67 results about "Pirfenidone" patented technology

The present invention relates to the use of a pharmaceutical composition in the form of extended-release tablets containing Pirfenidone for treating NAFLD / NASH and advanced liver fibrosis by decreased serum cholesterol and triglycerides as well as reducing the content of hepatic fat accumulation, both in the form of macrosteatosis and microsteatosis. Additionally, its use as an agonist for PPARgamma (peroxisome proliferation receptor activated gamma), PPARalpha (peroxisome proliferation receptor activated alpha), LXR and CPT1, key molecules in the metabolism of fatty degradation and inflammation of the liver. In addition, another use is the induction of decreased expression of NFKB master gene, transcriptional inducer of hepatic inflammatory process factor. All of these events results in the reversal of NAFLD / NASH and advanced liver fibrosis.

The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and / or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis.

The instant invention relates to a semi-solid topical composition containing Pirfenidone and an antimicrobial / antiseptic agent such as Modified Diallyl Disulfide Oxide (M-DDO) and its preparation process, offering advantages compared to other pharmaceutical forms of topical administration known in the state of the art, useful as antifibrotic, anti-inflammatory and antiseptic agent in the prevention, treatment and reversion of acne and post acne lesions. Said compositions is also useful for reducing skin redness, detaining the formation of new acne outbreaks, reversing already existing outbreaks and regenerating skin damage caused by acne.

Disclosed herein is a method of treating Idiopathic Pulmonary Fibrosis (IPF). The method includes administering to a subject in need thereof the deuterium-enriched pirfenidone LYT-100 at a total daily dose from about 1650 mg to about 2500 mg.

The invention belongs to the technical field of biological medicines, and particularly relates to a royal jelly acid derivative and a synthesis method, a pharmaceutical composition and application thereof. The royal jelly acid derivative is a compound shown as a formula (I), or an enantiomer, a diastereoisomer and a tautomer thereof, or a solvate or a pharmaceutically acceptable salt thereof. A series of royal jelly acid derivatives with novel structures are constructed by using a natural component royal jelly acid derived from royal jelly as an initial raw material, the royal jelly acid derivatives can play a role in resisting pulmonary fibrosis by inhibiting the activity of fibroblasts, the effect of the royal jelly acid derivatives is equivalent to that of pirfenidone, and the royal jelly acid derivatives are expected to be developed into candidate drugs for resisting pulmonary fibrosis. The ceramide NP has excellent effects in anti-inflammatory, anti-allergic and itching-relieving aspects, has a better effect than known ceramide NP, and can be used for preparing health care products, cosmetics and medicines. And # imgabs0 #.

The invention discloses a nano-drug delivery system for treating myocardial fibrosis as well as a preparation method and application of the nano-drug delivery system, and belongs to the technical field of biological medicines. According to the system, ZIF-8 is taken as a core carrier, the loading efficiency of pirfenidone is improved through high specific surface area and adjustable aperture, PCM myocardial targeting peptide is covalently coupled on the surface, and the limitation of tissue selectivity is broken through. Through coordination complexation, pi-pi conjugate accumulation and electrostatic interaction synergy, stable drug loading and microenvironment response release are guaranteed; a one-pot method and a carbodiimide method are adopted to wrap PFD and modify PCM on the surface of ZIF-8 to form a nano-drug delivery system; according to the system, the fibrosis process is intervened through multiple mechanisms, the enrichment degree and the acting time of the medicine at the diseased region are improved, the prepared medicine integrates the carrier structure advantage and the targeting peptide function, efficient medicine carrying, precise delivery and controllable release are achieved, a new scheme is provided for myocardial fibrosis treatment, and the system has wide application prospects.

