Duphar International Research Bv

Solvay Pharmaceuticals, B.v.

Abbvie Bahamas Limited

Jan Zorgdrager

Sebastianus J Halkes

Antonio Mourino

Jose L Mascarenas

Jan-Paul Van De Velde

Maria J Valles

Cornelis G Kruse

Wouter I Iwema Bakker

Hiskias G Keizer

Arnold Van Loevezijn

Martina A W Van Der Neut

Jose P Sestelo

Gerhardus D Dijkstra

Timo Heinrich

Axel Pahl

Emil Finner

Maria De Los Angeles Rey

Yagamare Fall

Ana Fernandez-Gacio

Bernd-Martin Luitjens

Koen M Halkes

Martina Aw Van Der Neut

Pieter C Verveer

Marcel P M Van Aar

Stefanus J Schouten

Michiel C Heslinga

This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HTreceptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.

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The present invention relates to the novel compound 4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo[2,3d]pyrimidine hydrogen mesylate, the polymorphic &#x3b1; and &#x3b2; forms thereof, and a method for the production of said compounds.

4-(4-trans-hydroxycyclohexyl)amino-2-phenyl-7H-pyrrolo [2,3D] pyrimidine hydrogen mesylate, its polymorphic forms, and methods for making same

The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3&#x2013;7C) methyl, benzyl or m-phenyl benzyl

Mesylates of piperazine derivatives and process for their preparation

The invention relates to a new method of preparing 16-dehydro vitamin D compounds having formula I ##STR1## wherein: R has the epi-configuration or the normal configuration and represents straight or branched C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.3-6 -cycloalkyl, or an aromatic group optionally substituted with halogen, C.sub.1-3 -alkyl or alkoxy,

Method of preparing 16-dehydro vitamin D compounds

Vitamin D.sub.3 analogues of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is (C.sub.1 -C.sub.3)alkyl, hydroxy(C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.2)alkoxymethyl, (C.sub.2 -C.sub.3)alkenyl, or (C.sub.2 -C.sub.3)alkynyl, R.sub.3 is a branched or unbranched, saturated or unsaturated aliphatic 3- to 5- membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy, R.sub.4 is sec. or tert. (C.sub.3 -C.sub.6)alkyl or (C.sub.3 -C.sub.6)cycloalkyl, A and B are each individually hydrogen or methyl, or A and B together from methylene. The compounds of the present invention exhibit pharmacotherapeutic activities, including in particular, the treatment of osteoporosis, renal osteodystrophy, osteomalacia, skin disorders such as psoriasis and other hyperproliferative skin diseases, eczema and dermatitis, nmyopathy, leukemia, breast and colon cancer, osteosarcomas, squamous cell carcinomas, melanoma, certain immunological disorders, and transplant rejections. Several methods of synthesis, including reaction of an ester compound of general formula (IX) with an inorganometallic compound of formula (III) followed by deprotection or, alternatively, first finalization of the C.sub.17 -side chain are also disclosed.

Vitamin D compounds and method of preparing these compounds

The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group. The invention also relates to a method of preparing said vitamin D compound and to a lactone and a hydrindane intermediate. The vitamin D compound is of the general formula ##STR1##

Synthesis of C.sub.18 -modified vitamin D compounds and compounds

Vitamin D compound, method of preparing this compound and intermediate

The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;

The invention relates to a new vitamin D compound, substituted in the 18-position with an alkyl group, a hydroxy group, an alkoxy group, an alkenyl group, an alkynyl group, a fluorinated alkyl group or a fluorinated alkenyl group.

Growing community of inventors

Weesp, Netherlands

Jan Zorgdrager