Janssen Pharmaceutica Nv

Other

Mcneil Ab

Janssen Pharmaceutica

Michael Joseph Kukla

Jan Heeres

Donald William Ludovici

Paul Adriaan Jan Janssen

Lucien Maria Henricus Koymans

Koen Jeanne Alfons Van Aken

Bart L De Corte

Robert William Kavash

Chih Yung Ho

Marc René De Jonge

Henry Joseph Breslin

Koenraad Jozef Lodewijk Marcel Andries

Marc Ren&eacute; De Jonge

Paul A J Janssen

Henri E L Moereels

Marcel August Constant Janssen

Paul A Janssen

Hans Louis Jos De Winter

Bart Lieven Daniel De Corte

Marc Rene De Jonge

Alain Krief

Alfons H Raeymaekers

Chris R Rasmussen

Robert W Tuman

Josephus L Van Gelder

Frederik Frans Desir&eacute; Daeyaert

Eddy Jean Edgard Freyne

Werner Constant Johan Embrechts

Jean Fernand Armand Lacrampe

Paulus Joannes Lewi

Marc Willems

Frederik Frans Desiré Daeyaert

Peter Jacobus Johannes Antonius Buijnsters

Ruben Gerardus George Leenders

Frank Xavier Jozef Herwig Arts, Legal Representative

Hugo Alfons Geerts

Frederik Frans Daeyaert

Lucien Maria Koymans

Johan Jozef Geysen

Alfons H M Raeymaekers

Marc Hubert Mercken

Rony Maria Nuydens

Hugo Alfons Gabriel Geerts

Theodora Joanna Francisca Arts

Maroussia Godelieve Frank Janssen, Legal Representative

Jasmine Josée Werner Janssen, Legal Representative

Graziella Maria Constantina Janssen, Legal Representative

Paul Peter Maria Janssen, Legal Representative

Herwig Josephus Margareta Janssen, Legal Representative

Josephus L H Van Gelder

Jan Janssen Pharmaceutica NV Heeres

Bart De Cort

Robert W Janssen Pharmaceutica Inc Kavash

Bart L D Janssen Pharmaceutical Inc De Corte

Maroussia Godelieve Frank Janssen

Jasmin Josee Werner Janssen

Jean Fernand Armand Janssen-Cilag Lacrampe

Graziella Maria Constantina Janssen

Herwig Josephus Margareta Janssen

Paul Peter Maria Janssen

Donald William Janssen Pharmac Inc Ludovici

Paul Andriaan Jan Janssen

Lucien M H Janssen Pharmaceutica NV Koymans

Alain Université Notre-Dame De La Paix Krief

Koen J A Janssen Pharmaceutica NV Van Aken

Donald W Janssen Pharmaceutica Inc Ludovici

Paul A J Janssen Pharmaceutica NV Janssen

Paul Adriaan Janssen

Koen Jeanne Van Aken

Bart Lieven De Corte

Hans Louis De Winter

Ruben Gerardus Leenders

This invention concerns the use of compounds of formula the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a=a-a=a- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, substituted Calkyl, or substituted CalkyloxyCalkylcarbonyl; each Rindependently is hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkylamino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or L is &#x2014;X&#x2014;Rwherein Ris optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl or an optionally substituted amino group; Y represents hydroxy, halo, Ccycloalkyl, optionally substituted Calkyl, Calkenyl or Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

HIV replication inhibiting pyrimidines

The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).

Tripeptidyl peptidase inhibitors

This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CRor N; n is 0 to 4; Q is hydrogen or &#x2014;NRR; Rand Rare selected from hydrogen, hydroxy, Calkyl, Calkyloxy, Calkylcarbonyl, Calkyloxycarbonyl, aryl, amino, mono- or di(Calkyl)-amino, mono- or di(Calkyl)aminocarbonyl wherein each Calkyl may optionally be substituted; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)aminoCalkylidene; Ris hydrogen, aryl, Calkylcarbonyl, optionally substituted Calkyl, Calkyloxy-carbonyl; and Ris hydroxy, halo, optionally substituted Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; Ris hydrogen or Calkyl; L is optionally substituted Calkyl, Calkenyl, Calkynyl, Ccycloalkyl; or L is &#x2014;X&#x2014;Ror &#x2014;X-Alk-Rwherein Rand Rare optionally substituted phenyl; Xand Xare &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Alk is Calkanediyl; aryl is optionally substituted phenyl; Het is an optionally substituted aliphatic or aromatic heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

HIV inhibiting pyrimidine derivatives

This invention concerns the use of compounds of formula the N-oxides, pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms thereof, wherein -a=a-a=a- forms phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl with the attached vinyl group; n is 0 to 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, substituted Calkyl, substituted CalkyloxyCalkylcarbonyl; Ris hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)R, 5-membered heterocyclic ring; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or &#x2014;X&#x2014;R; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl, optionally substituted amino group; Y represents hydroxy, halo, Ccycloalkyl, optionally substituted Calkyl, Calkenyl or Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono-or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, 13 NHC(&#x2550;O)R,&#x2014;C(&#x2550;NH)R, aryl; for the treatment of subjects suffering from HIV infection.

