Aminometradine CAS No. 642-44-4

Aminometradine is a weak diuretic which was used to control oedema in those who suffered mild congestive heart failure.

Systematic (IUPAC) name
6-amino-3-ethyl-1-prop-2-enylpyrimidine-2,4-dione
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 642-44-4
ATC code  ?
PubChem CID 12551
ChemSpider 12033 Yes
UNII PPM8SX5Q3V Yes
Chemical data
Formula C9H13N3O2 
Mol. mass 195.22 g/mol
InChI=1S/C9H13N3O2/c1-3-5-12-7(10)6-8(13)11(4-2)9(12)14/h3,6H,1,4-5,10H2,2H3 Yes
Key:NGXUUAFYUCOICP-UHFFFAOYSA-N
 Yes (what is this?)  (verify)

Alovudine

Alovudine
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 25526-93-6
ATC code None
PubChem CID 33039
ChemSpider 30578 Yes
UNII PG53R0DWDQ Yes
KEGG D02830 Yes
ChEMBL CHEMBL105318 Yes
Chemical data
Formula C10H13F2N2O4 
Mol. mass 244.22 g/mol
SMILES
  • O=C/1NC(=O)N(\C=C\1C)[C@@H]2O[C@@H]([C@@H](F)C2)CO
InChI
  • InChI=1S/C10H13FN2O4/c1-5-3-13(10(16)12-9(5)15)8-2-6(11)7(4-14)17-8/h3,6-8,14H,2,4H2,1H3,(H,12,15,16)/t6-,7+,8+/m0/s1 Yes
    Key:UXCAQJAQSWSNPQ-XLPZGREQSA-N Yes
 Yes (what is this?)  (verify)

Alovudine is an antiviral agent.

  • v
  • t
  • e
Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
Entry/fusion inhibitors
(Discovery & development)
  • gp41 (Enfuvirtide)
  • CCR5 (Maraviroc
  • Vicriviroc, Cenicriviroc, PRO 140)
  • CD4 (Ibalizumab)
Reverse-transcriptase
inhibitors(RTIs)
Nucleoside &
nucleotide (NRTI)
  • Nucleoside analogues/NARTIs: Abacavir (ABC)°#
  • Emtricitabine (FTC)°#
  • Lamivudine (3TC)°#
  • Didanosine (ddI)#
  • Zidovudine (AZT)#
  • Apricitabine
  • Stampidine
  • Elvucitabine
  • Racivir
  • Amdoxovir
  • Stavudine (d4T)#
  • Zalcitabine (ddC)
  • Festinavir
  • Nucleotide analogues/NtRTIs: Tenofovir°#
  • TAF
Non-nucleoside (NNRTI)
(Discovery & development)
  • (1st generation) Efavirenz°#
  • Nevirapine#
  • Loviride
  • Delavirdine
  • (2nd generation) diarylpyrimidines (Etravirine
  • Rilpivirine)
  • Lersivirine
Integrase inhibitors
  • Raltegravir°
  • Elvitegravir
  • Dolutegravir
  • Globoidnan A (experimental)
  • MK-2048
  • BI 224436
Maturation inhibitors
  • Bevirimat
  • Vivecon
Protease Inhibitors (PI)
(Discovery and development)
1stgeneration
  • Fosamprenavir°
  • Lopinavir°#
  • Nelfinavir#
  • Ritonavir#
  • Saquinavir#
  • Amprenavir
  • Indinavir#
2ndgeneration
  • Atazanavir°
  • Darunavir°
  • Tipranavir
Combined formulations
  • Lamivudine/zidovudine
  • Emtricitabine/tenofovir/efavirenz
  • Abacavir/lamivudine/zidovudine
  • Tenofovir/emtricitabine
  • Lopinavir/ritonavir
  • Abacavir/lamivudine
  • Emtricitabine/rilpivirine/tenofovir
  • Elvitegravir/cobicistat/emtricitabine/tenofovir
Experimental agents
Uncoating inhibitors
  • TRIM5alpha (gene)
Transcription inhibitors
  • Tat antagonists
Translation inhibitors
  • Trichosanthin
Other
  • Abzyme
  • Calanolide A
  • Ceragenin
  • Cyanovirin-N
  • Diarylpyrimidines
  • Epigallocatechin gallate (EGCG)
  • Foscarnet
  • Griffithsin
  • Hydroxycarbamide
  • Miltefosine
  • Portmanteau inhibitors
  • Seliciclib
  • Synergistic enhancers
  • Tre recombinase
  • Zinc finger protein transcription factor
  • KP-1461
  • Cobicistat
Failed agents
  • Dexelvucitabine
  • Capravirine
  • Emivirine
  • Lodenosine
  • Atevirdine
  • Brecanavir
  • Aplaviroc
  • #WHO-EM
  • Withdrawn from market
  • Clinical trials:
    • Phase III
    • §Never to phase III

°DHHS preferred first-line agent. Formerly or rarely used agent.

