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    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
    1.
    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：US06949536B2

    公开(公告)日：2005-09-27

    申请号：US10771861

    申请日：2004-02-03

    申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    IPC分类号： A61K31/33 ,  A61K31/4025 ,  A61K31/422 ,  A61K31/425 ,  A61K31/427 ,  A61K31/454 ,  C07D233/00 ,  C07D277/00 ,  C07D333/00

    CPC分类号： A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  C07C311/39 ,  C07C317/36 ,  C07D207/325 ,  C07D207/333 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

    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烷基氨基或氨基; R 4，R 4和R 5独立地是氢，卤素，C 1-4烷基，卤代 - 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 < 烷基氨基; m和n分别为1,2,3或4.本发明还提供了一种药物组合物，其用于治疗前列腺素涉及病原体的医疗状况。

    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
    2.
    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

    申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    IPC分类号： A61K3133

    CPC分类号： A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  C07C311/39 ,  C07C317/36 ,  C07D207/325 ,  C07D207/333 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

    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
    3.
    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

    申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    IPC分类号： A61K3141

    CPC分类号： C07D207/335 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

    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。

    Sulfonylbenzene compounds as anti-inflammatory/analgesic agents
    4.
    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：US06294558B1

    公开(公告)日：2001-09-25

    申请号：US09446049

    申请日：1999-12-15

    申请人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    发明人： Kazuo Ando ,  Tomoki Kato ,  Akiyoshi Kawai ,  Tomomi Nonomura

    IPC分类号： A61K3144

    CPC分类号： C07D207/335 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

    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; 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; m和n分别为1,2,3或4.本发明还提供了一种药物组合物，其用于治疗前列腺素涉及病原体的医疗状况。

    Sulfonyl benzimidazole derivatives
    10.
    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

    申请人： Tomoki Kato ,  Kana Kon-I ,  Yohei Yuki ,  Kazuo Ando

    发明人： Tomoki Kato ,  Kana Kon-I ,  Yohei Yuki ,  Kazuo Ando

    IPC分类号： A61K31/437 ,  A61K31/4184 ,  C07D471/04 ,  C07D235/08

    CPC分类号： C07D235/08 ,  C07D235/12 ,  C07D405/12 ,  C07D471/04

    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。