- PYRIDINONE DICARBOXAMIDE FOR USE AS BROMODOMAIN INHIBITORS
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The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
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Page/Page column 139
(2017/03/21)
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- AMINOACYLINDAZOLE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES
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2-Acylindazole compounds of formula I or formula II are disclosed. These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.
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Paragraph 87
(2017/12/29)
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- FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX
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Fused pyrimidine compounds having a saturated, unsaturated or aromatic A ring fused to a pyrimidine ring and having a complex substituents at the 2 position and a substituted amine at the 4 position of the pyrimidine ring as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine ring and A ring are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity such as cancer.
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- Development of a prostaglandin D2 receptor antagonist: Discovery of a new chemical lead
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A series of N-(p-alkoxy)benzoyl-5-methoxy-2-methylindole-3-acetic acids and N-(p-butoxy)benzoyl-2-methylindole-4-acetic acid were discovered as new chemical leads for a prostaglandin D2 (PGD2) receptor antagonist. Most of them exhibi
- Torisu, Kazuhiko,Kobayashi, Kaoru,Iwahashi, Maki,Egashira, Hiromu,Nakai, Yoshihiko,Okada, Yutaka,Nanbu, Fumio,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
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p. 505 - 519
(2007/10/03)
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- Development of prostaglandin D2 receptor antagonist: discovery of highly potent antagonists.
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The process of discovery for highly potent prostaglandin D(2) (PGD(2)) receptor antagonists is reported. A series of N-(p-alkoxy)benzoyl-2-methylindole-4-acetic acids were synthesized and identified as a new class of selective PGD(2) receptor antagonists.
- Torisu, Kazuhiko,Kobayashi, Kaoru,Iwahashi, Maki,Nakai, Yoshihiko,Onoda, Takahiro,Nagase, Toshihiko,Sugimoto, Isamu,Okada, Yutaka,Matsumoto, Ryoji,Nanbu, Fumio,Ohuchida, Shuichi,Nakai, Hisao,Masaaki Toda
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p. 4685 - 4700
(2007/10/03)
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- Discovery of new chemical leads for prostaglandin D2 receptor antagonists
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A series of Indomethacin analogs were synthesized and biologically evaluated. Among the compounds tested, N-(p-butoxy)benzoyl-2-methylindole-4- acetic acid 2 was discovered as a new chemical lead for a prostaglandin D 2 (PGD2) recept
- Torisu, Kazuhiko,Kobayashi, Kaoru,Iwahashi, Maki,Egashira, Hiromu,Nakai, Yoshihiko,Okada, Yutaka,Nanbu, Fumio,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
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p. 4557 - 4562
(2007/10/03)
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- INDOLE DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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Indole derivatives represented by formula (I) ???wherein all symbols represent the same as that in specification), production methods thereof, and DP receptor antagonist comprising them as active ingredients. Since the compounds of formula (I) binds and antagonizes to DP receptor, they are useful for the prevention and/or treatment against allergic diseases, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, cerebrovascular disorder, pleuritis complicated by rheumatoid arthritis, ulcerative colitis.
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Page 130-131
(2008/06/13)
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- Indole derivatives, process for preparation of the same and use thereof
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Indole derivatives represented by formula (I): (wherein all symbols are described in the description), a process for the preparation of the same and a DP receptor antagonist comprising it as an active ingredient. Since the compounds of formula (I) binds to and are antagonistic to a DP receptor, they are useful in for the prevention and/or treatment of diseases, for example, allergic diseases (allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma, food allergy, etc., systemic mastocytosis; disorders due to systemic mastocyte activation, anaphylactic shock, bronchoconstriction, urticaria, eczema, etc.), diseases accompanied with itching (atopic dermatitis, urticaria, etc.), secondary diseases caused by behaviors (scratching behaviors, beating, etc.) (cataract, retinal detachment, inflammation, infection, sleep disorder, etc.), inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, cerebrovascular disorder, pleuritis complicated by rheumatoid arthritis, ulcerative colitis, and the like.
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- Intramolecular cyclization reactions of unsaturated amino Fischer chromium carbenes forming indoles and quinolines
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A thermally induced intramolecular annulation reaction of N-(2-alkenylphenyl)amino substituted Fischer chromium carbenes has been extensively examined. The carbene complexes were prepared in moderate to good yields by reaction of 2-aminostyrenes with intermediately formed acyloxy substituted carbenes. Upon heating, the thermally labile carbenes decomposed producing indoles and quinolines as the major products. The product distribution was found to be highly dependent on the substitution pattern and electronic properties of the starting material, and on the solvent used.
- S?derberg, Bj?rn C. G.,Shriver, James A.,Cooper, Seth H.,Shrout, Timothy L.,Helton, E. Scott,Austin, Lucinda R.,Odens, Herman H.,Hearn, Brian R.,Jones, Paula C.,Kouadio, Tiara N.,Ngi, Tan H.,Baswell, Rachel,Caprara, H. John,Meritt, Mark D.,Mai, Than T.
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p. 8775 - 8791
(2007/10/03)
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- Synthesis of 2,4-disubstituted indoles via thermal cyclization of N-trifluoroacetyl enehydrazines
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Synthesis of naturally occurring indoles, 2,4-dimethylindole and 4-hydroxymethyl-2-methylindole by applying thermal cyclization of N-trifluoroacetyl enehydrazines is described.
- Miyata, Okiko,Takeda, Norihiko,Naito, Takeaki
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p. 1101 - 1107
(2007/10/03)
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- Novel Intramolecular Cycloaddition Reactions of Arylamino-Substituted Fischer Chromium Carbenes
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Thermal reaction of N-arylamino-substituted Fischer chromium carbenes having a pendant 2-(1-alkenyl)substituent on the benzene ring affords either substituted indoles or quinolines, depending on starting material, via an intramolecular cycloaddition forming a metallacyclobutane followed by metathesis to give indoles or β-elimination to give quinolines.
- Soederberg, Bjoern C.,Helton, E. Scott,Austin, Lucinda R.,Odens, Herman H.
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p. 5589 - 5591
(2007/10/02)
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