2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors

• US 8,993,573 B2
• Filed: 11/26/2013
• Issued: 03/31/2015
• Est. Priority Date: 08/02/2002
• Status: Expired due to Term

• Current Assignee: A+ Science AB (A+ Science Holding AB)
• Original Assignee: A+ Science AB (A+ Science Holding AB)
• Inventors: Ciufolini, Marco, Wermuth, Camille, Moussy, Alain, Giethlen, Bruno
• Primary Examiner(s): Pagonakis, Anna
• Application Number:
  US14/089,946
• Publication Number:
  US 20140088108A1
• Time in Patent Office: 490 Days
• US Class Current: 514/252.19
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
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• CPC Class Codes: A61P 11/06 Antiasthmatics
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• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/06 Antimigraine agents
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• CPC Class Codes: A61P 25/22 Anxiolytics
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• CPC Class Codes: A61P 25/30 : for treating abuse or dependence
• 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 3/00 : Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 : Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 : Antihyperlipidemics
• CPC Class Codes: A61P 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/00 : Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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• CPC Class Codes: A61P 35/02 : specific for leukemia
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• 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 41/00 : Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
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• CPC Class Codes: A61P 9/12 : Antihypertensives
• CPC Class Codes: C07D 277/42 : Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
• CPC Class Codes: C07D 277/56 : Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• CPC Class Codes: C07D 417/04 : directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 417/14 : containing three or more hetero rings

Abstract

Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.

Claims

1. A pharmaceutical composition comprising a compound of the formula:

2. The pharmaceutical composition of claim 1, which is an oral composition.

3. The pharmaceutical composition of claim 1, which is an aerosol composition.

4. The pharmaceutical composition of claim 1, which is a topical composition.

5. An oral pharmaceutical composition comprising 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-thiazol-2-ylamino)-phenyl]-benzamide:

6. The oral pharmaceutical composition of claim 5, which is in the form of a tablet, a pill, a dragee, a capsule, a liquid, a gel, a syrup, a slurry or a suspension.

7. The oral pharmaceutical composition of claim 6, which is in the form of a tablet.

8. The oral pharmaceutical composition of claim 6, which is in the form of a capsule.

9. The oral pharmaceutical composition of claim 6, which is in the form of a liquid.

10. The oral pharmaceutical composition of claim 6, which is in the form of a suspension.