42 results about "Bioisostere" patented technology

Methods of synthesis of intermediates that are useful as bioisosteres of the indole, benzofuran and benzothiophene scaffold are disclosed.

The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction.

Method for increasing (protracting) half-life of LGP analogs in plasma and novel derivatives of such peptides based on covalently linking them to a tetrazole moiety which acts as a carboxylic acid bioisostere.

The invention relates to cyclic bioisosteres of derivatives of a purine system having a general structural formula R1=—H, —NH2, —Br, —Cl, —OH, —COOH, B=—N═, —CH═, Z=—CH═, —N═, A=—N═ at B=—N═, Z=—CH—, A=—CH═ at B=—N═, Z=—CH—, A=—CH═ at B=—N═, Z=—N═, A=—CH═ at B=—CH═, Z=—CH═, A=—CH═ at B=—CH═, Z=—N═, and their pharmacologically acceptable salts having a normalizing effect on endocellular processes, in particular, it is capable eliminating endocellular metabolic acidosis and capable of binding excessively formed free radicals, in particular, free-radical forms of oxygen, capable of normalizing the nitrergic mechanisms of the cells, and also capable of interreacting with adenosine-sensitive receptors on the membrane of non-nuclear cells and in nuclei-containing cells to decrease the aggregation of thrombocytes. The compounds according to the invention have hepatoprotective effect and can be used for producing pharmaceutical compositions on their base.

An abscisic acid (1) is a plant hormone widely existing in a plant and has important physiological function, however, the application range is limited by the high-speed photo-isomerization characteristics. A bioisosteres cis 2, 3-cyclopropanated abscisic acid analogue of the abscisic acid is compounded through 2, 3-cyclopropanation, and the photostability is four times as that of the abscisic acid.

The present invention provides cysteine and cystine bioisosteres for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing such bioisosteres and methods of using the bioisosteres for treatment of schizophrenia and drug addiction.

The invention belongs to the field of biological medicine and particularly relates to 1,3,4-selenadiazole compound with drug activity. As a few types of heterocyclic selenium exist and BPTES (thiadiazole compounds) has a strong tumor growth suppressing function, a novel synthesizing method is utilized to synthesize multi functional groups substitutional selenadiazole compound, tests verify that the compound has a tumor inhibition effect, an antioxidation effect and a cell protection function; selenadiazole can serve as bioisostere of thiadiazole to substitute; presently, many drugs contain thiadiazole, so that synthesizing selenadiazole derivative with multi functional groups and further optimizing the activity of the medicinal thiadiazole compound have significance in aspects of new medicine development and application and the like.

The invention relates to a benzisoxazole compound and application thereof, in particular relates to the benzisoxazole compound, a stereisomer and pharmaceutically acceptable salt of the benzisoxazole compound, and application of the benzisoxazole compound, belonging to the technical field of medicines. The compound is characterized in that 6-fluorine-3-(4-piperidyl)-1,2-benzisoxazole hydrochloride containing an antipsychotic active structural segment is respectively connected with 6-hydroxychroman, 7-hydroxychroman, 6-hydroxy-4-chromanone, 7-hydroxy-4-chromanone, a flavonoids compound and an isoflavones compound through 1,3-dibromo chloropropane to synthesize nine benzisoxazole compounds based on the bioisosteres and splicing principle; the benzisoxazole compounds as shown in the structural formula below have high application value and wide development and application prospect. The benzisoxazole compounds and pharmaceutically acceptable acid addition salt of the benzisoxazole compound can be combined or individually used as 5-HT2 / D2 receptor antagonists for treating schizophrenia.

A compound and method for treating myocilin glaucoma using a selective Grp94 inhibitor is presented. Clearance of mutant myocilin can be promoted by selectively targeting the endoplasmic reticulum (ER) chaperone Grp94 using siRNA knockdown or small molecule inhibitors. Grp94 contributes to the intracellular accumulation of mutant myocilin. Tailored treatments aimed at disrupting the Grp94 / mutant myocilin interaction can be used as a new therapeutic strategy for myocilin glaucoma. The inventors developed a compound having a general backbone structure of geldanamycin (GDA) and radicicol (RDC) in which a more hydrophobic surrogate of the quinone in GDA is linked to the resorcinol in RDC through a cis-amide bioisostere.

The invention discloses a therapeutically active compositions of matter and member species thereof which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I<1>) or (I<2>), or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment R is hydrogen; R is cyclohexyl; and R is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisotere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic alpha 1-antagonist and beta 1-agonist activity, calcium channel inhibitory activity, antineoplastic activity, and phosphodiesterase type IV inhibitor activity.

The invention provides a marine organism health food formula and a manufacturing technology. According to the marine organism health food formula and the manufacturing technology disclosed by the invention, alitta succinea is optimally chosen, particularly, the alitta succinea produced in a water area of Dongshan Island of Zhangzhou, Fujian is utilized as a raw material, and a special technology is utilized to process and manufacture the alitta succinea into health food. The alitta succinea, especially the alitta succinea produced in the water area of Dongshan Island of Zhangzhou, Fujian contains rich amino acid of glutamic acid and the like, rich trace elements of Zn <2+> and the like and active substances of taurine, lumbrukinase, plasmin, bioactive peptide, biosterin and the like. According to the processing method disclosed by the invention, the special technology is utilized to process the alitta succinea, safety and hygiene of health food are guaranteed, the alitta succinea can be eaten directly, effective ingredients in the alitta succinea are prevented from being damaged, and the prepared health food has comprehensive nutritional ingredients and complete health care functions, can resist ageing and restore and soften blood vessels, improves a sexual hormone level in a human body, enhances human body immunity, prevents cancer, resists tumors and can prevent and treat refractory aphthous stom-atitis.

