pa:(Roland Humm)

1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS PCT/EP2011/063498
[BANNER, David, GABELLIERI, Emanuele, GUBA, Wolfgang, HILPERT, Hans, HORNSPERGER, Benoit, HUMM, Roland, MAUSER, Harald, MAYWEG, Alexander, V., NARQUIZIAN, Robert, PINARD, Emmanuel, ROGERS-EVANS, Mark, WOLTERING, Thomas, WOSTL, Wolfgang] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Strada del Petriccio e Belriguardo 35 I-53100 Siena;IT(IT)(IT)}{Neubadstrasse 129 CH-4054 Basel;CH(GB)(CH)}{Strada del Petriccio e Belriguardo 35 I-53100 Siena;IT(IT)(IT)}{Am Ruettacker 3 79379 Muellheim;DE(DE)(DE)}{Gustav Bay-Strasse 34 CH-4142 Muenchenstein;CH(CH)(CH)}{9, rue des Sources F-68130 Altkirch;FR(FR)(FR)}{Julius-Kibiger-Strasse 12 79424 Auggen;DE(DE)(DE)}{Muttenzerstr. 43 CH-4127 Birsfelden;CH(DE)(CH)}{Martinsgasse 8 CH-4051 Basel;CH(DE)(CH)}{37 rue de Wahlbach F-68130 Zaessingue;FR(FR)(FR)}{7, rue de Pujo F-68480 Linsdorf;FR(FR)(FR)}{Rosenweg 6 CH-4103 Bottmingen;CH(GB)(CH)}{Jaegerhaeusleweg 57 79104 Freiburg;DE(DE)(DE)}{Im Strick 2 79639 Grenzach-Wyhlen;DE(DE)(DE)} This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
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DIHYDROPYRIMIDINONES US12770802
[David Banner, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Fabienne Ricklin, Mark Rogers-Evans] CH,,Basel;CH,,Muenchenstein;DE,,Auggen;DE,,Schliengen;CH,,Basel;FR,,Hombourg;CH,,Bottmingen; This invention relates to dihydropyrimidinones of the formula wherein X and R1 to R7 are as defined in the description, as well as pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the treatment or prevention of diseases such as diabetes.
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Indolyl derivatives US10659664
[Alfred Binggeli, Beat Wirz, Uwe Grether, Hans Hilpert, Roland Humm, Hans Iding, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr] CH,,Binningen;CH,,Reinach;DE,,Loerrach;CH,,Muenchenstein;DE,,Freiburg;DE,,Rheinfelden;CH,,Riehen;CH,,Basle;DE,,Neuenburg;CH,,Basle; Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R8, A, A1 and n have the significance indicated in the specification.
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2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS PCT/EP2011/056990
[BANNER, David, GUBA, Wolfgang, HILPERT, Hans, HUMM, Roland, MAUSER, Harald, MAYWEG, Alexander, V., NARQUIZIAN, Robert, POWER, Eoin, ROGERS-EVANS, Mark, ROMBACH, Didier, WOLTERING, Thomas, WOSTL, Wolfgang] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Strada del Petriccio e Belriguardo 35 I-53100 Siena;IT(IT)(IT)}{Neubadstrasse 129 CH-4054 Basel;CH(GB)(CH)}{Am Ruettacker 3 79379 Muellheim;DE(DE)(DE)}{Gustav Bay-Strasse 34 CH-4142 Muenchenstein;CH(CH)(CH)}{Julius-Kibiger-Strasse 12 79424 Auggen;DE(DE)(DE)}{Muttenzerstrasse 43 CH-4127 Birsfelden;CH(DE)(CH)}{Martinsgasse 8 CH-4051 Basel;CH(DE)(CH)}{37 rue de Wahlbach F-68130 Zaessingue;FR(FR)(FR)}{25 Ard na Mara Blackrock, Co. Louth;IE(IE)(IE)}{Rosenweg 6 CH-4103 Bottmingen;CH(GB)(CH)}{92, rue de Belfort F-68200 Mulhouse;FR(FR)(FR)}{Jaegerhaeusleweg 57 79104 Freiburg;DE(DE)(DE)}{Im Strick 2 79639 Grenzach-Wyhlen;DE(DE)(DE)} This invention relates to compounds of the formula (I), wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as 5 medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
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DICARBOXAMIDE DERIVATIVES AND THEIR USE AS FACTOR XA INHIBITORS PCT/EP2005/011430
