[Bernhard LlNDENTHAL, Nico BRÄUER, Peter SERNO, Andrea ROTGERI, Ulrike FUHRMANN, Bernd BUCHMANN, Anne MENGEL, Ulrike RÖHN, Antonius TER LAAK] DE Berlin The invention relates to a pharmaceutical composition for non-hormonal, on-demand contraception and to processes for preparing this pharmaceutical composition. The latter comprises 2H-indazole as novel EP2 receptor antagonists in combination with COX inhibitors. The invention furthermore provides a method for non-hormonal female-controlled on-demand contraception where a pharmaceutical composition comprising EP2 receptor antagonists in combination with COX inhibitors is taken on demand prior to expected sexual intercourse.

[SCHMEES, Norbert, WORTMANN, Lars, KIRCHHOFF, Dennis, NGUYEN, Thi, Thanh, Uyen, WERBECK, Nicolas, BÖMER, Ulf, PETERSEN, Kirstin, KOBER, Christina, STÖCKIGT, Detlef, LECHNER, Christian, MEIER, Robin, Michael, HERBERT, Simon, Anthony, KERSCHGENS, Isabel, Patrizia, KOSEMUND, Dirk, LEFRANC, Julien, OFFRINGA, Rienk] Kaiser-Wilhelm-Allee 1, 51373 Leverkusen, DE

[GRADL, Stefan, Nikolaus, NGUYEN, Duy, EIS, Knut, GÜNTHER, Judith, STELLFELD, Timo, JANZER, Andreas, CHRISTIAN, Sven, MUELLER, Thomas, EL SHEIKH, Sherif, ZHOU, Han, Jie, ZHAO, Changjia, SYKES, David Brian, FERRARA, Steven, James, LIU, Kery, KRÖBER, Michael, MERZ, Claudia, NIEHUES, Michael, SCHÄFER, Martina, ZIMMERMANN, Katja, NISING, Carl, Friedrich] Kaiser-Wilhelm-Allee 1, 51373 Leverkusen, DE

[ZORN, Ludwig, RÖHN, Ulrike, GUTCHER, Ilona, RÖSE, Lars, BADER, Benjamin, KOBER, Christina, CARRETERO, Rafael, STÖCKIGT, Detlef, PLATTEN, Michael] Kaiser-Wilhelm-Allee 1, 51373 Leverkusen, DE

[Eva Maria Becker-Pelster, Hanna Tinel, Michael Hahn, Dieter Lang, Gerrit Weimann, Johannes Nagelschmitz, Lisa Dietz, Soundos Saleh, David Jung, Ildiko Terebesi, Tobias Mundry, Annett Richter, Britta Olenik, Birgit Keil, Bernd Rösler, Peter Fey, Heiko Schirmer, Guido Becker, Clemens Bothe, Helene Faber, Julian Egger, Mark Parry, David Ward, Cecile Vitre] DE Leverkusen The present invention relates to the use of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid of formula (I), prefer-ably in form of one of its salts or solvates or hydrates, preferably (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid in form of monohydrate (I) of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)-ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxylic acid inform of mono hydrate (II) of formula (I-M-II), in the inhalative treatment of cardiopulmonary and pulmonary disorders, such as pulmonary arterial hypertension (P AH), chronic tromboembolic pulmonary hypertension (CTEPH) and pulmonary hypertension (PH) associated with chronic lung disease (PH group 3) such as pulmonary hypertension in chronic obstructive pulmonary disease (PH-COPD) and pulmonary hypertension with idiopathic interstitial pneumonia (PH-IIP), characterized in that an inhalative dosage form comprising 240 to 4000 μg, preferably 480 to 2000 μg of (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid of formula (I), preferably in form of one of its salts or solvates or hydrates, preferably in form of monohydrate I of formula (I-M-I) or (5S)-{[2-(4-carboxyphenyl)ethyl][2-(2-{[3-chloro-4′-(trifluoromethyl)biphenyl-4-yl]methoxy}phenyl)ethyl]-amino}-5,6,7,8-tetrahydroquinoline-2-carboxy lie acid in form of mono hydrate (II) of formula (I-M-II), is administered to a patient in need thereof once or twice daily for a period of at least two consecutive days, preferably at least 2 to 7 consecutive days, preferably for a period of at least 14 consecutive days, in particular from after onset of treatment for the whole course of the disease, wherein the inhalative dosage form preferably comprises the combination of the active ingredient and a pharmaceutically suitable excipient or carrier, while preferably the active ingredient and a pharmaceutically suitable excipient are filled in a hard capsule.

[Julien LEFRANC, Norbert SCHMEES, Ulrike RÖHN, Ludwig ZORN, Judith GÜNTHER, Ilona GUTCHER, Lars RÖSE, Benjamin BADER, Detlef STÖCKIGT, Michael PLATTEN] DE Leverkusen The present invention covers 2-hetarylpyrimidine-4-carboxamide compounds of general formula (I): in which X, Y, Z, R1, R2 and R4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

[Kai Thede, Anne Mengel, Clara Christ, Joachim Kuhnke, Sarah Anna Liesa Johannes, Philipp Buchgraber, Ulrich Klar, Ulrike Sack, Stefan Kaulfuss, Amaury Ernesto Fernandez-Montalvan, Nicolas Werbeck, Ursula Mönning, Katrin Nowak-Reppel, Sven Wittrock, David McKinney, Michael H. Serrano-Wu, Christopher Lemke, Mark Fitzgerald, Christopher Nasveschuk, Kiel Lazarski, Steven James Ferrara, Laura Furst, Guo Wei, Patrick Ryan McCarren, Rebecca Ann Harvey] DE Leverkusen The present invention relates to substituted macrocyclic indole derivatives of general formula (I):in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

[Ilona Gutcher, Ulrike Röhn, Ludwig Zorn, Lars Röse, Benjamin Bader, Christina Kober, Rafael Carretero, Detlef Stöckigt, Michael Platten] DE Leverkusen The present invention covers 3-oxo-6-heteroaryl-2-phenyl-2,3-dihydropyri-dazine-4-carboxamide compounds of general formula (I): in which R1, R2, R4, R5, R6, X, Y and Z are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.

[Martina Delbeck, Michael Hahn, Thomas Müller, Klemens Lustig, Karl Collins, Niels Lindner, Janine Nicolai, Moritz Beck-Broichsitter, Udo Albus, Doris Gehring, Björn Rosenstein] DE Berlin The present invention relates to novel diazabicyclically substituted imidazo[1,2-a]pyrimidine derivatives, such as compounds of the general formula (I): to methods for producing the same, to the use thereof either alone or in combinations for the treatment and/or prevention of diseases, as well as to their use for preparing medicaments for the treatment and/or prevention of diseases, especially for treatment and/or prevention of breathing disorders, including sleep-related breathing disorders such as obstructive and central sleep apnoea and snoring.

[Stephan SIEGEL, Franziska SIEGEL, Volker SCHULZE, Markus BERGER, Keith GRAHAM, Ulrich KLAR, Jeremie Xavier G. MORTIER, Detlev SÜLZLE, Ulf BÖMER, Daniel KORR, Jens SCHRÖDER, Matthew MEYERSON, Heidi GREULICH, Bethany KAPLAN] DE Leverkusen Compounds of formula (I) processes for their production and their use as pharmaceuticals.