公开(公告)号：US20070037846A1

公开(公告)日：2007-02-15

申请号：US10562623

申请日：2004-06-16

申请人： Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

发明人： Heinz Fretz ,  Thomas Giller ,  Kurt Hilpert ,  Olivier Houille ,  Markus Riederer ,  Oliver Valdenaire

IPC分类号： A61K31/4152 ,  A61K31/4709 ,  A61K31/416

CPC分类号： A61K31/4152 ,  A61K31/416 ,  A61K31/4709

摘要： The present invention relates to compounds of alkylidene pyrazolidinedione derivatives, which are effective platelet ADP receptor antagonists that prevent platelet aggregation and thrombosis. Thus, the present invention also relates to pharmaceutical compositions that contain the compounds as well as methods of preventing or treating peripheral, visceral, hepatic, renal, cardio- and cerebro-vascular diseases and conditions that are associated with platelet aggregation, including thrombosis, in humans and other mammals. The present invention further provides a process for manufacturing the alkylidene pyrazolidinedione derivatives.

摘要翻译： 本发明涉及亚烷基吡唑烷二酮衍生物的化合物，其是有效的血小板聚集和血栓形成的血小板ADP受体拮抗剂。 因此，本发明还涉及含有化合物的药物组合物以及预防或治疗外周，内脏，肝，肾，心脑血管疾病和与血小板聚集相关的病症的方法，包括血栓形成 人类和其他哺乳动物。 本发明还提供了制备亚烷基吡唑烷二酮衍生物的方法。

公开(公告)号：US07727979B2

公开(公告)日：2010-06-01

申请号：US10549685

申请日：2004-03-22

申请人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

发明人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

IPC分类号： A01N43/00 ,  A01N43/46 ,  A61K31/55 ,  A01N43/42 ,  A61K31/44 ,  A01N43/78 ,  A61K31/425 ,  A01N37/52 ,  A61K31/155 ,  C07D277/60 ,  C07D277/62 ,  C07D277/82

CPC分类号： C07D277/60 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  C07D277/82 ,  C07D417/04 ,  C07D513/04

摘要： The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by —N(R′)— or —O— and R′ is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.

摘要翻译： 本发明涉及式（I）的胍衍生物，其中：A表示3-6个碳原子的链，其中一个可以被-N（R'） - 或-O-代替，R'是H或取代基 ; 环骨架仅含有噻唑组分的双键; 式（I）的碱性化合物的药学上可接受的酸加成盐，包含酸基的式（I）化合物与碱的药学上可接受的盐，含有羟基或羧基的式 （I）及其溶剂合物或水合物，其表现出神经肽FF受体拮抗剂作用。 以上适用于治疗疼痛和痛觉过敏，酒精戒断症状，​​精神药物和尼古丁依赖性，用于改善或治愈所述依赖性，调节胰岛素排泄，食物摄取，记忆功能，血压，电解质和能量管理以及 用于治疗尿失禁。 上述可以使用通常使用的方法制备并加工以得到药物。

公开(公告)号：US20060194788A1

公开(公告)日：2006-08-31

申请号：US10549685

申请日：2004-03-22

申请人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

发明人： Eva Caroff ,  Matthias Steger ,  Oliver Valdenaire ,  Anja Fecher ,  Volker Breu ,  Kurt Hilpert ,  Heinz Fretz ,  Thomas Giller

IPC分类号： A61K31/55 ,  A61K31/4745 ,  A61K31/43

CPC分类号： C07D277/60 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  C07D277/82 ,  C07D417/04 ,  C07D513/04

摘要： The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by —N(R′)— or —O— and R′ is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments.

摘要翻译： 本发明涉及式（I）的胍衍生物，其中：A表示3-6个碳原子的链，其中一个可以被-N（R'） - 或-O-代替，R'是H或取代基 ; 环骨架仅含有噻唑组分的双键; 式（I）的碱性化合物的药学上可接受的酸加成盐，包含酸基的式（I）化合物与碱的药学上可接受的盐，含有羟基或羧基的式 （I）及其溶剂合物或水合物，其表现出神经肽FF受体拮抗剂作用。 以上适用于治疗疼痛和痛觉过敏，酒精戒断症状，​​精神药物和尼古丁依赖性，用于改善或治愈所述依赖性，调节胰岛素排泄，食物摄取，记忆功能，血压，电解质和能量管理以及 用于治疗尿失禁。 上述可以使用通常使用的方法制备并加工以得到药物。

公开(公告)号：US07067549B2

公开(公告)日：2006-06-27

申请号：US10500604

申请日：2002-12-27

申请人： Markus Isler ,  Thomas Giller ,  Günter Schwalm ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

发明人： Markus Isler ,  Thomas Giller ,  Günter Schwalm ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

IPC分类号： A61K31/403 ,  C07D209/82

CPC分类号： C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14

摘要： Pyrrolidone carboxamides of formula (I) where R2=a group of formula (a) or (b), R5=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or —NR6R7 and R1, X, R3, R4, R6 and R7 have the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

摘要翻译： 式（I）的吡咯烷酮甲酰胺其中R 2 =式（a）或（b）的基团，R 5 =苯基，杂烷基，芳氧基，烷氧基，烷酰基或 R 6，R 7，R 12，R 11，R 4，R 4， >，R 6和R 7具有在说明书和权利要求书中给出的含义，药学上适用的与式（I）的碱式化合物的酸加成盐，药学上适用的盐 具有碱的式（I）酸化合物，含有羟基或羧基的式（I）化合物的药学上适用的酯及其水合物和溶剂合物抑制神经肽Y（NPY）与神经肽受体亚型之一的相互作用 NPY-Y5），特别适用于预防和治疗关节炎，糖尿病，特别是进食障碍和肥胖症。 上述可以通过已知方法制备并转化成盖仑剂型。

公开(公告)号：US20050192292A1

公开(公告)日：2005-09-01

申请号：US10500604

申请日：2002-12-27

申请人： Markus Isler ,  Thomas Giller ,  Gunter Schwaim ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

发明人： Markus Isler ,  Thomas Giller ,  Gunter Schwaim ,  Matthias Steger ,  Kurt Hilpert ,  Oliver Valdenaire ,  Volker Breu

IPC分类号： C07D207/26 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61K31/403 ,  C07D43/02 ,  C07D43/14

CPC分类号： C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14

摘要： Pyrrolidone carboxamides of formula (I) where R2=a group of formula (a) or (b), R5=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or —NR6R7 and R1, X, R3, R4, R6 and R7 have the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

摘要翻译： 式（I）的吡咯烷酮甲酰胺其中R 2 =式（a）或（b）的基团，R 5 =苯基，杂烷基，芳氧基，烷氧基，烷酰基或 R 6，R 7，R 12，R 11，R 4，R 4， >，R 6和R 7具有在说明书和权利要求书中给出的含义，药学上适用的与式（I）的碱式化合物的酸加成盐，药学上适用的盐 具有碱的式（I）酸化合物，含有羟基或羧基的式（I）化合物的药学上适用的酯及其水合物和溶剂合物抑制神经肽Y（NPY）与神经肽受体亚型之一的相互作用 NPY-Y5），特别适用于预防和治疗关节炎，糖尿病，特别是进食障碍和肥胖症。 上述可以通过已知方法制备并转化成盖仑剂型。