Bisamide sarcomere activating compounds and uses thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

PROCESS FOR PREPARING ALKYL PYROGLUTAMIC ACIDS

Disclosed are compounds of formulae: 17.-. (canceled)9. A composition according to further comprising at least one additive claim 8 , excipient or diluent.10. A composition according to claim 8 , comprising at least two compounds of formula (II).1320.-. (canceled) This application claims benefit of U.S. Provisional Application Ser. No. 61/576,023, filed Dec. 15, 2011, the disclosure of which is incorporated herein by reference in its entirety.This disclosure relates to compounds and compositions suitable for use in surfactants. In particular, the disclosure relates to alkyl pyroglutamic acid compounds.The large shift towards environmentally friendly surfactants has resulted in the need for the industry to provide readily biodegradable and non-toxic surfactants and additives. Surfactants and additives with renewable content can be preferable to their synthetic counterparts with demand being driven by life sustainability initiatives, preferred buying programs and consumer trends.Alcohol ethoxy sulfates (AES) is a class of anionic surfactant commonly used in personal care shampoo formulation. The trace byproduct from the manufacturing processes of AES (alkoxylation and sulfation), and the skin irritancy associated with AES are not desirable in personal care applications. An ethylene oxide-free (EO-free) and sulfate-free surfactant that is non-irritating is much more preferable in personal care.Common EO-free and sulfate-free surfactant personal care surfactants are fatty acid soaps, betaines, alpha olefin sulfonates, sulfosuccinates, esters, alkyl polyglucosides, fatty acyl amino acids, fatty amine oxides, and quaternaries. Two common commercially available amino acid surfactants are acyl glutamate and acyl sarcosinate. Acyl glutamate is derived from natural fatty acids and natural glutamic acid, while acyl sarcosinate is derived from natural fatty acids and synthetic glycine. In either case, these amino acid surfactants are commonly accepted as non-toxic and mild. ...

Process for preparing alkyl pyroglutamic acids

Disclosed are compounds of formulae: and salts, hydrates, or solvates thereof, where R 1 , R 2 , R 3 , R 5 , and R 6 are defined herein, compositions containing these compounds, methods of preparing these compounds, and methods of using these compounds in a variety of applications, such as a surfactant or additive in personal care products.

化合物和含有该化合物的润滑剂组合物

公开了包括(i)二羰基、(ii)聚胺的伯胺部分和(iii)烃基羰基的反应产物的咪唑啉化合物。还公开了包括咪唑啉化合物的润滑剂和燃料添加剂组合物。

HYDRAZIDE COMPOUND AND ITS APPLICATION FOR PEST CONTROL

1. Соединение гидразида, представленное формулой (1):где G представляет 5-членную гетероциклическую группу, представленную следующей формулой G-1, G-2 или G-3:гдеикаждая представляет связь, исвязана с фрагментомв формуле (1),Rпредставляет C1-C4 галогеналкильную группу,Yпредставляет атом кислорода, атом серы или группу NR,Yпредставляет атом кислорода, атом серы, группу NRили метиленовую группу,Yпредставляет атом кислорода, атом серы, группу NRили метиленовую группу,Rпредставляет C1-C6 алкильную группу, C2-C6 алкенильную группу, C2-C6 алкинильную группу, C3-C6 циклоалкильную группу, C4-C7 циклоалкилалкильную группу, C2-C6 алкилкарбонильную группу, C2-C6 алкоксикарбонильную группу, C2-C6 алкиламинокарбонильную группу, C3-C9 диалкиламинокарбонильную группу, фенильную группу, цианогруппу, формильную группу или атом водорода,M представляет атом кислорода или атом серы,Q, Q, Qи Qнезависимо представляют атом азота или группу CR,Rпредставляет необязательно галогенированную C1-C6 алкильную группу, необязательно галогенированную C1-C6 алкоксильную группу, нитрогруппу, цианогруппу, атом галогена или атом водорода,m представляет целое число от 0 до 5,Rпредставляет необязательно галогенированную C1-C6 алкильную группу, необязательно галогенированную C1-C6 алкоксильную группу, C1-C6 алкилтиогруппу, C1-C6 алкилсульфинильную группу, C1-C6 алкилсульфонильную группу, нитрогруппу, цианогруппу или атом галогена,при условии, что когда m является целым числом от 2 до 5, группы Rмогут быть одинаковыми или отличаться друг от друга,Rи Rнезависимо представляют углеводородную группу с цепью С1-С12, необязательно замещенную с помощью группы, выбранной из группы Е1, бензоильную группу, нео� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 207/18 (13) 2011 136 823 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2011136823/04, 05.02.2010 (71) Заявитель(и): СУМИТОМО КЕМИКАЛ КОМПАНИ, ЛИМИТЕД (JP) Приоритет(ы): (30) Конвенционный приоритет: ...

