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1. 发明授权

US06632823B1 Substituted pyridine compounds useful as modulators of acetylcholine receptors 失效
标题翻译：可用作乙酰胆碱受体调节剂的取代吡啶化合物
公开(公告)号：US06632823B1
公开(公告)日：2003-10-14
申请号：US08996308
申请日：1997-12-22
申请人： Jean-Michel Vernier , Nicholas D. P. Cosford , Ian A. McDonald
发明人： Jean-Michel Vernier , Nicholas D. P. Cosford , Ian A. McDonald
IPC分类号： C07D21300
CPC分类号： C07D213/70 , A61K31/4439 , A61K31/4545 , A61K31/46 , C07D213/32 , C07D213/52 , C07D401/12 , C07D451/02 , C07D451/04 , C07D471/08
摘要： In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma, cardiovascular dysfunction including hypertension and cardiac arrhythmias, as well as co-medication uses in surgical applications.
摘要翻译：已经发现，根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的吡啶化合物（任选地含有醚，酯，酰胺，酮或硫醚取代）。在具体方面，本发明的化合物能够调节乙酰胆碱受体。本发明的化合物能够调节乙酰胆碱受体。本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂。具有乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默氏病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力障碍），帕特森氏病，锥体运动功能障碍，进行性肌肉麻痹，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍，如抑郁，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经分泌障碍和食物摄入异常，包括贪食症和厌食症; 疾病或疼痛的伤害和控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤，心血管功能障碍，包括高血压和心律失常，以及在外科应用中的共同用药用途。

2. 发明授权

US06818661B2 Anthranylalkyl and cycloalkyl amides and use thereof as VEGF receptor inhibitors 失效
标题翻译：蒽基烷基和环烷基酰胺及其作为VEGF受体抑制剂的用途
公开(公告)号：US06818661B2
公开(公告)日：2004-11-16
申请号：US10275585
申请日：2003-05-09
申请人： Dieter Seidelmann , Martin Krüger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
发明人： Dieter Seidelmann , Martin Krüger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
IPC分类号： C07D21300
CPC分类号： C07D213/38
摘要： The invention relates to substituted anthranylalkyl and cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.
摘要翻译：本发明涉及通式（I）的取代的苯甲酰基烷基和环烷基酰胺，以及它们作为用于治疗由持续性血管发生引起的疾病的药物的用途。

3. 发明授权

US06218539B1 IL-8 receptor antagonists 失效
标题翻译： IL-8受体拮抗剂
公开(公告)号：US06218539B1
公开(公告)日：2001-04-17
申请号：US09202568
申请日：1999-05-10
申请人： Katherine L. Widdowson
发明人： Katherine L. Widdowson
IPC分类号： C07D21300
CPC分类号： C07D213/75 , A61K31/44 , A61K31/505 , C07D239/47 , C07D239/48 , C07D239/545 , C07D239/56 , Y02A50/411
摘要： The present invention relates to the use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
摘要翻译：本发明涉及苯脲类治疗由趋化因子介导的疾病状态白细胞介素-8（IL-8）的用途。

4. 发明授权

US06759407B2 Acyclic and cyclic guanidine- and acetamidine derivatives, their preparation and their use as pesticides, ESP as parasiticides 失效
标题翻译：无环和环胍和脒衍生物，它们的制备及其作为农药的用途，作为杀寄生物的ESP
公开(公告)号：US06759407B2
公开(公告)日：2004-07-06
申请号：US10348574
申请日：2003-01-21
申请人： Thomas Goebel , Eliane Humbert-Droz , Maurizio Schwarzenbach
发明人： Thomas Goebel , Eliane Humbert-Droz , Maurizio Schwarzenbach
IPC分类号： C07D21300
CPC分类号： C07D277/32 , A01N47/12 , A01N47/16 , A01N47/44 , C07D213/61 , C07D417/06
摘要： Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).
摘要翻译：描述了式（I）的新型农药，其中取代基R 1，R 2，R 2，R 2'，T，U，X和Y如权利要求1中所定义。还描述了适合用作包含那些化合物作为活性成分的杀寄生虫剂的组合物和控制基于这些化合物或组合物的施用的寄生虫的方法，以及所述化合物和组合物在控制寄生虫和在制造杀虫剂用于对抗寄生虫。还描述了式（XX）的中间体，其中R 1，R 2，R 2'，T，U，X和Y如权利要求1中所定义; 并且Hal是卤素，后者还具有杀寄生虫活性，并且适于制备式（I）化合物。

