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1. 发明申请

WO2009064752A3 HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS 审中-公开
标题翻译：杂环衍生物作为离子通道的调节剂
公开(公告)号：WO2009064752A3
公开(公告)日：2009-08-27
申请号：PCT/US2008083173
申请日：2008-11-12
申请人： VERTEX PHARMA , STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL DJAMEL , WHITNEY TARA , ZIMMERMANN NICOLE , HAMPTON TARA LEANNE
发明人： STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL DJAMEL , WHITNEY TARA , ZIMMERMANN NICOLE , HAMPTON TARA LEANNE
IPC分类号： C07D417/14 , A61K31/427 , A61K31/4427
CPC分类号： C07D417/14
摘要： The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及可用作离子通道抑制剂的杂环衍生物。本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

2. 发明申请

WO2009064747A3 4(-3-(-2-(PHENYL) MORPHOLINO)-2-OXOPYRROLIDIN-1-YL)-N-(THIAZOL-2-YL) BENZENESULFON AMIDE DERIVATIVES AND RELATED COMPOUNDS AS MODULATORS OF ION CHANNELS FOR THE TREATMENT OF PAIN 审中-公开
标题翻译： 4（-3 - （ - 2-（苯基）吗啉基）-2-氧代吡咯烷-1-基）-N-（噻唑-2-基）苯甲酰胺衍生物和作为治疗疼痛的离子通道调节剂的相关化合物
公开(公告)号：WO2009064747A3
公开(公告)日：2010-08-19
申请号：PCT/US2008083165
申请日：2008-11-12
申请人： VERTEX PHARMA , STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL DJAMEL , WHITNEY TARA , ZIMMERMANN NICOLE , KAWATKAR AARTI SAMEER
发明人： STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL DJAMEL , WHITNEY TARA , ZIMMERMANN NICOLE , KAWATKAR AARTI SAMEER
IPC分类号： C07D417/14 , A61K31/427 , A61P25/04
CPC分类号： C07D417/14
摘要： The present invention relates to heterocyclic derivatives of formula I useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, like, e.g. pain., (I) or a pharmaceutically acceptable salt thereof, wherein, independently for each occurrence: ring Z is a thiazole or thiadiazole optionally substituted with 0-2 occurrences of R; V is CH2, NH, O, or S; and R, R1, R2, and R3 are hydrogen, C1-C6 aliphatic, aryl, C3-C8 cycloaliphatic, halo, CN, NO2, CF3, OCF3, OH, NH2, NH(C1-C6 aliphatic), N(C1-C6 aliphatic) 2, COOH, COO(C1 -C6 aliphatic), O(C1-C6 aliphatic), CHF2, or CH2F.
摘要翻译：本发明涉及可用作离子通道抑制剂的式I的杂环衍生物。本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法，例如，疼痛，（I）或其药学上可接受的盐，其中独立地为每次出现：环Z是任选被0-2次出现的R取代的噻唑或噻二唑; V是CH 2，NH，O或S; R 1，R 2和R 3是氢，C 1 -C 6脂族基，芳基，C 3 -C 8脂环族基，卤素，CN，NO 2，CF 3，OCF 3，OH，NH 2，NH（C 1 -C 6脂族基） C 6脂族基）2，COOH，COO（C 1 -C 6脂族基），O（C 1 -C 6脂族基），CHF 2或CH 2 F。

3. 发明申请

WO2007075895A2 HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS 审中-公开
标题翻译：杂环衍生物作为离子通道的调节剂
公开(公告)号：WO2007075895A2
公开(公告)日：2007-07-05
申请号：PCT/US2006048802
申请日：2006-12-21
申请人： VERTEX PHARMA , WILSON DEAN , FANNING LEV T D , SHETH URVI , MARTINBOROUGH ESTHER , TERMIN ANDREAS , NEUBERT TIMOTHY , ZIMMERMANN NICOLE , KNOLL TARA , WHITNEY TARA , KAWATKAR AARTI , LEHSTEN DANIELLE , STAMOS DEAN , ZHOU JINGLAN , ARUMUGAM VIJAYALAKSMI , GUTIERREZ COREY
发明人： WILSON DEAN , FANNING LEV T D , SHETH URVI , MARTINBOROUGH ESTHER , TERMIN ANDREAS , NEUBERT TIMOTHY , ZIMMERMANN NICOLE , KNOLL TARA , WHITNEY TARA , KAWATKAR AARTI , LEHSTEN DANIELLE , STAMOS DEAN , ZHOU JINGLAN , ARUMUGAM VIJAYALAKSMI , GUTIERREZ COREY
CPC分类号： C07D417/12 , C07D239/42 , C07D401/12 , C07D405/12 , C07D417/14 , C07D471/10 , C07D491/10
摘要： The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及可用作离子通道抑制剂的杂环衍生物。本发明还提供包含本发明化合物的药学上可接受的组合物和使用该组合物治疗各种疾病的方法。

