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1. 发明申请

US20080167318A1 Pharmaceutically active pyrrolidine derivatives 审中-公开
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US20080167318A1
公开(公告)日：2008-07-10
申请号：US11783341
申请日：2007-04-09
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
IPC分类号： A61K31/497 , A61K31/40 , A61K31/403 , A61P15/06 , C07D209/56 , C07D455/02 , C07D403/02 , C07D207/02 , A61P15/02 , A61K31/47
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2—, —SO2NH—, —CH2—, B is either a group —C═O)—NR8R9 or represents a heterocyclic residue having the formula wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式I的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式I的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法。其中X选自CR 6，S 6，S 6，N 6，R 6，O 6， > 7 ; A选自 - （CO） - ， - （CO）-O-，-C（-NH） - ， - （CO）-NH-， - （CS）-NH， 2 - ， - SO 2 NH - ， - CH 2 - ， - B是基团-CO）-NR 8 - 或者表示具有下式的杂环残基：其中Q是NR 10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

2. 发明授权

US07211601B2 Pharmaceutically active pyrrolidine derivatives 有权
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US07211601B2
公开(公告)日：2007-05-01
申请号：US10239912
申请日：2001-03-20
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J Thomas , Anthony Baxter
IPC分类号： A61K31/40 , C07D207/10 , C07D207/14
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO22-, —SO2NH—, —CH2-, B is either a group —(C═O)—NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5–6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式（I）的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式（I）的吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法，其中X选自CR 6 R 7，NOR 6，NNR 6 R 7; A选自 - （CO） - ， - （CO）-O - ， - C（-NH） - ， - （CO）-NH-， - （CS）-NH，-SO 2 2-， SO 2 NH - ， - CH 2 - ，B为基团 - （CO）-NR 8 R 9，或表示具有式（a）的杂环残基，其中Q为NR10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

3. 发明授权

US07312358B2 Pharmaceutically active sulfanilide derivatives 有权
标题翻译：药物活性磺酰苯胺衍生物
公开(公告)号：US07312358B2
公开(公告)日：2007-12-25
申请号：US10399040
申请日：2001-10-15
申请人： Anna Quattropani , Matthias Schwarz , Catherine Joran-Lebrun , Dennis Church , Alexander Scheer
发明人： Anna Quattropani , Matthias Schwarz , Catherine Joran-Lebrun , Dennis Church , Alexander Scheer
IPC分类号： C07C303/00
CPC分类号： C07D213/53 , A61K31/18 , A61K31/4045 , A61K31/437 , A61K31/4402 , A61K31/4439 , A61K31/4706 , A61K31/472 , A61K31/5377 , A61K38/00 , C07D207/16 , C07D209/20 , C07D209/40 , C07D209/44 , C07D217/16 , C07D217/26 , C07D233/64 , C07D471/04 , C07K5/06026 , C07K5/06191
摘要： The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及式（I）的磺酰苯胺衍生物，其中R 1和R 2是任选取代的芳基和杂芳基，其它变量如用作药物活性化合物，以及含有这种磺酰苯胺衍生物的药物制剂。所述衍生物可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。特别地，本发明涉及展示催产素和/或加压素受体的实质性调节，特别是拮抗活性的磺酰苯胺衍生物。更优选地，所述化合物可用于治疗和/或预防催产素和/或加压素介导的疾病状态，包括早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。本发明还涉及新的磺酰苯胺衍生物及其制备方法。

4. 发明授权

US07189754B2 Pyrrolidine ester derivatives with oxytocin modulating activity 有权
标题翻译：吡咯烷酯衍生物与催产素调节活性
公开(公告)号：US07189754B2
公开(公告)日：2007-03-13
申请号：US10471290
申请日：2002-03-19
申请人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D401/10 , A61K31/401 , C07D207/22 , C07D403/10
摘要： The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1–C6-alkyl, C2–C6-alkenyl, C2–C6-alkynyl, aryl, heteroaryl, 3–8-membered cycloalkyl, acyl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1–2 further cycloalkyl or aryl or heteroaryl group
摘要翻译：本发明涉及式（I）的吡咯烷酯用于治疗和/或预防早产，早产和痛经的用途。特别地，本发明涉及式（I）的吡咯烷酯的用途，特别是拮抗催产素受体。本发明还涉及新的吡咯烷酯。 X选自CR 6，S 6，S 6，N 6，R 6，R 6， 7 ; R选自包含C 1 -C 6 -C 6烷基，C 2 -C 6 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，饱和或不饱和的3-8元环烷基，其可以含有1-3个选自N，O，S，芳基，杂芳基的杂原子 C 1 -C 6 - 烷基芳基，C 1 -C 6 - 烷基杂芳基，C 1 -C 6 - 烷基芳基，C 1 -C 6 - R 1选自由C 1 -C 6 - C 6 - 烷基，C 2 - （C 1 -C 6）烷基组成的组或由C 1 -C 6 - C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C

5. 发明申请

US20070129381A1 PHARMACEUTICALLY ACTIVE PYRROLIDINE ESTER DERIVATIVES 审中-公开
标题翻译：药用活性吡咯烷酮衍生物
公开(公告)号：US20070129381A1
公开(公告)日：2007-06-07
申请号：US11620359
申请日：2007-01-05
申请人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
IPC分类号： A61K31/506 , A61K31/4439 , A61K31/401 , C07D403/02
CPC分类号： C07D401/10 , A61K31/401 , C07D207/22 , C07D403/10
摘要： The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonise the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, saturated or unsaturated 3-8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, acyl, C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1-2 further cycloalkyl or aryl or heteroaryl group.
摘要翻译：本发明涉及式（I）的吡咯烷酯用于治疗和/或预防早产，早产和痛经的用途。特别地，本发明涉及式（I）的吡咯烷酯的用途，特别是拮抗催产素受体。本发明还涉及新的吡咯烷酯。 X选自CR 6，S 6，S 6，N 6，R 6，R 6， 7 ; R选自包含C 1 -C 6 -C 6烷基，C 2 -C 6 -C 6烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，饱和或不饱和的3-8元环烷基，其可以含有1-3个选自N，O，S，芳基，杂芳基的杂原子 C 1 -C 6 - 烷基芳基，C 1 -C 6 - 烷基杂芳基，C 1 -C 6 - 烷基芳基，C 1 -C 6 - R 1选自由C 1 -C 6 - C 6 - 烷基，C 2 - （C 1 -C 6）烷基组成的组或由C 1 -C 6 - C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C

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