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Other names | 1,3-benzodioxolyl-N-methyl-5-ethanamine; 3,4-methylenedioxy-N-methyl-2-phenylethylamine; Norlobivine |
Routes of administration | Various |
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Formula | C10H13NO2 |
Molar mass | 179.219 g·mol−1 |
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Homarylamine (INN; [1] also known as 3,4-methylenedioxy-N-methylphenethylamine and MDMPEA) is an antitussive (anti-cough) drug which was patented in 1956 by Merck & Co., [2] but has never been used medically as such.
Chemically it is a substituted phenethylamine. It is the N -methylated analog of methylenedioxyphenethylamine (MDPEA). It is a schedule I drug in the USA as a positional isomer of MDA.
Reaction of homoarylamine with formaldehyde gives hydrastinine.
Sildenafil, sold under the brand name Viagra among others, is a medication used to treat erectile dysfunction and pulmonary arterial hypertension. It is unclear if it is effective for treating sexual dysfunction in women. It is taken by mouth or injection into a vein. Onset is typically within 20 minutes and lasts for about 2 hours.
A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active chemical substance is the same, the medical profile of generics is believed to be equivalent in performance. A generic drug has the same active pharmaceutical ingredient (API) as the original, but it may differ in some characteristics such as the manufacturing process, formulation, excipients, color, taste, and packaging.
Imatinib, sold under the brand name Gleevec among others, is an oral chemotherapy medication used to treat cancer. Specifically, it is used for chronic myelogenous leukemia (CML) and acute lymphocytic leukemia (ALL) that are Philadelphia chromosome-positive (Ph+), certain types of gastrointestinal stromal tumors (GIST), hypereosinophilic syndrome (HES), chronic eosinophilic leukemia (CEL), systemic mastocytosis, and myelodysplastic syndrome. It is taken by mouth.
Celecoxib, sold under the brand name Celebrex among others, is a COX-2 inhibitor and nonsteroidal anti-inflammatory drug (NSAID). It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis. It may also be used to decrease the risk of colorectal adenomas in people with familial adenomatous polyposis. It is taken by mouth. Benefits are typically seen within an hour.
Etanercept, sold under the brand name Enbrel among others, is a biologic medical product that is used to treat autoimmune diseases by interfering with tumor necrosis factor (TNF), a soluble inflammatory cytokine, by acting as a TNF inhibitor. It has U.S. Food and Drug Administration (FDA) approval to treat rheumatoid arthritis, juvenile idiopathic arthritis and psoriatic arthritis, plaque psoriasis and ankylosing spondylitis. Tumor necrosis factor alpha (TNFα) is the "master regulator" of the inflammatory (immune) response in many organ systems. Autoimmune diseases are caused by an overactive immune response. Etanercept has the potential to treat these diseases by inhibiting TNF-alpha.
Fulvestrant, sold under the brand name Faslodex among others, is a medication used to treat hormone receptor (HR)-positive metastatic breast cancer in postmenopausal women with disease progression as well as HR-positive, HER2-negative advanced breast cancer in combination with palbociclib in women with disease progression after endocrine therapy. It is given by injection into a muscle.
Nimodipine, sold under the brand name Nimotop among others, is a calcium channel blocker used in preventing vasospasm secondary to subarachnoid hemorrhage. It was originally developed for the treatment of high blood pressure, but is not used for this indication.
In the manufacture of pharmaceuticals, encapsulation refers to a range of dosage forms—techniques used to enclose medicines—in a relatively stable shell known as a capsule, allowing them to, for example, be taken orally or be used as suppositories. The two main types of capsules are:
The pharmaceutical industry in India was valued at USD $33 billion in 2017 and generic drugs account for 20 per cent of global exports in terms of volume, making the country the largest provider of generic medicines globally. According to the Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, domestic pharmaceutical market turnover reached Rs 129,015 crore in 2018, growing 9.4 per cent year-on-year and exports revenue was US$17.28 billion in FY18 and US$19.14 billion in FY19.
Oxatomide, sold under the brand name Tinset among others, is a first-generation antihistamine of the diphenylmethylpiperazine family which is marketed in Europe, Japan, and a number of other countries. It was discovered at Janssen Pharmaceutica in 1975. Oxatomide lacks any anticholinergic effects. In addition to its H1 receptor antagonism, it also possesses antiserotonergic activity similarly to hydroxyzine.