The invention discloses a platinum (IV)-pirfenidone compound prodrug, a preparation method and microenvironment remodeling anti-tumor application, and belongs to the field of medical technology and drug synthesis. A series of molecules are characterized by being platinum prodrugs modified by pirfenidone derivatives. The synthesis method sequentially comprises the following steps: oxidizing platinum drugs, modifying hydroxyl groups, and introducing pirfenidone derivatives through esterification reaction. A series of molecules are reduced into Pt (II) drugs at the focus to kill cancer cells, and meanwhile, the released pirfenidone derivative can remodel the tumor microenvironment. The platinum prodrug disclosed by the invention not only has excellent cancer cell killing ability, but also is relatively low in drug resistance and excellent in safety, can trigger immunogenic cell death, and is a brand new chemotherapy-immunotherapy method. A series of molecules are convenient to synthesize, the preparation process is simple, and the amphipathicity is excellent, the anti-cancer capability is excellent, the drug resistance and toxicity are low, and the clinical application prospect is good.

A prolonged-release oral solid formulation of pirfenidone includes a sustained-release formulation. The sustained-release formulation contains a swelling material, a shaping material and an adhesive material. The weight percentage of the swelling material in the solid formulation is 10%-25%; the weight percentage of the shaping material in the solid formulation is 10%-25%; and the weight percentage of the adhesive material in the solid formulation is 1%-8%. The solid formulation only needs to be taken once a day, regardless of whether it is taken before or after meals. It takes effect quickly after taking it, and can be stably and effectively released for 24 hours, providing a pirfenidone product with significantly improved compliance and stable blood drug concentration.

A pharmaceutical composition for prevention or treatment of a disease or disorder characterized by chronic inflammation, associated with angiogenesis and fibrosis. The pharmaceutical composition includes a multi-target inhibitor, multi-phase modulator, or multi-kinase inhibitor, such as axitinib, nintedanib, pirfenidone, riociguat, sorafenib, sunitinib, lenvatinib, regorafenib, ponatinib, or pazopanib.

The invention provides a drug-loaded gelatin nanogel, a bionic nanogel, a preparation method of the drug-loaded gelatin nanogel, a preparation method of the bionic nanogel, a combined drug and application of the bionic nanogel, and belongs to the technical field of biological medicine. According to the invention, all-transretinoic acid, pirfenidone and gelatin react to form drug-loaded gelatin nanogel, and the drug-loaded gelatin nanogel can synergistically inhibit the activation of pancreatic stellate cells and block a fibrosis-promoting signal channel, so that the reversion of a pancreatic cancer fibrosis microenvironment is realized; meanwhile, the activated pancreatic stellate cell membrane is coated with the drug-loaded gelatin nanogel to construct the bionic nanogel, so that the bionic nanogel has active targeting property, and the delivery efficiency and the treatment effect of the drug are remarkably improved; and the drug-loaded gelatin nanogel, the bionic nanogel and the chemotherapeutic drug are combined for treating pancreatic cancer, so that a remarkable anti-tumor effect is achieved, and the combined treatment of the bionic nanogel and gemcitabine has a synergistic anti-tumor effect. The gel provided by the invention realizes effective regulation and control of a pancreatic cancer dense fibrosis microenvironment, and provides a feasible new strategy for treatment of pancreatic cancer.

The application discloses a pirfenidone nanosuspension inhalation solution for treating interstitial pneumonia and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The pirfenidone nanosuspension inhalation solution is composed of the following components in 1000ml: 8-12g of pirfenidone hydrochloride, 4-6g of polyethylene glycol-poly-L-histidine block copolymer, 45-55g of mannitol, 0.4-0.6g of antioxidant, 0.05mol / L of citric acid-sodium citrate buffer, and water for injection, wherein the amount of the citric acid-sodium citrate buffer is appropriate, and the water for injection is added to 1000ml. The application adopts a pulmonary targeted inhalation administration path of non-gastrointestinal absorption, so that the drug directly acts on the lung interstitial lesion part by bypassing the intestinal absorption link.

