Mom will teach you NMR

New Drug Approvals

Dedicated to all moms in the world
C=O group is dad
O atom is mom
Carbonyl is dad and oxygen mom hence c labelled methyl has higher chemical shift  and gets a little more attention
SEE BELOW
NMR IS EASY
A chemical has Formula: C5H10O2
C5H10O2
Rule 2, omit O, gives C5H10
5 – 10/2 + 1 = 1 degree of unsaturation.
Look for 1 pi bond or aliphatic ring.
IR
IR spectrum
The band at 1740 indicates a carbonyl, probably a saturated aliphatic ester. The bands at 3000-2850 indicate C-H alkane stretches. The bands in the region 1320-1000 could be due to C-O stretch, consistent with an ester.
NMR spectrum
Structure answerThis is the structure. See if you can assign the peaks on your…

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TIDEGLUSIB ..An NSAID and neuroprotective agent.

New Drug Approvals


Tideglusib

M.Wt: 334.39
Formula: C19H14N2O2S
CAS No.: 865854-05-3
4-Benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione

Glycogen Synthase Kinase 3 beta (GSK-3beta; tau Protein Kinase I) Inhibitors

Treatment of Neurologic Drugs (Miscellaneous)
Alzheimer’s Dementia, Treatment ofCerebrovascular Diseases, NP031112; NP-031112, Nypta  Zentylor

  • NP 031112
  • NP-12
  • NP031112
  • Tideglusib
  • UNII-Q747Y6TT42

Noscira (Originator)
Tideglusib (NP-12NP031112) is a potent, selective and irreversible[1] small molecule non-ATP-competitive GSK3 inhibitor that has been investigated as a potential treatment for Alzheimer’s disease and paralysis supranuclear palsy in Phase IIa[2] and IIb clinical trials.[3][4][5][6] The first clinical trial conducted with tideglusib to be published (in English, at least) was phase II and demonstrated that overall tideglusib was well tolerated, except for some moderate, asymptomatic, fully reversible increases in liver enzymes (≥2.5xULN; where ULN=Upper Limit of Normal).[4]

tideglusib

NP-031112 is an inhibitor of glycogen synthase kinase-3 beta (GSK-3beta) in early clinical development for the oral…

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MIDAZOLAM …A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties

New Drug Approvals

MIDAZOLAM

8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine

59467-70-8 CAS NO OF FREE BASE

59467-94-6 MALEATE, Launched – 1982, Roche (Originator)

59467-96-8 (HCl)

A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.

Midazolam (/mɪˈdæzəlæm/, marketed in English-speaking countries and Mexico under the trade names DormicumHypnovel, andVersed,) is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potentanxiolyticamnestichypnotic

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TEGOBUVIR ..IN PHASE II FOR HEPATITIS C

New Drug Approvals

TEGOBUVIR

A non-structural protein 5B polymerase inhibitor
for Treatment of chronic hepatitis C

5-[6-[2,4-Bis(trifluoromethyl)phenyl]pyridazin-3-ylmethyl]-2-(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine

CHEMICAL NAMES

1. 5H-Imidazo[4,5-c]pyridine, 5-[[6-[2,4-bis(trifluoromethyl)phenyl]-3-pyridazinyl]methyl]-
2-(2-fluorophenyl)-

2. 5-({6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl}methyl)-2-(2-fluorophenyl)-5H-
imidazo[4,5-c]pyridine

MOLECULAR FORMULA C25H14F7N5

MOLECULAR WEIGHT 517.4

MANUFACTURER Gilead Sciences, Inc.

CODE DESIGNATION

  • GS 333126
  • GS 9190
  • GS-333126
  • GS-9190
  • Tegobuvir
  • UNII-5NOK5X389M

CAS REGISTRY NUMBER 1000787-75-6

GS-9190, an RNA-directed RNA polymerase (NS5B) inhibitor, is in phase II clinical evaluation at Gilead for the treatment of hepatitis C virus (HCV) infection. A clinical trial with GS-9190 in combination with peginterferon alfa-2a and ribavirin and with GS-9451 or with GS-9256 in treatment-naive subjects with chronic genotype 1 HCV infection was discontinued due to serious adverse events.

Gilead (Originator)
Katholieke Universiteit Leuven (Originator)

……………………………………….

tegobuvir

PATENTS

WO 2005063744

WO 2008005519

WO 2009009001

WO 2010151488

WO 2010151487

WO 2010151472

WO 2011072370

WO 2011156757

WO 2012087596

WO 2013101550

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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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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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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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