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1. 发明申请

WO2002100861A1 1-(3-PHENYLOXYPROPYL)PIPERIDINE DERIVATIVES 审中-公开
标题翻译： 1-（3-苯基丙基）哌啶衍生物
公开(公告)号：WO2002100861A1
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006313
申请日：2002-06-07
申请人： AKZO NOBEL N.V. , COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
发明人： COWLEY, Phillip, Martin , COTTNEY, Jean , BARN, David, Raeburn , MORPHY, John, Richard , PALIN, Ronald , GROVE, Simon, James, Anthony
IPC分类号： C07D471/10
CPC分类号： C07D401/04 , C07D471/10
摘要： The present invention relates to 1(3-phenyloxypropyl)-piperidine derivative having general Formula (I), wherein R1 is (C 1-6 )alkyl or (C 4-8 )cycloalkyl or phenyl, optionally substituted with (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R2 is H or (C 1-6 )alkyl; or R1 and R2 form together with the carbon atom to which they are bound (C 4-8 )cycloalkyl, optionally substitutes with (C 1-6 )alkyloxy or halogen; R3 is H, OH, (C 1-6 )alkyloxy or (C 1-6 )alkylcarbonyloxy; R4 represents 1-5 substituents independently selected from H, (C 1-6 )alkyl, (C 1-6 )alkyloxy and halogen; Y represents (a), (b) and Z is H; or Y and Z together with the carbon atom to which they are bound represent the spiro atom in the spiro atom in the spiro system formed with (c) *represents the spiro carbon atom; R6 is H, (C 1-6 )alkyl or (CO)n-(CH 2 )m-R12; n is 0 or 1; m is 1-4; R8 and R10 are independently H or(C 1-6 )alkyl; R7, R9 and R11 are independently H, (C 1-6 )alkyl, (C 1-6 )alkyloxy or halogen; R12 is hydroxy, (C 1-4 )alkyloxy, (C 1-4 )alkylthio, (C 1-4 )alkyloxycarbonyl, (C 1-4 )alkylcarbonyloxy, 2-tetrahydrofuranyl, 4-morpholinyl or di(C 1-4 )alkylamino; or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 1-(3-phenyloxypropyl)-piperidine derivatives in therapy.
摘要翻译：本发明涉及具有通式（I）的1（3-苯氧基丙基） - 哌啶衍生物，其中R 1为（C 1-6）烷基或（C 4-8）环烷基或任选被（C 1-6）烷基取代的苯基，（C 1-6）烷氧基或卤素; R2是H或（C1-6）烷基; 或R 1和R 2与它们所连接的碳原子一起形成（C 4-8）环烷基，任选地与（C 1-6）烷氧基或卤素取代; R3是H，OH，（C1-6）烷氧基或（C1-6）烷基羰基氧基; R 4表示独立地选自H，（C 1-6）烷基，（C 1-6）烷氧基和卤素的1-5个取代基; Y表示（a），（b），Z表示H; 或者Y和Z与它们所连接的碳原子一起表示在（c）中形成的螺系中的螺原子中的螺原子*代表螺
碳原子; R6是H，（C1-6）烷基或（CO）n-（CH2）m-R12; n为0或1; m为1-4; R 8和R 10独立地为H或（C 1-6）烷基; R 7，R 9和R 11独立地为H，（C 1-6）烷基，（C 1-6）烷氧基或卤素; R 12是羟基，（C 1-4）烷氧基，（C 1-4）烷硫基，（C 1-4）烷氧基羰基，（C 1-4）烷基羰基氧基，2-四氢呋喃基，4-吗啉基或二（C 1-4）烷基氨基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些1-（3-苯氧基丙基） - 哌啶衍生物在治疗中的用途。

