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1. 发明申请

WO2005047270A2 SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 审中-公开
标题翻译：取代三唑作为钠通道阻断剂
公开(公告)号：WO2005047270A2
公开(公告)日：2005-05-26
申请号：PCT/US2004037280
申请日：2004-11-05
申请人： MERCK & CO INC , PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , GONZALEZ EDWARD , OK HYUN , PALUCKI BRENDA , PARSONS WILLIAM H , SISCO ROSEMARY , FISHER MICHAEL H
发明人： PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , GONZALEZ EDWARD , OK HYUN , PALUCKI BRENDA , PARSONS WILLIAM H , SISCO ROSEMARY , FISHER MICHAEL H
IPC分类号： C07D249/10 , C07D403/10 , A61K31/4196 , A61P25/00
CPC分类号： C07D249/10 , C07D403/10
摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.
摘要翻译：由式I，II或III表示的取代的三唑化合物或其药学上可接受的盐。药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，偏头痛，头痛，偏头痛，癫痫，肠易激综合征，糖尿病神经病，多发性硬化症，躁狂抑郁症和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。施用局部麻醉的方法包括单独或与一种或多种其它治疗活性化合物和药学上可接受的载体一起施用有效量的本发明化合物。

2. 发明专利

CL2010000143A1 Compuestos derivados de 3-[(3-fenil)-fenil]-1,2,4-triazol sustituidos; y su uso en el tratamiento o prevencion del dolor o a un trastorno asociado al dolor (solicitud divisional de cl 551-04). 未知
公开(公告)号：CL2010000143A1
公开(公告)日：2010-07-02
申请号：CL2010000143
申请日：2010-02-18
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , PALUCKI BRENDA , PARSONS WILLIAM H , FISHER MICHAEL H , CARE JAMES P , FRANTZ DOUGLAS E , KRESS MICHAEL
IPC分类号： A61K31/4196 , A61P25/00 , A61P25/04 , C07D249/08
摘要： Compuestos derivados de triazol sustituido con biarilo, bloqueadores del canal de sodio; y su uso para tratar o prevenir el dolor o un trastorno asociado al dolor (divisional de la solicitud 551-04).

3. 发明专利

BRPI0416319A 未知
公开(公告)号：BRPI0416319A
公开(公告)日：2007-01-09
申请号：BRPI0416319
申请日：2004-11-05
申请人： MERCK & CO INC
发明人： GONZALES EDWARD , OK HYUN , PALUCKI BRENDA , SISCO ROSEMARY , FISHER MICHAEL H , PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , PARSONS WILLIAM H
IPC分类号： C07D249/10 , C07D403/10 , A61K31/4196 , A61P25/00
摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).

4. 发明专利

CA2545254A1 SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 未知
公开(公告)号：CA2545254A1
公开(公告)日：2005-05-26
申请号：CA2545254
申请日：2004-11-05
申请人： MERCK & CO INC
发明人： ZHOU BISHAN , CHAKRAVARTY PRASUN K , PARK MIN K , GONZALEZ EDWARD , FISHER MICHAEL H , SISCO ROSEMARY , PARSONS WILLIAM H , OK HYUN , PALUCKI BRENDA
IPC分类号： C07D249/10 , A61K31/4196 , A61P25/00 , C07D403/10
摘要： Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associat ed with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).

