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1. 发明授权

US5795900A Symmetrical bis-heteroaryl-methoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
标题翻译：对称双杂芳基 - 甲氧基 - 苯基烷基羧酸盐作为白三烯生物合成的抑制剂
公开(公告)号：US5795900A
公开(公告)日：1998-08-18
申请号：US703441
申请日：1996-09-17
申请人： Clint D. Brooks , Pramila Bhatia , Teodozyj Kolasa , Andrew O. Stewart , David E. Gunn , Richard A. Craig
发明人： Clint D. Brooks , Pramila Bhatia , Teodozyj Kolasa , Andrew O. Stewart , David E. Gunn , Richard A. Craig
IPC分类号： C07D239/26 , A61K31/4184 , A61K31/421 , A61K31/4402 , A61K31/454 , A61K31/47 , A61K31/498 , A61K31/506 , A61P37/08 , A61P43/00 , C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14 , C07D401/10
CPC分类号： C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D241/42 , C07D277/64
摘要： Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d)--NR.sup.6 SO.sub.2 R.sup.9, (e)-NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.
摘要翻译：具有下式的化合物：其中W在每次出现时相同，并且选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基，取代的噻唑基; R 1和R 2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R3是价键或选自氢和烷基; X是价键或选自亚烷基，烯基和亚炔基; 并且Z选自（a）COM，（b）CH = NOA-COM，（c）CH2-ON = A-COM其中A选自亚烷基和亚环烷基，M选自（a）药学上可接受的代谢可裂解基团，（b）-OR6，（c）-NR7R8，（d）-NR6SO2R9，（e）-NH-四唑基，（f）甘氨酰抑制白三烯生物合成，可用于治疗过敏性和炎性疾病状态。还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

2. 发明授权

US5843968A Symmetrical bis-heteroarylmethoxy-phenylalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
标题翻译：对称双杂芳基甲氧基 - 苯基烷基羧酸盐作为白三烯生物合成的抑制剂
公开(公告)号：US5843968A
公开(公告)日：1998-12-01
申请号：US958301
申请日：1997-10-27
申请人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa , Andrew O. Stewart , David E. Gunn , Richard A. Craig
发明人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa , Andrew O. Stewart , David E. Gunn , Richard A. Craig
IPC分类号： C07D239/26 , A61K31/4184 , A61K31/421 , A61K31/4402 , A61K31/454 , A61K31/47 , A61K31/498 , A61K31/506 , A61P37/08 , A61P43/00 , C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14 , A61K31/38 , A61K31/405 , A61K31/42 , A61K31/425
CPC分类号： C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D241/42 , C07D277/64
摘要： Compounds having the formula: ##STR1## wherein W is the same at each occurrence and is selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halolalkyl, alkoxy, halogen; R.sup.3 is a valence bond or is selected from hydrogen and alkyl; X is a valence bond or is selected from alkylene, alkenylen, and alkynylene; and Z is selected from (a) COM, (b) CH.dbd.N--O--A--COM, (c) CH.sub.2 --O--N.dbd.A--COM wherein A is selected from alkylene and cycloalkylene, and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.6, (c) --NR.sup.7 R.sup.8, (d) --NR.sup.6 SO.sub.2 R.sup.9, (e) --NH-Tetrazolyl, and (f) glycinyl inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.
摘要翻译：具有下式的化合物：其中W在每次出现时相同，并且选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基，取代的噻唑基; R1和R2独立地选自氢，烷基，卤代烷基，烷氧基，卤素; R3是价键或选自氢和烷基; X是价键或选自亚烷基，烯基和亚炔基; 并且Z选自（a）COM，（b）CH = NOA-COM，（c）CH2-ON = A-COM其中A选自亚烷基和亚环烷基，M选自（a）药学上可接受的代谢可裂解基团，（b）-OR6，（c）-NR7R8，（d）-NR6SO2R9，（e）-NH-四唑基，（f）甘氨酰抑制白三烯生物合成，可用于治疗过敏性和炎性疾病状态。还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

