Patent classifications
A61K31/499
Compounds and compositions for the treatment of parasitic diseases
The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; ##STR00001## a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
Compounds and compositions for the treatment of parasitic diseases
The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; ##STR00001## a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
INHIBITORS OF CBL-B AND METHODS OF USE THEREOF
- Paul A. BARSANTI ,
- Neil F. BENCE ,
- Jennifa GOSLING ,
- Anjanabha SAHA ,
- Asad M TAHERBHOY ,
- Christoph W. ZAPF ,
- Kathleen BOYLE ,
- Mario CARDOZO ,
- Jeffrey MIHALIC ,
- Morgan LAWRENZ ,
- Mark GALLOP ,
- Jilliane BRUFFEY ,
- Thomas CUMMINS ,
- Daniel ROBBINS ,
- Hiroko TANAKA ,
- Chenbo WANG ,
- Frederick Cohen ,
- Wylie PALMER ,
- Arthur T. SANDS ,
- Hunter SHUNATONA
Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo.
COMBINATION ANTI-CANCER THERAPIES WITH INDUCERS OF IRON-DEPENDENT CELLULAR DISASSEMBLY
The invention provides methods of treating a cancer in a subject, comprising administering to the subject a combination of (a) an anti-neoplastic agent and (b) an agent that induces iron-dependent cellular disassembly, thereby treating the cancer in the subject. In some embodiments, the cancer is resistant to the anti-neoplastic agent.
COMBINATION ANTI-CANCER THERAPIES WITH INDUCERS OF IRON-DEPENDENT CELLULAR DISASSEMBLY
The invention provides methods of treating a cancer in a subject, comprising administering to the subject a combination of (a) an anti-neoplastic agent and (b) an agent that induces iron-dependent cellular disassembly, thereby treating the cancer in the subject. In some embodiments, the cancer is resistant to the anti-neoplastic agent.
ADMINISTRATION OF CALCIUM CHANNEL TRPC6 INHIBITORS USING BALLOONS, STENTS OR OTHER MEDICAL DEVICES
The present invention relates to a medical device suitable for being inserted into the lumen of an anatomic structure of a subject, said medical device comprising means for administration of TRPC6 inhibitor, wherein said means comprises the TRPC6 inhibitor. The present invention further concerns a method of manufacturing a medical device suitable for being inserted into the lumen of an anatomic structure of a subject. Also, the invention relates to a TRPC6 inhibitor for use in the treatment or prevention of a disease associated with neointimal hyperplasia associated with the migration of smooth muscular cells. The invention also relates to a method of treating or preventing a disease associated with neointimal hyperplasia, said method comprising administering a TRPC6 inhibitor to a subject in need thereof. Also envisaged is a method of inhibiting migration of smooth muscle cells. The invention additionally relates to an in vitro test kit comprising: (a) small muscle cells (SMCs); (b) a surface suitable for SMC cultivation coated with a TRPC6 inhibitor. Also concerned is a pharmaceutical composition comprising a TRPC6 inhibitor and a pharmaceutically acceptable carrier.
ADMINISTRATION OF CALCIUM CHANNEL TRPC6 INHIBITORS USING BALLOONS, STENTS OR OTHER MEDICAL DEVICES
The present invention relates to a medical device suitable for being inserted into the lumen of an anatomic structure of a subject, said medical device comprising means for administration of TRPC6 inhibitor, wherein said means comprises the TRPC6 inhibitor. The present invention further concerns a method of manufacturing a medical device suitable for being inserted into the lumen of an anatomic structure of a subject. Also, the invention relates to a TRPC6 inhibitor for use in the treatment or prevention of a disease associated with neointimal hyperplasia associated with the migration of smooth muscular cells. The invention also relates to a method of treating or preventing a disease associated with neointimal hyperplasia, said method comprising administering a TRPC6 inhibitor to a subject in need thereof. Also envisaged is a method of inhibiting migration of smooth muscle cells. The invention additionally relates to an in vitro test kit comprising: (a) small muscle cells (SMCs); (b) a surface suitable for SMC cultivation coated with a TRPC6 inhibitor. Also concerned is a pharmaceutical composition comprising a TRPC6 inhibitor and a pharmaceutically acceptable carrier.
ADVANTAGEOUS THERAPIES FOR DISORDERS MEDIATED BY IKAROS OR AIOLOS
New treatments for Ikaros and/or Aiolos mediated disorders are provided that comprise administering an effective amount of a cereblon binder that degrades Ikaros or Aiolos by the ubiquitin proteasome pathway.
Aromatic heterocyclic compound, and pharmaceutical composition and use thereof
Provided are novel heteroaromatic compound as an Autotaxin inhibitor, a pharmaceutical composition comprising the compound, and a use thereof in a treatment of a disease with a pathological feature of Autotaxin overexpression in a mammal, wherein the compound is according to formula (I), or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, tautomer, nitrogen oxide, metabolite, prodrug, or mixture thereof; wherein each of R.sup.1, Ar.sup.1, Ar.sup.2, Ar.sup.3, W, Y, Z, and Cy is defined in the present disclosure.