Abstract:A rising number of researchers are interested in thiophene-based analogs as they have wide possibilities of biological potential in the largely developing chemical world of the heterocyclic moiety. It also occupies a central position in synthetic organic chemistry and is of the highest theoretical and practical importance. It became an important moiety for researchers to discover combinatorial libraries and implement the efforts in search of the lead entity. Moreover, it helps medicinal chemists to improve sophisticated molecules with a broad range of pharmacological activities. Thiophene and its synthetic derivatives are a prominent heterocyclic compound class with intriguing uses in medical chemistry. It has been manifesting to be an effective drug in current respective diseases scenario. It has been discovered that thiophene had an extensive spectrum of pharmacological potential with numerous applications in academic interest, in the pharmaceutical industry, material science, and medicinal chemistry. Antimitotic, antimicrobial, anti-inflammatory, anticonvulsant, antipsychotic, antiarrhythmic, anti-anxiety, antifungal, antioxidant, estrogen receptor regulating, and anti-cancer are one of the pharmacological and physiological activities of thiophene moiety. However, there are some marketed formulations available such as Thiophenfurin, Teniposide, Cefoxitin, Ticaconazole, Sertaconazole, Suprofen, ketotifen, Brinzolamide, Dorzolamide, Tiotropium which contain thiophene nucleus. Thus, in brief, gathering recent data is necessary to comprehend the present scenario of thiophene moiety for scientific research purposes and highlights a broad view of the biological potential of compounds having a thiophene nucleus.

2022-11-01·Acta dermatovenerologica Croatica : ADC

Ketoprofen-induced Photoallergic Reaction.

Article

作者: Ljubojević Hadžavdić, Suzana ; Rosan, Tin

Dear Editor, Photoallergic reactions are classic T-cell-mediated or delayed-type hypersensitivity reactions of the skin in response to a photoallergen (or a cross-reacting chemical) to which a subject was sensitized in the past (1). The immune system recognizes the changes caused by ultraviolet (UV) radiation; it produces antibodies and causes inflammation of the skin in the exposed areas (2). Common photoallergic drugs and ingredients are included in some sunscreens, aftershave lotions, antimicrobials (especially sulfonamides), non-steroidal anti-inflammatory drugs (NSAIDs), diuretics, anticonvulsants, chemotherapy drugs, fragrances, and other hygiene products (1,3,4). A 64-year-old female patient was admitted to the Department of Dermatology and Venereology with erythema and underlining edema on her left foot (Figure 1). A few weeks earlier, the patient had had a fracture of the metatarsal bones and since then she had been taking NSAIDs systemically every day to suppress pain. Five days before being admitted to our Department, the patient started applying 2.5% ketoprofen gel to her left foot twice daily and was frequently exposed to the sun. For the last twenty years, the patient had been struggling with chronic back pain and was frequently taking different NSAIDs (ibuprofen, diclofenac, etc.). The patient also suffered from essential hypertension and was regularly taking ramipril. She was advised to discontinue ketoprofen application, avoid sunlight, and apply betamethasone cream twice daily for 7 days, which lead to complete resolution of the skin lesions in a few weeks. Two months later, we performed patch and photopatch tests to baseline series and topical ketoprofen. Only the irradiated side of the body where ketoprofen-containing gel was applied showed positive reaction to ketoprofen. Photoallergic reactions manifest as eczematous, pruritic lesions, which may spread to involve other areas of the skin that were not previously exposed to the sun (4). Ketoprofen is a nonsteroidal anti-inflammatory drug composed of a benzoylphenyl propionic acid that is commonly used both topically and systemically for the treatment of musculoskeletal diseases because of its analgesic and anti-inflammatory effects and low toxicity, but it is one of the most frequent photoallergens (1,5,6). Ketoprofen-induced photosensitivity reactions usually present as photoallergic dermatitis characterized as acute dermatitis with edema, erythema, papulovesicles, blisters, or erythema exsudativum multiforme-like lesions at the application site 1 week to 1 month after the initiation of use (7). Depending on the frequency and intensity of sun exposure, ketoprofen photodermatitis may continue or reoccur up to 1 to 14 years after discontinuing the medication (6,8). Moreover, ketoprofen contaminates clothing, shoes, and bandages, and some cases of photoallergy relapses have been reported that were induced by ketoprofen-contaminated objects after they were used again in the presence of UV radiation (5,6). Due to their similar biochemical structure, patients with ketoprofen photoallergy should avoid using some drugs such as some NSAIDs (suprofen, tiaprofenic acid), antilipidemic agent (fenofibrate) and sunscreens based on benzophenones (6,9). Physicians and pharmacists should advise patients of the potential risks when topical NSAIDs are applied on the photoexposed skin.

