Hoffmann-la Roche Inc.

Basilea Pharmaceutica Ag

Vernalis Research Limited

Basilea Pharmaceutica Ag, a Swiss Company

Vernal Research Limited

Neptune Technology Group Inc.

Marc Muller

Peter Mohr

Pierre Barbier

Lin Xu

Wolfgang Pirson

Franz Bauer

Hans G Richter

Stephan Roever

Paul Hebeisen

Patrizio Mattei

Sven Taylor

Milan Soukup

Jonathan Mark Bentley

Xiaoping Wu

Philippe Pflieger

Christopher Self

Werner Mueller

Philippe Guerry

Patrick Moreau

Josef Stadlwieser

C1-C6Alkyloxy- or benzyloxy-carbonyl esters of -{3-[(E)-(1-phenyl or naphthyl C1-C4alkyl)-imino]-propyl}-amino)-acetic acid, which are intermediates for producing known bridged monobactam compounds useful in the treatment of bacterial infections.

Bridged monobactam intermediates

A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C-Calkyl or 1-naphthyl-C-Calkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C-Calkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C-Calkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C-Calkoxy group and/or silyloxy group per carbon atom, and R2 represents a C-Calkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C-Calkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0&#xb0; C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I). 

Process for the manufacture of bridged monobactam intermediates

Disclosed is a process for the manufacture of a compound of formula (I) wherein Hal represents fluoro or chloro, and Rand Rrepresent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of &#x2212;10 to 50&#xb0; C. to give the compound of formula (I).

Process for the manufacture of epoxy triazole derivatives

Disclosed is a process for the manufacture of a compound of formula (I) whereinHal represents fluoro or chloro, and Rand Rrepresent, independently from one another, hydrogen or Hal; in which process a compound of formula (II) is converted to a corresponding alkyl, fluoroalkyl or aryl sulfonic acid ester, which is then reacted with an alkali metal nitrite in the presence of a suitable crown ether in a polar non-nucleophilic solvent at a temperature of &#x2212;10 to 50&#xb0; C. to give the compound of formula (I).

Process for the manufacture of epoxybutanol intermediates

The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein Rto Rhave the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

Anti-obesity 1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles

The invention is concerned with a process for the manufacture of vinylpyrrolidinone-cephalosporin derivatives from 3-amino-pyrrolidine derivatives of the formula wherein

Process for the manufacture of 3-amino-pyrrolidine derivatives

The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I):as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.

The invention is concerned with a process for the manufacture of 3-amino-pyrrolidine derivatives of the formulawherein

The present invention provides piperazine derivatives in accordance with formula (I)as well as salts, hydrates and esters thereof. The substituent designations are as provided in the specification. The compounds of the present invention can be used in the treatment of type II diabetes or obesity.

Piperazine derivatives

Substituted 5-benzyl-2,4-diaminopyrimidines

Cyclohexanediol derivatives

Compounds of formula (I) ##STR1## as defined by the specification. The compounds are useful in the treatment or prevention of vitamin D dependent disorders, particularly psoriasis, basal cell carcinomas, disorders of keratinization and keratosis, leukemia, osteoporosis, hyperparathyroidism accompanying renal failure, transplant rejection and graft vs. host disease.

Arylsecocholadiene derivatives

The present invention relates to vitamin D derivatives of the formula I ##STR1## wherein X is C.dbd.CH.sub.2 or CH.sub.2 ;

Vitamin D derivatives

Polyunsaturated 24a,24b-dihomo-9,10-secocholestane derivatives of formula ##STR1## wherein A is a single or double bond,

Dihomo-seco-cholestanes

Compounds of formula I: ##STR1## wherein the dotted carbon-carbon bond in the D-ring is C--C or C.dbd.C; C(R,R) is CH.sub.2 or C.dbd.CH.sub.2,

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Saint-Louis, France

Marc Muller