The invention provides an application of a pharmaceutical composition in preparation of an anti-pulmonary fibrosis drug, and belongs to the technical field of biological medicines. The invention provides a pharmaceutical composition containing schizandrin C, ginsenoside Rg2 and homoisohydroflavone. Multi-target intervention is realized aiming at key pathological mechanisms (such as cell senescence, proinflammatory factor release and extracellular matrix deposition) of pulmonary fibrosis. Experiments show that the composition can remarkably reverse the senescence phenotype of pulmonary fibrosis cells, inhibit activation of p53 / p21 signal channels, reduce fibrosis marker expression and the like. Compared with an existing medicine such as pirfenidone, the natural component combination has the advantage of being higher in safety, a safer, more effective and more economical treatment choice is provided for clinic, and remarkable conversion value and market potential are achieved.

The present invention relates to a process for the synthesis of Pirfenidone (1) from 5-Methyl-3,4-dihydro-2-pyridone and halobenzene (chlorobenzene, bromobenzene, or iodobenzene) in the presence of a catalytic system consisting of a copper salt and an organic ligand, in the presence of a base.

The invention belongs to the technical field of targeted drugs, and particularly relates to a 293T exosome for targeted delivery of pirfenidone through a membrane-loaded FAP and a preparation method and application thereof.The exosome secreted by 293T cells serves as a natural nano-carrier, an FAP antibody with fibroblast targeting performance is modified on the exosome membrane surface through a copper-free click chemical method, and the exosome membrane surface is modified through a copper-free click chemical method; an anti-fibrosis drug PFD is efficiently loaded into the exosome by adopting an ultrasonic method, so that an engineered exosome system (293Texo antiFAP + PFD) with targeted recognition and drug delivery functions is constructed. The system is delivered to the lung in an aerosol inhalation mode, accurate enrichment and stable release of PFD at the pulmonary fibrosis focus can be achieved, and therefore lung tissue structure damage and collagen deposition are effectively relieved, and the anti-fibrosis curative effect is remarkably improved. According to the technology, the problems of low drug delivery efficiency, large side effect, poor targeting property and the like in traditional treatment are solved, and a safe, efficient and accurate treatment strategy is provided for pulmonary fibrosis.

Disclosed herein are deuterium-rich pirfenidones, optionally in combination with one or more additional therapeutic agents, and methods of use thereof; and deuterium-rich pirfenidones, optionally in combination with one or more additional therapeutic agents; pharmaceutical compositions comprising the compounds, processes for the preparation of the compounds; and methods of using the compounds. The compounds and compositions are useful, for example, in the treatment of diseases, disorders, or conditions such as edema.

The application belongs to the technical field of medicines, and particularly relates to a pirfenidone co-crystal, a preparation method thereof, a pharmaceutical composition and application. The pirfenidone co-crystal is prepared from pirfenidone and a co-crystal ligand, and the co-crystal ligand is selected from one of heptanedioic acid, cinnamic acid and saccharin. The pirfenidone co-crystal can not only improve the effect of pirfenidone in relieving acute pancreatitis, but also improve the safety of pirfenidone.

The present invention concerns the compounds of formula (I)wherein R1, R2, R3, X, and Y are as described in the description, and their use as antagonists of the LPA1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and / or nintedanib, in the prevention and / or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.

The present application relates to the technical field of medicine, and particularly relates to an anti-pulmonary fibrosis prodrug compound and a preparation method and application thereof. The prodrug compound is a novel prodrug, and the structure comprises: a) an active drug unit selected from pirfenidone and nintedanib; b) a lung targeting unit selected from diphenyl chloroiodonium salt and a mimic thereof 521; and c) a linker unit which is a responsive linkage sensitive to a biomarker specifically overexpressed in a pulmonary fibrosis microenvironment. The prodrug is stable in the systemic circulation and has no activity or low activity, and can be actively targeted to a pulmonary fibrosis lesion; under the specific stimulation of the PFM, the linker is broken, and the original drug molecule is accurately released, so that the concentration of the drug in the lesion site is significantly increased, the toxic side effects caused by systemic exposure are reduced, and the anti-pulmonary fibrosis effect is enhanced.