2. 发明申请

WO2011076723A1 AMINO-HETEROARYL DERIVATIVES AS HCN BLOCKERS 审中-公开
标题翻译： AMINO-HETEROARYL DERIVATIVES作为HCN阻隔剂
公开(公告)号：WO2011076723A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070213
申请日：2010-12-20
申请人： N.V. Organon , GROVE, Simon James Anthony , MORRISON, Angus John , JAMIESON, Craig , PALIN, Ronald , MACLEAN, John Kinnaird Ferguson
发明人： GROVE, Simon James Anthony , MORRISON, Angus John , JAMIESON, Craig , PALIN, Ronald , MACLEAN, John Kinnaird Ferguson
IPC分类号： C07D213/73 , C07D239/42 , C07D401/12 , C07D403/12 , A61K31/435 , A61K31/497 , A61K31/506 , A61K31/53 , A61P25/00
CPC分类号： C07D239/42 , A61K31/435 , A61K31/497 , A61K31/506 , A61K31/53 , C07D213/73 , C07D401/12 , C07D403/12
摘要： The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
摘要翻译：本发明涉及具有通式I的氨基 - 杂芳基衍生物或其药学上可接受的盐，其涉及包含其的药物组合物，以及这些衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

3. 发明申请

WO2010052198A1 ( PYRROLIDIN-2 -YL) PHENYL DERIVATIVES FOR USE IN THE TREATMENT OF PAIN 审中-公开
标题翻译：（吡咯烷-2-基）苯基衍生物用于治疗疼痛
公开(公告)号：WO2010052198A1
公开(公告)日：2010-05-14
申请号：PCT/EP2009/064490
申请日：2009-11-03
申请人： N.V. ORGANON , GROVE, Simon, James, Anthony , MISTRY, Ashvinkumar, Dhirubhai , PALIN, Ronald , MACLEAN, John, Kinnaird, Ferguson
发明人： GROVE, Simon, James, Anthony , MISTRY, Ashvinkumar, Dhirubhai , PALIN, Ronald , MACLEAN, John, Kinnaird, Ferguson
IPC分类号： C07D401/10 , A61K31/4439 , A61P25/02
CPC分类号： C07D401/10
摘要： The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula (I), wherein R 1 is (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, or halo(C 1-4 )alkyloxy; R 2 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; R 3 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 4 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 5 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C 3-6 )cycloalkyl group, optionally substituted with halogen; R 6 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
摘要翻译：本发明涉及具有通式（I）的（吡咯烷-2-基）苯基衍生物，其中R 1为（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基或卤素 -4）烷氧基; R 2是H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; R3是H，（C1-4）烷基或卤代（C1-4）烷基; R4是H，（C1-4）烷基或卤代（C1-4）烷基; R5是H，（C1-4）烷基或卤代（C1-4）烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺（C 3-6）环烷基; R 6为H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; 或其药学上可接受的盐，包含其的药物组合物，以及这些（吡咯烷-2-基）苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

4. 发明申请

WO2007054474A1 2-(BENZIMIDAZOL-1-YL)-N-(4-PHENYLTHIAZOL-2-YL) ACETAMIDE DERIVATIVES USEFUL IN TREATMENT OF TRPV1 RELATED DISORDERS 审中-公开
标题翻译：用于治疗TRPV1相关疾病的2-（苯并咪唑-1-基）-N-（4-苯乙烯基-2-基）乙酰胺衍生物
公开(公告)号：WO2007054474A1
公开(公告)日：2007-05-18
申请号：PCT/EP2006/068109
申请日：2006-11-06
申请人： N.V. ORGANON , PALIN, Ronald , GRAY, Colin Alasdair
发明人： PALIN, Ronald , GRAY, Colin Alasdair
IPC分类号： C07D417/12 , A61K31/427
CPC分类号： C07D417/12
摘要： The invention relates to 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives having the general Formula (I) wherein R 1 is H, (C 1-4 )alkyl, (C 1-4 )alkyloxy or halogen; R 2 represents 1-3 substituents selected from H, (C 1-4 )alkyl (optionally substituted with 1 or more halogens), (C 1-4 )alkyloxy (optionally substituted with 1 or more halogens), halogen, CF 3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives in the treatment of TRPV1 mediated disorders.
摘要翻译：本发明涉及具有通式（I）的2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物，其中R 1是H，（C < （C 1-4）烷氧基或卤素;（C 1-4）烷氧基或卤素; R 2表示1-3个选自H，（C 1-4烷基）烷基（任选被1个或多个卤素取代）的取代基，（C 1-4）烷氧基（任选被一个或多个卤素取代），卤素，CF 3或氰基; 或其药学上可接受的盐; 涉及包含其的药物组合物和所述2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物在治疗TRPV1介导的病症中的用途。