The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or &#x2014;(CRR)&#x2014; wherein m is an integer 1 or 2; Rand Rare each independently from each other hydrogen or Calkyl; Ris Calkylcarbonyl optionally substituted with hydroxy; Calkyloxycarbonyl; aminoCalkylcarbonyl wherein the Calkyl group is optionally substituted with Ccycloalkyl; mono- and di(Calkyl)aminoCalkylcarbonyl; aminocarbonyl substituted with aryl; CalkylcarbonyloxyCalkylcarbonyl; CalkyloxycarbonylaminoCalkylcarbonyl wherein the amino group is optionally substituted with Calkyl; an amino acid; Calkyl substituted with amino; or arylcarbonyl; Ris an optionally substituted 5-membered heterocycle, or Ris optionally substituted benzimidazole; Ris a bivalent radical &#x2014;CHCH&#x2014; optionally substituted with halo or phenylmethyl; or Ris a bivalent radical of formula. 

The present invention concerns compounds of formula (A)(A)N&#x2014;R(I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Ris substituted Calkyl; &#x2014;S(&#x2550;O)&#x2014;R; &#x2014;S(&#x2550;O)&#x2014;R; Calkylcarbonyl; optionally substituted CalkyloxycarbonylCalkylcarbonyl; with Rbeing Calkyl, arylor Het; (A)(A)N&#x2014; is the covalently bonded form of the corresponding intermediate of formula (A)(A)N&#x2014;H, which is a HIV replication inhibiting pyrimidine of formula 

Prodrugs of HIV replication inhibiting pyrimidines

This invention concerns the compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein Rand Rare each independently selected from hydrogen; hydroxy; amino; optionally substituted Calkyl; Calkyloxy; Calkylcarbonyl; Calkyloxycarbonyl; Ar; mono- or di(Calkyl)amino; mono- or di(Calkyl)-aminocarbonyl; dihydro-2(3H)-furanone; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)amino-Calkylidene; Ris hydrogen, Ar, Calkylcarbonyl, Calkyl, Calkyloxy-carbonyl, Calkyl substituted with Calkyloxycarbonyl; and R, R, R, Rand Rare each independently selected from hydrogen, halo, Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted Calkyl; Calkenyl; Calkynyl; Ccycloalkyl; Aris optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

Substituted diamino-1,3,5-triazine derivatives

This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, provided that when Q is halo then Z is N; or when Q is polyhaloCalkyl then Y is hydrogen or Calkyl; their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

HIV replication inhibitors

This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A represents a 6-membered heterocycle; Ris hydrogen; aryl; formyl; Calkylcarbonyl; optionally substituted Calkyl; Calkyloxycarbonyl; optionally substituted CalkyloxyCalkylcarbonyl; X is a direct bond or a linker atom or group; Z is O or S; Ris hydrogen, Calkyl, Calkenyl, Calkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; Ris hydrogen; hydroxy; halo; optionally substituted Calkyl or Calkenyl or Calkynyl; Calkyloxy; Calkylthio; Calkyloxycarbonyl; Calkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(Calkyl)amino; polyhaloCalkyl; polyhaloCalkyloxy; polyhaloCalkylthio; R; R&#x2014;Calkyl; R&#x2014;O&#x2014;; R&#x2014;S&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;S(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;; &#x2014;NHC(&#x2550;O)H; &#x2014;C(&#x2550;O)NHNH; R&#x2014;C(&#x2550;O)&#x2014;NH&#x2014;; R&#x2014;C(&#x2550;O)&#x2014;NH&#x2014;; &#x2014;C(&#x2550;NH)R; &#x2014;C(&#x2550;NH)R; Ror Reach independently represent hydrogen, R, &#x2014;Y&#x2014;NR&#x2014;Y&#x2014;NRR, &#x2014;Y&#x2014;NR&#x2014;Y&#x2014;R, &#x2014;Y&#x2014;NRR; provided that &#x2014;X&#x2014;Rand/or Ris other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.

