Leo-pharma A/s

Topotarget A/s

Novo Nordisk A/s

Novo Industri A/s

Leo Pharmaceuticals Products Ltd. A/s (l.o Slashed.vens Kemiske Fabrik

Fredrik Bjorkling

Sven Erik Godtfredsen

Mette Knak Christensen

Ole Kirk

Heinz Wilhelm Dannacher

Willy Jean Malaisse

The present application discloses novel squaric acid derivatives of the formula A: from &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;C(&#x2550;S)&#x2014; and &#x2014;P(&#x2550;O)(R)&#x2014;; B: -, &#x2014;O&#x2014;, &#x2014;NR&#x2014; and &#x2014;C(&#x2550;O)&#x2014;NR&#x2014;; D: -, &#x2014;O&#x2014;, &#x2014;CRR&#x2014; and &#x2014;NR; m=0-12; n=0-12; m+n=1-20; p=0-2; R: heteroaryl, aryl; R: H, C-alkyl, C-cycloalkyl, &#x2014;[CHCHO]&#x2014;(C-alkyl), C-alkenyl, aryl, heterocyclyl, heteroaryl; R: C-alkyl, C-cycloalkyl, &#x2014;[CHCHO]&#x2014;(C-alkyl), C-alkenyl, aryl, heterocyclyl, heteroaryl; or Rand R: N-containing heterocyclic/heteroaromatic ring; Rand R*: H, C-alkyl, C-alkenyl; and pharmaceutically acceptable salts and prodrugs thereof, and their use in the treatment of diseases/conditions caused by an elevated level of NAMPRT (inflammatory and tissue repair disorders, particularly rheumatoid arthritis, inflammatory bowel disease, asthma and CPOD, osteoarthritis, osteoporosis and fibrotic diseases; dermatosis; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, atherosclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and viral infections, adult respiratory distress syndrome, ataxia telengiectasia).

Squaric acid derivatives as inhibitors of the nicotinamide

The present application discloses compounds of formula (I) wherein X is &#x2550;O, &#x2550;S, &#x2550;NH, &#x2550;NOH and &#x2550;NO-Me; A is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;C(&#x2550;S)&#x2014; and P(&#x2550;O)(R)&#x2014;; B is, &#x2014;O&#x2014;, &#x2014;(CH)&#x2014;, and O&#x2014;(CH)&#x2014;; D is, &#x2014;O&#x2014;, &#x2014;CRR&#x2014; and &#x2014;NR; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; Ris opt. sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia. 

Urea and thiourea derivatives

Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R, X, Rand Rare as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases. 

Cyanoguanidine compounds

Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated Chydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated Chydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0), C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated Chydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring; and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.

Pyridyl cyanoguanidine compounds

Polyol succinates and their pharmaceutical formulation

Fatty acid esters of methyl glycosides are prepared by reacting a fatty acid or ester with a methyl glycoside in the presence of an enzyme catalyst, in particular a lipase. The resulting fatty acid esters are preferably monoesters. The methyl glycoside fatty acid esters may be used as surface-active agents in cleaning compositions or personal care products.

Process for producing methyl glycoside esters

An epoxy group in a molecule can enzymatically be transferred to another molecule, thereby synthesizing carbohydrates carrying an epoxy group in the aglycone position.

Growing community of inventors

Helsingborg, Sweden

Fredrik Bjorkling