5. 发明授权

US06538013B2 Acyclic and cyclic guanidine-and acetamidine derivatives, their preparation and their use as pesticides, esp. as parasiticides 失效
标题翻译：非环和环胍和乙脒衍生物，它们的制备及其作为农药的用途，作为杀寄生虫剂
公开(公告)号：US06538013B2
公开(公告)日：2003-03-25
申请号：US09850378
申请日：2001-05-07
申请人： Thomas Goebel , Eliane Humbert-Droz , Maurizio Schwarzenbach
发明人： Thomas Goebel , Eliane Humbert-Droz , Maurizio Schwarzenbach
IPC分类号： C07D21300
CPC分类号： C07D277/32 , A01N47/12 , A01N47/16 , A01N47/44 , C07D213/61 , C07D417/06
摘要： Novel pesticides of formula (I) wherein the substituents R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1 and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).
摘要翻译：描述了式（I）的新型农药，其中取代基R，R 1，R 2，R 2'，T，U，X和Y如权利要求1中所定义。还描述了适合用作包含那些化合物作为活性成分的杀寄生虫剂的组合物和控制基于这些化合物或组合物的施用的寄生虫的方法，以及所述化合物和组合物在控制寄生虫和在制造杀虫剂用于对抗寄生虫。还描述了式（XX）的中间体，其中R 1，R 2，R 2'，T，U，X和Y如权利要求1中所定义，Hal是卤素。后者还具有杀寄生虫活性，适用于制备式（I）化合物。

6. 发明授权

US06207829B1 Process for preparation of pyrazolo[4,3-d]pyrimidin-7-ones and intermediates thereof 失效
标题翻译：吡唑并[4,3-d]嘧啶-7-酮的制备方法及其中间体
公开(公告)号：US06207829B1
公开(公告)日：2001-03-27
申请号：US09415440
申请日：1999-10-08
申请人： Peter James Dunn , Philip Charles Levett
发明人： Peter James Dunn , Philip Charles Levett
IPC分类号： C07D21300
CPC分类号： C07D295/26 , C07D487/04
摘要： A process is provided for the preparation of a compound of formulae (IA) (sidenafil) and (IB) comprising reacting a compound of formula (IIA) and (IIB) respectively in the presence of —OR, wherein R in the case of formation of compound (IA) is CH2CH3 and R in the case of formation of compound (IB) is CH2CH2CH3, where X is a leaving group:
摘要翻译：提供了制备式（IA）（西多那非）和（IB）化合物的方法，包括分别在-OR存在下使式（IIA）和（IIB）化合物反应，其中在形成化合物（IA）为CH 2 CH 3，在形成化合物（IB）的情况下，R为CH 2 CH 2 CH 3，其中X为离去基团：

7. 发明授权

US06670480B2 Process for preparing substituted pyridines 失效
标题翻译：制备取代吡啶的方法
公开(公告)号：US06670480B2
公开(公告)日：2003-12-30
申请号：US10317720
申请日：2002-12-12
申请人： Robert L. Dow , Steven R. Schneider
发明人： Robert L. Dow , Steven R. Schneider
IPC分类号： C07D21300
CPC分类号： C07F7/1892 , C07F7/1804 , C07F7/188 , Y02P20/55
摘要： A process for preparing a compound of the formula wherein n, R1, R2, R3 and X are as defined above, used as an intermediate in the synthesis of &bgr;-adrenergic receptor agonists.
摘要翻译：制备n，R 1，R 2，R 3和X的化合物的方法如上所定义，用作β-肾上腺素能受体激动剂的合成中的中间体。