3. 发明授权

US5863946A Iminoxyderivatives of fenamates as inhibitors of prostaglandin biosynthesis 失效
标题翻译：作为前列腺素生物合成抑制剂的灭火剂的亚硝基衍生物
公开(公告)号：US5863946A
公开(公告)日：1999-01-26
申请号：US660046
申请日：1996-06-06
申请人： Clint D. W. Brooks , Richard A. Craig , Teodozyj Kolasa , Andrew O. Stewart
发明人： Clint D. W. Brooks , Richard A. Craig , Teodozyj Kolasa , Andrew O. Stewart
IPC分类号： C07C251/58 , C07D257/04 , A61K31/195
CPC分类号： C07D257/04 , C07C251/58
摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein Y is selected from halogen, alkyl, and haloalkyl; n is 0, 1, 2, or 3; X is absent or is alkylene; A is absent or is selected from optionally substituted alkylene, optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, optionally substituted alkenylene, and ##STR2## or R.sup.2 and A together define a saturated 5- to 8-membered optionally substituted carbocyclic or heterocyclic ring to which the group Z is attached; Z is selected from (a) hydrogen, (b) COM wherein M is selected from the group consisting of --OR.sup.5, a pharmaceutically acceptable cation, --NR.sup.7 R.sup.8, and a pharmaceutically acceptable, metabolically cleavable group, (c) --OR.sup.3, (d) tetrazolyl, (e) --CH(OR.sup.3)--CH.sub.2 OR.sup.9, (f) --CH(OR.sup.3)--CH.sub.2 --CH.sub.2 OR.sup.9, (g) --CH(OR.sup.3)--CH(OR.sup.9)--CH.sub.2 OR.sup.10, and (h) .dbd.N--OR.sup.3 ; and R.sup.1, R.sup.2, R.sup.3, R.sup.9, and R.sup.10 are independently selected from (a) hydrogen, (b) alkyl, and (c) optionally substituted phenyl, are prostaglandin biosynthesis inhibitors and are useful in the treatment of inflammatory disease states. Also disclosed are prostaglandin inhibiting compositions, a method of inhibiting prostaglandin biosynthesis in a mammal.
摘要翻译：具有式“IMAGE”的化合物或其药学上可接受的盐，其中Y选自卤素，烷基和卤代烷基; n为0,1,2或3; X不存在或是亚烷基; A不存在或选自任选取代的亚烷基，任选取代的亚环烷基，任选取代的亚环烷基，其中一个或两个碳原子被一个或两个独立地选自O，S和N的杂原子，任选取代的亚烯基取代，以及

4. 发明授权

US5668146A Symmetrical bis-heteroarylmethoxyphenyliminoxyalkyl carboxylates as inhibitors of leukotriene biosynthesis 失效
标题翻译：对称双杂芳基甲氧基苯基亚氨基烷基羧酸盐作为白三烯生物合成的抑制剂
公开(公告)号：US5668146A
公开(公告)日：1997-09-16
申请号：US703442
申请日：1996-09-17
申请人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa
发明人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa
IPC分类号： C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14 , A61K31/47 , A61K31/44
CPC分类号： C07D213/30 , C07D215/14 , C07D215/18 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14
摘要： Compounds having the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein W and Y at each occurrence are the same and W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; Y is selected from optionally substituted phenylene and optionally substituted ##STR2## wherein the alkylene portion is of one to six carbon atoms; A is selected from alkylene, alkenylene, cycloalkylene, and optionally substituted ##STR3## wherein the alkylene portion is of one to six carbon atoms; and M is selected from hydrogen, a pharmaceutically acceptable cation, a pharmaceutically acceptable, metabolically cleavable group, --OR.sup.3, and --NR.sup.4 R.sup.5, inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis in a mammal.
摘要翻译：具有下式的化合物或其药学上可接受的盐，其中W和Y在每次出现时相同，W选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选地取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基和任选取代的噻唑基; Y选自任选取代的亚苯基和任选取代的，其中亚烷基部分具有1至6个碳原子; A选自亚烷基，亚烯基，亚环烷基和任选取代的，其中亚烷基部分为1至6个碳原子; 并且M选自氢，药学上可接受的阳离子，药学上可接受的，代谢可切割的基团-OR3和-NR4R5，抑制白三烯生物合成，并且可用于治疗过敏性和炎性疾病状态。还公开了白三烯生物合成抑制组合物和抑制哺乳动物中白细胞三烯生物合成的方法。

