NETUPITANT

New Drug Approvals

NETUPITANT

  • Ro 67-3189/000
  • UNII-7732P08TIR
  • Ro-67-3189
  • Netupitant, an NK-1 antagonist is under development for the treatment of overactive bladder. HELSINN GROUP

CAS:  290297-26-6

290296-54-7 (di HCl)

U.S. Pat. Nos. 6,303,790, 6,531,597, 6,297,375 and 6,479,4836,719,996 and 6,593,472  to Hoffmann La Roche(originator).

IUPAC/Chemical name: 

2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide

Chemical Formula: C30H32F6N4O
Exact Mass: 578.24803
Molecular Weight: 578.59
Elemental Analysis: C, 62.28; H, 5.57; F, 19.70; N, 9.68; O, 2.77

Netupitant is another selective NKi receptor antagonist under development by Helsinn Healthcare, having the formula 2-[3,5-bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2- methylphenyl)-6-(4-methylpiperazin- l-yl)pyridin-3-yl]propanamide, or Benzeneacetamide, N,a,a-trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-l-piperazinyl)-3-pyridinyl]-3,5- bis(trifluoromethyl)-, and the below chemical structure:

Figure imgf000004_0001

Netupitant is a tachykinin NK-1 antagonist which had been in phase III clinical trials at Helsinn for the prophylaxis of chemotherapy-induced nausea and vomiting and in phase II clinical studies for the treatment of overactive bladder. However, no recent development has been reported for this research.

NK-1 receptor antagonists work by blocking the action of neurokinin-1 (Substance…

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AZASETRON..a selective 5-HT3 receptor antagonist

New Drug Approvals

AZASETRON,  NAZASETRON

N-(1-azabicyclo[2.2.2]octan-8-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide

6-chloro-3,4-dihydro-4-methyl-3-oxo-N-(3-quinuclidinyl)-2H-1,4-benzoxazine-8-carboxamide

123039-99-6 , 123040-69-7 (free base)

141922-90-9 HYD SALT

Y-25130 (hydrochloride)LAUNCHED 1994 AS HCL SALT FORM SEROTONE

a selective 5-HT3 receptor antagonist , ANTIEMETIC

  • UNII-77HC7URR9Z

Mitsubishi Tanabe Pharma, JAPAN TOBACCO (Originator)

FOR..Nausea and Vomiting, Treatment of
Prokinetic Agents

Azasetron is an antiemetic which acts as a 5-HT3 receptorantagonist.

Chemical and Pharmaceutical Bulletin, 1992 ,  vol. 40,  3  p. 624 – 630, ENTRY 15 , MP 305 OF HCL SALT

Biological and Pharmaceutical Bulletin, 2006 ,  vol. 29,  9  p. 1931 – 1935, AS MERCK 903

US 4892872…

CN 101786963…

WO 1996001630..

WO 2006006595..

WO 2007134077..

CN 102526740,  CN 102451166, US 4892872, JP 2008297277

US5773436 A1, WO2006/119295 A2, EP1336602 A1, US4892872 A1,

US2003/18008 A1, US2002/147197 A1, US4892872

AZASETRON

 

The nitration of 5-chloro-2-hydroxybenzoic acid methyl ester (I) with nitric acid in sulfuric acid gives 5-chloro-2-hydroxy-3-nitrobenzoic acid methyl ester (II), which is reduced with Fe and NH4Cl in water yielding 3-amino-5-chloro-2-hydroxybenzoic acid methyl ester (III)…

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TEDIGLUTIDE ..Glucagon-like peptide 2 (GLP-2) analog; protects small intestinal stem cells from radiation damage.

New Drug Approvals

File:Teduglutide.png

TEDUGLUTIDE
Glucagon-like peptide 2 (GLP-2) analog; protects small intestinal stem cells from radiation damage.

Gattex (teduglutide) is a recombinant analog of human glucagon-like peptide 2 for the treatment of adults with short bowel syndrome.

  • (Gly2)GLP-2
  • ALX 0600
  • ALX-0600
  • Gattex
  • Gly(2)-GLP-2
  • Teduglutide
  • UNII-7M19191IKG

[Gly2]hGLP-2, [Gly2]-hGLP-2, ALX-0600,

Gattex, Revestive

CAS number 197922-42-2

L-histidylglycyl-L-α-aspartylglycyl-L-seryl-L-phenylalanyl-L-seryl-L-α-aspartyl-L-α-glutamyl-L-methionyl-L-asparaginyl-L-threonyl-L-isoleucyl-L-leucyl-L-α-aspartyl-L-asparaginyl-L-leucyl-L-alanyl-L-alanyl-L-arginyl-L-α-aspartyl-L-phenylalanyl-L-isoleucyl-L-asparaginyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-glutaminyl-L-threonyl-L-lysyl-L-isoleucyl-L-threonyl-L-aspartic acid

