U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 2551 - 2560 of 8583 results

Status:
Possibly Marketed Outside US
Source:
VIVACE by Takeda Chemical Industries
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Delapril is a lipophilic nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been shown to exert potent ACE inhibitory activity and is marketed as an antihypertensive drug. Delapril has been shown to exist in solution as a mixture of s-cis and s-trans conformational isomers, as a result of restricted rotation about the amide bond.
Status:
Possibly Marketed Outside US
Source:
Unknown by Santhera Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pimasertib) (N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]isonicotinamide hydrochloride; AS703026), a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2. It binds to MEK1/2 in an allosteric site that is distinct from, yet in close proximity to, the ATP binding site. Binding to this allosteric site prevents the activation of MEK1/2. Pimasertib continues to be investigated in patients with NRAS mutant malignant melanoma in a Phase II trial. This drug was discontinued in a combination with SAR245409 for Phase II study in low-grade serous ovarian cancer. This decision was based on the results of a futility analysis, conducted by the IDMC, which indicated that the trial was no longer expected to achieve its objective of showing a meaningful difference between the efficacies of the combination compared with pimasertib alone. The further development of pimasertib in pancreatic cancer was also discontinued, as a Phase II study in this indication did not reach its primary endpoint of prolongation of progression-free survival
Status:
Possibly Marketed Outside US
Source:
APOQUEL by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Oclacitinib (PF03394197) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nM. Oclacitinib as oclacitinib maleate is approved for control of pruritus associated with allergic dermatitis and control of atopic dermatitis in dogs at least 12 months of age.
Status:
Possibly Marketed Outside US
Source:
DEBERZA by Chugai Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tofogliflozin is a SGLT2 selective inhibitor which was developed by Chugai Pharmaceutical for the treatment of Type 2 Diabetes Mellitus. The drug was approved in Japan in 2013 and it is being marketed under the names Apleway and Debereza.
Equilin sulfate is one of the main component, which is responsible for the pharmacological action of the PREMARIN, conjugated estrogens tablets. Premarin is used to treat the moderate to severe vasomotor symptoms, vulvar and vaginal atrophy due to menopause. It is also used to treat hypoestrogenism due to hypogonadism, castration or primary ovarian failure; to treat breast cancer and advanced androgen-dependent carcinoma of the prostate (for Palliation Only). In addition, premarin is used to prevent postmenopausal osteoporosis. Equilin sulfate is a prodrug, which is hydrolyzed to the corresponding free estrogen equilin, an inhibitor of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1). Human 17beta-HSD1 catalyzes the reduction of inactive estrone (E1) to the active 17beta-estradiol in breast tissues, is a key enzyme responsible for elevated levels of E2 in breast tumor tissues. Thus equilin reduce the E2 levels in breast tissues and hence the reduce risk of estrogen-dependent breast cancer.
Status:
Possibly Marketed Outside US
Source:
SULFATYF by Gabriel, K.L.|Scheidy, S.F.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sulfachloropyrazine, a sulfonamide, was developed as a drug for poultry coccidiosis. Sulfachloropyrazine was found to be a therapeutic option for T. gondii infection in animals.
Vitexin, identified as apigenin-8-C-β-D-glucopyranoside, is a flavonoid compound found in Anthurium versicolor, Ficaria verna Huds. (Ranunculaceae), Cucumis sativus L. (Cucurbitaceae), and Acer palmatum (Aceraceae). Vitexin is an active component of many traditional Chinese medicines. Vitexin has recently received increased attention due to its wide range of pharmacological effects, including but not limited to anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
Testosterone valerate, or testosterone pentanoate, is a synthetic, steroidal androgen. It is a short-to-medium duration C17β valerate ester of testosterone, with a terminal half-life of approximately twice that of the short-acting testosterone propionate. Testosterone valerate is available exclusively as a component of the veterinary drug Deposterona developed by Syntex Animal Health Company, which is marketed in Mexico. Deposterona also contains testosterone acetate and testosterone undecanoate and is used to treat impotence, weakness, fatigue and hypogonadism in male breeding animals (cows, pigs, canines, sheep), as well as a general protein-sparing anabolic. It is administered via intramuscular injection and acts as a long-lasting prodrug of testosterone. Esterified forms of testosterone are designed to prolong the window of therapeutic effect following administration, allowing for less frequent injection schedule compared to injections of unesterified steroid. Deposterona is also used for bodybuilding purposes in men and not recommended for women performance-enhancing purposes due to its strong androgenic nature, side effects, and slow-acting characteristics (making blood levels difficult to control). Deposterona is only known to be manufactured in Mexico. Because it contains a low concentration of steroid,this product is not in high demand, and not readily diverted for illicit sale.
Status:
Possibly Marketed Outside US
Source:
Пикамилон by Budesinsky, Z.|Zikmund, E.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Picamilon (also known as N-nicotinoyl-GABA, Pycamilon, and Pikamilon) is a drug formed by a synthetic combination of niacin and GABA. It was developed in the Soviet Union in 1969 and further studied in both Russia and Japan as a prodrug of GABA. Picamilon permeated the blood-brain barrier and then is hydrolyzed into GABA and niacin. The released GABA, in theory, would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin, is a vasodilator. Today picamilon is sold in Russia as a prescription drug and is used for the treatment of a variety of illnesses and disorders, ranging from depression to a migraine, neuro infections, senile psychosis, certain types of glaucoma, and even acute alcohol intoxication. As of 2015, the FDA classified picamilon as a substance that does not meet the requirements of a dietary supplement and is therefore no longer permitted to be sold in the United States.
Status:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tetramethylglycoluril (MEBICAR, Adaptol, Mebicarum) is an anxiolytic similar to organism natural metabolites with nootropic and stress-protective characteristics. Tetramethylglycoluril belongs to a group of non-benzodizepam tranquilizers. It works by effecting on the structure of limbic-reticular activity and 4 main neuromediator systems – γ aminobutyric acid, choline -, serotonin- and adrenergic. Tetramethylglycoluril increases serotonin levels, decreases noradrenaline level with no effect on dopamine and no anticholinergic activity. It acts on hypothalamus emotional zone, thus providing moderate tranquilizing effect. Tetramethylglycoluril improves oxygen consumption by myocardium, normalizes blood electrolyte balance, stimulates protein synthesis and increases cell's energy resource. Tetramethylglycoluril is used to treat neurotic disorders (anxiety, awareness, fear, emotional density, irritability) caused by exhausting psycho-emotional, nervous and physical loads. Mebicar relieves or completely removes nicotine abstinence.

Showing 2551 - 2560 of 8583 results