4. 发明申请

WO2008147797A2 ION CHANNEL MODULATORS AND METHODS OF USE 审中-公开
标题翻译：离子通道调制器和使用方法
公开(公告)号：WO2008147797A2
公开(公告)日：2008-12-04
申请号：PCT/US2008064314
申请日：2008-05-21
申请人： VERTEX PHARMA , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , WHITNEY TARA , LEHSTEN DANIELLE , KNOLL TARA , ZIMMERMANN NICOLE , TERMIN ANDREAS
发明人： MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , WHITNEY TARA , LEHSTEN DANIELLE , KNOLL TARA , ZIMMERMANN NICOLE , TERMIN ANDREAS
IPC分类号： C07C311/58 , A61K31/18 , C07C311/51 , C07C311/53 , C07C311/59 , C07C311/60
CPC分类号： C07D209/08 , C07C311/51 , C07C311/53 , C07C2602/08 , C07D209/42 , C07D215/06 , C07D215/233 , C07D317/60 , C07D401/04 , C07D401/06 , C07D405/12
摘要： In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
摘要翻译：通常，本发明涉及可用作离子通道调节剂的化合物。现在已经发现本发明的化合物及其药学上可接受的组合物可用作电压门控钠通道的抑制剂。

5. 发明申请

WO2007030618A3 BICYCLIC DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS 审中-公开
标题翻译：作为电压离子通道调制器的双相衍生物
公开(公告)号：WO2007030618A3
公开(公告)日：2007-05-31
申请号：PCT/US2006034857
申请日：2006-09-08
申请人： VERTEX PHARMA , NEUBERT TIMOTHY , ZIMMERMANN NICOLE , KAWATKAR ARTIS , MARTINBOROUGH ESTHER , TERMIN ANDREAS
发明人： NEUBERT TIMOTHY , ZIMMERMANN NICOLE , KAWATKAR ARTIS , MARTINBOROUGH ESTHER , TERMIN ANDREAS
IPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , A61K31/4709 , A61P25/00 , C07D277/52
CPC分类号： C07D417/12 , C07D277/52
摘要： Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
摘要翻译：本文公开了可用作离子通道拮抗剂的双环衍生物。其组合物可用于治疗或缓解疼痛相关病症。

6. 发明申请

WO2007047474A2 BIPHENYL DERIVATIVES AS MODULATORS OF VOLTAGE GATED ION CHANNELS 审中-公开
标题翻译：作为电压离子通道的调节剂的联苯衍生物
公开(公告)号：WO2007047474A2
公开(公告)日：2007-04-26
申请号：PCT/US2006040156
申请日：2006-10-12
申请人： VERTEX PHARMA , MARTINBOROUGH ESTHER , LEHSTEN DANIELLE , NEUBERT TIMOTHY , KAWATKAR AARTI SAMEER , ZIMMERMANN NICOLE , TERMIN ANDREAS
发明人： MARTINBOROUGH ESTHER , LEHSTEN DANIELLE , NEUBERT TIMOTHY , KAWATKAR AARTI SAMEER , ZIMMERMANN NICOLE , TERMIN ANDREAS
IPC分类号： C07D275/02 , A61K31/425 , C07D417/10
CPC分类号： C07D417/12 , C07D275/03 , C07D277/44
摘要： Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
摘要翻译：本文公开了可用作离子通道拮抗剂的联苯衍生物。其组合物可用于治疗或缓解疼痛相关病症。

7. 发明专利

ES2383090T3 Derivados de bifenilo como moduladores de los canales iónicos dependientes de voltaje 未知
公开(公告)号：ES2383090T3
公开(公告)日：2012-06-18
申请号：ES06816908
申请日：2006-10-12
申请人： VERTEX PHARMA
发明人： MARTINBOROUGH ESTHER , LEHSTEN DANIELLE , NEUBERT TIMOTHY , KAWATKAR AARTI , ZIMMERMANN NICOLE , TERMIN ANDREAS
IPC分类号： C07D275/02 , A61K31/425 , C07D417/10
摘要： Un compuesto de fórmula I:**Fórmula**o una sal farmacéuticamente aceptable del mismo;en la que:el anillo Z es, en la que Z está opcionalmente sustituido con hasta z apariciones de Rz;z es 0 a 4;cada Rz se selecciona independientemente entre R1, R2, R3, R4 y R5;el grupo SO2 se une a cualquiera de los carbonos nº 1 ó 2;el grupo NRM-C(O)-Q-RQ se une a cualquiera de los carbonos nº 3' o 4';en la que el anillo fenilo que contiene el carbono nº 3' está opcionalmente sustituido con hasta 4sustituyentes seleccionados entre halo, CN, NO2 CF3, OCF3, OR6, SR6, S(O)R2, SO2R2, NH2, N(R2)2,COOR2 y una cadena alquilidino C1-C6 lineal o ramificada, en la que hasta dos unidades metileno noadyacentes de dicho alquilidino se reemplazan opcional e independientemente por -CO-, -CS-, -COCO-, -CONR2-, -CONR2NR2- -CO2-, -OCO-, -NR2CO2-, -O-, -NR2CONR2-, -OCONR2-, -NR2NR2-, -NR2NR2CO-, -NR2CO-, -S-, -SO-, -SO2-,-NR2-, -SO2NR2-, NR2SO2- o -NR2SO2NR2-;Q es un enlace o es una cadena alquilidino C1-C6 lineal o ramificada, en la que hasta dos unidades metilenono adyacentes de Q se reemplazan opcional e independientemente por -O-, -S- o en la que hasta unaunidad metileno de Q se reemplazan por NH o N(alquilo C1-C4)RQ es fenilo, quinolina o indolen la que RQ está opcionalmente sustituido con hasta 4 sustituyentes seleccionados entre R1, R2, R3, R4 yR5;cada uno de RN y RM es independientemente R2;