Provided are alcohol amine derivatives, a preparation method therefor and the use thereof, and a drug for treating organ fibrosis or pulmonary inflammations caused by acute injury, belonging to the technical field of medicine. The alcohol amine derivatives have structures represented by formula R-1 or formula R-2 and are R-configuration compounds, and exhibit good therapeutic effects on organ fibrosis or pulmonary inflammations caused by acute injury. The results in the pharmacological embodiments show that the alcohol amine derivatives have excellent pharmaceutical effects both on pulmonary inflammations caused by acute injury and various types of organ fibrosis models, the pharmaceutical effects thereof being overall superior to that of S-configuration compounds and positive drugs Nintedanib and Pirfenidone.

The invention discloses an application of a small molecular medicine composition in transdifferentiation of glioma cells. The small molecular medicine composition comprises LiCl, Pirfenidone, Forskolin and RO4929097, and the small molecular medicine composition comprises LiCl, Pirfenidone, Forskolin and RO4929097. The invention further discloses application of the small molecule medicine composition in treating glioma, preparing a medicine for treating glioma and preparing a medicine for inducing glioma cells to be transdifferentiated into neuron-like cells. According to the present invention, with the application of the small molecule drug combination, the glioblastoma line U251 can be induced into the neuron-like cells, the tumor proliferation and the subcutaneous tumor formation ability can be inhibited, and the median lifetime of the xenotransplantation brain glioma model mouse can be prolonged.

In particular, the present invention relates to methods of (i) treating a disease in a subject, (ii) ameliorating a decrease in forced vital capacity in a subject in need thereof, (iii) modulating an avf36 integrin, an avf31 integrin, or both an avf36 integrin and an avf31 integrin in a subject in need thereof, (iv) increasing expression of one or more genes in a subject in need thereof, (v) reducing the expression of one or more genes in a subject in need thereof, and (vi) modulating the activity of at least one gene that affects fibrosis activity in a subject in need thereof, comprising administering a compound of Formula (A), Formula (I), Formula (II) as described herein or (S)-4-((2-methoxyethyl) (4-(5, 6, 7, 8-tetrahydro-1, 3, 4, 5, 6, 7, 8-tetrahydro-1, 3, 4, 5, 6, 7, 8-tetrahydro-1, 3, 4, 5, 6, 7, 8-tetrahydro-1, 3, 4-tetrahydro-1, 3, 4-tetrahydro-1, 3, 4-tetrahydro-1, 3, 4-tetrahydro-1, 3, 4-tetrahydro-1, 3-tetrahydro-1, 3 The present invention relates to a pharmaceutically acceptable salt of 2-(5, 8-naphthyridine-2-yl) butyl) amino)-2-(quinazoline-4-ylamino) butyric acid or a pharmaceutically acceptable salt thereof; and administering to the subject a second drug selected from at least pirfenidone and nintedanib or a salt thereof.

The present application provides a method for removing metal impurities in pirfenidone. The method comprises the following steps: (1) mixing crude pirfenidone, solvent A, water and 1,2-propylenediamine, stirring and dissolving under heating, and stirring for 2 hours under insulation; (2) cooling, crystallization under insulation, collecting filter cake by filtration, washing, and drying under reduced pressure to obtain pirfenidone finished product. The method uses 1,2-propylenediamine as a decontamination reagent, which effectively forms a stable metal complex with metal impurities in the drug. In the provided appropriate solvent system, the complex is dissolved in the solvent system, thereby effectively separating from the pirfenidone solid, and achieving the purpose of removing metal impurities. The method is simple to operate, does not require large-scale equipment modification, completely achieves the requirement of metal impurity control limit of less than 10 ppm, and is suitable for industrial production.