Legal scholars, economists, activists, policymakers, industries, and trade organizations have held differing views on patents and engaged in contentious debates on the subject. Critical perspectives emerged in the nineteenth century that were especially based on the principles of free trade. Contemporary criticisms have echoed those arguments, claiming that patents block innovation and waste resources that could otherwise be used productively, and also block access to an increasingly important "commons" of enabling technologies, apply a "one size fits all" model to industries with differing needs, that is especially unproductive for industries other than chemicals and pharmaceuticals and especially unproductive for the software industry. Enforcement by patent trolls of poor quality patents has led to criticism of the patent office as well as the system itself. Patents on pharmaceuticals have also been a particular focus of criticism, as the high prices they enable puts life-saving drugs out of reach of many people. Alternatives to patents have been proposed, such Joseph Stiglitz's suggestion of providing "prize money" as a substitute for the lost profits associated with abstaining from the monopoly given by a patent.
United States v. Glaxo Group Ltd., 410 U.S. 52 (1973), is a 1973 decision of the United States Supreme Court in which the Court held that (1) when a patent is directly involved in an antitrust violation, the Government may challenge the validity of the patent; and (2) ordinarily, in patent-antitrust cases, "[m]andatory selling on specified terms and compulsory patent licensing at reasonable charges are recognized antitrust remedies."
Benocyclidine, also known as benzo
AM-1248 is a drug that acts as a moderately potent agonist for both the cannabinoid receptors CB1 and CB2, but with some dispute between sources over its exact potency and selectivity. Replacing the 3-(1-naphthoyl) group found in many indole derived cannabinoid ligands, with an adamantoyl group, generally confers significant CB2 selectivity, but reasonable CB1 affinity and selectivity is retained when an N-methylpiperidin-2-ylmethyl substitution is used at the indole 1-position. The related compound 1-pentyl-3-(1-adamantoyl)indole was identified as having been sold as a cannabinoid designer drug in Hungary in 2011, along with another synthetic cannabinoid AM-679.
AM-1220 is a drug that acts as a potent and moderately selective agonist for the cannabinoid receptor CB1, with around 19 times selectivity for CB1 over the related CB2 receptor. It was originally invented in the early 1990s by a team led by Thomas D'Ambra at Sterling Winthrop, but has subsequently been researched by many others, most notably the team led by Alexandros Makriyannis at the University of Connecticut. The (piperidin-2-yl)methyl side chain of AM-1220 contains a stereocenter, so there are two enantiomers with quite different potency, the (R)-enantiomer having a Ki of 0.27 nM at CB1 while the (S)-enantiomer has a much weaker Ki of 217 nM.
Camfetamine (N-methyl-3-phenyl-norbornan-2-amine) is a stimulant drug closely related to the appetite suppressant fencamfamine, being its N-methyl homologue. It has been sold as a designer drug following the banning of mephedrone and related substituted cathinone derivatives in many countries, and reportedly has slightly stronger stimulant effects than fencamfamine, but with correspondingly more severe side effects.
APINACA (AKB48, N-(1-adamantyl)-1-pentyl-1H-indazole-3-carboxamide) is a drug that acts as a reasonably potent agonist for the cannabinoid receptors, with a Ki of 304.5nM and an EC50 of 585nM at CB1. It had never previously been reported in the scientific or patent literature, and was first identified by laboratories in Japan in March 2012 as an ingredient in synthetic cannabis smoking blends, along with a related compound APICA. Structurally, it closely resembles cannabinoid compounds from a University of Connecticut patent (WO 2003/035005), but with a simple pentyl chain on the indazole 1-position, and APINACA falls within the claims of this patent despite not being disclosed as an example.
APICA is an indole based drug that acts as a potent agonist for the cannabinoid receptors.
U-47700, also known as pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models.
Flumezapine is an abandoned, investigational antipsychotic drug that was studied for the treatment of schizophrenia. Flumezapine failed clinical trials due to concern for liver and muscle toxicity. Flumezapine is structurally related to the common antipsychotic olanzapine—a point that was used against its manufacturer, Eli Lilly and Company, in a lawsuit in which generic manufacturers sought to void the patent on brand name olanzapine (Zyprexa). Although flumezapine does not differ greatly from olanzapine in terms of its structure, the difference was considered to be non-obvious, and Eli Lilly's patent rights on Zyprexa were upheld.