. Jonathan Rudolph , Mark J. Wall , Kenneth J. Wilson , Renee L. Desjarlais , Carl L. Manthey , Christopher Flores , Christopher J. Molloy
IPC分类号: A61K31/5377 , A61K31/454 , C07D413/14 , C07D401/02
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.
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公开(公告)号:US20070117852A1
公开(公告)日:2007-05-24
申请号:US10582040
申请日:2004-12-22
申请人: Markus Gewehr , Bernd Muller , Thomas Grote , Wassilios Grammenos , Jordi Tormo i Blasco , Anja Schwogler , Joachim Rheinheimer , Carsten Blettner , Peter Schafer , Frank Schieweck , Oliver Wagner , John-Bryan Speakman , Jan Rether , Siegfried Strathmann , Reinhard Stierl
发明人: Markus Gewehr , Bernd Muller , Thomas Grote , Wassilios Grammenos , Jordi Tormo i Blasco , Anja Schwogler , Joachim Rheinheimer , Carsten Blettner , Peter Schafer , Frank Schieweck , Oliver Wagner , John-Bryan Speakman , Jan Rether , Siegfried Strathmann , Reinhard Stierl
IPC分类号: A01N43/56 , A01N43/40 , A01N43/78 , C07D213/24
CPC分类号: C07D213/82 , A01N43/40 , A01N43/56 , A01N43/78 , A01N47/48 , C07C251/38 , C07D207/34 , C07D231/14 , C07D263/34 , C07D277/56 , C07D279/12 , C07D307/30 , C07D307/54 , C07D307/71 , C07D333/38
摘要: The present invention relates to (hetero)cyclylcarboxanilides of the formula I, in which n is 0, 1, 2, 3 or 4; and m is 1, 2 or 3, Y is oxygen or sulfur; A is unsubstituted or substituted phenyl or is an at least monounsaturated, unsubstituted or substituted 5- or 6-membered heterocycle, R1, R2, R3m, R4m, R5 and R6 are as defined in claim 1, and their agriculturally useful salts. Moreover, the present invention relates to the use of the (hetero)cyclylcarboxanilides of the formula I and their agriculturally useful salts as fungicides, and to crop protection compositions comprising these compounds.
摘要翻译: 本发明涉及式(I)的(杂)环己基甲酰苯胺,其中n为0,1,2,3或4; m为1,2或3,Y为氧或硫; A是未取代或取代的苯基,或至少是一个不饱和的,未取代的或取代的5元或6元杂环,R 1,R 2,R 3, R 4,R 5,R 5和R 6如权利要求1所定义,及其农业上有用的盐。 此外,本发明涉及式I的(杂)环己基甲酰苯胺及其农业上有用的盐作为杀真菌剂,以及包含这些化合物的作物保护组合物的用途。
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公开(公告)号:US07135487B2
公开(公告)日:2006-11-14
申请号:US10447619
申请日:2003-05-29
申请人: Macklin B Arnold , Stephen R Baker , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Hamideh Zarrinmayeh , Dennis M Zimmerman
发明人: Macklin B Arnold , Stephen R Baker , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Hamideh Zarrinmayeh , Dennis M Zimmerman
IPC分类号: A61K31/44 , C07D213/06 , C07D333/12 , C07C255/03 , C07C303/00
CPC分类号: A61K31/18 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/4418 , A61K31/451 , A61K31/455 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/14 , C07C311/16 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/277 , C07D211/18 , C07D211/28 , C07D213/42 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/68 , C07D409/04
摘要: The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
摘要翻译: 本发明涉及新型磺酰胺衍生物,其制备方法和含有它们的药物组合物。
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公开(公告)号:US07067538B2
公开(公告)日:2006-06-27
申请号:US10442917
申请日:2003-05-21
申请人: Larry D. Bratton , Alexander J. Bridges , David T. Connor , Steven R. Miller , Yuntao Song , Kuai-Lin Sun , Bharat K. Trivedi , Paul C. Unangst
发明人: Larry D. Bratton , Alexander J. Bridges , David T. Connor , Steven R. Miller , Yuntao Song , Kuai-Lin Sun , Bharat K. Trivedi , Paul C. Unangst
CPC分类号: C07C311/03 , C07C311/27 , C07C317/18 , C07C317/24 , C07C317/28 , C07C317/44 , C07D213/50 , C07D233/64 , C07D239/26 , C07D261/08 , C07D263/32 , C07D277/10 , C07D277/26 , C07D307/46 , C07D307/71 , C07D307/80 , C07D333/22 , C07D333/38 , C07D333/44 , C07D413/04
摘要: The present invention relates to sulfones that are useful in the treatment of chemokine-mediated disorders. In certain embodiments, the present invention concerns the compounds that are MCP-1 receptor antagonists.