This invention belongs to the field of biomedicine, specifically relating to the application of APOL2 (Apolipoprotein L2) inhibitors in the preparation of products for treating liver fibrosis. The inventors isolated a series of natural tetrodopane-type diterpenes from *Euphorbia pekinensis*, a plant in the Euphorbiaceae family. Anti-liver fibrosis-related activity tests on this series of diterpenes revealed that they significantly inhibited the expression of fibronectin, type I collagen, and α-smooth muscle actin in LX-2 cells. In animal studies, their therapeutic effect was superior to that of pirfenidone, a phase II clinical trial drug for treating liver fibrosis, and they showed no significant toxicity. Mechanistic studies showed that TD1 is an APOL2 inhibitor, and knocking out APOL2 protein in vivo can alleviate the progression of liver fibrosis. In summary, this series of tetrodopane-type diterpenes, especially TD1, shows promise as a candidate drug for treating liver fibrosis and provides a new target for researching novel drugs for treating liver fibrosis.

Disclosed herein are methods of stabilizing or improving lung function in subjects with an interstitial lung disease (ILD) by orally administering a daily amount of between 1600 mg and 2500 mg deupirfenidone. Also disclosed are methods of dose escalation for initial titration, methods of reducing the incidence of emerging adverse events, and methods of directly transitioning patients from other drugs to deupirfenidone without titration.

The treatment of idiopathic pulmonary fibrosis (IPF) using a therapeutically effective amount of a combination of tranilast and pirfenidone, or a therapeutically effective amount of a combination of tranilast and nintedanib, is described. Tranilast may be administered as an adjunctive therapy to the treatment of IPF by either pirfenidone or nintedanib. The combination of tranilast and pirfenidone and the combination of tranilast and nintedanib may also be synergistically effective to treat IPF. Methods and pharmaceutical compositions for treating idiopathic pulmonary fibrosis (IPF) are also described.

Disclosed herein are methods of stabilizing or improving lung function in subjects with idiopathic pulmonary fibrosis by orally administering a daily amount of between 1600 mg and 2500 mg deupirfenidone. Also disclosed are methods of dose escalation for initial titration, methods of reducing the incidence of emerging adverse events, and methods of directly transitioning patients from other drugs to deupirfenidone without titration.

A class of N-substituted phenyl-2-pyridone endoperoxides and their applications belong to the field of organic compound synthesis and pharmaceutical technology. The present invention discloses that this class of endoperoxide compounds can be converted into N-substituted phenyl-2-pyridone at a certain temperature, while releasing singlet oxygen and triplet oxygen. The series of endoperoxides have excellent anti-pulmonary fibrosis effects and can significantly inhibit inflammatory factors, and the effect is significantly better than the marketed drug pirfenidone. The results of anti-lung cancer experiments show that the series of compounds can not only inhibit the proliferation and migration of cancer cells at the cellular level, but also inhibit the growth of tumors at the living level. The safety assessment results show that the series of endoperoxides have good safety, and can treat pulmonary fibrosis, lung cancer, and pulmonary fibrosis combined with lung cancer without obvious damage to other organs. This class of endoperoxides combines multiple therapeutic factors in one, and is expected to be developed into a first-line drug for the treatment of pulmonary fibrosis, lung cancer, and pulmonary fibrosis combined with lung cancer.

The present application relates to the field of drug delivery technology and chronic kidney disease treatment, in particular, a kidney tissue targeted chronic kidney disease treatment drug nano delivery system, which solves the problems of poor targeting, low bioavailability, obvious side effects of existing chronic kidney disease treatment drugs, and insufficient responsiveness and poor safety of existing nano delivery systems. The system comprises a double-responsive nano carrier, an anti-kidney fibrosis drug and a targeting mediation layer. The double-responsive nano carrier is based on methoxy polyethylene glycol modified chitosan-polylactic acid copolymer, contains pH-sensitive hydrazone bonds and redox-sensitive disulfide bonds, and has a core-shell structure. The surface of the carrier is covalently connected with CD13 receptor affinity peptides, and is coated with a polylysine modified hyaluronic acid targeting mediation layer. The drug is pirfenidone or mycophenolate mofetil, which is covalently combined with the carrier through a disulfide bond. The system can realize precise enrichment of kidney lesions and double-responsive controlled drug release, improve the treatment effect, and reduce systemic and local toxicity.