Claims for Patent: 5,795,891

Summary for Patent: 5,795,891

Title:	Acylphenylglycine derivative and preventive and remedy for diseases caused by increased collagenase activity containing said compound as active ingredient
Abstract:	An acylphenylglycine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, and a preventive and remedy for diseases caused by an increased collagenase activity containing the same as the active ingredient, wherein R.sup.1 represents hydrogen atom, methyl, methylaminomethyl or morpholinomethyl; R.sup.2 represents hydrogen atom, hydroxy, fluorine atom, or C.sub.1 -C.sub.4 linear or branched alkyl; and R.sup.3 represents C.sub.1 -C.sub.4 linear or branched alkyl. The compound (I) and the salt maintains a potent collagenase inhibitor activity in the blood for long after being administered, and are useful as a remedy for various diseases believed to be caused by an increased collagenase activity. ##STR1##
Inventor(s):	Hirayama; Ryoichi (Akashi, JP), Tsukida; Takahiro (Osaka, JP), Yamamoto; Minoru (Osaka, JP), Ikeda; Shoji (Kobe, JP), Sakamoto; Fumio (Daito, JP), Obata; Yuji (Osaka, JP), Matsuo; Konomi (Osaka, JP)
Assignee:	Kanebo Ltd. (Tokyo, JP)
Application Number:	08/596,278
Patent Claims:	1. An acylphenylglycine compound of formula (I), ##STR10## wherein R.sup.1 is hydrogen, methyl, methylaminomethyl or morpholinomethyl; R.sup.2 is hydrogen, hydroxy, fluorine, or C.sub.1 -C.sub.4 linear or branched chain alkyl; and R.sup.3 is C.sub.1 -C.sub.4 linear or branched chain alkyl, or a pharmaceutically acceptable salt thereof. 2. The acylphenylglycine compound or the pharmaceutically acceptable salt thereof according to claim 1 wherein R.sup.1 and R.sup.3 are both methyl and R.sup.2 is hydrogen. 3. A method for the treatment of diseases caused by increased collagenase activity, comprising administering an agent which comprises as an active principle the acylphenylglycine derivative or the pharmaceutically acceptable salt thereof according to claim 1. 4. The method according to claim 3 wherein the diseases caused by increased collagenase activity are joint diseases or diseases due to bone resorption. 5. A method for the treatment of diseases caused by increased collagenase activity, comprising administering an agent which comprises as an active principle the acylphenylglycine derivative or the pharmaceutically acceptable salt thereof according to claim 2. 6. The acylphenylglycine compound or salt of claim 1, wherein R.sup.1 and R.sup.2 are hydrogen and R.sup.3 is methyl. 7. A compound according to claim 1 which is [4-(N-hydroxyamino)-2(R)-isobutylsuccinyl]-L-phenylglycine-N-methylamide. 8. A compound according to claim 1 which is [4-(N-hydroxyamino)-2(R)-isobutyl-3-methylsuccinyl]-L-phenylglycine-N-meth ylamide. 9. A compound according to claim 1 which is: [4-(N-hydroxyamino)-2(R)-isobutylsuccinyl]-L-(p-hydroxyphenyl)glycine-N-met hylamide, [4-(N-hydroxyamino)-2(R)-isobutyl-3-(morpholinomethyl)succinyl]-L-phenylgly cine-N-methylamide hydrochloride, [4-(N-hydroxyamino)-2(R)-isobutyl-3-(methylaminomethyl)succinyl]-L-phenylgl ycine-N-methylamide, [4-(N-hydroxyamino)-2(R)-isobutylsuccinyl]-L-phenylglycine-N-ethylamide, [4-(N-hydroxyamino)-2(R)-isobutylsuccinyl]-L-(p-fluorophenyl)glycine-N-meth ylamide, or [4-(N-hydroxyamino)-2(R)-isobutylsuccinyl]-L-(p-isopropylphenyl)glycine-N-m ethylamide. 10. An agent for treatment of diseases caused by increased collagenase activity which agent comprises as an active principle the acylphenylglycine derivative or the pharmaceutically acceptable salt thereof according to claim 1. 11. A method according to claim 4, wherein the diseases are rheumatoid arthritis, osteoarthritis, hypercalcemia or osteoporosis. 12. An acylphenylglycine compound of formula (I), ##STR11## wherein R.sup.1 is hydrogen, methyl, methylaminomethyl or morpholinomethyl; R.sup.2 is hydrogen or hydroxy; and R.sup.3 is C.sub.1 -C.sub.4 linear or branched chain alkyl, or a pharmaceutically acceptable salt thereof.

Details for Patent 5,795,891

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Smith & Nephew, Inc.	SANTYL	collagenase	Ointment	101995	06/04/1965		2013-08-09