A1R antagonists(Adenosine A1 receptor antagonists), A2aR antagonists(Adenosine A2a receptor antagonists), cGMP-PDE inhibitors(3',5'-cyclic phosphodiesterase inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesCardiovascular Diseases+ [1]

Active Indication

AsthmaAsthmatic bronchitisHeart Failure

Inactive Indication-

Originator Organization

Nichi-Iko Pharmaceutical Co., Ltd.

Active Organization

Nichi-Iko Pharmaceutical Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (20 Feb 1959),

AsthmaAsthmatic bronchitisHeart Failure

Regulation-

Structure/Sequence

Molecular FormulaC10H14N4O3

InChIKeyKYHQZNGJUGFTGR-UHFFFAOYSA-N

CAS Registry603-00-9

100 Clinical Results associated with Proxyphylline

100 Translational Medicine associated with Proxyphylline

100 Patents (Medical) associated with Proxyphylline

347

Literatures (Medical) associated with Proxyphylline

01 Nov 2024·Nature Chemistry

Modular alkene synthesis from carboxylic acids, alcohols and alkanes via integrated photocatalysis

Article

Author: Ma, Jun-An ; Wu, Jie ; Yin, Ruize ; Zeng, Hao ; Zhao, Yu

Alkenes serve as versatile building blocks in diverse organic transformations. Despite notable advancements in olefination methods, a general strategy for the direct conversion of carboxylic acids, alcohols and alkanes into alkenes remains a formidable challenge owing to their inherent reactivity disparities. Here we demonstrate an integrated photochemical strategy that facilitates a one-pot conversion of these fundamental building blocks into alkenes through a sequential C(sp³)-C(sp³) bond formation-fragmentation process, utilizing an easily accessible and recyclable phenyl vinyl ketone as the 'olefination reagent'. This practical method not only offers an unparalleled paradigm for accessing value-added alkenes from abundant and inexpensive starting materials but also showcases its versatility through various complex scenarios, including late-stage on-demand olefination of multifunctional molecules, chain homologation of acids and concise syntheses of bioactive molecules. Moreover, initiating from carboxylic acids, alcohols and alkanes, this protocol presents a complementary approach to traditional olefination methods, making it a highly valuable addition to the research toolkit for alkene synthesis.

01 Jul 2024·YAKUGAKU ZASSHI

Investigation of Mechanism of Creming-down Phenomenon and Development of High-order Functions Using Tea Catechins

Review

Author: Ishizu, Takashi

An aqueous solution of 2,3-cis gallate type catechin (-)-epigallocatechin-3-O-gallate (EGCg) and caffeine afforded a precipitate of Creaming-down Phenomenon, which crystallized slowly for about three months to give a colorless block crystal. By X-ray crystallographic analysis, the crystal was determined to be a 2 : 2 complex of EGCg and caffeine, in which caffeine molecules were captured in a hydrophobic space formed with three aromatic A, B, and B' rings of EGCg. It was considered that the solubility of the 2 : 2 complex in water rapidly decreased and the 2 : 2 complex precipitated from aqueous solution. The hydrophobic spaces of EGCg captured a variety of heterocyclic compounds, and the molecular capture abilities of heterocyclic compounds using EGCg from the aqueous solutions were evaluated. Since the C ring of EGCg has two chiral carbon atoms, C₂ and C₃, the hydrophobic space of EGCg was a chiral space. EGCg captured diketopiperazine cyclo(Pro-Xxx) (Xxx=Phe, Tyr) and pharmaceuticals with a xanthine skeleton, proxyphylline and diprophylline, in the hydrophobic space, and recognized their chirality.

05 Jun 2024·Crystal Growth & Design

Unraveling a Unique Metastable Phase of a Proxyphylline Cocrystal Exclusively Produced by Compressed Carbon Dioxide

Author: Subra-Paternault, Pascale ; Cercel, Hugo ; Marre, Samuel ; Ziri, Isabelle ; Denux, Dominique ; Cartigny, Yohann ; Nimod, Léa ; Ercicek, Fatma ; Brandel, Clément ; Harscoat-Schiavo, Christelle ; Monnier, Olivier ; Marchivie, Mathieu

In this work, racemic proxyphylline (( ± )-PXL, a chiral drug) was cocrystd. for the first time with 4-hydroxybenzoic acid (4-HBA) from three solvents (acetone, Et acetate, and isobutanol) and using CO₂ as an antisolvent.The obtained solid forms were compared to those produced by liquid-assisted grinding (LAG).It is shown that though both methods produce a racemic compound ( ± )-PXL₁:4-HBA₁ cocrystal, LAG promotes the crystallization of an orthorhombic Pna2₁ form (Phase I), whereas CO₂-assisted crystallization gives rise to an original monoclinic C2/c form with partial inclusion of CO₂ and water mols. (Phase II).The structure of Phase II originates from this inclusion since this phase is never obtained in the absence of CO₂.Concomitant cocrystn. of Phase I and Phase II occurs during CO₂-assisted crystallization in proportions that vary with solvents and temperatureOur study shows that Phase II transforms progressively into Phase I upon storage or heating.

100 Deals associated with Proxyphylline

External Link

KEGG	Wiki	ATC	Drug Bank
D01771	Proxyphylline	R03DA03	DB13449

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Asthma	Japan	Nichi-Iko Pharmaceutical Co., Ltd.	20 Feb 1959
Asthmatic bronchitis	Japan	Nichi-Iko Pharmaceutical Co., Ltd.	20 Feb 1959
Heart Failure	Japan	Nichi-Iko Pharmaceutical Co., Ltd.	20 Feb 1959

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