摘要翻译: 本发明涉及可用于治疗趋化因子介导的病症的砜。 在某些实施方案中,本发明涉及作为MCP-1受体拮抗剂的化合物。
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公开(公告)号:US20050004112A1
公开(公告)日:2005-01-06
申请号:US10831216
申请日:2004-04-26
申请人: Mark Player , Nand Baindur , Benjamin Brandt , Naresh Chadha , Raymond Patch , Davoud Asgari , Taxiarchis Georgiadis
发明人: Mark Player , Nand Baindur , Benjamin Brandt , Naresh Chadha , Raymond Patch , Davoud Asgari , Taxiarchis Georgiadis
IPC分类号: A61K31/16 , A61K31/195 , A61K31/452 , A61K31/4545 , A61K31/55 , A61P35/00 , C07D207/34 , C07D207/42 , C07D213/81 , C07D223/12 , C07D231/16 , C07D231/38 , C07D261/18 , C07D265/02 , C07D265/30 , C07D279/12 , C07D295/14 , C07D307/68 , C07D307/71 , C07D307/72 , C07D401/12 , C07D405/00 , C07D405/12 , C07D491/04
CPC分类号: C07D213/81 , C07D231/38 , C07D265/02 , C07D307/68 , C07D307/71 , C07D405/12 , C07D491/04
摘要: The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W 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,II和III的化合物:其中A,R 1,R 2,R 3,R 4,X,Y和W在说明书中列出,以及溶剂合物,水合物,互变异构体或其药学上可接受的盐 ,抑制蛋白酪氨酸激酶,特别是c-fms激酶。
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公开(公告)号:US20040054009A1
公开(公告)日:2004-03-18
申请号:US10275335
申请日:2002-11-06
IPC分类号: A61K031/18
CPC分类号: C07D213/42 , A61K31/18 , C07C307/06 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/13 , C07C311/14 , C07C311/18 , C07C311/29 , C07C311/41 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/16 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/10 , C07D277/12 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D295/135 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/70
摘要: The present invention provides (bis) sulfonamide derivatives of formula (I) useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
摘要翻译: 本发明提供式(I)的(双)磺酰胺衍生物,其用于增强哺乳动物的谷氨酸受体功能,因此可用于治疗各种各样的病症,例如精神病和神经障碍。
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公开(公告)号:US06403644B1
公开(公告)日:2002-06-11
申请号:US09709439
申请日:2000-11-13
IPC分类号: C07C31142
CPC分类号: C07D213/81 , C07C311/19 , C07C311/29 , C07C311/46 , C07C311/47 , C07D209/20 , C07D213/55 , C07D233/64 , C07D307/71 , C07D333/38
摘要: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia); wherein R1 is hydrogen, C1-4 alkyl; R2 is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is — (CH2)m—, in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP. The diseases such as above, for example, are rheumatoid, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cell, autoimmune disease (Crohn's disease, Sjogren's syndrome etc.), disease caused by vascular emigration or infiltration of leukocytes, arterialization.
摘要翻译: 本发明涉及:(i)含有式(Ia)的磺酰氨基酸衍生物的基质金属蛋白酶抑制剂; 其中R1是氢,C1-4烷基; R2是氢,C1-8烷基等; E是-CONR 3 - ,其中R 3是氢,C 1-4烷基等,-NR 3 CO-,-CO-O-,-O-CO-等; A是氢,C 1-8烷基,C 3-7环烷基或Ar; J为键,C2-4亚烷基等; G为 - (CH 2)m - ,其中m为2,3或4,其中R 6和R 7为氢,C 1-8烷基等; 和其无毒盐,(ii)式(Ib)的磺酰氨基酸衍生物:其中所有符号与(i)相同; 及其无毒盐,和(iii)制备式(Ib)化合物的方法。式(Ia)化合物可用于预防和/或治疗由过表达和过度活性引起的疾病 MMP。 例如上述疾病是类风湿,关节炎,异常骨吸收,骨质疏松症,牙周炎,间质性肾炎,动脉硬化,肺气肿,肝硬化,角膜损伤,肿瘤细胞侵袭或生长的转移,自身免疫性疾病(Crohn's 疾病,干燥综合征等),血管移行或白细胞浸润引起的疾病,动脉化。
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公开(公告)号:US20020002158A1
公开(公告)日:2002-01-03
申请号:US09912809
申请日:2001-07-25
发明人: MacKlin B. Arnold , Stephen R. Baker , Thomas J. Bleisch , Buddy E. Cantrell , Ana M. Escribano , Ken Matsumoto , Tracey E. McKennon , Paul L. Ornstein , Richard L. Simon , Edward C.R. Smith , Hamideh Zarrinmayeh , Dennis M. Zimmerman
IPC分类号: A61K031/55 , A61K031/535 , A61K031/495 , A61K031/445 , A61K031/415 , A61K031/18
CPC分类号: A61K31/18 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/4418 , A61K31/451 , A61K31/455 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/14 , C07C311/16 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/277 , C07D211/18 , C07D211/28 , C07D213/42 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/68 , C07D409/04
摘要: Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R1nullLnullNHSO2R2 nullnullI in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are novel compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.
