Carboxylic acid aromatic amides

Patent metadata

Field	Value
Publication number	US-12023319-B2
Application number	US-202117478192-A
Country	US
Kind code	B2
Filing date	Sep 17, 2021
Priority date	Dec 23, 2016
Publication date	Jul 2, 2024
Grant date	Jul 2, 2024

Abstract

The present invention relates to carboxylic acid aromatic amides compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease as a sole agent or in combination with other active ingredients.

First claim

The invention claimed is:

1. A method for the treatment of a disease, condition, or symptoms thereof, associated with pain or inflammation comprising administering to a subject in need thereof a pharmaceutical composition comprising a compound of formula 2-(1-cyclobutyl-1H-pyrazol-4-yl)-5-[({1-[2-fluoro-4 (trifluoromethyl)phenyl]cyclopropyl}carbonyl)amino] benzoic acid,
or an isomer, enantiomer, diastereomer, racemate, hydrate, solvate, or pharmaceutically acceptable salt thereof, or a mixture thereof;
and a pharmaceutically acceptable carrier.

2. The method according to claim 1 , wherein said disease or disease, condition or symptoms thereof are selected from the group consisting of
visceral pain associated with pancreatitis, interstitial cystitis, bladder pain syndrome, renal colic, or prostatitis, chronic pelvic pain, or pain related to infiltrating endometriosis;
neuropathic pain associated with post herpetic neuralgia, acute zoster pain, pain related to nerve injury, vulvodynia, phantom limb pain, pain related to root avulsions, pain related to radiculopathy, painful traumatic mononeuropathy, painful entrapment neuropathy, pain related to carpal tunnel syndrome, ulnar neuropathy, pain associated with tarsal tunnel syndrome, painful diabetic neuropathy, painful polyneuropathy, trigeminal neuralgia, and pain related to familial amyloid polyneuropathy;
pain associated with stroke, multiple sclerosis, and spinal cord injury;
postsurgical pain syndromes, postmastectomy pain syndrome, postthoracotomy pain syndrome, stump pain, bone and joint pain, osteoarthritis, spine pain, acute and chronic low back pain, neck pain, pain associated with spinal stenosis, shoulder pain, repetitive motion pain, dental pain, pain related to sore throat, cancer pain, burn pain, sun-burn pain, myofascial pain, postoperative and perioperative pain; and
acute and chronic pain, chronic pelvic pain, endometriosis associated pain, primary and secondary dysmenorrhea associated pain, pain associated with uterine fibroids, vulvodynia associated pain, pain associated with angina, and pain associated with osteoarthritis, rheumatoid arthritis, rheumatic disease, tenosynovitis, gout, ankylosing spondylitis, and bursitis.

3. The method according to claim 2 , wherein said disease or disease, condition, or symptoms thereof are selected from the group consisting of
endometriosis, uterine fibroids, pre-eclampsia, hormonal deficiency, spasms of the uterus, and heavy menstrual bleeding;
chronic obstructive pulmonary disease, asthma, atopic or non-atopic allergic asthma, exercise-induced bronchoconstriction, occupational asthma, viral or bacterial exacerbation of asthma, other non-allergic asthmas and wheezy-infant syndrome, chronic obstructive pulmonary disease, emphysema, adult respiratory distress syndrome, bronchitis, pneumonia, cough, lung injury, lung fibrosis, allergic rhinitis vasomotor rhinitis, angioedema, pneumoconiosis, aluminosis, anthracosis, asbestosis, chalicosis, ptilosis, siderosis, silicosis, tabacosis and byssinosis, bowel disease, irritable bowel syndrome, pancreatitis, nephritis, cystitis interstitial cystitis, bladder pain syndrome, kidney fibrosis, kidney failure, hyperactive bladder, and overactive bladder;
pruritus, itch, inflammatory skin disorders, psoriasis, eczema, and atopic dermatitis;
rheumatoid arthritis, gout, osteoporosis, osteoarthritis, and ankylosing spondylitis;
Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis (ALS), epilepsy, dementia, headache, migraine, stroke, closed head trauma, and multiple sclerosis;
HIV infection, and tuberculosis;
cerebral oedema, burns, sunburns, and sprains or fracture;
poisoning, aluminosis, anthracosis, asbestosis, chalicosis, ptilosis, siderosis, silicosis, tabacosis, and byssinosis uveitis;
diabetes type 1, diabetes type 2, diabetic vasculopathy, diabetic neuropathy, diabetic retinopathy, post capillary resistance, diabetic symptoms associated with insulitis, hyperglycaemia, diuresis, proteinuria and increased nitrite and kallikrein urinary excretion, diabetic macular oedema, metabolic syndrome, insulin resistance, obesity, fat or muscle metabolism;
cachexia associated with cancer, AIDS, coeliac disease, chronic obstructive pulmonary disease, multiple sclerosis, rheumatoid arthritis, congestive heart failure, tuberculosis, familial amyloid polyneuropathy, mercury poisoning, and hormonal deficiency;
congestive heart failure, atherosclerosis, congestive heart failure, myocardial infarct, and heart fibrosis; and
primary peritonitis, secondary peritonitis, septic shock, sepsis, muscle atrophy, spasms of the gastrointestinal tract, benign prostatic hyperplasia, and liver disease, non-alcoholic and alcoholic steatohepatitis, liver fibrosis, and liver cirrhosis.

4. The method according to claim 2 wherein said disease or disease syndromes, conditions, or symptoms is endometriosis or endometriosis-associated pain, or pain associated with dysmenorrhea, dyspareunia, dysuria, or dyschezia.

5. The method according to claim 3 wherein said disease, condition, or symptoms thereof are selected from the group consisting of overactive bladder, fibrosis of lung, kidney, heart and/or liver, diabetes type 1 and/or type 2, metabolic syndrome, gout, rheumatoid arthritis, and osteoarthritis.

Assignees

• Bayer Pharma AG

Inventors

• BÄURLE Stefan
• Davenport Adam James
• Stimson Christopher
• Nagel Jens
• Schmidt Nicole
• Rotgeri Andrea
• Gröticke Ina
• Rausch Alexandra
• Klar Juergen
• Dyrks Thomas

Classifications

• C07D495/04

  Ortho-condensed systems · CPC title

• C07D405/04

  directly linked by a ring-member-to-ring-member bond · CPC title

• C07D333/58

  Radicals substituted by nitrogen atoms · CPC title

• C07D333/38

  Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals · CPC title

• C07D333/28

  Halogen atoms · CPC title