Disclosed are compounds of formula (I):or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.

Augmented or synergized anti-inflammatory constructs are disclosed including anti-inflammatory amino acids covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids and ketone bodies. Further conjugation with a choline bioisostere or an additional anti-inflammatory moiety further augments the anti-inflammatory activity.

The invention belongs to the field of biological medicines and specifically relates to a method and a technique forsynthesizing a bioactive poly-functional group substituted 1,3,4-selenadiazole derivative by adopting a mild condition. According to the method, a selenadiazole ring has various functional groups, so that the selenadiazole can be used as bioisosteres of thiadiazole. The requirements for the reaction conditions of thiadiazole and similar derivatives are higher, so that the method disclosed by the invention is mild in reaction condition; the selenadiazole derivative with various functional groups can be synthesized, the activity of the officinal thiadiazole compound can be further optimized and the method has significance at the aspects of development and application for new drugs.

Provided herein are compounds of the formula (I):as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Described are processes for the preparation of 2,2′-di(pyridin-4-yl)-1H,1′H-5,5′-bibenzo[d]imidazole (which may also be known as 5,5′bis-[2-(4-pyridinyl)-1H-benzimidazole]), referenced herein by the INN name ridinilazole, and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites or prodrugs thereof. The invention also relates to various compositions of purified ridinilazole, to various crystalline forms of ridinilazole, to processes for their preparation and to related pharmaceutical preparations and uses thereof (including their medical use and their use in the efficient large-scale synthesis of ridinilazole).

Pharmaceutical, odontological, cosmetic and dermatological compositions comprising addition salts of trichloroacetic acid, one or more hydroxyacids and optionally glutamic acid or glutamic acid bioisosteres and phytic acid are useful for the peeling of the gingival collar, skin peeling, for resurfacing, treating skin hyper pigmentation, control sebum production, acne, pore size reduction and reducing the appearance of scars without causing undesirable side effects and contrast in coloration of the treated skin, for stimulation of the fibroblasts, transdermal biorevitalization, stimulation of the production of new collagen, for aesthetic improvement, for skin lightening, skin beautifying, skin firming and skin rejuvenation.

Described are methods of making 2, 2 '-bis (pyridin-4-yl)-1H, 1' H-5, 5 '-dibenzo [d] imidazole (also can be referred to as 5, 5'-bis-[2-(4-pyridinyl)-1H-benzimidazole]) (as mentioned herein as the INN name ridinilazole), and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites, or prodrugs thereof. The present invention also relates to various compositions of purified ridinilazole, various crystal forms of ridinilazole, methods for their preparation, and related pharmaceutical formulations and uses thereof, including their medical uses and their uses in efficient large scale synthesis of ridinilazole.

Provided herein are compounds of the formula (I):as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

The invention discloses a hydroxyl cyclohexanediamide compound and a preparation method and application thereof, the compound has a structure as shown in a formula I, and the structure of an R group is as shown in A1-A5. According to the drug nucleus similarity principle and the bioisostere principle, 1 alpha, 2 beta-O, O-dicaffeoyl cyclopent-3beta-alcohol which is naturally sourced is used as a primer, and the hydroxyl cyclohexanediamide compound with the antiviral effect is designed and synthesized. The hydroxyl cyclohexanediamide compounds designed and synthesized by the invention have strong anti-respiratory syncytial virus activity and low cytotoxicity, the anti-RSV selectivity index of the hydroxyl cyclohexanediamide compounds is higher than that of a positive control drug ribavirin and a natural primer methyl 3, 4-O, O-dicaffeoylquinate, and part of the hydroxyl cyclohexanediamide compounds are superior to that of 1 alpha, 2 beta-O, O-dicaffeoylcyclopent-3 beta-alcohol. Meanwhile, the half-life period is prolonged, and the oxidation stability is improved.

The invention discloses sulfonium salt derivatives as well as a preparation method and medical application thereof, and particularly relates to a compound as shown in a formula I. The sulfonium salt derivatives with brand new structures are designed according to a bioisostere principle, and the compounds have good tolerance to gastric acid; compared with a natural product, the sulfonium salt compound provided by the invention has stronger alpha-glucosidase inhibitory activity, can be used as an onium salt type alpha-glucosidase inhibitor, and is mainly prepared from 1, 2-O-isopropylidene furan D-glucose as a raw material through a one-pot method. The onium salt derivative molecule with alpha-glucosidase inhibitory activity is obtained through multi-step reaction, and the molecule has hypoglycemic activity.

Prolyl endopeptidase (PE) activity in lung samples is detected by contacting the lung sample with a probe comprising a —P—X— (or —X—P—, —P—X—P—) PE recognition site, wherein P is a prolyl bioisostere, X is a residue that is not a prolyl bioisostere or is a prolyl bioisostere flanked on each side by a residue that is not a prolyl bioisostere, and “-” is an amide bond, under conditions wherein PE activity of the sample specifically hydrolyzes an amide bond of the recognition site to generate an optical signal; and (b) detecting the signal.

The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.

Pharmaceutical, odontological, cosmetic and dermatological compositions comprising addition salts of trichloroacetic acid, one or more hydroxyacids and optionally glutamic acid or glutamic acid bioisosteres and phytic acid are useful for the peeling of the gingival collar, skin peeling, for resurfacing, treating skin hyper pigmentation, control sebum production, acne, pore size reduction and reducing the appearance of scars without causing undesirable side effects and contrast in coloration of the treated skin, for stimulation of the fibroblasts, transdermal biorevitalization, stimulation of the production of new collagen, for aesthetic improvement, for skin lightening, skin beautifying, skin firming and skin rejuvenation.