Eli Lilly and Company

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Istituto Di Ricerche Di Biologia P. Angeletti S.p.a.

Victor Giulio Matassa

John Joseph Masters

Peter Thaddeus Gallagher

Sandra Ann Filla

Alessia Petrocchi

Steven Harper

Cristina Gardelli

Brian Michael Mathes

Serge Louis Boulet

Richard Edmund Rathmell

Kevin John Hudziak

Anette Margareta Johansson

Rushad Eruch Karanjawala

Chad Nolan Wolfe

Maria Emilia Di Francesco

Vincenzo Summa

Marco Poma

Maria Ann Whatton

Paola Pace

Emanuela Nizi

Barbara Pacini

Ester Murgalia

Frank Narjes

Uwe Koch

Jesus Maria Ontoria Ontoria

Ester Muraglia

Ian Stansfield

Simona Ponzi

Stefania Colarusso

Maria Ann (nee Fagan) Whatton

Benjamin Gerlach

Vicenzo Summa

4,5-Dihydroxypyrimidine-6-carboxamides of formula:  are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Dihydroxypyrimidine carboxamide inhibitors of HIV integrase

There is provided a compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro, acetyl, &#x2014;CF, &#x2014;SCFand cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C-Calkyl; Z is selected from H, ORor F, wherein Ris selected from H, C-Calkyl and phenyl C-Calkyl; Rand Rare each independently H or C-Calkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl. 

3-aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake

There is provided a compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C-Calkyl and C-Calkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C-Calkyl, and C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro, acetyl, &#x2014;CF, &#x2014;SCFand cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C-Calkyl; Z is selected from ORor F, wherein Ris selected from H, C-Calkyl and phenyl C-Calkyl; Rand Rare each independently H or C-Calkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is ORand X is optionally substituted phenyl then A is &#x2014;S&#x2014;. 

3-aryloxy/thio-2,3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake

There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C-Calkyl and C-Calkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C-Calkyl, and C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl &#x2014;S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro acetyl, &#x2014;CF, &#x2014;SCFand cyano; Z is selected from H, ORor F, wherein Ris selected from H, C-Calkyl and phenyl CCalkyl; Rand Rare each independently H or C-Calkyl; and pharmaceutically acceptable salts thereof. 

Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors

4,5-Dihydroxypyrimidine-6-carboxamides of formula (I); are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein R, R, Rand Rare defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described 

Compounds of formula (I), and pharmaceutically acceptable salts and esters thereof: (I); wherein Q, R2, X, Y and Z are as defined herein; are inhibitors of the hepatitis C virus (HCV) NS3 protease 

Peptides and their use as inhibitors of hepatitis C virus ns3 protease

Growing community of inventors

Hirschberg, Germany

Victor Giulio Matassa