Topadur Pharma Ag

Takeda Gmbh

Nycomed Gmbh

Hermann Tenor

Dieter Flockerzi

Reto Naef

Beate Schmidt

Hans-Peter Kley

Armin Hatzelmann

Steffen Weinbrenner

Raimund Külzer

Christof Zitt

Clemens Braun

Geert Jan Sterk

Anke Heuser

Imre Schlemminger

Thomas Maier

Raimund Kuelzer

Degenhard Marx

Ulrich Kautz

Martin Viertelhaus

Christian Hesslinger

Rolf-Peter Hummel

Stefan Fischer

Christian Schudt

Torsten Dunkern

Ewald Benediktus

Rolf Beume

Thomas Stengel

Serge Adnot

Saadia Eddahibi

Manuela Hessmann

Harald Ohmer

Alexander Mann

Josef Stadlwieser

Hans Christof Holst

Tobias Kanacher

Raimund c/o Nycomed Gmbh Külzer

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein Ris C-Calkyl optionally substituted with F, C-Ccycloalkyl, C-Calkoxy; X represents a bond or C-Calkylene optionally substituted with OH, ONO, ONO; Ris H, OH, ONO, ONO, C(O)OH, C(O)OC-Calkyl, CHO, CN, C-Calkoxy, OC(O)H, OC(O)—C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl, CR═N—OR, CR═N—NRR, CR═NRor CR═N—ONO; Ris C-Calkyl optionally substituted with F, OH, ONO, ONO, C-Calkoxy, C-Ccycloalkyl; C-Ccycloalkyl, C-Calkenyl, C-Calkynyl; Ris C-Calkyl optionally substituted with C-Ccycloalkyl, C-Calkoxy, F, ONO, ONO; C-Calkenyl, C-Calkynyl, C-Ccycloalkyl; Ris H, SON—RR, NHSONRR; Ris H or C-Calkyl; Ris H, C-Calkyl, C-Calkoxy, C-Calkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or said heterocyclic ring are independently optionally substituted by C-Calkyl, F; Ris H, CHor CH; R: H, C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-Calkyl, C-Calkoxy, OC(O)H, OC(O)—C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl; Rand Rare each independently H, C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-C, C-Calkoxy, OC(O)H, OC(O)—C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl; i or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrolidine, piperidine, morpholine, piperazine and homopiperazine, wherein said heterocyclic ring is optionally substituted with C-Calkyl; Ris C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-Calkyl, C-Calkoxy, OC(O)H, OC(O)—C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl; Rand Rare each independently H or C-Calkyl optionally substituted with F, OH, ONO, ONO, COOH, C-Calkoxy, C-CCycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrolidine, piperidine, morpholine, piperazine, homopiperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with R; Ris C-Calkyl optionally substituted with halogen, OH, ONO, ONO, C-Calkoxy, C-Chaloalkoxy, COOR, NRR, C═NR, or with a tetrazole group which is optionally substituted with C-Calkyl; or a heteroaryl ring which is optionally substituted with F, wherein the at least one heteroatom of said heteroaryl ring is nitrogen; Ris H, or C-Calkyl optionally substituted with F, OH, ONO, ONO, NRR, or with a heteroaryl ring, wherein the at least one heteroatom of said heteroaryl ring is nitrogen, and wherein preferably said heteroaryl ring is selected from pyrrolidine, piperidine, piperazine, morpholine, pyrrole, and imidazole, wherein nitrogen atom is directly bound to C-Calkyl; Rand Rare each independently H or C-Calkyl optionally substituted with ONO, ONO; Ris C-Calkyl optionally substituted with F, ONO, ONO; C-CCycloalkyl; and their use in methods of treating or preventing a disease alleviated by inhibition of PDE-5 in a human or in a non-human mammal.

2-phenyl-3,4-dihydropyrrolo[2,1-f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.

Dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof

The present invention relates to compounds of formula I

2-phenyl-3,4-dihydropyrrolo[2,1 -f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein

2-phenyl-3,4-dihydropyrrolo[2,1-Ff] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof, whereinRis C-Calkyl optionally substituted with F, C-Ccycloalkyl, C-Calkoxy;X represents a bond or C-Calkylene optionally substituted with OH, ONO, ONO;Ris H, OH, ONO, ONO, C(O)OH, C(O)OC-Calkyl, CHO, CN, C-Calkoxy, OC(O)H, OC(O)&#x2014;C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl, CR&#x2550;N&#x2014;OR, CR&#x2550;N&#x2014;NRR, CR&#x2550;NRor CR&#x2550;N&#x2014;ONO;Ris C-Calkyl optionally substituted with F, OH, ONO, ONO, C-Calkoxy, C-Ccycloalkyl; C-Ccycloalkyl, C-Calkenyl, C-Calkynyl;Ris C-Calkyl optionally substituted with C-Ccycloalkyl, C-Calkoxy, F, ONO, ONO; C-Calkenyl, C-Calkynyl, C-Ccycloalkyl;Ris H, SONRR, NHSONRR;Ris H or C-Calkyl;Ris H, C-Calkyl, C-Calkoxy, C-Calkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or said heterocyclic ring are independently optionally substituted by C-Calkyl, F;Ris H, CHor CH;R: H, C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-Calkyl, C-Calkoxy, OC(O)H, OC(O)&#x2014;C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl;Rand Rare each independently H, C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-C, C-Calkoxy, OC(O)H, OC(O)&#x2014;C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine and homopiperazine, wherein said heterocyclic ring is optionally substituted with C-Calkyl;Ris C-Calkyl optionally substituted with OH, ONO, ONO, CN, COOH, COOC-Calkyl, C-Calkoxy, OC(O)H, OC(O)&#x2014;C-Calkyl, C(O)N(R)OR, OC-Calkylene-C(O)OH, OC-Calkylene-C(O)OC-Calkyl, OC-Calkylene-C(O)N(R)OR, S(O)C-Calkyl;Rand Rare each independently H or C-Calkyl optionally substituted with F, OH, ONO, ONO, COOH, C-Calkoxy, C-Ccycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homopiperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with R;Ris C-Calkyl optionally substituted with halogen, OH, ONO, ONO, C-Calkoxy, C-Chaloalkoxy, COOR, NRR, C&#x2550;NR, or with a tetrazole group which is optionally substituted with C-Calkyl; or a heteroaryl ring which is optionally substituted with F, wherein the at least one heteroatom of said heteroaryl ring is nitrogen;Ris H, or C-Calkyl optionally substituted with F, OH, ONO, ONO, NRR, or with a heteroaryl ring, wherein the at least one heteroatom of said heteroaryl ring is nitrogen, and wherein preferably said heteroaryl ring is selected from pyrrolidine, piperidine, piperazine, morpholine, pyrrole, and imidazole, wherein nitrogen atom is directly bound to C-Calkyl;Rand Rare each independently H or C-Calkyl optionally substituted with ONO, ONO; Ris C-Calkyl optionally substituted with F, ONO, ONO; C-Ccycloalkyl;and their use in methods of treating or preventing a disease alleviated by inhibition of PDE-5 in a human or in a non-human mammal.

2-phenyl-3,4-dihydropyrrolo[2,1 -F] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof

The compounds of Formula (I), are novel effective inhibitors of the type 4 phosphodiesterase.

Pyrazolone-derivatives and their use as PDE-4 inhibitors

The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.

3,4,4a,10b-Tetrahydro-1H-thiopyrano-[44,3-c] isoquinoline derivatives

The invention relates to the use of Roflumilast, Roflumilast N-Oxide or a pharmaceutically acceptable salt of either for the treatment of pulmonary hypertension. The invention additionally relates to the use of Roflumilast, Roflumilast N-oxide or a pharmaceutically acceptable salt of either in combination with a PDE5 inhibitor or a pharmaceutically acceptable salt thereof for the treatment of pulmonary hypertension.

Roflumilast for the treatment of pulmonary hypertension

The compounds of formula (I) in which R1, R2 and R3 have the meanings as given in the description are novel effective PDE2 inhibitors.

Triazolophthalazines

The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.

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Radolfzell, Germany

Hermann Tenor