68 3 1 5"! Patent Request: Standard Patent/Patent of Addition

68 3 1 5"! Patent Request: Standard Patent/Patent of Addition

Λ _ ___ _ KWU/lXHJIMI AUSTRALIA Patents Act 1990 68 3 1 5"! PATENT REQUEST: STANDARD PATENT/PATENT OF ADDITION We, being the persons identified below as the Applicant, request the grant of a patent to the person identified below as the Nominated Person, for an invention described in the accompanying standard complete specification. ,· Full application details follow. [71] Applicant: ADIR ET COMPAGNIE Address: 1 RUE cXrLE HEBERT, F-92415 COURBEVOIE CEDEX, FRANCE [70] Nominated Person: ADIR ET COMPAGNIE Address: 1 RUE CARLE HEBERT, F-92415 COURBEVOIE CEDEX, FRANCE [54] Invent»·* Title: NOVEL N-PYRIDYL CARBOXAMIDES AND DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS WHICH CONTAIN THEM Name(s) of actual inventor(s): JEAN-MICHEL ROBERT, ODILE RIDEAU, SYLVIE ROBERT-PIESSARD, JACQUELINE COURANT, GUILLAUME LE BAUT, DANIEL-HENRI CAIGNARD, PIERRE RENARD and GERARD ADAM Address for service in Australia: c/o WATERMARK PATENT & TRADEMARK ATTORNEYS, of 290 Burwood Road, Hawthorn, Victoria 3122, Australia Attorney Code: WM :,.··. BASIC CONVENTION APPLICATION(S) DETAILS .... [31] Application Number [33] Country Country [32] Date of Application : Code 9406412 FRANCE FR 27 MAY 1994 Basic Applicants): ADIR ET COMPAGNIE • · · · • · · *· Di awing number recommended to accompany the abstract ............................... By our Patent Attorneys, WATERMARK PATENT & TRADEMARK ATTORNEYS ...CM&/.VV2...... ....... DATED this 25th day of May 1995,. Carolyn J, Harris Registered Patent Attorney i P/00/008b 12/11/91 Section 29 (η Regulation 3.1 (2) AUSTRALIA Patents Act 1990 NOTICE OF ENTITLEMENT We, ADIR ET COMPAGNIE of, 1 Rue Carle Hebert, F-92415 Courbevoie Cedex, France, being the applicant in respect of Application No. 20288/95 state the following:- 9 9 9 • · · The Person nominated for the grant of the patent has entitlement from the actual e * ··.· . 9» ΟΪ 9* ·ί / «9 · inventors by virtue of an assignment from the inventors. • \ «s · • .·· V ea···· · 9 *9 _ · 9 9 ··* 9 • %9 0 9 ··.;· ; The person nominated for the grant of the patent r. the applicant of the basic <99· .···.- 9 · application listed on the patent request form. ·· 9 9 0 The basic application listed on the request form is the first application made in a 9 9 0 0 9 9 Convention country in respect of the invention. 9 6 · A By our Patent Attorneys, ······ WATERMARK PATENT g. TRADEMARK A TORNEYS • · /Ο 9 • 9 9 9 9 9 • 9 ...................................................................................................................................... ..^..-..7.-.42. • · 9 i 9 9 Louis C. Gebhardt 23 July 1997 9 Registered Patent Attorney • •99 • 9 • · 9 9 9 9 9 9 e • · 9 9 9 9 9 • · 9 9 9 9 9 9 · • 9 9 9 9 9 9 9 AU9520288 (12) PATENT ABRIDGMENT (11) Document No. AU-B-20288/95 (19) AUSTRALIAN PATENT OFFICE (10) Acceptance no. 683151 (54) Title NOVEL N-PYRIDYL CARBOXAMIDES AND DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS WHICH CONTAIN THEM International Patent Classiflcation(s) (51)6 C07D40S/12 A61K 031/44 C07D 213/75 C07D 213/78 C07D 213/81 C07D 213/82 C07D 213/88 C07D 401 /12 C07D 405/12 (21) Application No. : 20288/95 (22) Application Date : 25.05.95 (30) Priority Data (31) Number (32) Date (33) Country 94 06412 27.05.94 FR FRANCE (43) Publication Date : 07.12.95 (44) Publication Date of Accepted Application : 30.10.97 (71) Applicant(s) ADIR ET COMPAGNIE (72) Inventor(s) JEAN-MICHEL ROBERT; ODILE RIDEAU; SYLVIE ROBERT-PIESSARD; JACQUELINE COURANT; GUILLAUME LE BAUT; DANIEL-HENRI CAIGNARD; PIERRE RENARD; GERARD ADAM (74). Attorney or Agent WATERMARK PATENT & TRADEMARK ATTORNEYS , Locked Bag 5, HAWTHORN VIC 3122 (57) The Applicant has now discovered that novel N-pyridyl carboxamide derivatives were non­ toxic derivatives endowed with high-level anti-inflammatory and/or diuretic properties. The anti-inflammatory activity of the derivatives of the invention has the particularly advantageous feature of manifesting itself after systemic administration, but also after topical administration, which, besides the standard indications of anti-inflammatory agents, renders the compounds of the invention particularly valuable in skin diseases such as psoriasis. In addition, the diuretic component of certain products of the invention makes them very valuable in certain renal inflammatory diseases. Claim 1. A compound of general formula (I): Het—A—C—N (I) II I X R in which m is equal to 0 or 1, the symbol (O)m .../2 (11) AU-B-20288/95 -2- (10) 683151 representing the pyridine ring when m is equal to 0 and pyridine N-oxide when m is equal to 1, the pyridine system------ N being to the group —N— which bears it either in the (O)m R 2- position or in the 3-position of pyridine; R-l and R2, which