摘要:
The present invention relates to a CXCR3 antagonist comprising a compound represented by formula (I) (wherein all the symbols have the same meaning as defined in the description),a salt thereof, a quaternary ammonium salt thereof, an N-oxide form thereof or a solvate thereof, or a prodrug thereof.This antagonist is useful as a preventive, therapeutic and/or progression-suppressing agent for a CXCR3-mediated disease such as an immune or an allergic disease [e.g., an atopic disease, an autoimmune disease (e.g., multiple sclerosis, rheumatoid arthritis, systemic lupus erythematosus, type I diabetes, glomerulonephritis, Sjogren's syndrome and the like), systemic inflammatory response syndrome (SIRS), a rejection response to transplanted organ, tissue and/or cell or the like], a gastrointestinal disease [e.g., an inflammatory bowel disease or the like], or a respiratory disease [e.g., asthma, a chronic obstructive pulmonary disease or the like].
摘要:
Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 is H or alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.
摘要翻译:式(I)的三氮杂螺[5.5]十一烷衍生物,其季铵盐,其N-氧化物,其无毒盐或包含它们的药物组合物作为活性成分(其中R 1〜 式(II)或式(III); R 2是烷基或炔基等; R 3,R 4是H,(取代的 )烷基等,或R 3和R 4一起形成式(IV); R 5是H或烷基)。 因此,式(I)化合物调节趋化因子/趋化因子受体的作用,它们用于预防和治疗各种炎性疾病,哮喘,特应性皮炎,荨麻疹,过敏性疾病,肾炎,肾病,肝炎,关节炎或类风湿关节炎 等等
摘要:
The present invention relates to a medicament comprising the compound of formula (I) wherein all symbols have the same meanings as defined in the specification, a salt thereof or a prodrug thereof. The compound of the present invention is useful for the prevention and/or treatment of immune diseases such as various types of inflammation, autoimmune disease, allergic diseases, etc.; infection concerning inflammation or HIV infections (e.g. asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), organ transplantation rejection, immunosuppression, psoriasis, multiple sclerosis, optic neuritis, polymyalgia rheumatica syndrome, uveitis, vasculitis, human immunodeficiency virus infection (acquired immunodeficiency syndrome etc.), atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, osteoarthritis, ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacteria infection, diabetes, cancer metastasis, atherosclerosis, etc.).
摘要:
Triazaspiro[5.5]undecane derivatives, quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as an active ingredient. So the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.
摘要:
Triazaspiro[5.5]undecane derivatives of the formula (I), quaternary ammonium salts thereof, N-oxides thereof, non-toxic salts thereof, or pharmaceutical compositions comprising them, as active ingredients (wherein R1 is formula (II) or formula (III); R2 is alkyl or alkynyl etc.; R3, R4 is H, (substituted) alkyl etc., or R3 and R4 together to form formula (IV); R5 is H or alkyl). Therefore the compounds of the formula (I) regulate the effect of chemokine/chemokine receptor, they are used for prevention and treatment of various inflammatory diseases, asthma, atopic dermatitis, urticaria, allergic diseases, nephritis, nephropathy, hepatitis, arthritis or rheumatoid arthritis etc.
摘要翻译:式(I)的三氮杂螺[5.5]十一烷衍生物,其季铵盐,其N-氧化物,其无毒盐或包含它们的药物组合物作为活性成分(其中R 1〜 式(II)或式(III); R 2是烷基或炔基等; R 3,R 4是H,(取代的 )烷基等,或R 3和R 4一起形成式(IV); R 5是H或烷基)。 因此,式(I)化合物调节趋化因子/趋化因子受体的作用,它们用于预防和治疗各种炎性疾病,哮喘,特应性皮炎,荨麻疹,过敏性疾病,肾炎,肾病,肝炎,关节炎或类风湿关节炎 等等
摘要:
A compound having an ability to bind to an SIP receptor and represented by formula (I), a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like: wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.
摘要:
A therapeutic and/or preventing agent for a disease due to vascular constriction or vasodilation comprising a EDG-5 modulator. Since EDG-5 modulator specifically binds EDG-5 and shows antagonistic or agonistic action, EDG-5 antagonist is useful for treating and/or preventing for a disease due to vascular constriction, for example, cerebrovascular spasmodic disorder after subarachnoid hemorrhage or stroke, cardiovasucular spasmodic disorder, hypertension, renal disease, cardiac infarction, cardiac angina, arrhythmia, facilitation of the portal blood pressure involved in liver cirrhosis, varicosity involved in liver cirrhosis and the like, or EDG-5 agonist is useful for treating and/or preventing for a disease due to vasodilation of blood vessels, for example, chronic headache (such as migraine, tension-type headache, mixed-type headache thereof, or migrainous neuralgia), haemorrhoid, congestive disorder and the like.
摘要:
A compound of the general formula (I) (wherein the symbols are as defined in the description), or a prodrug or a salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be caused by spinal cord neoplasm, nucleous hernia, spinal canal stenosis or diabetes, lower urinary tract symptom (for example, occlusion disease of lower urinary tract), inflammatory disease of lower urinary tract, polyuria), carcinoma association disease (solid tumor, solid tumor metastasis, angiofibroma, myeloma, multiple myeloma, Kaposi's sarcoma, leucemia and carcinomatous infiltration transition), proliferative disease (disorder with aberrant angiogenesis, artery obstruction and pulmonary fibrosis), inflammation/immune system disease (psoriasis, nephropathy, hepatitis and pneumonitis symptom), disease by secretion fault (Sjogren syndrome) or brain association disease (brain infarction, cerebral apoplexy and brain or peripheral neuropathy).
摘要:
The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.
摘要:
A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention and/or treatment of rejection of transplantation, graft-versus-host disease, autoimmune disease, allergic disease and the like. wherein ring A is a cyclic group; ring B is a cyclic group which may have substituent(s); X is a spacer having 1 to 8 atoms in its main chain, etc.; Y is a spacer having 1 to 10 atoms in its main chain, etc.; n is 0 or 1, wherein when n is 0, m is 1 and R1 is a hydrogen atom or a substituent, and wherein when n is 1, m is 0 or an integer of 1 to 7 and R1 is a substituent, and wherein m is 2 or more, R1s are the same or different.