Roberta L Alexander

US Patent:

20190241610, Aug 8, 2019

Filed:

Nov 26, 2018

Appl. No.:

16/199308

Inventors:

- Stamford CT, US
Frédérique Menzaghi - Rye NY, US
Guangcheng Jiang - San Diego CA, US
Roberta Vezza Alexander - San Diego CA, US
Robert H. Spencer - New Hope PA, US
Derek T. Chalmers - Riverside CT, US
Robert Zhiyong Luo - New City NY, US

Assignee:

CARA THERAPEUTICS, INC. - Stamford CT

International Classification:

C07K 5/107
C07K 7/02
C07K 5/10
A61K 38/07
C07K 5/103

Abstract:

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I:These compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

US Patent:

20190177365, Jun 13, 2019

Filed:

Jul 9, 2018

Appl. No.:

16/029776

Inventors:

- Stamford CT, US
Frédérique Menzaghi - Rye NY, US
Guangcheng Jiang - San Diego CA, US
Roberta Vezza Alexander - San Diego CA, US
Robert H. Spencer - New Hope PA, US
Derek T. Chalmers - Riverside CT, US
Zhiyong Luo - New City NY, US

Assignee:

CARA THERAPEUTICS, INC. - Stamford CT

International Classification:

C07K 5/107
C07K 5/103
C07K 7/06
C07K 5/117

Abstract:

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure:The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

US Patent:

20160376308, Dec 29, 2016

Filed:

May 4, 2016

Appl. No.:

15/145901

Inventors:

- Shelton CT, US
Frédérique Menzaghi - Rye NY, US
Guangcheng Jiang - San Diego CA, US
Roberta Vezza Alexander - San Diego CA, US
Robert H. Spencer - New Hope PA, US
Derek T. Chalmers - Riverside CT, US
Zhiyong Luo - New City NY, US

Assignee:

CARA THERAPEUTICS, INC. - SHELTON CT

International Classification:

C07K 5/107
C07K 7/06

Abstract:

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure:The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

US Patent:

20160362450, Dec 15, 2016

Filed:

Jun 1, 2016

Appl. No.:

15/170201

Inventors:

- Stamford CT, US
Frédérique Menzaghi - Rye NY, US
Guangcheng Jiang - San Diego CA, US
Roberta Vezza Alexander - San Diego CA, US
Robert H. Spencer - New Hope PA, US
Derek T. Chalmers - Riverside CT, US
Robert Zhiyong Luo - New City NY, US

Assignee:

Cara Therapeutics, Inc. - Stamford CT

International Classification:

C07K 5/107

Abstract:

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I:Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

US Patent:

20160310558, Oct 27, 2016

Filed:

Apr 25, 2016

Appl. No.:

15/137033

Inventors:

- Shelton CT, US
Frédérique MENZAGHI - Rye NY, US
Guangcheng JIANG - San Diego CA, US
Roberta Vezza ALEXANDER - San Diego CA, US
Robert H. SPENCER - New Hope PA, US
Derek T. CHALMERS - Riverside CT, US
Robert Zhiyong LUO - New City NY, US

Assignee:

Cara Therapeutics, Inc. - Shelton CT

International Classification:

A61K 38/07
A61K 38/08

Abstract:

The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-1β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.

US Patent:

20150152138, Jun 4, 2015

Filed:

Dec 2, 2014

Appl. No.:

14/557576

Inventors:

- Shelton CT, US
Frédérique MENZAGHI - Rye NY, US
Guangcheng JIANG - San Diego CA, US
Roberta Vezza ALEXANDER - San Diego CA, US
Robert H. SPENCER - New Hope PA, US
Derek T. CHALMERS - Riverside CT, US
Robert Zhiyong LUO - New City NY, US

Assignee:

CARA THERAPEUTICS, INC. - Shelton CT

International Classification:

C07K 5/11

Abstract:

The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-1β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.