# US 8,569,344 B2 · N-piperidinyl acetamide derivatives as calcium channel blockers

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- Number: US 8,569,344 B2
- Document ID: US8569344B2
- Status: Granted
- Kind: B2
- Application number: 13/601,357
- Filed: 2012-08-31
- Published: 2013-03-14
- Granted: 2013-10-29
- Earliest claimed: 2008-06-02
- Assignees: Zalicus Pharmaceuticals Ltd.
- Applicants: Hassan Pajouhesh; Ramesh Kaul; Yanbing Ding; Yongbao Zhu; Lingyun Zhang; Nagasree Chakka; Mike Grimwood; Jason Tan; Yuanxi Zhou
- Inventors: Hassan Pajouhesh; Ramesh Kaul; Yanbing Ding; Yongbao Zhu; Lingyun Zhang; Nagasree Chakka; Mike Grimwood; Jason Tan; Yuanxi Zhou
- Web page: https://patentgrep.com/patent/US8569344B2

## CPC

- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/4525: containing a five-membered ring with oxygen as a ring hetero atom
- A61K 31/453: containing a six-membered ring with oxygen as a ring hetero atom
- A61K 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 13/10: of the bladder
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/16: Masculine contraceptives
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/30: for treating abuse or dependence
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 211/26: with hydrocarbon radicals, substituted by nitrogen atoms
- C07D 211/28: to which a second hetero atom is attached
- C07D 211/38: Halogen atoms or nitro radicals
- C07D 211/46: having a hydrogen atom as the second substituent in position 4
- C07D 211/62: attached in position 4
- C07D 211/66: having a hetero atom as the second substituent in position 4
- C07D 401/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 405/06: linked by a carbon chain containing only aliphatic carbon atoms
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

## Claims

### Claim 1

A method to treat a condition selected from chronic and acute pain, said method comprising administering to a subject in need of such treatment an amount of a pharmaceutical composition effective to ameliorate said condition, wherein said pharmaceutical composition comprises a compound having the structure,
or a pharmaceutically acceptable salt or conjugate thereof, in admixture with a pharmaceutically acceptable excipient.

### Claim 2 (depends on 1)

The method of claim 1, wherein said condition is chronic pain.

### Claim 3 (depends on 2)

The method of claim 2, wherein said chronic pain is peripheral neuropathic pain, central neuropathic, musculoskeletal pain, inflammatory pain, headache, visceral pain, or mixed pain.

### Claim 4 (depends on 3)

The method of claim 3, wherein said chronic pain is visceral pain.

### Claim 5 (depends on 1)

The method of claim 1, wherein said condition is acute pain.