5. 发明申请

WO2012063085A2 DRUG DERIVATIVES 审中-公开
标题翻译：药物衍生物
公开(公告)号：WO2012063085A2
公开(公告)日：2012-05-18
申请号：PCT/GB2011/052211
申请日：2011-11-11
申请人： REDX PHARMA LIMITED , CRAIGHEAD, Mark , PALIN, Ronald , MURRAY, Neil , LINDSAY, Derek
发明人： CRAIGHEAD, Mark , PALIN, Ronald , MURRAY, Neil , LINDSAY, Derek
IPC分类号： C07D205/08
CPC分类号： C07D487/04 , C07C43/205 , C07C57/00 , C07C63/64 , C07C63/66 , C07C69/12 , C07C215/46 , C07C217/58 , C07C229/18 , C07C233/22 , C07C233/36 , C07C235/16 , C07C235/28 , C07C237/20 , C07C251/40 , C07C251/48 , C07C251/54 , C07C251/58 , C07C255/25 , C07C257/14 , C07C2601/16 , C07C2602/10 , C07C2603/74 , C07D205/08 , C07D209/18 , C07D213/60 , C07D233/54 , C07D235/16 , C07D241/04 , C07D257/04 , C07D277/40 , C07D281/06 , C07D295/02 , C07D307/00 , C07D309/32 , C07D313/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D407/06 , C07D411/10 , C07D413/04 , C07D413/12 , C07D417/06 , C07D417/12 , C07D471/04 , C07D473/00 , C07D491/04 , C07D498/06 , C07D499/88 , C07D501/00 , C07D513/06 , C07D519/00 , C07H19/052 , C07H19/06 , C07H19/173 , C07J5/00 , C07J71/0031
摘要： The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets.
摘要翻译：本发明涉及已知活性药物化合物的衍生物。这些衍生物由于是活性化合物的氧化还原衍生物而与母体活性化合物不同。这意味着活性化合物中的一个或多个官能团已经在一个或多个反应中转化为另一个基团，这可能被认为代表了氧化态的变化。我们通常称这些化合物为氧化还原衍生物。本发明的衍生物可以通过单一步骤转化与原始的母体活性药物化合物相关，或者可以通过包括氧化态的一种或多种改变的若干合成步骤相关。在某些情况下，经过两次或多次转化后获得的官能团可能与母体活性化合物处于相同的氧化态（我们在氧化还原衍生物的定义中包括这些化合物）。在其他情况下，本发明衍生物的氧化态可以认为与母体化合物的氧化态不同。在许多情况下，本发明的化合物本身具有固有的治疗活性。在某些情况下，相对于母体化合物的相同靶点或靶点的这种活性与母体化合物针对靶点或靶点的活性一样好或者更好。

6. 发明申请

WO2010091009A1 ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： ISOXAZOLE-3-CARBOXAMIDE衍生物
公开(公告)号：WO2010091009A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/022869
申请日：2010-02-02
申请人： N.V. ORGANON , PHARMACOPEIA, LLC , PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
发明人： PALIN, Ronald , RATCLIFFE, Paul, David , KULTGEN, Steven, G. , HO, Koc-Kan , ROUGHTON, Andrew, Laird , OHLMEYER, Michael
IPC分类号： C07D261/18 , C07D413/06 , C07D413/12 , A61P25/00 , A61K31/42 , A61K31/422 , A61K31/45 , A61K31/4468 , A61K31/4453 , A61K31/4439 , A61K31/5377
CPC分类号： C07D261/18 , C07D413/06 , C07D413/12
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式I的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，其涉及包含该异构体的药物组合物，以及所述异恶唑-3-甲酰胺衍生物用于治疗TRPV1介导的急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性疼痛，呼吸系统疾病和下尿路疾病。

