2053 results about "Pyrrolidine" patented technology

The invention provides compounds of formula (1),

and the pharmaceutically acceptable salt thereof, wherein R¹, n and R² are as described herein; compositions thereof; and uses thereof.

A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

The present invention provides a preparation method of (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide. The preparation method comprises: (S)-4-halogen-3-hydroxyl butyric ester as a raw material reacts under the conditions with polar solvent and alkalinity to prepare the crude product of (S)-4-hydroxyl-2-oxo-1-pyrrolidine acetamide; and the crude product is purified. The preparation method is characterized in that inorganic alkali is added for a plurality of times in the reaction process under the condition with alkalinity so as to control the pH value in the reaction to be less than or equal to 8.5. A large quantity of repeated tests are completed to determine that the optimum pH value of the reaction under the condition with alkalinity is less than or equal to 8.5, and the alkali is added in batches to strictly control the pH value of the whole reaction process, so that the alkali conditions required in the reaction can be satisfied and the reaction can be performed completely, and the target product (S)-oxiracetam is prevented from being damaged in the alkaline solution, thereby improving the yield rate of the target product (S)-oxiracetam and reducing the cost.

Compounds which are 1-(2'-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2,3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1-C6 alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d-C6H4-W5 and (CH2)eSW6, where a is 2-5, b is 1-4, c is 1-2, d is 1-2, e is 1-3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1-C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n-C5H3N-Y, where n is 2-4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are -(CH2)p-where p is 3 or 4; R3 is selected from H, C1-C6 alkyl and phenyl; R4 is selected from H, C1-C6 alkyl, benzyl and optionally substitued phenyl; R5 and R6 are each independently selected from H and C<highlight>

Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.

The present invention belongs to gas producing technology. The absorbing liquid for eliminating sulfide from gas mixture includes main absorbent comprising steric hindrance amine and N-methyl diethanolamine; cosolvent of one or several of sulfolane, N-methyl pyrrolidine, polyglycol dialkyl ether, morpholine and its derivative; catalyst of one or several of C2-C12 alkanolamine, piperazine and its derivative, quinoline, urea and metal phthalocyanine complex. Using the absorbing liquid can eliminate H2S, COS, mercaptan, thioether and other sulfide in less steps.

The present invention relates to heterocyclic compounds represented by the formula I or pharmaceutically acceptable salts thereof and antitumor agents containing the heterocyclic compounds as effective components:

wherein X represents nitrogen atom or CH; R₁ represents CH_nF_3-n (wherein n is 1 or 2), hydroxy C₁–C₆ alkyl, NHR₆ [wherein R₆ represents hydrogen atom or COR (wherein R represents hydrogen atom, C₁–C₆ alkyl or C₁–C₆ alkoxy)]; R₂ represents morpholino (which may be substituted with one to four C₁–C₆ alkyl), thiomorpholino, piperidino, pyrrolidinyl (which may be substituted with hydroxy C₁–C₆ alkyl), oxazolidinyl (which may be substituted with one or two C₁–C₆ alkyl) or tetrahydro-1,4-thiazin-1-oxo-4-yl; R₃ and R₄ each represent hydrogen atom or C₁–C₆ alkyl; and R₅ represents hydrogen atom, amino or hydroxyl.

The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I:

wherein A, Q, X₁, X₂, Y, R₁, R₂, R₃, R₄, R₄′, R₅, R₆′ and R₆′ are as described herein.

The present invention relates to pharmaceutical compositions, kits and methods comprising combinations of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof and estrogens. The present invention also relates to pharmaceutical compositions, kits and methods comprising combinations of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof, estrogens and progestins.

Abstract of Disclosure The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain;B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

Provided are an optically-active diazabicyclooctane derivative represented by a formula (F) that is useful as a medicinal intermediate of a ss-lactamase inhibitor, and a method for manufacturing the same. In the formula (F), R1 represents CO2R, CO2M, or CONH2; R represents a methyl group, a tert-butyl group, an allyl group, a benzyl group, or a 2,5-dioxopyrrolidine-1-yl group; M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.

This invention relates to certain 3-aminomethylpyrrolidine derivatives of Formula (I): that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

The present invention relates to the manufacture of the compounds of formula (I)

said compounds of formula (I) being valuable intermediates in the manufacture of Dolastatin 10 analogues, which are useful in the treatment of cancer.

The invention discloses a new synthesizing technique of chiral drug (S)-alpha-ethyl-2-oxo-1-pyrrolidine acetamide ( left Piracetam) intermediate (S)-(+)-2-aminobutanamide hydrochlorate, which comprises the following steps: adopting 2-brobutyrate as initial raw material; aminating; esterifying; ammonolyzing; detaching; looping; obtaining the object compound; making mixed rotary free alkaline (+-)-2-aminobutanamide; adopting half-quantum resolution method to connect chemical detaching salt to evolve salt; removing the detaching agent through alkalization; obtaining the (S)-(+)-2-aminobutanamide hydrochlorate with optical activity; using the mother liquor to make the product. The invention improves the receiving rate and saves the cost of raw material with simply technical operation and low cost, which resolves the resolved mother liquor after racemic action again to reduce the pollution of environment, therefore fitting for industrialized manufacturing.

The present invention is directed to pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

Primary intermediates useful hair coloring systems comprise quaternized pyrrolidine compounds. The invention provides new quaternized pyrrolidine of Formula (1): wherein X is Cl, Br, I, or R3 SO4; R is a C1 to C22 alkyl group or a C1 to C22 mono or dihydroxyalkyl group; R1 and R2 are each independently a C1 to C4 alkyl group; R3 is a C1 to C22 alkyl group or a C1 to C22 mono or dihydroxyalkyl group; R4 is a hydrogen atom, a C1 to C5 alkyl group or such an alkyl group substituted with one or more hydroxy or amino moieties; and R5 is a hydrogen atom or a hydroxy group.

The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.