摘要翻译: 哺乳动物中的谷氨酸受体功能可以使用有效量的式(I)所示化合物加强,其中R 1为直链式> R1-L-NHSO2R2 I 表示未取代或取代的芳族或杂芳族基团; (1-6C)烷基,(3-6C)环烷基,(1-6C)氟代烷基,(1-6C)氯烷基,(2-6C)烯基,(1-4C)烷氧基(1-4C)烷基, 未取代或被卤素取代的苯基,(1-4C)烷基或(1-4C)烷氧基或式R3R4N基团,其中R3和R4各自独立地表示(1-4C)烷基,或与氮 它们所连接的原子形成氮杂环丁烷基,吡咯烷基,哌啶基,吗啉代,哌嗪基,六氢氮杂基或八氢az嗪基; (1-6C)烷基,(2-6C)烷基,(2-6C)烯基,芳基(2-甲基苯基)丙烯基, 6C)烯基和芳基,或两个与它们所连接的碳原子或碳原子一起形成(3-8C)碳环的取代基; 及其药学上可接受的盐。 还公开了式I的新化合物,其制备方法和含有它们的药物组合物。
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公开(公告)号:US06303816B1
公开(公告)日:2001-10-16
申请号:US09355605
申请日:1999-10-18
申请人: Macklin B Arnold , Stephen R Baker , David Bleakman , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Joseph P Tizzano , Hamideh Zarrinmayeh , Dennis M Zimmerman
发明人: Macklin B Arnold , Stephen R Baker , David Bleakman , Thomas J Bleisch , Buddy E Cantrell , Ana M Escribano , Ken Matsumoto , Tracey E McKennon , Paul L Ornstein , Richard L Simon , Edward C. R. Smith , Joseph P Tizzano , Hamideh Zarrinmayeh , Dennis M Zimmerman
IPC分类号: C07C3103
CPC分类号: A61K31/18 , A61K31/381 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/4418 , A61K31/451 , A61K31/455 , C07C307/08 , C07C311/03 , C07C311/04 , C07C311/05 , C07C311/06 , C07C311/09 , C07C311/14 , C07C311/16 , C07C311/24 , C07C311/29 , C07C311/39 , C07C311/53 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D207/277 , C07D211/18 , C07D211/28 , C07D213/42 , C07D213/81 , C07D213/82 , C07D239/26 , C07D257/04 , C07D261/08 , C07D261/10 , C07D261/18 , C07D271/06 , C07D277/24 , C07D277/28 , C07D277/56 , C07D277/66 , C07D279/02 , C07D307/12 , C07D307/52 , C07D307/68 , C07D307/71 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/28 , C07D333/34 , C07D333/38 , C07D333/58 , C07D333/68 , C07D409/04
摘要: Glutamate receptor function in a mammal may be potentiated using an effective amount of a compound of formula R1—L—NHSO2R2 I in which R1 represents an unsubstituted or substituted aromatic or heteroaromatic group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or a group, of formula R3R4N in which R3 and R4 each independently represents (1-4C)alkyl or, together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; and L represents a (2-4C)alkylene chain which is unsubstituted or substituted by one or two substituents selected independently from (1-6C)alkyl, aryl(1-6C)alkyl, (2-6C)alkenyl, aryl(2-6C)alkenyl and aryl, or by two substituents which, together with the carbon atom or carbon atoms to which they are attached form a (3-8C)carbocyclic ring; and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula I, processes for preparing them and pharmaceutical compositions containing them.
摘要翻译: 哺乳动物的谷氨酸受体功能可以使用有效量的化合物,R1表示未取代或取代的芳族或杂芳族基团,R2表示(1-6C)烷基,(3-6C)环烷基,(1-6C) 氟代烷基,(1-6C)氯烷基,(2-6C)烯基,(1-4C)烷氧基(1-4C)烷基,未被取代或被卤素取代的苯基,(1-4C)烷基或(1-4C) 烷氧基或式R3R4N的基团,其中R3和R4各自独立地表示(1-4C)烷基,或者与它们所连接的氮原子一起形成氮杂环丁烷基,吡咯烷基,哌啶基,吗啉代,哌嗪基,六氢氮杂或八氢吖辛因 组; 和(1-6C)烷基,芳基(1-6C)烷基,(2-6C)链烯基,芳基(2-6C)烷基,(1-6C)烷基, )烯基和芳基,或两个与它们所连接的碳原子或碳原子一起形成(3-8C)碳环的取代基;及其药学上可接受的盐。还公开了式I的化合物, 制备它们和含有它们的药物组合物。
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