Patent classifications
C07D231/00
PYRAZOLE DERIVATIVES AS INHIBITORS OF STAT3
Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.
Pyrazolo[3,4-c]pyridine compounds and methods of use
Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R.sup.1 and R.sup.2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. ##STR00001##
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.
Filtration process for purifying liquid azole heteroaromatic compound-containing mixtures
A process for removing impurities from a liquid azole heteroaromatic compound-containing (e.g., triazole-containing) mixture by: (a) providing a liquid azole heteroaromatic compound-containing mixture having impurities; and (b) passing the azole heteroaromatic compound-containing mixture through at least one filtration membrane which is a nanofiltration membrane and/or ultrafiltration membrane having a molecular pore size in the range of from about 200 daltons to about 1 kilodaltons to provide a permeate that is an at least partially purified azole heteroaromatic compound-containing mixture and a retentate with at least some impurities.
N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
Compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Ring A, Ring C and X are as defined herein, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis or pelvic pain syndrome. ##STR00001##
Pyrazole derivatives as inhibitors of STAT3
Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.
Non-systemic TGR5 agonists
The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. ##STR00001##
Compounds for controlling arthropods
The invention relates inter alia to compounds of the general formula (I) ##STR00001##
in which the A.sub.1-A.sub.4, T, n, W, Q, R.sup.1 and B.sub.1-B.sub.4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
Compounds for controlling arthropods
The invention relates inter alia to compounds of the general formula (I) ##STR00001##
in which the A.sub.1-A.sub.4, T, n, W, Q, R.sup.1 and B.sub.1-B.sub.4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.