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公开(公告)号:US06586445B1
公开(公告)日:2003-07-01
申请号:US09719455
申请日:2001-06-13
申请人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan , Dennis C. H. Bigg , Jacques Pommier
发明人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan , Dennis C. H. Bigg , Jacques Pommier
IPC分类号: A61K314165
CPC分类号: C07D471/04 , C07D471/10 , C07D495/04
摘要: The present invention is directed to compounds of the formula wherein the variables are defined in the specification, which bind to somatostatin receptors and block Na channels.
摘要翻译: 本发明涉及在说明书中定义的变体的化合物,其结合生长抑素受体并阻断Na通道。
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公开(公告)号:US07566734B2
公开(公告)日:2009-07-28
申请号:US10333556
申请日:2001-07-31
申请人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Thomas D. Gordon , Barry A. Morgan , Christophe Philippe Moinet , Dennis C. H. Bigg
发明人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Thomas D. Gordon , Barry A. Morgan , Christophe Philippe Moinet , Dennis C. H. Bigg
IPC分类号: A61K31/4164 , A61K31/417 , C07D233/02 , C07D233/61
CPC分类号: C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D497/04
摘要: The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonists or antagonists of somatostatin receptors.
摘要翻译: 本发明涉及式(I)的咪唑基衍生物,其中取代基在说明书中定义,其可用作促生长素抑制素受体的激动剂或拮抗剂。
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公开(公告)号:US07638546B1
公开(公告)日:2009-12-29
申请号:US11927104
申请日:2007-10-29
申请人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Thomas D. Gordon , Barry A. Morgan , Christophe Philippe Moinet , Dennis C. H. Bigg
发明人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Thomas D. Gordon , Barry A. Morgan , Christophe Philippe Moinet , Dennis C. H. Bigg
IPC分类号: A61K31/4985
CPC分类号: C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D491/10 , C07D497/04
摘要: The present invention is directed to imidazolyl derivatives of formula (I) where the substituents are defined in the specification, which are useful as agonist or antagonists of somatostatin receptors.
摘要翻译: 本发明涉及式(I)的咪唑基衍生物,其中取代基在说明书中定义,其可用作促生长素抑制素受体的激动剂或拮抗剂。
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公开(公告)号:US07238695B2
公开(公告)日:2007-07-03
申请号:US10771725
申请日:2004-02-04
申请人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan
发明人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan
IPC分类号: A01N43/50 , A61K31/415 , C07D233/00 , C07D413/00 , C07D403/00
CPC分类号: C07D233/64 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/14
摘要: The present invention is directed to imidazolyl derivatives or pharmaceutically acceptable salts thereof which are useful as agonists or antagonists of somatostatin receptors, having the following formula (I), wherein the substituents are defined in the specification.
摘要翻译: 本发明涉及咪唑基衍生物或其药学上可接受的盐,其可用作生长抑素受体的激动剂或拮抗剂,具有下式(I),其中取代基在说明书中定义。
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公开(公告)号:US06852725B1
公开(公告)日:2005-02-08
申请号:US09719457
申请日:1999-06-08
申请人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan
发明人: Christophe Alain Thurieau , Lydie Francine Poitout , Marie-Odile Galcera , Christophe Philippe Moinet , Thomas D. Gordon , Barry A. Morgan
IPC分类号: C07D233/60 , A61K31/40 , A61K31/415 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4985 , A61P1/04 , A61P1/06 , A61P1/12 , A61P1/18 , A61P3/06 , A61P3/10 , A61P5/02 , A61P5/06 , A61P5/18 , A61P5/48 , A61P7/04 , A61P9/00 , A61P9/02 , A61P9/10 , A61P13/12 , A61P15/00 , A61P17/00 , A61P25/00 , A61P25/22 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , A61P43/00 , C07D209/56 , C07D211/30 , C07D233/00 , C07D233/54 , C07D233/64 , C07D235/16 , C07D401/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/10 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/14
CPC分类号: C07D233/64 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D491/14
摘要: The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to the somatostatin subtype receptors and elicit either an agonist or antagonist effect from the somatostatin subtype receptors. The derivatives are useful for treating a variety of diseases including acromegaly, restenosis, Crohn's disease, systemic sclerosis, external and internal pancreatic pseudocysts and ascites, VIPoma, nesidoblastosis, hyperinsulinism, gastrinoma, Zollinger-Ellison Syndrome, diarrhea, AIDS related diarrhea, chemotherapy related diarrhea, scleroderma, Irritable Bowel Syndrome, pancreatitis, small bowel obstruction, gastroesophageal reflux, duodenogastric reflux, Cushing's Syndrome, gonadotropinoma, hyperparathyroidism, Graves' Disease, diabetic neuropathy, Paget's disease, polycystic ovary disease, cancer, cancer cachexia, hypotension, postprandial hypotension, panic attacks, GH secreting adenomas or TSH secreting adenomas.
摘要翻译: 本发明涉及下式的咪唑基衍生物:其中取代基在说明书中定义,或其药学上可接受的盐。 衍生物选择性地结合生长抑素亚型受体并引发生长抑素亚型受体的激动剂或拮抗剂作用。 该衍生物可用于治疗各种疾病,包括肢端肥大症,再狭窄,克罗恩病,系统性硬化症,外部和内部胰腺假性囊肿和腹水,VIPoma,成囊胚细胞瘤,高胰岛素血症,胃泌素瘤,佐林格 - 埃里森综合征,腹泻,艾滋病相关性腹泻,化疗相关 腹泻,硬皮病,肠易激综合征,胰腺炎,小肠阻塞,胃食管反流,十二指肠胃反流,库兴综合征,促性腺激素,甲状旁腺功能亢进,格雷夫斯病,糖尿病性神经病,佩吉特氏病,多囊卵巢疾病,癌症恶病质,低血压,餐后低血压 ,惊恐发作,GH分泌腺瘤或TSH分泌腺瘤。
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公开(公告)号:US07361656B2
公开(公告)日:2008-04-22
申请号:US11353518
申请日:2006-02-14
申请人: Thomas D. Gordon , Barry A. Morgan
发明人: Thomas D. Gordon , Barry A. Morgan
IPC分类号: A61P35/00 , A61K31/495 , A61K31/50 , C07D487/02
CPC分类号: C07D487/04 , C07D513/14
摘要: A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R25); and the remaining substituents are as defined in the disclosure.
摘要翻译: 用于抑制异戊烯基转移酶活性的咪唑化合物家族。 化合物被下式所覆盖:其中X是(CHR 11)n 3(CH 2)n 4 Z(CH 2)n N 5其中Z是O,N(R 12),S或键; Y是CO,CH 2,CS或键; R 1是或N(R 24,R 25); 并且其余的取代基如本公开中所定义。
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公开(公告)号:US07323484B2
公开(公告)日:2008-01-29
申请号:US11287996
申请日:2005-11-28
申请人: Thomas D. Gordon , Barry A. Morgan
发明人: Thomas D. Gordon , Barry A. Morgan
IPC分类号: A61K31/415 , C07D233/58
CPC分类号: C07D233/64 , C07D277/28 , C07D277/56 , C07D487/04
摘要: The present invention is directed to compounds of the formula wherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.
摘要翻译: 本发明涉及下式的化合物,其中变量如说明书中所定义。 该化合物可用于抑制法呢基转移酶和治疗肿瘤和再狭窄。
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公开(公告)号:US07094753B2
公开(公告)日:2006-08-22
申请号:US10302431
申请日:2002-11-21
IPC分类号: A61K38/00
CPC分类号: C07K14/6555 , A61K38/00
摘要: Claimed is a somatostatin agonist according to formula (I), D-Phe-c(Cys-Tyr(I)-D-Trp-Lys-Val-Cys)-Thr-NH2, (I) or a pharmaceutically acceptable salt thereof, and uses thereof.
摘要翻译: 要求的是根据式(I)的生长抑素激动剂,<?in-line-formula description =“In-line Formula”end =“lead”?> D-Phe-c(Cys-Tyr(I)-D-Trp -Lys-Val-Cys)-Thr-NH 2,(I)<?in-line-formula description =“In-line Formulas”end =“tail”?>或其药学上可接受的盐 及其用途。
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公开(公告)号:US07022704B2
公开(公告)日:2006-04-04
申请号:US10273735
申请日:2002-10-18
申请人: Thomas D. Gordon , Barry A. Morgan
发明人: Thomas D. Gordon , Barry A. Morgan
IPC分类号: A61K31/496 , C07D487/04
CPC分类号: C07D233/64 , C07D277/28 , C07D277/56 , C07D487/04
摘要: A family of tetrahydroimidazo[1,2a]pyrazine based compounds capable of inhibiting the activity of farnesyl transferase and treating tumors and restenosis having the following structure: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined in the specification.
摘要翻译: 能够抑制法呢基转移酶活性和治疗具有以下结构的肿瘤和再狭窄的四氢咪唑并[1,2a]吡嗪类化合物家族:或其药学上可接受的盐,其中变量如说明书中所定义。
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公开(公告)号:US5378803A
公开(公告)日:1995-01-03
申请号:US912949
申请日:1992-07-10
CPC分类号: C07K5/0821 , C07K5/0207
摘要: Azole-fused peptides useful as Substance P antagonists and analgesics, for example ##STR1## wherein ##STR2## represents ##STR3## wherein X is O, S or NH and * is D, or as intermediates therefor are prepared by azole and peptide forming methods.
摘要翻译: 可用作物质P拮抗剂和止痛剂的唑固定肽例如
其中X是O,S或NH和*是D,或其中间体通过唑和肽形成方法制备 。
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