Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-?]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.
Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
Abstract: The invention relates to a product containing the compound of formula (I) below or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.
Abstract: The present invention relates to a new process for the preparation of 2-imino-thiazolidin-4-one compounds of the Formula (I) and (II) and to compounds of Formula (II) as such. The present compounds of Formula (II) can be used as intermediates in the preparation of thiazolidin-4-one derivatives of the General Formula (II), which thiazolidin-4-one derivatives being described in WO 2005/054215 to act as immunosuppressive agents.
Type:
Grant
Filed:
November 22, 2007
Date of Patent:
September 11, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Stefan Abele, Martin Bolli, Gunther Schmidt
Abstract: The present invention relates to the compound of formula 7*acetate (see below), a process for its preparation, and its use
Type:
Grant
Filed:
July 2, 2009
Date of Patent:
August 21, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Maria Andreas Hendrikus De Vries, Doris Domin, Matthias Helms, Christoph Imboden, Ralph Koberstein, Zarghun Nazir, Wolfgang Skranc, Michael Stanek, Wilhelm Tschebull, Maria Gerardus Karel Verzijl, Jurgen Stichler
Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.
Type:
Grant
Filed:
March 27, 2009
Date of Patent:
August 14, 2012
Assignee:
DSM IP Assets B.V.
Inventors:
Daniel D'Orazio, Antoine De Saizieu, Goede Schueler, Daniel Raederstorff, Sandra Renata Teixeira, Ying Wang Schmidt, Peter Weber, Swen Wolfram
Abstract: The invention relates to novel 2-aza-bicyclo[2.2.1]heptane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
Type:
Grant
Filed:
February 19, 2009
Date of Patent:
August 7, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
Abstract: The invention relates to novel thiazolidine derivatives of the formula (I) wherein A and R1 are as described in the description and their use as medicaments, especially as orexin receptor antagonists.
Type:
Grant
Filed:
March 25, 2008
Date of Patent:
August 7, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen
Abstract: An apparatus for supporting the calyx of a flower of a plant having a lockable stem clip from which extend projections for supporting the calyx of the flower.
Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
Type:
Grant
Filed:
April 25, 2008
Date of Patent:
June 19, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Kurt Hilpert, Francis Hubler, Dorte Renneberg
Abstract: The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
Type:
Grant
Filed:
December 20, 2007
Date of Patent:
May 29, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Hamed Aissaoui, Christoph Boss, Markus Gude, Raif Koberstein, Thierry Sifferien
Abstract: A method and device for discharging an electrical defibrillation pulse or an electrical demand pacer pulse or delivering at least one pharmaceutical agent to treat conditions such as cardiac arrest, bradycardia, arrhythmia, cardiac standstill, PEA, EMD and other heart conditions are disclosed. The pharmaceutical agent can be delivered into the heart tissue, the heart cavity, or the peritoneal cavity. The pharmaceutical agent can also include analgesics such as morphine. Also included are pharmaceutical agents used to increase myocardial contractility or inhibit platelet aggregation and vasoactive intestinal polypeptide (VIP) and thyroid hormones such as T3 and T4 can be delivered. A method for the treatment of cardiac arrest or pulmonary hypertension patients by administering a therapeutically effective amount of vasoactive intestinal polypeptide is also encompassed by the invention.
Type:
Grant
Filed:
September 25, 2009
Date of Patent:
May 22, 2012
Assignee:
Avant Garde Therapeutics & Technologies LLC
Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.
Type:
Grant
Filed:
June 4, 2008
Date of Patent:
May 22, 2012
Assignee:
Intra-Cellular Therapies, Inc.
Inventors:
Lawrence P. Wennogle, Peng Li, Jun Zhao
Abstract: The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
Type:
Grant
Filed:
January 23, 2007
Date of Patent:
May 15, 2012
Assignee:
Actelion Pharmaceuticals, Ltd.
Inventors:
Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Joerg Velker
Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention also relates to methods for screening compounds and compositions useful for inhibiting or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
Abstract: The invention relates to novel thiophene derivatives (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I).
Type:
Grant
Filed:
December 9, 2008
Date of Patent:
April 3, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner