1145-59-1Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS FOR TREATING HELMINTH INFECTIONS
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Page/Page column 39, (2013/02/28)
Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein L is (CR13aR13b)t,, CR14=CR14, C≡C, CR15aR15bX, XCR15aR15b, CO, O, S(O)p, NR
Synthesis and biological activity of various derivatives of a novel class of potent, selective, and orally active prostaglandin D2 receptor antagonists. 1. Bicyclo[2.2.1]heptane derivatives
Mitsumori, Susumu,Honma, Tsunetoshi,Tsuri, Tatsuo,Hiramatsu, Yoshiharu,Okada, Toshihiko,Hashizume, Hiroshi,Inagaki, Masanao,Arimura, Akinori,Yasui, Kiyoshi,Asanuma, Fujio,Kishino, Junji,Ohtani, Mitsuaki
, p. 2436 - 2445 (2007/10/03)
Novel prostaglandin D2 (PGD2) receptor antagonists were synthesized as a potential new class of antiallergic agents having a bicyclo[2.2.1] heptane ring system with sulfonamide groups. Some of them exhibit extremely potent antagonism of the PGD2 receptor in radioligand binding and cAMP formation assays with IC50 values below 50 nM and much less antagonism of TXA2 and PGI2 receptors. These potent PGD2 receptor antagonists, when given orally, dramatically suppress various allergic inflammatory responses such as increased vascular permeability in allergic rhinitis, conjunctivitis, and asthma models. The excellent pharmacological profiles of PGD2 receptor antagonists, originally synthesized in our laboratories, are of potentially great clinical significance. This study also provides experimental evidence suggesting that PGD2 plays an important role in the pathogenesis of allergic diseases.
Keratinocyte growth inhibitors and hydroxamic acid derivatives
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Page 25; 26, (2010/02/06)
This invention relates to a keratinocyte-proliferation inhibitor comprising as active ingredient a compound having an activity of inhibiting the solubilization of heparin-binding EGF-like growth factor bound to cell membranes and a compound of the formula (I); or pharmaceutically acceptable salt thereof, wherein R1, R2, R3 are hydrogen atom or alkyl and X is substituted benzene or the like.
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives
Tamura, Yoshinori,Watanabe, Fumihiko,Nakatani, Takuji,Yasui, Ken,Fuji, Masahiro,Komurasaki, Tadafumi,Tsuzuki, Hiroshige,Maekawa, Ryuji,Yoshioka, Takayuki,Kawada, Kenji,Sugita, Kenji,Ohtani, Mitsuaki
, p. 640 - 649 (2007/10/03)
Various N-sulfonylamino acid derivatives were synthesized and evaluated for their in vitro and in vivo activities to inhibit type IV collagenase (MMP-9 and MMP-2). When the amino acid residue and the sulfonamide moiety were modified, their inhibitory activities were greatly affected by the structure of the sulfonamide moiety. A series of aryl sulfonamide derivatives containing biaryl, tetrazole, amide, and triple bond were found to be potent and highly selective inhibitors of MMP-9 and MMP-2. In addition, these compounds were orally active in animal models of tumor growth and metastasis. These results revealed the potential of the N-sulfonylamino acid derivatives as a new type of candidate drug for the treatment of cancer.