[BOEHRINGER, Markus, GROEBKE ZBINDEN, Katrin, HAAP, Wolfgang, HILPERT, Hans, HIMBER, Jacques, HUMM, Roland, IDING, Hans, KNOPP, Dietmar, PANDAY, Narendra, RICKLIN, Fabienne, STAHL, Christoph, Martin] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Dachsweg 4 CH-4313 Moehlin;CH(CH)(CH)}{Wettsteinallee 64 CH-4058 Basel;CH(CH)(CH)}{Fridolin-Engel-Strasse 51 79540 Loerrach;DE(DE)(DE)}{Gustav Bay-Strasse 34 CH-4142 Muenchenstein;CH(CH)(CH)}{1, Chemin du Peternit F-68500 Guebwiller;FR(FR)(FR)}{Lindenweg 32 79424 Auggen;DE(DE)(DE)}{Bahnhofstrasse 45 79618 Rheinfelden;DE(DE)(DE)}{Blaesiring 10 CH-4057 Basel;CH(DE)(CH)}{Gueterstrasse 213 CH-4053 Basel;CH(FR)(CH)}{6, impasse des Cerisiers F-68490 Hombourg;FR(FR)(FR)}{Lerchenstrasse 28 79104 Freiburg;DE(DE)(DE)} The invention is concerned with novel dicarboxamide derivatives of formula (I) wherein A, B, RC, D and E are as defined in the description and in the claims, as well 5as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
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N-[3-(5-AMINO-3,3A,7,7A-TETRAHYDRO-1H-2,4-DIOXA-6-AZA-INDEN-7-YL)-PHENYL]-AMIDES AS BACE1 AND/OR BACE2 INHIBITORS PCT/EP2012/051910
[HILPERT, Hans, HUMM, Roland] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Gustav Bay-Strasse 34 CH-4142 Muenchenstein;CH(CH)(CH)}{Julius-Kibiger-Strasse 12 79424 Auggen;DE(DE)(DE)} The present invention relates to N-[3-(5-Amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides of formula (I) having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
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FLUOROMETHYL-5,6-DIHYDRO-4H-[1,3]OXAZINES PCT/EP2013/051166
[HILPERT, Hans, HUMM, Roland, WOLTERING, Thomas] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Strada del Petriccio e Belriguardo 35 I-53100 Siena;IT(IT)(IT)}{Gustav Bay-Strasse 34 CH-4142 Muenchenstein;CH(CH)(CH)}{Julius-Kibiger-Strasse 12 79424 Auggen;DE(DE)(DE)}{Jaegerhaeusleweg 57 79104 Freiburg;DE(DE)(DE)} The present invention provides a compound of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
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PHOSPHINIC ACIDS DERIVATIVES, BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER’S DISEASE PCT/EP2004/012371
[HILPERT, Hans, HUMM, Roland, KNOPP, Dietmar, WEISS, Peter] {Grenzacherstrasse 124 CH-4070 Basel;CH(CH)(CH)}{Gustav Bay-Strasse 34 CH-4142 Münchenstein;CH(CH)(CH)}{In den Sigristmatten 2a 79115 Freiburg;DE(DE)(DE)}{Blaesiring 10 CH-4057 Basel;CH(DE)(CH)}{Rosentalstrasse 52 CH-4058 Basel;CH(CH)(CH)} The present invention relates to phosphinic acid derivatives of formula (I) wherein R1 is aryl or heteroaryl, R2 is (C1-C5)-alkyl or phenyl, R3 is hydrogen, (C1-C5)-alky, O-(C1-C5)-alkyl or phenyl, R4 is (C1-C6)-alkyl, (C3-C6)-cycloalkyl, phenyl, pyridyl or indolyl, and pharmaceutically acceptable salts thereof. The compounds can be used in the treatment or prevention of a disease related to the inhibition of beta-secretase, inter alia for the treatment of Alzheimer’s disease.
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Tetronic and tetramic acids US10994823
[Thierry Godel, Hans Hilpert, Roland Humm, Mark Rogers-Evans, Didier Rombach, Christoph Stahl, Peter Weiss, Wolfgang Wostl] CH,,Basel;CH,,Muenchenstein;DE,,Freiburg;CH,,Binningen;FR,,Mulhouse;DE,,Freiburg;CH,,Basel;DE,,Grenzach-Wyhlen; This invention relates to new tetronic and tetramic acid derivatives with beta-secretase inhibitory activity of formula I: wherein R1, R2, R3, R4, R5, R5′, R6 and R6′ are as defined hereinabove, to processes for their preparation, compositions containing said tetronic and tetramic acid derivatives and their use in the treatment and prevention of diseases modulated by an inhibitor of β-secretase, such as Alzheimer's disease.
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2,5,6,7-TETRAHYDRO-[1,4]OXAZEPIN-3-YLAMINE OR 2,3,6,7-TETRAHYDRO-[1,4]OXAZEPIN-5-YLAMINE COMPOUNDS US13096059
[David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl] CH,,Basel;DE,,Muellheim;CH,,Muenchenstein;DE,,Auggen;CH,,Birsfelden;CH,,Basel;FR,,Zaessingue;IE,,Blackrock;CH,,Bottmingen;FR,,Mulhouse;DE,,Freiburg;DE,,Grenzach-Wyhlen; This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
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