M: VIR

virs(prot)/clss

cutn/syst (hppv/hiva,infl/zost/zoon)/epon

drug(dnaa, rnaa, rtva,vacc)

  • v
  • t
  • e
DNA virus antivirals (primarily J05, also S01AD and D06BB)
Baltimore I
Herpesvirus
DNA-synthesis
inhibitor
TKactivated
Purine analogue
  • guanine (Aciclovir#/Valacyclovir
  • Ganciclovir/Valganciclovir
  • Penciclovir/Famciclovir)
  • adenine (Vidarabine)
Pyrimidine analogue
  • uridine (Idoxuridine
  • Trifluridine
  • Edoxudine)
  • thymine (Brivudine)
  • cytosine (Cytarabine)
Not TK activated
  • Foscarnet
Other
  • Docosanol
  • early protein (Fomivirsen)
  • Tromantadine
HPV/MC
  • Imiquimod/Resiquimod
  • Podophyllotoxin
Vaccinia
  • assembly: Rifampicin
Poxviridae
  • Methisazone
Hepatitis B (VII)
  • Nucleoside analogues/NARTIs: Entecavir
  • Lamivudine
  • Telbivudine
  • Clevudine
  • Nucleotide analogues/NtRTIs: Adefovir
  • Tenofovir
Multiple/general
Nucleic acid inhibitors
  • Cidofovir
Interferon
  • Interferon alfa-2b
  • Peginterferon alfa-2a
Multiple/unknown
  • Ribavirin#/Taribavirin
  • Moroxydine
  • #WHO-EM
  • Withdrawn from market
  • Clinical trials:
    • Phase III
    • §Never to phase III

M: VIR

virs(prot)/clss

cutn/syst (hppv/hiva,infl/zost/zoon)/epon

drug(dnaa, rnaa, rtva,vacc)

 

Alogliptin

Alogliptin
Systematic (IUPAC) name
2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-
3,4-dihydropyrimidin-1(2H)-yl}methyl)benzonitrile
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral
Identifiers
CAS number 850649-62-6
ATC code A10BH04
PubChem CID 11450633
ChemSpider 9625485 Yes
UNII JHC049LO86 Yes
KEGG D06553 Yes
ChEMBL CHEMBL376359 Yes
Chemical data
Formula C18H21N5O2 
Mol. mass 339.39 g/mol
SMILES
  • N#Cc3ccccc3CN\1C(=O)N(C)C(=O)/C=C/1N2CCC[C@@H](N)C2
InChI
  • InChI=1S/C18H21N5O2/c1-21-17(24)9-16(22-8-4-7-15(20)12-22)23(18(21)25)11-14-6-3-2-5-13(14)10-19/h2-3,5-6,9,15H,4,7-8,11-12,20H2,1H3/t15-/m1/s1 Yes
    Key:ZSBOMTDTBDDKMP-OAHLLOKOSA-N Yes
 Yes (what is this?)  (verify)

Alogliptin (codenamed SYR-322)[1] is an orally administered,[citation needed]anti-diabetic drug in the DPP-4 inhibitor class,[2]developed by Takeda Pharmaceutical Company.

Clinical study

A randomized clinical trial reporting in 2011 aimed to determine the efficacy and safety of alogliptin versus placebo and voglibose among newly diagnosed Type 2 diabetes patients in Japan. The main outcome indicated that alogliptin was statistically superior to both comparitors.[3]

A randomized clinical trial reporting in 2012 aimed to demonstrate that alogliptin was “non-inferior” to a “very low fat/calorie traditional Japanese diet” among newly diagnosed Type 2 diabetes patients in Japan. The outcome indicated that both the drug and dietary treatments comparably impacted indicators of the diabetic condition, such as HbA1c levels and glycemic efficacy. The drug treatment had its impact without changingbody mass index (BMI), but the dietary treatment was accompanied by a significant reduction in the BMI.

A randomized clinical trial reporting in 2011 aimed to demonstrate the efficacy of alogliptin as an add-on agent in combination with metforminand pioglitazone versus simply increasing the dosage of pioglitazone in combination with metformin; in other words, this was a study to look at a three-agent therapy versus a two-agent therapy. The outcome of this study suggested that the addition of alogliptin to metformin and pioglitazone provided superior impact on diabetes biomarkers (e.g. HbA1c) than increasing the dose of pioglitazone in a two agent therapy with metformin.[5]

Reported adverse events

Adverse events appear to be restricted to mild hypoglycemia based on clinical studies.

Market access

In December 2007, Takeda submitted a New Drug Application (NDA) for alogliptin to the United States Food and Drug Adminiistration (USFDA),[6]after positive results from Phase III clinical trials.[1] In September of 2008, the company also filed for approval in Japan,[7] winning approval in April 2010.[6] The company also filed a Marketing Authorization Application (MAA) elsewhere outside the United States, which was withdrawn in June 2009 needing more data.[7] The first USFDA NDA failed to gain approval and was followed by a pair of NDAs (one for alogliptin and a second for a combination of alogliptin and pioglitazone) in July 2011.[6] In 2012, Takeda received a negative response from the USFDA on both of these NDAs, citing a need for additional data.[6]

Orotic acid

Orotic acid
Systematic (IUPAC) name
1,2,3,6-tetrahydro-2,6-dioxo-4-pyrimidinecarboxylic acid
Clinical data
AHFS/Drugs.com International Drug Names
Pregnancy cat.  ?
Legal status  ?
Identifiers
CAS number 65-86-1 Yes
ATC code None
PubChem CID 967
DrugBank DB02262
ChemSpider 942 
UNII 61H4T033E5 
KEGG C00295 
Chemical data
Formula C5H4N2O4
Mol. mass 156.10 g/mol
SMILES
  • O=C(O)\C1=C\C(=O)NC(=O)N1
InChI
  • InChI=1S/C5H4N2O4/c8-3-1-2(4(9)10)6-5(11)7-3/h1H,(H,9,10)(H2,6,7,8,11) 
    Key:PXQPEWDEAKTCGB-UHFFFAOYSA-N 
  (what is this?)  (verify)

Orotic acid is a heterocyclic compound and an acid; it is also known aspyrimidinecarboxylic acid. Historically it was believed to be part of the Vitamin B complex and was called vitamin B13, but it is now known that it is not a vitamin.

The compound is manufactured in the body by intestinal flora. It is sometimes used as amineral carrier in some dietary supplements (to increase their bioavailability), most commonly for lithium orotate.

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