Ono Pharmaceutical Co., Ltd.

The Green Cross Corporation

University of Pennsylvania

Yoshitomi Pharmaceutical Industries, Ltd.

Ono Pharmaceuticals Co., Ltd.

Kaoru Kobayashi

Kousuke Tani

Fumio Nambu

Shinobu Kuwae

Takayuki Maruyama

Tomoshi Ohya

Toru Maruyama

Mikio Ogawa

Toyoo Ohda

Takao Ohmura

Tohru Kambe

Atsushi Naganawa

Kazuhiko Torisu

Maki Iwahashi

Kenji Tomomitsu

Michael D Kaufman

Amos B Smith, Iii

David R Jones

Yuping Qiu

Masaki Asada

Masami Narita

Yoshihiko Nakai

Tetsuji Saito

Wataru Ohtani

Shinsuke Hashimoto

Tsutomu Shiroya

Atsushi Kinoshita

Hideyuki Yoshida

Akinori Sumi

Akio Nishiura

Thomas James Beauchamp

Haruhide Kawabe

Toshihiko Nagase

Koji Yano

Masao Naka

Seiji Ogawa

Naoyuki Taniguchi

Hirokazu Arimoto

Atsushi Shimabukuro

Nobutaka Abe

Yutaka Okada

Hirokaza Arimoto

Yoko Kishida

Shouji Kawauchi

Kohki Tsukamoto

Yoko Matsunaga

Hirotoshi Fukutsuka

Kazumasa Yokoyama

Tadakazu Suyama

Hiroyuki Ohno

Matthew J LaMarche

Yahiro Uemura

Hirofumi Arimura

Masayuki Nishida

Tomoyuki Hasegawa

Kiyoshi Tsutsui

Hiroshi Morise

Ken Okabayashi

Tadashi Tatsumi

Hiromichi Mukai

Yutaka Ishida

Kazuo Ikegaya

Hajime Horii

Yukimitsu Nakagawa

Naoto Fuluhata

Naofumi Hayasuke

Kohji Murakami

Hitoshi Minamino

Sadao Ueda

Muneo Tsujikawa

Shinsei Fujimura

Atsushi Masaki

Kazutoyo Sato

Ken Yoshikawa

Kiyoto Sakata

Kiyoyuki Sato

Masao Ohyama

Tomoshi Ooya

Atsushi c/o Ono Pharmaceutical Co Ltd Naganawa

Kohki c/o Ono Pharmaceutical Co Ltd Tsukamoto

Atsushi c/o Ono Pharmaceutical Co Ltd Shimabukuro

Yutaka c/o Ono Pharmaceutical Co Ltd Okada

Seiji c/o Ono Pharmaceutical Co Ltd Ogawa

Atsushi c/o Ono Pharmaceutical Co Ltd Kinoshita

Yoko c/o Ono Pharmaceutical Co Ltd Matsunaga

Koji c/o Ono Pharmaceutical Co Ltd Yano

Maki c/o Ono Pharmaceutical Co Ltd Iwahashi

Fumio c/o Ono Pharmaceutical Co Ltd Nambu

Tetsuji Saitoh

A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EPagonist as an active ingredient. An EPagonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).

Pharmaceutical composition for treatment of diseases associated with decrease in bone mass comprising EP4 agonist as active ingredient

Carboxylic acid compounds and medicinal compositions containing the same as the active ingredient

An N-phenylarylsulfonylamide compound of formula (I) (Ris COOH etc.; Ris hydrogen, methyl, etc.; Rand Rare a combination of methyl and methyl, etc.; Ris isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin Ereceptor, especially an EPsubtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

N-phenylarylsulfonamide compound, pharmaceutical composition comprising the compound as active ingredient, synthetic intermediate for the compound and process for its preparation

An 8-azaprostaglandin represented by formula (I) (wherein all symbols have the same meanings as described in the specification), a pharmaceutically acceptable salt thereof or a cyclodextrin clathrate thereof. Since the compound represented by formula (I) binds to EP2 subtype among PGE receptor strongly, it is useful for preventive and/or treatment for immune diseases, allergic diseases, neuronal cell death, dysmenorrhea, premature birth, abortion, baldness, retinal neuropathy such as glaucoma, erectile dysfunction, arthritis, pulmonary injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, hepatic injury, acute hepatitis, liver cirrhosis, shock, nephritis, renal failure, circulatory diseases, systemic inflammatory response syndrome, sepsis, hemophagocytosis syndrome, macrophage activation syndrome, still disease, Kawasaki Disease, burn, systemic granuloma, ulcerative colitis, Crohn disease, hypercytokinemia at dialysis, multiple organ failure, or bone diseases etc.

8-azaprostaglandin derivative compound and agent comprising the compound as active ingredient

A carboxylic acid derivative of formula (I): wherein Ris &#x2014;COOH, &#x2014;COOR, etc.; A is a single bond, alkylene, etc.; Ris alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and Ris alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGEreceptor, especially subtypes EPand/or EPand show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.

Carboxylic acid derivatives and pharmaceutical agent comprising the same as active ingredient

Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.

Synthetic techniques and intermediates for polyhydroxy dienyl lactones and mimics thereof

The present invention relates to a carboxylic acid compound of formula (I): wherein Ris H, alkyl; m is 2, 3; n is 0-2; Ris phenyl, naphthyl, benzofuran, benzothiophene; Q is &#x2014;CH&#x2014;O-Cyc1, &#x2014;CH-Cyc2, -L-Cyc3; Rand Reach independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGEreceptor, specifically EPreceptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

Carboxylic acid compounds

Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient

8-azaprostaglandin derivative compounds and drugs containing the compounds as the active ingredient

A carboxylic acid compound represented by formula (I): (meanings of the symbols in the formula are as mentioned in the specification) and a pharmaceutical agent comprising the compound. Since the compound represented by formula (I) binds to a DP receptor and shows antagonistic activity for the DP receptor, it is useful for prevention and/or treatment of diseases such as allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

Carboxylic acid compounds and a pharmaceutical agent comprising the compound as the active ingredient

Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.

Indole derivatives

The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EPagonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc. Furthermore, the compounds also have an action of accelerating bone formation, so it is expected to be useful for the prevention and/or treatment of diseases associated with loss in bone mass, for example, primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss, osteonecrosis, bone formation after bone operation, alternative treatment for bone grafting.

8-azaprostaglandin derivatives and medical use thereof

Growing community of inventors

Mishima-gun, Japan

Kaoru Kobayashi