8. 发明专利

NZ581309A ION CHANNEL MODULATORS AND METHODS OF USE 未知
公开(公告)号：NZ581309A
公开(公告)日：2012-02-24
申请号：NZ58130908
申请日：2008-05-21
申请人： VERTEX PHARMA
发明人： MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , WHITNEY TARA , LEHSTEN DANIELLE , KNOLL TARA , ZIMMERMANN NICOLE , TERMIN ANDREAS
IPC分类号： C07C311/58 , A61K31/18 , C07D215/18
摘要： Disclosed is a 4-propanamido-phenylsulfonyl) carboxamide of formula I or a pharmaceutically acceptable salt thereof, wherein R'1 and R1, R2 and R3 are defined in the specification for treating or lessening the severity of femur cancer pain; non-malignant chronic bone pain; rheumatoid arthritis; osteoarthritis; spinal stenosis; neuropathic low back pain; neuropathic low back pain; myofascial pain syndrome; fibromyalgia; temporomandibular joint pain; chronic visceral pain, including, abdominal; pancreatic; IBS pain; chronic and acute headache pain; migraine; tension headache, including, cluster headaches; chronic and acute neuropathic pain, including, post-herpetic neuralgia; diabetic neuropathy; HIV associated neuropathy; trigeminal neuralgia; Charcot-Marie Tooth neuropathy; hereditary sensory neuropathies; peripheral nerve injury; painful neuromas; ectopic proximal and distal discharges; radiculopathy; chemotherapy induced neuropathic pain; radiotherapy-induced neuropathic pain; post-mastectomy pain; central pain; spinal cord injury pain; post-stroke pain; thalamic pain; complex regional pain syndrome; phantom pain; intractable pain; acute pain, acute post-operative pain; acute musculoskeletal pain; joint pain; mechanical low back pain; neck pain; tendonitis; injury/exercise pain; acute visceral pain, including, abdominal pain; pyelonephritis; appendicitis; cholecystitis; intestinal obstruction; hernias; etc; chest pain, including, cardiac pain; pelvic pain, renal colic pain, acute obstetric pain, including, labor pain; cesarean section pain; acute inflammatory, burn and trauma pain; acute intermittent pain, including, endometriosis; acute herpes zoster pain; sickle cell anemia; acute pancreatitis; breakthrough pain; orofacial pain including sinusitis pain, dental pain; multiple sclerosis (MS) pain; pain in depression; leprosy pain; Behcet's disease pain; adiposis dolorosa; phlebitic pain; Guillain-Barre pain; painful legs and moving toes; Haglund syndrome; erythromelalgia pain; Fabry's disease pain; bladder and urogenital disease, including, urinary incontinence; hyperactivity bladder; painful bladder syndrome; interstitial cyctitis (IC); or prostatitis; complex regional pain syndrome (CRPS), type I and type II; or angina-induced pain.

9. 发明专利

AT540036T 未知
公开(公告)号：AT540036T
公开(公告)日：2012-01-15
申请号：AT08848685
申请日：2008-11-12
申请人： VERTEX PHARMA
发明人： STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL , WHITNEY TARA , ZIMMERMANN NICOLE , HAMPTON TARA
IPC分类号： C07D417/14 , A61K31/427 , A61K31/4427
摘要： The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

10. 发明专利

CA2705336A1 HETEROCYCLIC DERIVATIVES AS MODULATORS OR ION CHANNELS 未知
公开(公告)号：CA2705336A1
公开(公告)日：2009-05-22
申请号：CA2705336
申请日：2008-11-12
申请人： VERTEX PHARMA
发明人： STAMOS DEAN , MARTINBOROUGH ESTHER , NEUBERT TIMOTHY , NUMA MEHDI MICHEL DJAMEL , WHITNEY TARA , ZIMMERMANN NICOLE , KAWATKAR AARTI SAMEER
IPC分类号： C07D417/14 , A61K31/427 , A61P25/04
摘要： The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

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