2022-08-23·ACS Omega

Computational Studies of the Photodegradation Mechanism of the Highly Phototoxic Agent Benoxaprofen

Article

作者: Musa, Klefah A. K. ; Eriksson, Leif A.

Computational quantum chemistry within the density functional theory (DFT) and time-dependent density functional theory (TD-DFT) framework is used to investigate the photodegradation mechanism as well as the photochemical and photophysical properties of benoxaprofen (BP), a non steroid anti-inflammatory molecule (2-[2-(4-chlorophenyl)-1,3-benzoxazol-5-yl] propanoic acid). BP is a highly phototoxic agent that causes cutaneous phototoxicity shortly after its administration. On the grounds of concern about serious side effects, especially hepatotoxicity, it was withdrawn from the world market after only 2 years of its release. Our study shows that the drug has the capability to absorb radiation in the UV region, mainly between 300 and 340 nm, and undergoes spontaneous photoinduced decarboxylation from the triplet state. It shows very similar photochemical properties to the highly photolabile non-steroidal anti-inflammatory drugs (NSAIDs) ketoprofen, suprofen, and tiaprofenic acid. Like ketoprofen, BP can also decarboxylate from excited singlet states by overcoming low energy barriers. The differences in molecular orbital (highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO)) distributions between the neutral and deprotonated BP, their absorption spectra, and the energetics and fate of various photoproducts produced throughout the photodegradation are discussed. Initiation and termination of decarboxylated BP radical species and initiation of propagating lipid peroxidation reactions due to the addition of molecular oxygen giving rise to the corresponding peroxyl radical are also explored in detail.

项与舒洛芬相关的新闻（医药）

2022-07-13

·Endpoints

Sanofi CEO Paul Hudson offloads two portfolios to German pharma company in continued effort to prune products

Sanofi warned earlier this year that some serious cuts were in order. CEO Paul Hudson made good on that promise this week, pruning more than a dozen marketed products. Germany-based Neuraxpharm revealed yesterday that it struck a deal for Sanofi’s CNS and pain and vascular disease portfolios. While the companies are keeping the financial terms under wraps for now, Neuraxpharm did say it’s swallowing 17 products representing 38 brands, including neuroleptics Nozinan and Tiapridal, anxiety med Tranxene and antipsychotics Dogmatil and Largactil. Within the pain and vascular portfolio, Neuraxpharm is getting pain narcotic Topalgic and Trental, which is used to improve blood flow. Neuraxpharm expects that the new products will boost sales to about $600 million this year. “There is significant growth potential in the pharmaceutical sector, especially in the CNS market driven by an aging population and an increasing awareness of mental health,” CEO Jörg-Thomas Dierks said in a news release. “With the upcoming acquisition, we will not only strengthen our presence in Europe, but also lay the ground for further expanding our international presence.” The new drugs will contribute to a portfolio of CNS drugs, as well as generics and consumer healthcare products such as nutraceuticals and probiotics, according to Neuraxpharm’s website. The company has main offices in Germany and Spain, with additional locations throughout Europe. Hudson has been on a mission to reshape Sanofi since he took the helm in 2019. He said earlier this year that nothing is off the table when it comes to restructuring, and has already culled a handful of programs. During the Q1 call, EVP of general medicines Olivier Charmeil said the company is looking to shave the general medicines unit down to about 125 product families, either by divesting or discontinuing programs. That’s a big difference from late 2019 and early 2020, when the unit boasted more than 350 product families. The company also revealed in its Q4 results that it plans on axing about 6,000 jobs in an effort to become more “agile.” Execs said at the time that they were aiming for a headcount of around 90,000 by the end of the year.