5. 发明专利

ES2314387T3 TRIAZOLES SUSTITUIDOS CON BIARILO COMO BLOQUEADORES DE CANALES DE SODIO. 未知
公开(公告)号：ES2314387T3
公开(公告)日：2009-03-16
申请号：ES04720360
申请日：2004-03-12
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PALUCKI BRENDA , PARK MIN K , PARSONS WILLIAM H , ZHOU BISHAN
IPC分类号： C07D249/08 , A61K31/4196 , A61P25/00 , C07D249/10
摘要： Una composición farmacéutica que comprende una cantidad eficaz terapéuticamente de un compuesto representado por las Fórmulas (I) o (II): (Ver fórmulas) o una sal del mismo aceptable farmacéuticamente, en las que R 1 es (a) H; (b) alquilo C1-C6, alquenilo C2-C4, alquinilo C2-C4, cicloalquilo C3-C6 o alquileno C1-C4-[cicloalquilo C3-C6], cualquiera de los cuales está sustituido opcionalmente con uno o más de los siguientes sustituyentes: F, CF3, OH, O-alquilo C1-C4, S(O)0 - 2-alquilo C1-C4, O-CONR a R b , NR a R b , N(R a )CONR a R b , COO-alquilo C1-C4, COOH, CN, CONR a R b , SO3NR a R b , N(R a )SO2NR a R b , -C(=NH)NH2, tetrazolilo, triazolilo, imidazolilo, oxazolilo, oxadiazolilo, isoxazolilo, tiazolilo, furilo, tienilo, pirazolilo, pirrolilo, piridilo, pirimidinilo, pirazinilo, fenilo, piperidinilo, morfolinilo, pirrolidinilo o piperazinilo; (c) -alquileno C0-C4-perfluoroalquilo C1-C4; (d) NO2; (e) NR a R b , -N(COR a )R b , -N(SO2R a )R b , -N(R a )SO2R a , -N(OR a )CONR a R b , -N(R a )CON(R a )2 o -N(R a )SO2N (R a )2; (f) -CH(OR a )R a , -C(OR b )CF3, -CH(NHR b )R a , -C(=O)R a , C(=O)CF3, -SOCH3, -SO2CH3, COOR a , CN, CONR a R b , -COCONR a R b , -SO2NR a R b , -CH2O-SO2NR a R b , SO2N(R a )OR a , -C(=NH)NH2, -CR 2 =NOR a , CH= CHCONR a R b ; (g) -CONR a (CH2)0 - 2C(R a )(R b )(CH2)0 - 2CONR a R b ; (h) tetrazolilo, tetrazolinonilo, triazolilo, triazolinonilo, imidazolilo, imidazolonilo, oxazolilo, oxadiazolilo, isoxazolilo, tiazolilo, furilo, tienilo, pirazolilo, pirazolonilo, pirrolilo, piridilo, pirimidinilo, pirazinilo o fenilo, cualquiera de los cuales está sustituido opcionalmente con 1-3 sustituyentes independientes seleccionados entre i) F, Cl, Br, I, ii) -CN, iii) -NO2, iv) -C(=O)R a , v) alquilo C1-C6, vi) -O-R a , vii) -NR a R b , viii) -alquileno C0-C4-CO-OR a , ix) -(alquileno C0-C4)-NH-CO-OR a , x) -(alquileno C0-C4)-CO-NR a R b , xi) -S (O)0 - 2R a , xii) -SO2NR a R b , xiii) -NHSO2R a , xiv) -perfluoroalquilo C1-C4 y xv) -O-perfluoroalquilo C1-C4; (i) -C(R a )=C(R b )-COOR a o -C(R a )=C(R b )-CONR a R b ; (j) (Ver fórmula) (k) piperidin-1-ilo, morfolin-4-ilo, pirrolidin-1-ilo, piperazin-1-ilo o piperazin-1-ilo 4-sustituido, cualquiera de los cuales está sustituido opcionalmente con 1-3 sustituyentes seleccionados entre i) -CN, ii) -C(=O)(R a ), iii) alquilo C1-C6, iv) -OR a , v) -NR a R b , vi) -alquileno C0-C4-CO-OR a , vii) -(alquileno C0-C4)-NH-CO-OR a , viii) -(alquileno C0-C4)-CON(R a )(R b ), ix) -SR a , x) -S(O)0 - 2R a , xi) -SO2N(R a )(R b ), xii) -NR a SO2R a , xiii) -perfluoroalquilo C1-C4 y xiv) -O-perfluoroalquilo C1-C4; R a es...

6. 发明专利

SI1606269T1 BIARILNI SUBSTITUIRANI TRIAZOLI KOT BLOKATORJI NATRIJEVIH KANALÄŚKOV 未知
公开(公告)号：SI1606269T1
公开(公告)日：2009-02-28
申请号：SI200430959
申请日：2004-03-12
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PALUCKI BRENDA , PARK MIN K , PARSONS WILLIAM H , ZHOU BISHAN , CAREY JAMES P , FRANTZ DOUGLAS E , KRESS MICHAEL H , WEAVER DAMIAN
IPC分类号： C07D249/00 , A61K31/00 , A61K31/4196 , A61P25/00 , C07D249/08 , C07D249/10

