Imidazoquinolines as lipid kinase inhibitors

• US 20120207751A1
• Filed: 04/23/2012
• Published: 08/16/2012
• Est. Priority Date: 05/20/2005
• Status: Abandoned Application

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: Garcia-Echeverria, Carlos, Stauffer, Frédéric, Furet, Pascal
• Application Number:
  US13/453,225
• Publication Number:
  US 20120207751A1
• Time in Patent Office: Days
• US Class Current: 424/133.1
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/16 Central respiratory analeptics
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 13/12 of the kidneys
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease
• CPC Class Codes: A61P 21/04 for myasthenia gravis
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/02 specific for leukemia
• CPC Class Codes: A61P 37/02 Immunomodulators
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 37/08 : Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/06 : Antianaemics
• CPC Class Codes: C07D 471/04 : Ortho-condensed systems

Abstract

The invention relates to a combination comprising compounds of formula (I)

and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.

Claims

1. A combination comprising (a) a compound according to Formula (I)

2. A combination according to claim 1, wherein the compound of formula I is

2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile or a tautomer thereof or a pharmaceutically acceptable salt thereof.

3. A combination according to claim 1, wherein the compound of formula I is

8-(6-Methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one or a tautomer thereof or a pharmaceutically acceptable salt thereof.

4. A combination according to claim 1, wherein the one or more antiproliferative compound is selected from the group consisting of aromatase inhibitors, antiestrogens, topoisomerase I inhibitors, topoisomerase II inhibitors, microtubule active compounds, alkylating compounds, histone deacetylase inhibitors, compounds which induce cell differentiation processes, cyclooxygenase inhibitors, MMP inhibitors, mTOR inhibitors, antineoplastic antimetabolites, platin compounds, compounds targeting/decreasing a protein or lipid kinase activity and further anti-angiogenic compounds, compounds which target, decrease or inhibit the activity of a protein or lipid phosphatase, gonadorelin agonists, anti-androgens, methionine aminopeptidase inhibitors, bisphosphonates, biological response modifiers, antiproliferative antibodies, heparanase inhibitors, inhibitors of Ras oncogenic isoforms, telomerase inhibitors, proteasome inhibitors, compounds used in the treatment of hematologic malignancies, compounds which target, decrease or inhibit the activity of Flt-3, Hsp90 inhibitors, kinesin spindle protein inhibitors and MEK inhibitors, or a combination thereof.

5. A combination according to claim 1, wherein the one or more antiproliferative compound is selected from the group consisting of exemestane, ketokonazole, anastrozole, letrozole, tamoxifen, fulvestrant, gimatecan, irinotecan, doxorubicin, paclitaxel, docetaxel, vincristine, epothilones and derivatives thereof, N-hydroxy-3-[4-[[2-hydroxyethyl)[2-(1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide, N-hydroxy-3-[4][[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide, 5-fluorouracil, capecitabine, gemcitabine, pemetrexed, carboplatin, cis-platin, cisplatinum, oxaliplatin, ARRY142886, AZ6244, imatinib, nilotinib, trastuzumab, cetuximab, Iressa, Tarceva, rapamycin, everolimus, Bortezomid, PKC412, bevacizumab, rituximab, PKC412, octreotide, SOM230, and FTY720, or a combination thereof.

6. A combination according to claim 1, wherein the compound of formula I is administered in combination with hormones or radiation.

7. A combination according to claim 1 for use in the treatment of one or more tumors.

8. A pharmaceutical preparation comprising the combination according to claim 1 and, optionally, a pharmaceutically acceptable carrier.

9. A method for the treatment of a tumor comprising the administration to a subject in need thereof a therapeutically effective amount of a compound of formula (I)

10. A combination comprising (a) 2-Methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile or a tautomer thereof or a pharmaceutically acceptable salt thereof and (b) one or more antiproliferative compounds selected from the group consisting of exemestane, letrozole, fulvestrant, irinotecan, doxorubicin, paclitaxel, docetaxel, capecitabine, carboplatin, cis-platin, cisplatinum, imatinib, nilotinib, trastuzumab, cetuximab, everolimus, bevacizumab, and SOM230, or a combination thereof.

11. A combination according to claim 10 for use in the treatment of one or more tumors.