5. 发明申请

US20060189639A1 Antagonists of the mGlu receptor and uses thereof 审中-公开
标题翻译： mGlu受体的拮抗剂及其用途
公开(公告)号：US20060189639A1
公开(公告)日：2006-08-24
申请号：US11333035
申请日：2006-01-17
申请人： Andrew Stewart , Guo Zheng , Teodozyj Kolasa , Pramila Bhatia , Jerome Daanen , Steven Latshaw , Xueqing Wang
发明人： Andrew Stewart , Guo Zheng , Teodozyj Kolasa , Pramila Bhatia , Jerome Daanen , Steven Latshaw , Xueqing Wang
IPC分类号： A61K31/519 , C07D498/14
CPC分类号： C07D493/14 , C07D495/14
摘要： The present invention discloses compounds of general formula (I) wherein X1-X4 and R1-R3 are as defined in the description. The present invention also discloses methods of treatment for pain, neurodegeneration and convulsive states in a host mammal in need thereof, and pharmaceutical compositions including those compounds.
摘要翻译：本发明公开了通式（I）的化合物，其中X 1 -X 4 -X 3和R 1 -R 3 >如说明书中所定义。本发明还公开了在有需要的宿主哺乳动物中治疗疼痛，神经变性和惊厥状态的方法，以及包括那些化合物的药物组合物。

6. 发明申请

US20060009461A1 Acetamides and benzamides that are useful in treating sexual dysfunction 审中-公开
公开(公告)号：US20060009461A1
公开(公告)日：2006-01-12
申请号：US11223857
申请日：2005-09-09
申请人： Pramila Bhatia , Jerome Daanen , Ahmed Hakeem , Teodozyj Kolasa , Mark Matulenko , Kathleen Mortell , Meena Patel , Andrew Stewart , Xueqing Wang , Zhiren Xia , Henry Zhang
发明人： Pramila Bhatia , Jerome Daanen , Ahmed Hakeem , Teodozyj Kolasa , Mark Matulenko , Kathleen Mortell , Meena Patel , Andrew Stewart , Xueqing Wang , Zhiren Xia , Henry Zhang
IPC分类号： A61K31/506 , A61K31/501 , A61K31/496
CPC分类号： A61K31/00 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/427 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4523 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/501 , A61K31/506
摘要： The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.

7. 发明授权

US5714488A Bis-heteroarylylmethoxyphenyl ketone derivatives as inhibitors of leukotriene biosynthesis 失效
标题翻译：双杂芳基甲氧基苯基酮衍生物作为白三烯生物合成的抑制剂
公开(公告)号：US5714488A
公开(公告)日：1998-02-03
申请号：US703440
申请日：1996-09-17
申请人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa
发明人： Clint D. W. Brooks , Pramila Bhatia , Teodozyj Kolasa
IPC分类号： C07D213/30 , C07D213/36 , C07D215/14 , C07D215/18 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14 , A61K31/47
CPC分类号： C07D213/30 , C07D213/36 , C07D215/14 , C07D215/18 , C07D235/12 , C07D239/26 , C07D241/42 , C07D263/56 , C07D277/24 , C07D277/64 , C07D417/14
摘要： Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.5, inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states. Also disclosed are leukotriene biosynthesis inhibiting compositions and a method of inhibiting leukotriene biosynthesis.
摘要翻译：具有式“IMAGE”的化合物或其药学上可接受的盐，其中W选自任选取代的喹啉基，任选取代的苯并噻唑基，任选取代的苯并恶唑基，任选取代的苯并咪唑基，任选取代的喹喔啉基，任选取代的吡啶基，任选取代的嘧啶基，和任选取代的噻唑基; R1和R2是独立地选自氢，烷基，卤代烷基，烷氧基和卤素的一个或多个基团; Z选自N-OH，NOA-COM，CH-COM和CH-CH = N-O-A-COM，其中A选自亚烷基，亚烯基，亚环烷基和任选取代的烷基苯基，其中烷基部分为1至6个碳原子，M选自药学上可接受的，可代谢的基团-OR3和-NR4R5，抑制白三烯生物合成，并且可用于治疗过敏和炎症疾病状态。还公开了白三烯生物合成抑制组合物和抑制白三烯生物合成的方法。

