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    • 3. 发明申请
    • 4-OXO-4,5-DIHYDRO-FURAN-2-CARBOXYLIC AND ACID DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF
    • 4-氧代-4,5-二氢 - 呋喃-2-羧酸和酸衍生物及其代谢相关疾病的治疗方法
    • WO2005051937A8
    • 2006-08-31
    • PCT/US2004038920
    • 2004-11-18
    • ARENA PHARM INCJUNG JAE-KYUSEMPLE GRAEMEJOHNSON BENJAMIN R
    • JUNG JAE-KYUSEMPLE GRAEMEJOHNSON BENJAMIN R
    • C07D307/68C07D409/04C07D409/10
    • C07D307/68C07D405/04C07D409/04C07D409/10
    • The present invention relates to certain 4-oxo-4,5-dihydro-furan-2-carboxylic acid and ester derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X, and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of a-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, and the like.
    • 本发明涉及式(I)的某些4-氧代-4,5-二氢呋喃-2-羧酸和酯衍生物及其药学上可接受的盐,其表现出有用的药理学性质,例如作为RUP25的激动剂 受体。 本发明还提供含有本发明化合物的药物组合物和使用本发明化合物和组合物治疗代谢相关疾病(包括血脂异常,动脉粥样硬化,冠心病,胰岛素抵抗,2型糖尿病, 综合征-X等。 此外,本发明还提供了本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类,醛糖还原酶抑制剂,双胍类,HMG-CoA还原酶抑制剂,角鲨烯合成 抑制剂,贝特类,LDL分解代谢增强剂,血管紧张素转换酶(ACE)抑制剂,胰岛素分泌增强剂等。
    • 6. 发明专利
    • CANNABINOID RECEPTOR MODULATORS
    • SG10201901293RA
    • 2019-03-28
    • SG10201901293R
    • 2010-08-27
    • ARENA PHARM INC
    • JONES ROBERT MHAN SANGDONTHORESEN LARSJUNG JAE-KYUSTRAH-PLEYNET SONJAZHU XIUWENXIONG YIFENGYUE DAWEI
    • CANNABINOIDRECEPTOR MODULATORS The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CBI receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, 10 inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate 15 cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease. (NO SUITABLE FIGURE) -343-
    • 7. 发明专利
    • Cannabinoid receptor modulators
    • NZ598288A
    • 2014-02-28
    • NZ59828810
    • 2010-08-27
    • ARENA PHARM INC
    • JONES ROBERT MHAN SANGDONTHORESEN LARSJUNG JAE-KYUSTRAH-PLEYNET SONJAZHU XIUWENXIONG YIFENGYUE DAWEI
    • C07D231/54A61K31/416A61K31/4439A61K31/497A61K31/661A61P19/02A61P29/00C07D401/04C07D401/14C07D403/04C07D405/14C07F9/09
    • IP No. 598288 The present disclosure relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present disclosure further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present disclosure and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer’s disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson’s disease. Compounds of the disclosure: (1aR,5aR)-2-(5-Chloro-pyridin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide Phosphoric acid mono-(2-{ [(1aR,5aR)-2-(4-cyano-pyridin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carbonyl]-amino} -2-methyl-propyl) ester (1aR,5aR)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((S)-2,2-dimethyl-1-methylcarbamoyl-propyl)-amide (1aS,5aS)-(S)-2-Amino-3-methyl-butyric acid (S)-3,3-dimethyl-2-{ [2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carbonyl]-amino} -butyl ester (1aS,5aS)-2-(4-Oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid ((1S,2S)-2-hydroxy-indan-1-yl)-amide And (1aR,5aR)-2-(4-Fluoro-pyridin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diazacyclopropa[a]pentalene-4-carboxylic acid (2-hydroxy-1,1-dimethyl-ethyl)-amide