# US 9,434,711 B2 · Sulfonamides as TRPM8 modulators

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- Number: US 9,434,711 B2
- Document ID: US9434711B2
- Status: Granted
- Kind: B2
- Application number: 14/322,554
- Filed: 2014-07-02
- Published: 2014-10-23
- Granted: 2016-09-06
- Earliest claimed: 2007-07-18
- Assignees: Janssen Pharmaceutica NV
- Applicants: Janssen Pharmaceutica, NV
- Inventors: Shawn T Branum; Raymond W Colburn; Scott L Dax; Christopher M Flores; Michele C Jetter; Yi Liu; Donald Ludovici; Mark J Macielag; Jay M Matthews; James J McNally; Laura M Andraka; Ronald K Russell; Ning Qin; Christopher Teleha; Kenneth M Wells; Scott C Youells; Mark A Youngman
- Web page: https://patentgrep.com/patent/US9434711B2

## CPC

- C07D 333/66: Nitrogen atoms not forming part of a nitro radical
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/14: Antitussive agents
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/08: of the prostate
- A61P 13/10: of the bladder
- A61P 17/00: Drugs for dermatological disorders
- A61P 19/00: Drugs for skeletal disorders
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 29/02: without antiinflammatory effect
- A61P 31/10: Antimycotics
- C07D 333/36: Nitrogen atoms
- C07D 409/12: linked by a chain containing hetero atoms as chain links
- C07D 409/14: containing three or more hetero rings
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 495/04: Ortho-condensed systems
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

## Claims

### Claim 1

A method of treating inflammatory pain in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound selected from the group consisting of:
N-(3-Methyl-benzo[b]thiophen-2-yl)-N-(4-fluoro-3-trifluoromethyl-benzyl)-4-carboxy-benzenesulfonamide;
N-(3-Methyl-benzo[b]thiophen-2-yl)-N-(4-trifluoromethoxy-benzyl)-4-carboxy-benzenesulfonamide; and
N-(4-Fluoro-3-trifluoromethylbenzyl)-N-(3-(1-hydroxy-1-methyl-ethyl)-benzo[b]thiophen-2-yl)-4-carboxy-benzenesulfonamide.

### Claim 2 (depends on 1)

The method of claim 1 wherein the inflammatory pain is due to inflammatory bowel disease, visceral pain, migraine, post operative pain, osteoarthritis, rheumatoid arthritis, back pain, lower back pain, joint pain, abdominal pain, chest pain, labor, musculoskeletal diseases, skin diseases, toothache, pyresis, burn, sunburn, snake bite, venomous snake bite, spider bite, insect sting, neurogenic bladder, interstitial cystitis, urinary tract infection, rhinitis, contact dermatitis/hypersensitivity, itch, eczema, pharyngitis, mucositis, enteritis, irritable bowel syndrome, cholecystitis, pancreatitis, postmastectomy pain syndrome, menstrual pain, endometriosis, sinus headache, tension headache, or arachnoiditis.