Patent classifications
C07D271/06
USE OF STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI CONTAINING AN AMINO ACID SUBSTITUTION F129L IN THE MITOCHONDRIAL CYTOCHROME B PROTEIN CONFERRING RESISTANCE TO QO INHIBITORS I
- Andreas Koch ,
- Marcus Fehr ,
- Vanessa Tegge ,
- Chandan Dey ,
- Manojkumar Poonoth ,
- Sarang Kulkarni ,
- Ronan Le Vezouet ,
- Christian Harald Winter ,
- Georg Christoph Rudolf ,
- Rakesh Rath ,
- Smriti Khanna ,
- lan Robert Craig ,
- Wassilios Grammenos ,
- Thomas Grote ,
- Gerd Stammler ,
- Tobias Mentzel ,
- Egon Haden ,
- Joachim Rheinheimer
The present invention relates to the use of strobilurin type compounds of formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi containing an amino acid substitution F129L in the mitochondrial cytochrome b protein (also referred to as F129L mutation in the mitochondrial cytochrome b gene) conferring resistance to Qo inhibitors, and to methods for combating such fungi. The invention also relates to novel compounds, processes for preparing these compounds, to compositions comprising at least one such compound, and to seeds coated with at least one such compound.
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
- Manuel Ellermann ,
- Gaelle Valot ,
- Yolanda Cancho Grande ,
- Jorma HAßFELD ,
- Tom Kinzel ,
- Johannes KÖBBERLING ,
- Kristin BEYER ,
- Susanne RÖHRIG ,
- Michael Sperzel ,
- Jan STAMPFUß ,
- Imke Meyer ,
- Maria KÖLLNBERGER ,
- Nils Burkhardt ,
- Karl-Heinz Schlemmer ,
- Christian Stegmann ,
- Joachim Schuhmacher ,
- Matthias Werner ,
- Jörg HEIERMANN ,
- Willem Jan Hengeveld
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE
- Manuel Ellermann ,
- Gaelle Valot ,
- Yolanda Cancho Grande ,
- Jorma HAßFELD ,
- Tom Kinzel ,
- Johannes KÖBBERLING ,
- Kristin BEYER ,
- Susanne RÖHRIG ,
- Michael Sperzel ,
- Jan STAMPFUß ,
- Imke Meyer ,
- Maria KÖLLNBERGER ,
- Nils Burkhardt ,
- Karl-Heinz Schlemmer ,
- Christian Stegmann ,
- Joachim Schuhmacher ,
- Matthias Werner ,
- Jörg HEIERMANN ,
- Willem Jan Hengeveld
The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.
1,2,4-Oxadiazole Derivatives as Immunomodulators
The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)
##STR00001##
In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.
1,2,4-Oxadiazole Derivatives as Immunomodulators
The present invention relates to pharmaceutical compositions of 1,2,4-oxadiazole compounds or a pharmaceutically acceptable salt thereof of formula (I)
##STR00001##
In the formula Q is O, R.sub.1 is the side chain of Ser, R.sub.2 is —CO-Thr, R.sub.3 is the side chain of Asn or Glu, and R.sub.4, R.sub.5 and R.sub.6 are each H.
CRYSTAL FORMS OF IMMUNOMODULATORS
The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.
CRYSTAL FORMS OF IMMUNOMODULATORS
The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where R.sup.1-R.sup.6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
PREPARATION OF AROMATIC CARBOXYAMIDES BY PALLADIUM-CATALYZED CARBONYLATION REACTION
Preparation of aromatic carboxyamides by palladium-catalyzed carbonylation reaction The present invention relates to a process for the preparation of aromatic carboxyamides of formula I, which can be obtained by palladium-catalyzed carbonylation reaction of aromatic chlorides of formula II, amines of formula III and carbon monoxide in the presence of a base. The invention further relates to a process for the preparation of aryl-5-trifluoromethyl-1,2,4-oxadiazoles, which are known for controlling phytopathogenic fungi.
##STR00001##