Leo Pharmaceutical Products Ltd. A/s

Leo-pharma A/s

Other

Leo Pharmaceutical Products Ltd. A/s (lovens Kemiske Fabrik Produktionsaktieselskab)

Leo Pharmaceutical Products, Ltd.

Leo Pharmaceuticals Products Ltd.

Leo Pharmaceuticals Products Ltd. A/s

Erik Rytter Ottosen

Xifu Liang

Anne Marie Horneman

Søren Christian Schou

Charlotte Schou Hunneche

Anthony Murray

Daniel Rodriguez Greve

Simon Feldbæk Nielsen

Gunnar Grue-Sørensen

Carsten Ryttersgaard

Thomas Peter Sabroe

Sophie Elisabeth Havez

Tina Dahlerup Poulsen

Heinz Wilhelm Dannacher

Fredrik Bj&ouml;rkling

Schneur Rachlin

Charlotte Schou

Soren Christian Schou

The invention relates to compounds of general formula (I) wherein A, R, R, R, R, R, R, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use&#x2014;alone or in combination with one or more other pharmaceutically active compounds&#x2014;in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation. 

Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors

The invention relates to novel compounds according to formula Ia and Ib, said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases, or cancer.

Triazole substituted aminobenzophenone compounds

The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer. 

Aminobenzophenone compounds

The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Aminobenzoephenones

The present invention relates to compounds of formula (I) wherein R, Rand Rindependently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C-C)alkyl, (C-C)olefinic group, (C-C)alkoxy, (C-C)alkylthio, (C-C)alkylamino, (C-C)alkoxycarbonyl, cyano, carbamoyl, or phenyl; Rand Rfurther represented by nitro and Rby carboxy; Rrepresents hydrogen, (C-C)alkyl, or allyl; Q represents a bond, or &#x2014;C(R)(R)(&#x2014;O&#x2014;C&#x2550;O)&#x2014;, in which formula Rand Rindependently represent hydrogen, trifluoromethyl, or (C-C)alkyl; Y represents either (C-C)alkyl, (C-C)olefinic group, (C-C)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R; or (C-C)alkyl substituted with at least one or more substituents with the formula R; or Y represents a group of formula &#x2014;CH&#x2014;(Z&#x2014;O)&#x2014;Z where Z is a (C-C)alkyl, where n is a integer&#x3e;1 and no continuous linear sequence of atoms in the group Y&#x3e;15; Rrepresents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C-C)alkoxy, (C-C)alkylthio, (C-C)alkylamino, (C-C)alkoxycarbonyl, cyano, azido, nitro, &#x2014;COOH, &#x2014;CONH, &#x2014;CONHR', or &#x2014;COONR&#x2032;R&#x2032; wherein R&#x2032; stands for (C-C)alkyl; X represents oxygen or sulphur, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.

Aminobenzophenones as inhibitors of IL-1&#x3b2; and TNF-&#x3b1;

Aminobenzophenones as inhibitors of il-1&bgr; and tnf-&agr;

Cyanoguanidines as cell proliferation inhibitors

Aminobenzophenones

The present invention relates to a compound of general formula (I) wherein R , R , and R represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C -C )alkyl, (C -C )olefinic group, (C -C )alkoxy, (C -C )akylthio, (C -C )alkylamino, (C -C )alkoxycarbonyl, cyano, &mdash;CONH , phenyl, or nitro; further R can be hydrogen, and R can be carboxy and carbamoyl; R represents hydrogen, (C -C )alkyl, or allyl; X represents oxygen or sulphur; Q represents &mdash;(CO)&mdash;, &mdash;(CS)&mdash;, or a bond; Y represents (C -C )alkyl; (C -C )olefinic group; (C -C )monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R defined below; (C -C )alkyl substituted by one or more substituents selected for the group R ; or a group of the formula &mdash;(Z&mdash;O) &mdash;Z, wherein Z is a (C -C )alkyl, n is an integer >1; and no continuous linear sequence of atoms in the group Y exceeds 15; R represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C -C )alkoxy, (C -C )alkylthio, (C -C )alkylamino, (C -C )alkoxycarbonyl, cyano, azido, nitro, &mdash;COOH, &mdash;CONH , &mdash;CONHR&prime;, or COONR&prime;R&prime; wherein R&prime; represents (C -C )alkyl; or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.

Aminobenzophenones as inhibitors of IL-1&bgr; and TNF-&agr;

The present invention relates to compounds of formula (I) wherein R and R independently represent one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino (C -C )alkyl, (C -C )olefinic group, (C -C )alkoxy, (C -C )alkylthio, (C -C )alkylamino, (C -C )alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro; R further being represented by hydrogen; R represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C -C )alkyl, (C -C )olefinic group, (C -C )alkoxy, (C -C )alkylthio, (C -C )alkylamino, (C -C )alkoxycarbonyl, phenyl, cyano, carboxy or carbomoyl; R represents hydrogen, (C -C )alkyl, or allyl; X represents oxygen or sulpher; with the proviso that formula (I) does not comprise the compound 2,2,2-trifluoro-N-&lsqb;2-&lsqb;3-chloro-4-(2-methylbenzoyl)-phenylamino&rsqb;-phenyl&rsqb;acetamide wherein R is a 2-methyl, R is 2-chloro, R and R is hydrogen, and X is oxygen; and a salt thereof with a pharmaceutically acceptable acid, a hydrate or a solvate thereof. The compounds are valuable in the human and veterinary therapy.

Aminobenzophenones as inhibitors of IL-1 &bgr; and TNF-&agr;

Aminobenzophenones as inhibitors of IL 1&bgr; and TNF-&agr;

The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C -C alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C -C divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carboxy, C -C alkoxycarbonyl, di(C -C alkoxy)phosphinoyloxy, amino, C -C alkoxycarbonylamino or tetrahydropyranyloxy; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

The compounds of the present invention are represented by general formula (I) in which formula R,and R,stand independently for one or more, similar or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, cyano, carboxy, carbamoyl, phenyl, or nitro; R,stands for hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, phenyl, cyano, carboxy, or carbamoyl; R,, R,and R,stand independently for hydrogen, trifluoromethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkyloxo, the C-content of which can be from 1 to 5; X stands for oxygen, N&mdash;OH, N&mdash;O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, the C-content of which can be from 1 to 5. The present compounds are of value in the human and veterinary practice as systemic and topical therapeutic agents for the treatment and prophylaxis of asthma, allergy, rheumatoid arthritis, spondyloarthritis, gout, atherosclerosis, chronic inflammatory bowel disease, proliferative and inflammatory skin disorders, such as psoriasis, and atopic dermatitis.

Aminobenzophenones as inhibitors of interleukin and TNF

Compounds of the following formula are used for inhibiting cell proliferation:

Cyanoamidines as cell proliferation inhibitors

The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine being in the 3- or 4-position, in which formula R,stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl nitro, amino, cyano, carboxy, or alkyl, alkoxy, or alkoxycarbonyl, the C-content of which can be from 1 to 4; X stands for a straight or branched C,-C,carbon chain, saturated or unsaturated or Q&mdash;Ar&mdash;R; in which formula Ar stands for phenyl, Q stands for a C,-C,divalent hydrocarbon radical which can be straight, branched, saturated or unsaturated and R stands for hydrogen or for one or more substituents which can be the same or different and are selected from the group consisting of: hydroxy, amino, halogen, trifluoromethyl, cyano, nitro, carboxy, carbamoyl, or alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 4; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

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Ølstykke, Denmark

Erik Rytter Ottosen