Amide derivatives as glycogen synthase kinase 3-&#x3b2; inhibitors

The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. wherein n is an integer 0 or 1; X represents O; S; or &#x2014;(CRR)&#x2014; wherein m is an integer 1 or 2; Rand Rare each independently from each other hydrogen or Calkyl; Ris Calkylcarbonyl optionally substituted with hydroxy; Calkyloxycarbonyl; aminoCalkylcarbonyl wherein the Calkyl group is optionally substituted with Ccycloalkyl; mono- and di(Calkyl)aminoCalkylcarbonyl; aminocarbonyl substituted with aryl; CalkylcarbonyloxyCalkylcarbonyl; CalkyloxycarbonylaminoCalkylcarbonyl wherein the amino group is optionally substituted with Calkyl; an amino acid; Calkyl substituted with amino; or arylcarbonyl; Ris an optionally substituted 5-membered heterocycle, or Ris optionally substituted benzimidazole; Ris a bivalent radical &#x2014;CHCH&#x2014; optionally substituted with halo or phenylmethyl; or Ris a bivalent radical of formula 

This invention concerns the use of compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a=a-a=a- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, substituted Calkyl, or substituted CalkyloxyCalkylcarbonyl; each Rindependently is hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or L is &#x2014;X&#x2014;Rwherein Ris optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Q is hydrogen, Calkyl, halo, polyhalo-Calkyl or an optionally substituted amino group; Y represents hydroxy, halo, Ccycloalkyl, optionally substituted Calkyl, Calkenyl or Calkynyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror aryl; aryl is optionally substituted phenyl; Het is an optionally substituted heterocyclic radical; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

The present invention concerns compounds of formula (A)(A)N&#x2014;R(I),the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Ris substituted Calkyl; &#x2014;S(&#x2550;O)&#x2014;R; &#x2014;S(&#x2550;O)&#x2014;R; Calkylcarbonyl; optionally substituted CalkyloxycarbonylCalkylcarbonyl; with Rbeing Calkyl, arylor Het; (A)(A)N&#x2014; is the covalently bonded form of the corresponding intermediate of formula (A)(A)N&#x2014;H, which is a HIV replication inhibiting pyrimidine of formula

This invention concerns the use of the compounds of formulathe N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a=a-a=a- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; Ris hydrogen, aryl, formyl, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl or substituted Calkyl; each Rindependently is hydroxy, halo, optionally substituted Calkyl, Calkenyl or Calkynyl, Ccycloalkyl, Calkyloxy, Calkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(Calkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, &#x2014;S(&#x2550;O)R, &#x2014;NH&#x2014;S(&#x2550;O)R, &#x2014;C(&#x2550;O)R, &#x2014;NHC(&#x2550;O)H, &#x2014;C(&#x2550;O)NHNH, &#x2014;NHC(&#x2550;O)R, &#x2014;C(&#x2550;NH)Ror a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted Calkyl, Calkenyl, Calkynyl or Ccycloalkyl; or L is &#x2014;X&#x2014;Rwherein Ris optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is &#x2014;NR&#x2014;, &#x2014;NH&#x2014;NH&#x2014;, &#x2014;N&#x2550;N&#x2014;, &#x2014;O&#x2014;, &#x2014;C(=O)&#x2014;, &#x2014;CHOH&#x2014;, &#x2014;S&#x2014;, &#x2014;S(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.

2,4-disubstituted triazine derivatives

This invention concerns the compounds of formulathe pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein Rand Rare each independently selected from hydrogen; hydroxy; amino; optionally substituted Calkyl; Calkyloxy; Calkylcarbonyl; Calkyloxycarbonyl; Ar; mono- or di(Calkyl)amino; mono- or di(Calkyl)aminocarbonyl; dihydro-2(3H)-furanone; or Rand Rtaken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(Calkyl)amino-Calkylidene; Ris hydrogen, Ar, Calkylcarbonyl, Calkyl, Calkyloxycarbonyl, Calkyl substituted with Calkyloxycarbonyl; and R, R, R, Rand Rare each independently selected from hydrogen, halo, Calkyl, Calkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl or trihalomethyloxy; L is optionally substituted Calkyl; Calkenyl; Calkynyl; Ccycloalkyl; Aris optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection. It further relates to new compounds being a subgroup of the compounds of formula (I), their preparation and compositions comprising them.

This invention concerns the use of the compounds of formula

Growing community of inventors

Maple Glen, PA, United States of America

Michael Joseph Kukla