Formula C164H252N44O55S 
Mol. mass 3752.082 g/mol

Gattex, ALX-0600, (Gly2)GLP-2, Gly(2)-GLP-2, ALX 0600, [Gly2]GLP-2, Glucagon-like peptide II (2-glycine) (human), UNII-7M19191IKG

LAUNCHED 2013, NPS Pharmaceuticals

APPROVAL FDA

Company: NPS Pharmaceuticals, Inc.
Date of Approval: December 21, 2012 FDA

NDA 203441

POWDER; SUBCUTANEOUS GATTEX

U-1320=TREATMENT OF ADULT PATIENTS WITH SHORT BOWEL SYNDROME WHO ARE DEPENDENT ON PARENTERAL SUPPORT

Patent No Patent Expiry Date Patent use code
5789379 Apr 14, 2015 U-1320
7056886 Sep 18, 2022 U-1320
7847061 Nov 1, 2025 U-1320
Exclusivity Code Exclusivity_Date
ORPHAN DRUG EXCLUSIVITY Dec 21, 2019
NEW CHEMICAL ENTITY

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APREMILAST, … ORALLY ACTIVE PDE4 INHIBITOR

New Drug Approvals

APREMILAST

PDE4 inhibitor

N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide

(+)-2-[l-(3-ethoxy-4-methoxyphenyl)-2- methanesulfonylethyl]-4-acetylaminoisoindolin-l,3-dione,

(S)—N-{2-[1-(3-ethoxy-4-methoxy-phenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
(S)-N-{2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide
Molecular Formula: C22H24N2O7S   Molecular Weight: 460.50016

608141-41-9 CAS NO

Celgene (Originator)
CC-10004 (apremilast) is an oral compound that is being studied in multiple Phase III clinical trials for the treatment of psoriasis, psoriatic arthritis and other chronic inflammatory diseases. We successfully completed our early stage studies, demonstrating clinical activity and tolerability and meeting safety endpoints in a placebo controlled proof-of mechanism trial in moderate-to-severe psoriasis and psoriatic arthritis. With the initiation of six multi-center international clinical trials, we are advancing the clinical development of CC-10004.

Celgene's apremilast could be game-changer in PsA

CC-10004, , Apremilast (USAN), SureCN302992, Apremilast (CC-10004), QCR-202,

Apremilast is an orally available small molecule inhibitor of PDE4 being developed byCelgene for ankylosing spondylitispsoriasis, and 

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DANOPREVIR (ITMN-191) …..a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV)

New Drug Approvals

Danoprevir (ITMN-191) Chemical Structure

Danoprevir

Danoprevir(ITMN-191) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A. Phase 2.

Array BioPharma (Originator)

RG7227
ITMN-191
RO5190591

2H-Isoindole-2-carboxylic acid, 4-fluoro-1,3-dihydro-, (2R,6S,12Z,13aS,14aR,16aS)-
14a-[[(cyclopropylsulfonyl)amino]carbonyl]-6-[[(1,1-dimethylethoxy)carbonyl]amino]-
1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydro-5,16-
dioxocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-2-yl ester

2. (2R,6S,12Z,13aS,14aR,16aS)-14a-[(cyclopropylsulfonyl)carbamoyl]-6-{[(1,1-
dimethylethoxy)carbonyl]amino}-5,16-dioxo-
1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-
a][1,4]diazacyclopentadecin-2-yl 4-fluoro-1,3-dihydro-2H-isoindole-2-carboxylate
Treatment of hepatitis C

MOLECULAR FORMULA C35H46FN5O9S

MOLECULAR WEIGHT 731.8

MANUFACTURER Genentech

CODE DESIGNATION R05190591

CAS REGISTRY NUMBER 850876-88-9, 916881-67-9

Danoprevir(ITMN-191) is a peptidomimetic

ITMN-191 (R-7227), a macrocyclic protease inhibitor, is in phase II clinical evaluation for the treatment of chronic hepatitis C virus (HCV) infection as monotherapy and in combination with Pegasys(R) (pegylated interferon alpha-2a) and Copegus(R) (ribavirin). The product candidate is also being evaluated in combination with R-7128 in treatment-naive patients infected with HCV genotype 1.

Danoprevir (ITMN-191; RG-7227), under development by InterMune Inc and Roche Holding AG, is a promising, potent NS3/4A protease inhibitor for…

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TELMISARTAN ..Actavis’ Generic Version of Micardis Receives FDA Approval

New Drug Approvals

DUBLIN, Jan. 8, 2014 /PRNewswire/ — Actavis plc today announced that it has received approval from the U.S. Food and Drug Administration (FDA) on its Abbreviated New Drug Application (ANDA) for Telmisartan Immediate-Release Tablets, 20 mg, 40 mg and 80 mg, a generic equivalent to Boehringer Ingelheim’s Micardis. Actavis intends to launch the product immediately.

http://www.drugs.com/news/actavis-version-micardis-receives-fda-approval-49915.html?utm_source=ddc&utm_medium=email&utm_campaign=Today%27s+news+summary+-+January+8%2C+2014

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