Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity
    61.
    发明授权
    Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity 失效
    具有5-HT 4受体激动活性的喹诺酮羧酸化合物

    公开(公告)号:US07964727B2

    公开(公告)日:2011-06-21

    申请号:US10595948

    申请日:2004-11-10

    摘要: This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

    摘要翻译: 本发明提供式(I)化合物:其中Het表示具有一个氮原子的杂环基团,B直接与该碳原子结合,并且具有4至7个碳原子,所述杂环基团未被取代或被1至4个取代基取代 独立地选自取代基α1; A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R1表示异丙基,正丙基或环戊基; R2表示甲基,氟原子或氯原子; R3独立地表示(i)氧代基,羟基,氨基,烷基氨基或羧基; (ii)具有3至8个碳原子的环烷基,所述环烷基被1至5个取代基取代,或(iii)具有3至8个原子的杂环基,所述杂环基未被取代或被1 至5个取代基,n为1,2或3,或其药学上可接受的盐。 这些化合物具有5-HT 4受体激动活性,因此可用于治疗哺乳动物特别是人类的胃食管反流病,非溃疡性消化不良,功能性消化不良,肠易激综合征等。

    Sulfonyl benzimidazole derivatives
    62.
    发明授权
    Sulfonyl benzimidazole derivatives 失效
    磺酰基苯并咪唑衍生物

    公开(公告)号:US07700618B2

    公开(公告)日:2010-04-20

    申请号:US12280586

    申请日:2007-02-23

    摘要: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.

    摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,其中A,R 1,R 2,R 3,R 4,R 5,m和n各自如本文所述,和含有这些化合物的组合物, 治疗由CB2受体活性介导的病症,例如但不限于炎症性疼痛,伤害性疼痛,神经性疼痛,纤维肌痛,慢性腰痛,内脏痛,急性脑缺血,疼痛,慢性疼痛, 急性疼痛,疱疹后神经痛,神经病,神经痛,糖尿病性神经病,HIV相关神经病,神经损伤,类风湿关节炎疼痛,骨关节炎疼痛,背痛,癌症疼痛,牙痛,纤维肌痛,神经炎,坐骨神经痛,炎症,神经变性疾病,咳嗽 ,支气管收缩,肠易激综合征(IBS),炎性肠病(IBD),结肠炎,脑血管缺血,呕吐如癌症化疗诱发的呕吐,类风湿性关节炎,哮喘,克罗恩病 溃疡性结肠炎,哮喘,皮炎,季节性过敏性鼻炎,GERD,便秘,腹泻,功能性胃肠道疾病,肠易激综合征,皮肤T细胞淋巴瘤,多发性硬化症,骨关节炎,牛皮癣,系统性红斑狼疮,糖尿病,青光眼,骨质疏松症,肾小球性肾炎, 肾缺血,肾炎,肝炎,脑中风,血管炎,心肌梗死,脑缺血,可逆性气道阻塞,成人呼吸道疾病综合征,COPD,隐源性纤维化肺泡炎和支气管炎。

    SULFONYL BENZIMIDAZOLE DERIVATIVES
    63.
    发明申请
    SULFONYL BENZIMIDAZOLE DERIVATIVES 失效
    磺酰苯并咪唑衍生物

    公开(公告)号:US20090137584A1

    公开(公告)日:2009-05-28

    申请号:US12280586

    申请日:2007-02-23

    摘要: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R1, R2, R3, R4, R5, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis.

    摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,其中A,R 1,R 2,R 3,R 4,R 5,m和n各自如本文所述,和含有这些化合物的组合物, 治疗由CB2受体活性介导的病症,例如但不限于炎症性疼痛,伤害性疼痛,神经性疼痛,纤维肌痛,慢性腰痛,内脏痛,急性脑缺血,疼痛,慢性疼痛, 急性疼痛,疱疹后神经痛,神经病,神经痛,糖尿病性神经病,HIV相关神经病,神经损伤,类风湿关节炎疼痛,骨关节炎疼痛,背痛,癌症疼痛,牙痛,纤维肌痛,神经炎,坐骨神经痛,炎症,神经变性疾病,咳嗽 ,支气管收缩,肠易激综合征(IBS),炎性肠病(IBD),结肠炎,脑血管缺血,呕吐如癌症化疗诱发的呕吐,类风湿性关节炎,哮喘,克罗恩病 溃疡性结肠炎,哮喘,皮炎,季节性过敏性鼻炎,GERD,便秘,腹泻,功能性胃肠道疾病,肠易激综合征,皮肤T细胞淋巴瘤,多发性硬化症,骨关节炎,牛皮癣,系统性红斑狼疮,糖尿病,青光眼,骨质疏松症,肾小球性肾炎, 肾缺血,肾炎,肝炎,脑中风,血管炎,心肌梗死,脑缺血,可逆性气道阻塞,成人呼吸道疾病综合征,COPD,隐源性纤维化肺泡炎和支气管炎。

    1-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity
    64.
    发明申请
    1-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity 失效
    具有5-Ht4受体激动活性的1-异丙基-2-氧代-1,2-二氢吡啶-3-甲酰胺衍生物