8. 发明授权

US07528134B2 Acetamides and benzamides that are useful in treating sexual dysfunction 有权
标题翻译：可用于治疗性功能障碍的乙酰胺和苯甲酰胺
公开(公告)号：US07528134B2
公开(公告)日：2009-05-05
申请号：US10444687
申请日：2003-05-23
申请人： Pramila A. Bhatia , Jerome F. Daanen , Ahmed A. Hakeem , Teodozyj Kolasa , Mark A. Matulenko , Kathleen H. Mortell , Meena V. Patel , Andrew O. Stewart , Xueqing Wang , Zhiren Xia , Henry Q. Zhang
发明人： Pramila A. Bhatia , Jerome F. Daanen , Ahmed A. Hakeem , Teodozyj Kolasa , Mark A. Matulenko , Kathleen H. Mortell , Meena V. Patel , Andrew O. Stewart , Xueqing Wang , Zhiren Xia , Henry Q. Zhang
IPC分类号： A61K31/501 , A61K31/497
CPC分类号： C07D213/82 , A61K31/40 , A61K31/41 , A61K31/445 , A61K31/4453 , A61K31/4523 , C07D207/06 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/70 , C07D213/74 , C07D213/85 , C07D235/30 , C07D239/42 , C07D277/38 , C07D277/82 , C07D295/13 , C07D295/15 , C07D295/155 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14
摘要： The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
摘要翻译：本发明涉及式（I）化合物用于治疗性功能障碍的用途，以及含有式（I）化合物用于治疗性功能障碍的组合物的用途。

9. 发明授权

US07022728B2 Benzimidazoles that are useful in treating male sexual dysfunction 有权
标题翻译：苯并咪唑可用于治疗男性性功能障碍
公开(公告)号：US07022728B2
公开(公告)日：2006-04-04
申请号：US10094265
申请日：2002-03-08
申请人： Marlon D. Cowart , Pramila A. Bhatia , Jerome F. Daanen , Andrew O. Stewart , Meena V. Patel , Teodozyj Kolasa , Jorge D. Brioni , Jeffrey Rohde
发明人： Marlon D. Cowart , Pramila A. Bhatia , Jerome F. Daanen , Andrew O. Stewart , Meena V. Patel , Teodozyj Kolasa , Jorge D. Brioni , Jeffrey Rohde
IPC分类号： A61K31/415 , A61K31/495 , A61K31/50
CPC分类号： A61K31/496
摘要： The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
摘要翻译：本发明涉及式（I）化合物用于治疗性功能障碍的用途，以及含有式（I）化合物用于治疗性功能障碍的组合物的用途。

10. 发明授权

US06960589B2 Benzimidazoles that are useful in treating sexual dysfunction 有权
标题翻译：可用于治疗性功能障碍的苯并咪唑
公开(公告)号：US06960589B2
公开(公告)日：2005-11-01
申请号：US10236812
申请日：2002-09-06
申请人： Marlon D. Cowart , Pramila A. Bhatia , Jerome F. Daanen , Andrew O. Stewart , Meena V. Patel , Teodozyj Kolasa , Jorge D. Brioni , Jeffrey Rohde , Kenneth M. Engstrom
发明人： Marlon D. Cowart , Pramila A. Bhatia , Jerome F. Daanen , Andrew O. Stewart , Meena V. Patel , Teodozyj Kolasa , Jorge D. Brioni , Jeffrey Rohde , Kenneth M. Engstrom
IPC分类号： A61K31/496 , C07D401/12 , C07D403/12 , A61P15/00
CPC分类号： C07D401/12 , A61K31/496 , C07D403/12
摘要： The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein L is C1-4 alkyl; RA, RB, RC, RD, and RE, are as described in the specification; Z is selected from the group consisting of N, C and CH; and A is aryl and heteroaryl as described in the specification.
摘要翻译：本发明涉及式（I）化合物用于治疗性功能障碍的用途，以及含有式（I）化合物用于治疗性功能障碍的组合物的用途，其中L为C 1-4 烷基; R A，R B，R C，R D和R E，，如说明书所述; Z选自N，C和CH; 并且A是如说明书中所述的芳基和杂芳基。

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