Hoechst Japan Limited

Koichi Shudo

Hoechst Aktiengesellschaft

Hoechst Marion Roussel

Aventis Pharma S.a.

Kazuyuki Kitamura

Mizuho Inazu

Tsutomu Inoue

Tatsuo Sugioka

Hideyuki Tanaka

Osamu Komiyama

Robert S McDowell

Volkmar Wehner

Thomas Gadek

Jochen Knolle

Christoph Naumann

Hans-Ulrich Stilz

Katsuhiro Yoshikawa

Roland Baron

Hiroyasu Tobe

Hiroshi Watanabe

Masakazu Katoh

Mikio Akita

Kohsei Gotoh

Kazuyuki Doi

Yusuke Satoh

Kunikazu Sakai

Agents for promoting bone formation

Compounds useful as preventive and therapeutic agents for bone and cartilage diseases; and drug compositions containing the same. The compounds are polyhydroxyphenol derivatives of general formula (I)

Polyhydroxyphenol derivatives and preventive and therapeutic agents for bone and cartilage diseases containing the same

There are described compounds of the formula I ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.10)-alkyl, (C.sub.1 -C.sub.8)-alkanoyl, (C.sub.6 -C.sub.10)-aryl or Het, each of which can be substituted by halogen, --OH, --NH.sub.2, --NH--CO--R.sup.7, --O--CO--R.sup.7 and --N--(R.sup.8).sub.2 where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl and R.sup.8, independently of one another, is hydrogen or (C.sub.1 -C.sub.2)-alkyl or in which R.sup.1 is the radical of the formula II ##STR2## in which n is an integer from 3 to 10, m is zero to 3, R.sup.6, independently of one another, is (C.sub.1 -C.sub.6)-alkyl which is optionally substituted by halogen or --NH--CO--R.sup.7, where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl, and X is absent or is (C.sub.1 -C.sub.10)-alkyl, and R.sup.2, R.sup.3, R.sup.4 or R.sup.5, independently of one another, are hydrogen, (C.sub.1 -C.sub.5) -alkyl, lithium, sodium, potassium or Si(R), where R=(C.sub.1 -C.sub.5)-alkyl, and their physiologically tolerable salts, a process for preparation of these compounds of the formula I and their use as pharmaceuticals in the prophylaxis and treatment of osteoporosis and hypercalcemia.

Imidobisphosphoric acids, and use thereof

An anti-osteopathic composition comprising as an active ingredient a compound represented by the following formula (I), (II) or (Ill): ##STR1## which is useful for therapeutic and prophylactic treatment of osteopathia such as osteoporosis and bone fracture.

Anti-osteopathic composition

Imidobisphosphoric acids, process for their preparation, and use thereof. There are described compounds of the formula I ##STR1## in which R.sup.1 is (C.sub.1 -C.sub.10)-alkyl, (C.sub.1 -C.sub.8)-alkanoyl, (C.sub.6 -C.sub.10)-aryl or Het, each of which can be substituted by halogen, --OH, --NH.sub.2, --NH--CO--R.sup.7, --O--CO--R.sup.7 and --N--(R.sup.8).sub.2 where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl and R.sup.8, independently of one another, is hydrogen or (C.sub.1 -C.sub.4)-alkyl or in which R.sup.1 is the radical of the formula II ##STR2## in which n is an integer from 3 to 10, m is zero to 3, R.sup.6, independently of one another, is (C.sub.1 -C.sub.6)-alkyl which is optionally substituted by halogen or --NH--CO--R.sup.7, where R.sup.7 =(C.sub.1 -C.sub.6)-alkyl, and X is absent or is (C.sub.1 -C.sub.10)-alkyl, and R.sup.2, R.sup.3, R.sup.4 or R.sup.5, independently of one another, are hydrogen, (C.sub.1 -C.sub.5)-alkyl, lithium, sodium, potassium or Si(R), where R=(C.sub.1 -C.sub.5) -alkyl, and their physiologically tolerable salts, a process for preparation of these compounds of the formula I and their use as pharmaceuticals in the prophylaxis and treatment of osteoporosis and hypercalcemia.

Imidobisphosphoric acids, and use therefor

A method of treating metabolic bone diseases comprising using a pharmaceutical composition which comprises as an active ingredient IL-1 receptor, a soluble fragment consisting of an extracellular domain of IL-1R or a fragment thereof derived from mammals. The composition has a bone resorption inhibiting activity and is useful for the therapy and prophylaxis of metabolic bone diseases.

Method of treating metabolic bone diseases with an IL-1 receptor

An anti-osteopathic composition comprising as an active ingredient a compound represented by the following formula (I), (II) or (III): ##STR1## which is useful for therapeutic and prophylactic treatment of osteopathia such as osteoporosis and bone fracture.

A therapeutic agent for osteoporosis comprising as an active ingredient xanthohumol. Xanthohumol obtained from hop extracts has a bone resorption inhibiting activity and is useful as a therapeutic agent for osteoporosis.

Pharmaceutical composition for treating osteoporosis

A pharmaceutical composition for treating osteoporosis which comprises as an active ingredient an effective amount of one or more compounds selected from the-group comprising humulone, cohumulone, adhumulone, isohumulone, isocohumulone and isoadhumulone in combination with a pharmaceutically acceptable carrier or excipient. Humulone, cohumulone, adhumulone are the compounds belonging to .alpha. acids which are an ingredient extracted from hops, whilst isohumulone, isocohumulone and isoadhumulone are the compounds belonging to iso .alpha. acid derivatives which are isomers of .alpha. acids. The above described compounds have a bone resorption inhibiting activity and are useful for treating osteoporosis.

Treating osteoporosis with humulones

Treatment of osteopathic comprising administering as an active ingredient a compound represented by the following formula (I), (II) or (III): ##STR1##

Method of treating bone disease with pyridine, carboxamide and

An animal tissue antigen for osteoporotic patients that reacts with antibody in a serum of human osteoporotic patients, but does not react with that in normal human serum. Preferably, a specific antigen for osteoporotic patients in rat or mouse epithelium of tongue mucous membrane, epithelium of tracheal mucous membrane, upper lip epidermis or follicular epithelium containing upper lip hair shafts, or a specific antigen for osteoporotic patients contained in cultured cells of a human squamous cell tongue carcinoma cell lines such as SCC-9 and fibroblast cell lines such as MRC-5. Osteoporosis can be both specifically and easily diagnosed by bringing the above-mentioned antigen in contact with a serum of a subject and then testing for the presence of an antigen-antibody reaction.

Growing community of inventors

Sakado, Japan

Kazuyuki Kitamura