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2022-07-12

·PRNewswire

Neuraxpharm to increase branded business through upcoming acquisition of established products from Sanofi

Neuraxpharm, the central nervous system (CNS) specialist, to acquire two portfolios of established products for CNS disorders, pain and vascular diseases DUSSELDORF, Germany and BARCELONA, Spain, July 12, 2022 /PRNewswire/ -- Neuraxpharm Group ("Neuraxpharm") today announced that it has entered into a definitive agreement to acquire two product portfolios for CNS disorders, pain and vascular diseases from Sanofi. With the upcoming acquisition, Neuraxpharm will strengthen its position as a leading European specialty pharmaceutical company focused on CNS. The well-established products that Neuraxpharm will acquire are marketed globally in more than 50 countries. The first portfolio combines 15 products addressing CNS disorders and ranging across psychiatry and neurology. The second portfolio includes two products in pain and vascular diseases. Following the acquisition of these new portfolios, Neuraxpharm's annual gross sales will be around EUR 0.6 billion. The products benefit patients across a large spectrum of diseases including depression, anxiety, psychosis, alcohol dependence, myasthenia gravis and Parkinson disease. The CNS portfolio notably includes Nozinan®, Tranxene®, Tiapridal®, Dogmatil®, Largactil®. The pain and vascular portfolio includes Topalgic® and Trental®. Combined, both portfolios include 17 molecules representing 38 brands. These global brands will further solidify Neuraxpharm's position as a leading CNS pharmaceutical company in Europe and increase the company's global footprint and business. Dr. Jörg-Thomas Dierks, CEO of Neuraxpharm, said: "There is significant growth potential in the pharmaceutical sector, especially in the CNS market driven by an ageing population and an increasing awareness of mental health. This phenomenon is a global trend. With the upcoming acquisition, we will not only strengthen our presence in Europe, but also lay the ground for further expanding our international presence." About the Group Neuraxpharm – the European CNS specialist Neuraxpharm is a leading European specialty pharmaceutical company focused on the treatment of central nervous system disorders (CNS) with a direct presence in 19 countries. Backed by funds advised by Permira, Neuraxpharm has a unique understanding of the CNS market built over 35 years. With its focus on CNS, Neuraxpharm develops and commercializes established brands, value added medicines, generics, Consumer Healthcare products, medical cannabis and beyond-the-pill solutions and is continuously striving to offer a wide range of effective, high quality and affordable CNS treatment options in Europe. Present with its products in more than 50 countries, Neuraxpharm also manufactures pharmaceutical products and active pharmaceutical ingredients in its own manufacturing sites, Lesvi and Inke, in Spain. For more information please visit SOURCE Neuraxpharm

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100 项与舒洛芬相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00452	舒洛芬	M01AE07	DB00870

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性湿疹	日本	Sun Pharma Japan Ltd.	1989-06-30
慢性湿疹	日本	Sun Pharma Japan Ltd.	1989-06-30
特应性皮炎	日本	Sun Pharma Japan Ltd.	1989-06-30
特应性皮炎	日本	Alfresa Pharma Corp.	1989-06-30
接触性皮炎	日本	Alfresa Pharma Corp.	1989-06-30
接触性皮炎	日本	Sun Pharma Japan Ltd.	1989-06-30
口周皮炎	日本	Sun Pharma Japan Ltd.	1989-06-30
湿疹	日本	Alfresa Pharma Corp.	1989-06-30
带状疱疹	日本	Sun Pharma Japan Ltd.	1989-06-30
带状疱疹	日本	Alfresa Pharma Corp.	1989-06-30
酒渣鼻样皮炎	日本	Sun Pharma Japan Ltd.	1989-06-30