PF 04995274, a 5-HT4Partial Agonist

New Drug Approvals

PF-04995274,

(R)-4-((4-(((4-(Tetrahydrofuran-3-yloxy)-1,2-benzisoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol

4-(4-{4-[(R)-(Tetrahydro-furan-3-yl)oxy]-benzo[d]isoxazol-3-yloxymethyl}-piperidin-1-ylmethyl)-tetrahydro-pyran-4-ol

CAS  1331782-27-4
UNII: XI179PG9LV

MF C23-H32-N2-O6

MW 432.5138

a 5-HT4Partial Agonist

PHASE 1 Alzheimer’s type dementia.

Pfizer Inc. INNOVATOR

5-HT4 agonists have attracted attention for therapeutic value in the treatment of Alzheimer’s Disease (AD) and cognitive impairment.Acting to increase levels of acetylcholine and soluble APP alpha, 5-HT4 agonists have the potential to demonstrate both ameliorative and disease modifying effects

(R)-4-((4-((4-(tetrahydrofuran-3-yloxy)benzo[d]isoxazol-3-yloxy)methyl)piperidin-1-yl)methyl)tetrahydro-2/-/-pyran-4-ol and pharmaceutically acceptable salts thereof. This invention also is directed, in part, to a method for treating a 5-HT4 mediated disorder in a mammal. Such disorders include acute neurological and psychiatric disorders, stroke, cerebral ischemia, spinal cord trauma, head trauma, perinatal hypoxia, cardiac arrest, hypoglycemic neuronal damage, dementia, Alzheimer’s disease, Huntington’s Chorea, amyotrophic lateral sclerosis, ocular damage, retinopathy, cognitive disorders, idiopathic and drug- induced Parkinson’s disease, muscular spasms and disorders associated with muscular spasticity including tremors, depression, epilepsy, convulsions, migraine, urinary incontinence, substance tolerance, substance…

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WO 2016012938, New patent, LINACLOTIDE, DR. REDDY’S LABORATORIES LIMITED,

New Drug Approvals

Linaclotide structure.svgWO2016012938,  IMPROVED PROCESS FOR PREPARATION OF AMORPHOUS LINACLOTIDE

DR. REDDY’S LABORATORIES LIMITED [IN/IN]; 8-2-337, Road No 3, Banjara Hills, Telangana, INDIA Hyderabad 500034 (IN)

KALITA, Dipak; (IN).
NIVRUTTI, Ramrao Jogdand; (IN).
BALAKUMARAN, Kesavan; (IN).
DESHMUKH, Shivshankar; (IN).
VUTUKURU, Naga Chandra Sekhar; (IN).
KASINA, Vara Prasad; (IN).
NALAMOTHU, Sivannarayana; (IN).
VILVA, Mohan Sundaram; (IN).
KHAN, Rashid Abdul Rehman; (IN).
TIRUMALAREDDY, Ramreddy; (IN).
MUSTOORI, Sairam; (IN)

The present application relates to an improved process for the formation of disulfide bonds in linaclotide. The present application also relates to an improved process for the purification of linaclotide.

The present application relates to an improved process for the preparation of amorphous linaclotide. Specifically, the present application relates to an improved process for the formation of disulfide bonds in linaclotide. The present application further relates to a purification process for the preparation of…

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