New use of neferine

• US 20120108629A1
• Filed: 04/13/2010
• Published: 05/03/2012
• Est. Priority Date: 04/14/2009
• Status: Abandoned Application

• Current Assignee: Institute of Chinese Materia Medica China Academy
• Original Assignee: Institute of Chinese Materia Medica China Academy
• Inventors: Jiang, Tingliang, Sui, Feng, Huo, Hairu, Li, Lanfang, Guo, Shuying
• Application Number:
  US13/264,375
• Publication Number:
  US 20120108629A1
• Time in Patent Office: Days
• US Class Current: 514/308
• CPC Class Codes: A61K 31/4709 Non-condensed quinolines and containing further heterocyclic rings
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• 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 1/18 for pancreatic disorders, e.g. pancreatic enzymes
• 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 11/04 for throat disorders
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/14 Antitussive agents
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis
• 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 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• 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 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 35/04 : specific for metastasis
• CPC Class Codes: A61P 37/08 : Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

The present invention reveals a new use of neferine. Neferine regulates M8 and V1 subtype of transient receptor potential ion channel (TRPM8 and TRPV1), respectively, in mammalians, including humans, and can be used for preparing medicaments for treating disease related to said ion channel (such as hyperalgesia, Parkinson'"'"'s disease, painful bladder syndrome, chronic obstructive pulmonary disease, and tumor of skin, prostate, mammary gland, lung, colon, etc). The potency of neferine in the present invention is higher than that of hexahydrothymol.

Claims

1. ) Use of neferine in the preparation of medicaments of compounds for the up-regulation of TRPM8 in mammalians, wherein the medicaments do not comprise antitumor drugs.

2. ) The use claimed in claim 1 comprising the use in the preparation of medicaments for the prevention and/or treatment of chronic obstructive lung disease, Parkinson'"'"'s disease, painful bladder syndrome, hypersensitivity to cold.

10. ) The use claimed in claim 1, wherein the compounds are further combined with pharmaceutically acceptable carriers.

11. ) The use claimed in claim 10, wherein the carriers include diluents, adhesives, absorbents, disintegrants, dispersants, wetting agents, auxiliary solvent, buffers and surfactants.

12. ) The use claimed in claim 2, wherein the compounds are further combined with pharmaceutically acceptable carriers.

13. ) The use claimed in claim 12, wherein the carriers include diluents, adhesives, absorbents, disintegrants, dispersants, wetting agents, auxiliary solvent, buffers and surfactants.

18. ) The use claimed in claim 1, wherein the mammalian is human.

19. ) The use claimed in claim 2, wherein the mammalian is human.

22. ) The use claimed in claim 1, wherein the neferine was prepared in powder, liquid and gas dosage form.

23. ) The use claimed in claim 22, wherein the dosage form include intestinal tract, oral, intramuscular, subcutaneous, nasal cavity, oral mucosa, skin, rectum and peritoneal administration dosage form.

24. ) The use claimed in claim 2, wherein the neferine was prepared in powder, liquid and gas dosage form.

25. ) The use claimed in claim 24, wherein the dosage form include intestinal tract, oral, intramuscular, subcutaneous, nasal cavity, oral mucosa, skin, rectum and peritoneal administration dosage form.

3. ) Use of neferine for the preparation of medicaments of compounds for the down-regulation of TRPV1 in mammalians, wherein the medicaments do not comprise antitumor drugs.

4. ) The use claimed in claim 3 comprising the use in the preparation of medicaments for the prevention and/or treatment of hyperalgesia to heat, allodynia, migraine, tooth pain, vulvodynia, painful gastrointestinal disease, esophagitis, gastro-esophageal reflux, functional bowel disorders, ulcerative colitis, pancreatitis, cystitis, hyper-reactivity of bladder, osteoarthritis, cough, chronic obstructive lung disease, asthma, allergic rhinitis, non-insulin-dependent diabetes, myasthenia syndrome, schizophrenia.

14. ) The use claimed in claim 3, wherein the compounds are further combined with pharmaceutically acceptable carriers.

15. ) The use claimed in claim 14, wherein the carriers include diluents, adhesives, absorbents, disintegrants, dispersants, wetting agents, auxiliary solvent, buffers and surfactants.

16. ) The use claimed in claim 4, wherein the compounds are further combined with pharmaceutically acceptable carriers.

17. ) The use claimed in claim 16, wherein the carriers include diluents, adhesives, absorbents, disintegrants, dispersants, wetting agents, auxiliary solvent, buffers and surfactants.

20. ) The use claimed in claim 3, wherein the mammalian is human.

21. ) The use claimed in claim 4, wherein the mammalian is human.

26. ) The use claimed in claim 3, wherein the neferine was prepared in powder, liquid and gas dosage form.

27. ) The use claimed in claim 26, wherein the dosage form include intestinal tract, oral, intramuscular, subcutaneous, nasal cavity, oral mucosa, skin, rectum and peritoneal administration dosage form.

28. ) The use claimed in claim 4, wherein the neferine was prepared in powder, liquid and gas dosage form.

29. ) The use claimed in claim 28, wherein the dosage form include intestinal tract, oral, intramuscular, subcutaneous, nasal cavity, oral mucosa, skin, rectum and peritoneal administration dosage form.

5. ) (canceled)

6. ) (canceled)

7. ) (canceled)

8. ) (canceled)

9. ) (canceled)