7. 发明申请

WO2009016241A1 5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS 审中-公开
标题翻译：作为TRPV1调节剂的5-苯基 - 异恶唑-3-羧酰胺衍生物
公开(公告)号：WO2009016241A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/060090
申请日：2008-07-31
申请人： N.V. ORGANON , ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
发明人： ROUGHTON, Andrew, Laird , HO, Koc-Kan , OHLMEYER, Michael , NEAGU, Irina , KULTGEN, Steven, G. , ANSARI, Nasrin , RONG, Yajing , RATCLIFFE, Paul, David , PALIN, Ronald
IPC分类号： C07D261/14 , A61K31/4155 , A61P25/00 , A61P29/00
CPC分类号： C07D413/12 , C07D261/18
摘要： The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式（I）的异恶唑-3-甲酰胺衍生物或其药学上可接受的盐，涉及含有该异构体的异恶唑-3-甲酰胺衍生物用于治疗的药物组合物的TRPV1介导的疾病，例如急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性疼痛，呼吸系统疾病和下尿路疾病。

8. 发明申请

WO2010089297A1 ISOXAZOLE-5-CARBOXAMIDE DERIVATIVES 审中-公开
标题翻译：异佛唑-5-羧酰胺衍生物
公开(公告)号：WO2010089297A1
公开(公告)日：2010-08-12
申请号：PCT/EP2010/051251
申请日：2010-02-02
申请人： N.V. ORGANON , RATCLIFFE, Paul, David , PALIN, Ronald
发明人： RATCLIFFE, Paul, David , PALIN, Ronald
IPC分类号： C07D261/08 , C07D261/10 , A61K31/42
CPC分类号： C07D261/08 , C07D261/10
摘要： The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatorypain, respiratorydiseases, and lower urinary tract disorders.
摘要翻译：本发明涉及具有通式（I）的异恶唑-5-甲酰胺衍生物或其药学上可接受的盐，其涉及包含该异构体的异恶唑-5-甲酰胺衍生物用于治疗的TRPV1介导的疾病，例如急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎性炎症，呼吸道疾病和下尿路疾病。

9. 发明申请

WO2007054480A1 2-(BENZIMIDAZOL-1-YL)-ACETAMIDE BIARYL DERIVATIVES AND THEIR USE AS INHIBITORS OF THE TRPV1 RECEPTOR 审中-公开
标题翻译： 2-（苯并咪唑-1-基） - 乙酰胺二异氰酸酯衍生物及其作为TRPV1受体的抑制剂
公开(公告)号：WO2007054480A1
公开(公告)日：2007-05-18
申请号：PCT/EP2006/068125
申请日：2006-11-06
申请人： N.V. ORGANON , PALIN, Ronald , GRAY, Colin Alasdair
发明人： PALIN, Ronald , GRAY, Colin Alasdair
IPC分类号： C07D235/06 , A61K31/4184 , A61P29/00 , C07D401/12 , A61K31/4439 , C07D417/14 , C07D417/12 , A61K31/433 , C07D403/12 , C07D413/12 , A61K31/422
CPC分类号： C07D235/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14
摘要： The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula (I) wherein n is 0 or 1; Ar 1 represents a diradical derived from a 5- or 6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C 1-4 )alkyl, (C 1-4 )alkyloxy, halogen, CF 3 or cyano; Ar 2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C 1-4 )alkyl (optionally substituted with 1 or more halogens), (C 1-4 )alkyloxy (optionally substituted with 1 or more halogens), di(C 1-4 )alkylamino, halogen, CF 3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.
摘要翻译：本发明涉及具有通式（I）的2-（苯并咪唑-1-基） - 乙酰胺双芳基衍生物，其中n为0或1; Ar 1代表衍生自5-或6-元芳环的双基，任选地包含1-3个选自N，O和S的杂原子，所述的环任选地被（C 1〜 -4 C 1-4烷基，（C 1-4）烷氧基，卤素，CF 3或氰基; Ar 2表示任选地包含1-3个氮原子的6元芳环，所述环任选被1-3个选自（C 1-4 - ）烷基的取代基取代，烷基（任选被1个或多个卤素取代），（C 1-4 - ）烷氧基（任选被1个或多个卤素取代），二（C 1-4 - 烷基）烷基，卤素，CF 3或氰基; 或其药学上可接受的盐; 包括其的药物组合物和所述2-（苯并咪唑-1-基） - 乙酰胺双芳基衍生物在治疗TRPV1介导的病症中的用途。

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