    公开(公告)号:US20080293767A1

    公开(公告)日:2008-11-27

    申请号:US10597480

    申请日:2005-01-18

    CPC分类号: C07D401/12 C07D405/14

    摘要: This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

    摘要翻译: 本发明提供式(I)化合物:其中R 1表示具有1至4个碳原子的烷基或卤原子,R 2表示具有1至4个碳原子的烷基,R 3表示氢原子或羟基 基团,A表示氧原子或式-C(R4)(R5) - (其中R4表示氢原子或具有1至4个碳原子的烷基,R5表示羟基或式 具有1至4个碳原子的烷氧基)或其药学上可接受的盐。 这些化合物具有5-HT 4受体激动活性,因此可用于治疗哺乳动物特别是人类的胃食管反流病,非溃疡性消化不良,功能性消化不良,肠易激综合征等。

    Indazole Derivatives
    65.
    发明申请
    Indazole Derivatives 失效
    吲唑衍生物

    公开(公告)号:US20080269211A1

    公开(公告)日:2008-10-30

    申请号:US11995179

    申请日:2006-07-14

    摘要: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 agonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.

    摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,其中:R 1,R 2,R 3, A和m各自如本文所述,含有这些化合物的组合物和这些化合物在治疗由5-HT 4激动剂活性介导的病症中的用途,例如但不限于胃食管反流 疾病,胃肠道疾病,胃动力障碍,非溃疡性消化不良,功能性消化不良,肠易激综合征(IBS),便秘,消化不良,食管炎,胃食管疾病,恶心,中枢神经系统疾病,阿尔茨海默氏病,认知障碍,呕吐,偏头痛, 神经疾病,疼痛,心血管疾病,心力衰竭,心律失常,糖尿病和呼吸暂停综合征。

    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
    67.
    发明授权
    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents 失效
    磺酰苯化合物作为抗炎/止痛剂

    公开(公告)号:US06727238B2

    公开(公告)日:2004-04-27

    申请号:US10465767

    申请日:2003-06-18

    IPC分类号: A61K3133

    摘要: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

    摘要翻译: 本发明提供下式的化合物或其药学上可接受的盐,其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环,其中4-(磺酰基)苯基和4-取代的苯基 在式(I)中,与环A相邻的环原子相连; R 1是任选取代的芳基或杂芳基,条件是当A是吡唑时,R 1是杂芳基; R 2是C 1-4烷基,卤素取代的C 1-4烷基,C 1-4烷基氨基,C 1-4二烷基氨基或氨基; R 3,R 4和R 5独立地是氢,卤素,C 1-4烷基,卤素取代的C 1-4烷基等; 或R 3,R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢,卤素,C 1-4烷基,卤素取代的C 1-4烷基,C 1-4烷氧基,C 1-4烷硫基,C 1-4烷基氨基或N,N-二C1- 4烷基氨基; 并且m和n独立地为1,2,3或4.本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。

    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
    68.
    发明授权
    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents 失效
    磺酰苯化合物作为抗炎/止痛剂

    公开(公告)号:US06608095B2

    公开(公告)日:2003-08-19

    申请号:US09841348

    申请日:2001-04-24

    IPC分类号: A61K3141

    摘要: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

    摘要翻译: 本发明提供下式的化合物或其药学上可接受的盐,其中A是部分不饱和或不饱和的五元杂环或部分不饱和或不饱和的五元碳环,其中4-(磺酰基)苯基和4-取代的苯基 在式(I)中,与环A相邻的环原子相连; R1是任选取代的芳基或杂芳基,条件是当A是吡唑时,R 1是杂芳基; R2是C1-4烷基,卤素取代的C1-4烷基,C1-4烷基氨基,C1-4二烷基氨基或氨基; R 3,R 4和R 5独立地为氢,卤素,C 1-4烷基,卤素取代的C 1-4烷基等; 或者R 3,R 4和R 5中的两个与它们所连接的原子一起形成4-7元环; R 6和R 7独立地是氢,卤素,C 1-4烷基,卤素取代的C 1-4烷基,C 1-4烷氧基,C 1-4烷硫基,C 1-4烷基氨基或N,N-二C 1-4烷基氨基; 并且m和n独立地为1,2,3或4.本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。

    Organic EL multi-color light-emitting device

    公开(公告)号:US10276637B2

    公开(公告)日:2019-04-30

    申请号:US14114880

    申请日:2012-05-09

    摘要: An organic EL multi-color emitting device including a substrate, and a first light-emitting element and a second light-emitting element arranged on the surface of the substrate; the first light-emitting element including, between an anode and a cathode, a first organic layer, a second organic layer and a third organic layer in this sequence in a direction perpendicular to the surface of the substrate; the second light-emitting element including, between an anode and a cathode, a second organic layer and a third organic layer in this sequence in a direction perpendicular to the surface of the substrate; the first organic layer including a first light-emitting dopant; the third organic layer including a second light-emitting dopant; the second organic layer including any of (A) a compound including an arylamine site, and a furan site or a thiophene site, (B) a compound including an arylamine site and a site comprising a nitrogen-containing six-membered ring structure, (C) a compound including a carbazole site, and a furan site or a thiophene site, and (D) a compound including a carbazole site and a site including a nitrogen-containing six-membered ring structure.