8. 发明授权

US06657063B1 Combinations of &bgr;3 agonists and growth hormone secretagogues 失效
标题翻译： β3激动剂和生长激素促分泌素的组合
公开(公告)号：US06657063B1
公开(公告)日：2003-12-02
申请号：US09649622
申请日：2000-08-28
申请人： Robert L. Dow
发明人： Robert L. Dow
IPC分类号： C07D21300
CPC分类号： C07D213/73 , C07D487/04
摘要： This invention is directed to pharmaceutical compositions comprising &bgr;3 adrenergic agonists including (4-(2-(2-(6-aminopyridin-3-yl)-2(R)-hydroxyethylamino)ethoxy)phenyl)acetic acid and growth hormone or growth hormone secretagogues, prodrugs thereof or pharmaceutically acceptable salts of said compounds or said prodrugs. The invention is also directed to methods of using those compositions in the treatment of obesity, diabetes, hypertension and frailty in animals and particularly in humans.
摘要翻译：本发明涉及包含β3肾上腺素能激动剂的药物组合物，其包括（4-（2-（2-（6-氨基吡啶-3-基）-2（R） - 羟乙基氨基）乙氧基）苯基）乙酸和生长激素或生长激素促分泌素，前药或所述化合物或所述前药的药学上可接受的盐。本发明还涉及使用这些组合物治疗肥胖症，糖尿病，高血压和动物，特别是人体虚弱的方法。

9. 发明授权

US06635766B1 Process for the preparation of arylamides of heteroaromatic carboxylic acids 失效
标题翻译：用于制备杂芳族羧酸芳基酰胺的方法
公开(公告)号：US06635766B1
公开(公告)日：2003-10-21
申请号：US08829512
申请日：1997-03-28
申请人： Jean-Paul Roduit , Georges Kalbermatten
发明人： Jean-Paul Roduit , Georges Kalbermatten
IPC分类号： C07D21300
CPC分类号： B01J31/2409 , B01J31/04 , B01J31/26 , B01J2231/4205 , B01J2531/824 , C07D213/81 , C07D213/82 , C07D239/34 , C07D241/24
摘要： A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.
摘要翻译：制备下式的杂芳族羧酸的芳基酰胺的方法：其中每个A n为氮或CR n（n = 1至5），条件是至少一个环成员为氮并且两个氮原子彼此不直接键合; R 1至R 5如果存在，彼此独立; C 1-4 - 烷基或芳基，取代基R 1至R 5之一是式-OR的基团，其中R是任选取代的芳族或杂芳族基团; R 6是氢或C 1-4 - 烷基; 并且R 7是任选取代的芳族或杂芳族基团。在钯二膦配合物的存在下，酰胺由相应的杂芳族卤素化合物，相应的芳族胺和一氧化碳获得。该类化合物（式I）是重要的除草剂。

10. 发明授权

US06235909B1 Preparation of is-[1A,2B,3B,4A(S*)]-4-[7-[[1-(3-chloro-2-Thienyl)methyl]amino]-3H-imidazo [4,5-B]pyridin-3-YL]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide 失效
标题翻译：制备is- [1A，2B，3B，4A（S *）] - 4- [7 - [[1-（3-氯-2-噻吩基）甲基]氨基] -3H-咪唑并[4,5-B ]吡啶-3-基] -N-乙基-2,3-二羟基环戊烷甲酰胺
公开(公告)号：US06235909B1
公开(公告)日：2001-05-22
申请号：US09627657
申请日：2000-07-28
申请人： Herve Garcia , Patrick Leon , Benoit J. Vanasse
发明人： Herve Garcia , Patrick Leon , Benoit J. Vanasse
IPC分类号： C07D21300
CPC分类号： C07D213/69 , C07D409/12 , C07D409/14 , C07D471/04
摘要： This invention is directed to methods for the preparation of [1S-[1a,2b,3b,4a(S*)]]-4-[7-[[-(3-chloro-2-thienyl)methyl]propyl]amino]-3 H-imidazo[4,5-b]pyridin-3-yl]]-N-ethyl-2,3-dihydroxycyclopentanecarboxamide, methods for the preparation of intermediates thereto, and to said intermediates themselves.
摘要翻译：本发明涉及制备[1S- [1a，2b，3b，4a（S *）]] - 4- [7 - [[ - （3-氯-2-噻吩基）甲基]丙基]氨基 ] -3H-咪唑并[4,5-b]吡啶-3-基]] - N-乙基-2,3-二羟基环戊烷甲酰胺，制备其中间体的方法和所述中间体本身。

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