may be identical or different, are chosen, independently of each other, from hydrogen, amino, alkylamino, dialkylamino, alkyl, hydroxy, alkoxy, nitro and halogen, R3 and R4, which may be identical or different, are chosen, independently of each other, from amino, alkylamino, dialkylamino, alkyl, hydroxy, alkoxy, nitro and halogen, R represents a hydrogen atom or an alkyl group, A represents a single bond; and in this case Het represents a group chosen from pyrazine, substituted pyrazine, benzothiophene, substituted benzothiophene, 4-oxo[4H]benzopyran, substituted 4-oxo[4H]benzopyran, pyrrole, substituted pyrrole, pyrroline, substituted pyrroline, pyrrolidine, substituted pyrrolidine, piperidine, substituted piperidine, pyridine, substituted pyridine, benzopyran, benzopyran substituted with one or more alkyl groups, chromane, chromane substituted with one or more alkyl groups, 3-carboxy-5-alkylisoxazole, 3- alkoxycarbony!-5-alkylisoxazole, phthalimido and substituted phthalimido, or alternatively A represents an alkylene group which is unsubstituted or substituted with one or more alkyl groups, or an alkenylene group which is unsubstituted or substituted with one or more alkyl groups; and in this case Het represents a group chosen from thiophene, substituted thiophene, pyrazine, substituted pyrazine, benzothiophene, substituted benzothiophene, 4-oxo[4H]benzopyran, substituted 4-oxo[4H]benzopyran, pyrrole, substituted pyrrole, pyrroline, substituted pyrroline, pyrrolidine, substituted pyrrolidine, piperidine, substituted piperidine, pyridine, substituted pyridine, benzopyran, benzopyran substituted with one or more alkyl groups, chromane, chromane substituted with one or more alkyl groups, 3-carboxy-5-alkylisoxazole, 3-alkoxycarbonyl-5-alkylisoxazole, phthalimido and substituted phthalimido, X represents an oxygen atom, a sulfur atom, an imino group or an imino group substituted with a group chosen from alkyl, alkoxy, hydroxy, amino, arylalkyloxy and aryloxy, the enantiomers and diastereoisomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, .../3 (11) AU-B-20288/95 (10) 683151 it being understood that, except where otherwise mentioned: the term “substituted" relating to the thiophene, pyrazine, benzothiophene, 4-oxo- [4H]benzopyran, pyrrole, pyrroline, pyrrolidine, piperidine, pyridine and phthalimido systems means that these systems are substituted with one or more groups chosen from alkyl, alkoxy, trifluoromethyl, hydroxy, halogen, thiol and alkylthio, the terms “alkyl", "alkoxy” and "alkylene", denote linear or branched groups containing from 1 to 6 carbon atoms, the term "aryl" denotes a phenyl or naphthyl radical, the term "alkenylene" denotes a linear or branched unsaturated chain containing from 2 to 6 carbon atoms. 12. A method of treating inflammatory disorders, including administering to a patient requiring such treatment an effective amount of at least one compound as claimed in any one of claims 1 to 9 or a composition as claimed in claim 11. 17. A process for preparing a pharmaceutical composition as claimed in claim 11, including admixing, in a pharmaceutically acceptable ratio, a compound as claimed in any one of claims 1 to 9 with a pharmaceutically acceptable excipient or vehicle. s Η/υυ/υη 2e/srtt Regulation 32(2) AUSTRALIA Patents Act 1990 ORIGINAL COMPLETE SPECIFICATION STANDARD PATENT Application Number: Lodged: Invention Title: NOVEL N-PYRIDYL CARBOXAMIDES AND DERIVATIVES, PROCESSES • · · β · · FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS WHICH CONTAIN THEM • » V « t · «c, < e * · · « »■ · The following statement is a full description of this invention, including the best method of performing it known to us :- The present invention relates to novel N-pyridyl carboxamides and derivatives, to processes for their preparation and to the pharmaceutical compositions which contain them. N-Pyridyl carboxamide structures are already described. Thus, patent application WO 9304580 describes N-(4-pyridyl)arylacetamides as pesticides. s · · The Applicant has now discovered that novel N-pyridyl carboxamide derivatives were non­ » • · ·· · • · · toxic derivatives endowed with high-level anti-inflammatory and/or diuretic properties. The • • · · · · • · · anti-inflammatory activity of the derivatives of the invention has the particularly advantageous • · · • ·· • · · · feature of manifesting itself after systemic administration, but also after topical administration, • · • · 9 · • · · • · · which, besides the standard indications of anti-inflammatory agents, renders the compounds • · · 10 of the invention particularly valuable in skin diseases such as psoriasis. In addition, the • · · β · β diuretic component of certain products of the invention makes them very valuable in certain ···

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