7. 发明专利

CA2519252C BIARYL SUBSTITUTED TRIAZOLES AS SODIUM CHANNEL BLOCKERS 未知
公开(公告)号：CA2519252C
公开(公告)日：2008-11-18
申请号：CA2519252
申请日：2004-03-12
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , FISHER MICHAEL H , PALUCKI BRENDA , ZHOU BISHAN , CAREY JAMES P , PARSONS WILLIAM H , PARK MIN K , FRANTZ DOUGLAS E , WEAVER DAMIAN , KRESS MICHAEL H
IPC分类号： C07D249/08 , A61K31/4196 , A61P25/00 , A61P29/02 , C07D249/10
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, o r pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effecti ve amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptab le carrier. Methods of treating conditions associated with, or caused by, sodiu m channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrom e, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effectiv e amount of a compound of the instant invention, either alone, or in combinati on with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

8. 发明专利

NO20054775D0 未知
公开(公告)号：NO20054775D0
公开(公告)日：2005-10-17
申请号：NO20054775
申请日：2005-10-17
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , PARSONS WILLIAMS H , FISHER MICHAEL H , PALUCKI BRENDA , PARK MIN K , ZHOU BISHAN , CAREY JAMES P , FRANTZ DOUGLAS E , KRESS MICHAEL H , WEAVER DAMIAN
IPC分类号： A61K31/4196 , A61P25/00 , C07D249/08 , C07D249/10 , C07D
摘要： Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

9. 发明专利

PE10662004A1 TRIAZOLES SUSTITUIDOS CON BIARILO COMO BLOQUEANTES DEL CANAL DE SODIO 未知
公开(公告)号：PE10662004A1
公开(公告)日：2005-01-22
申请号：PE0002802004
申请日：2004-03-16
申请人： MERCK & CO INC
发明人： CHAKRAVARTY PRASUN K , ZHOU BISHAN , FISHER MICHAEL H , PARK MIN K , KRESS MICHAEL H , PALUCKI BRENDA , WEAVER DAMIAN , FRANTZ DOUGLAS E , CAREY JAMES P , PARSONS WILLIAM H
IPC分类号： A61K31/4196 , A61P25/00 , C07D249/08 , C07D249/10
CPC分类号： C07D249/08 , C07D249/10
摘要： SE REFIERE A TRIAZOLES SUSTITUIDOS CON BIARILO DE FORMULA I DONDE R1 ES H, ALQUILO C1-C6, ALQUENILO C2-C4, ALQUINILO C2-C4, CICLOALQUILO C3-C6, ENTRE OTROS; R2 ES H, ALQUILO C1-C4, ALQUIL C0-C4-PERFLUOROALQUILO C1-C4, ENTRE OTROS; Rb ES H, ALQUILO C1-C6 OPCIONALMENTE SUSTITUIDO CON F, CF3, OH, O-ALQUILO, ENTRE OTROS; R2 ES H, ALQUILO C1-C4, CICLOALQUILO C3-C6 CON F, CF3, OH, ENTRE OTROS; R3 Y R4 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R5, R6 Y R7 SON H, ALQUILO C1-C6, ALQUENILO C2-C4, ALQUINILO C2-C4, CICLOALQUILO C3-C6 ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE COMPRENDE ADEMAS UN SEGUNDO AGENTE TERAPEUTICO. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION. SON COMPUESTOS PREFERIDOS 3-[3-(2-TRIFLUOROMETOXIFENIL)FENIL]-1,2,4-TRIAZOL, 3-[3-(2-(2,2,2-TRIFLUOROETOXIFENIL)FENIL]-1,2,4-TRIAZOL, 3-[3-((2-(2,2,2-TRIFLUOROETOXIFENIL)FENIL]-(4-FLUORO)FENIL]-1,2,4-TRIAZOL, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS ACTUAN COMO BLOQUEANTES DEL CANAL DE SODIO Y SON UTILES PARA EL TRATAMIENTO DE DOLOR, DEPRESION, ANSIEDAD

10. 发明专利

DE602004031667D1 SUBSTITUIERTE TRIALZOLE ALS BLOCKER DES NATRIUMKANALS 未知
公开(公告)号：DE602004031667D1
公开(公告)日：2011-04-14
申请号：DE602004031667
申请日：2004-11-05
申请人： MERCK & CO INC
发明人： PARK MIN K , CHAKRAVARTY PRASUN K , ZHOU BISHAN , GONZALEZ EDWARD , OK HYUN , PALUCKI BRENDA , PARSONS WILLIAM H , SISCO ROSEMARY , FISHER MICHAEL H
IPC分类号： C07D249/10 , A61K31/4196 , A61P25/00 , C07D403/10

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