Hydrazide compound and use of the same in pest control

There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitro-gen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

(1S,3aR,9bS)-1-Phenyl-2,3,3a,4,5,9b-hexahydro-1H-benzo[e]indole derivatives and 3,4-diarylpyrrolidin-2-one derivatives having inhibition of monoamine reuptake

본 발명은 단가아민 재흡수 억제 활성을 보이는 (1S,3aR,9bS)-1-페닐-2,3,3a,4,5,9b-헥사하이드로-1H-벤조[e]인돌 유도체와 3,4-다이아릴피롤리딘-2-온 유도체, 이들 화합물의 제조방법, 그리고 이들 화합물이 유효성분으로 함유된 약학적 조성물에 관한 것이다. The present invention provides (1S, 3aR, 9bS) -1-phenyl-2,3,3a, 4,5,9b-hexahydro-1H-benzo [e] indole derivative with 3,4 showing monovalent amine reuptake inhibitory activity. -Diarylpyrrolidin-2-one derivatives, methods for preparing these compounds, and pharmaceutical compositions containing these compounds as active ingredients.

Method for preparing protected 4-aminomethyl-pyrrolidone-3-on

본 발명은 제 1 단계에서 하기 화학식 5의 화합물을 용매중에서 수소압력하에 라니-니켈 촉매와 반응시켜 하기 화학식 6의 화합물을 제조하고, 제 2 단계에서 염기 존재하에 용매중에서 화학식 6 화합물의 아미노기를 보호기화 반응시켜 하기 화학식 7의 화합물을 제조한 후, 제 3 단계에서 화학식 7의 화합물을 용매중에서 수소압력하에 금속 촉매와 반응시켜 이중결합을 선택적으로 환원시킴을 특징으로 하여 퀴놀론계 항생제를 합성하는데 필수적으로 사용되는 중간체인 하기 화학식 1의 보호된 4-아미노메틸-피롤리딘-3-온을 제조하는 방법 및 이 방법을 수행하는데 중간체로서 생성되는 신규한 화학식 6 및 7의 화합물에 관한 것이다: 상기식에서 P 1 및 P 2 는 각각 독립적으로 아세틸, t-부톡시카보닐 또는 피발로일을 나타낸다.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

A process for preparing a compound of formula (1) in which P1 and P2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P1 and P2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

PROCESS FOR PREPARING A PROTECTED 4-AMINOMETHYL-PYRROLIDIN-3-ONE

Azabicyclo compound derivatives

Azabicycloamine compounds and their salts of formula (I) are prepared. In the formula (I), R=H or amine protecting groups; R1,R2=H, lower alkyl, acyl, substituted (or unsubstituted) benzoyl, or naphtoyl, alkoxycarbonyl or substituted (or unsubstituted) benzyloxycarbonyl; n = 1-4. (I) are useful as intermediates in the preparation of antibacterial quinolone carboxylic acid derivatives, cephalosporin antibiotics and other drugs.

Process for preparing protected 4-aminomethyl-pyrrolidin-3-one

本文公开了制备式(1)化合物的方法,其中P 1 和P 2 是保护基;该方法包括a)使其中P 1 如式(1)中定义的式(5)化合物与阮内镍催化剂在溶剂中,在氢气中反应产生其中P 1 如式(1)中定义的式(6)化合物;b)保护氨基产生其中P 2 如式(1)中定义的式(7)化合物;和c)选择性地还原双键产生式(1)化合物。

Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak)

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Process for preparing a protected 4-aminomethyl-pyrrolidi-3-one

A process for preparing a compound of formula (1) in which P 1 and P 2 are protecting groups; comprising a) reaction of a compound of formula (5) wherein P 1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P 1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P 1 and P 2 are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

Process for preparing alkyl pyroglutamic acids

Disclosed are compounds of formulae: and salts, hydrates, or solvates thereof, where R 1 , R 2 , R 3 , R 5 , and R 6 are defined herein, compositions containing these compounds, methods of preparing these compounds, and methods of using these compounds in a variety of applications, such as a surfactant or additive in personal care products.

Parasite- and hygienic pest-controlling agent

There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: wherein A 1 is C—X 3 or nitrogen atom, etc., A 2 and A 3 are C—H, etc., A 4 is C—H or nitrogen atom, etc., G is G-2a, etc., W is oxygen atom or sulfur atom, X 1 is halogen atom, trifluoromethyl, etc., X 2 is hydrogen atom, halogen atom, trifluoromethyl, etc., X 3 is hydrogen atom, halogen atom, etc., Y 1 is hydrogen atom, halogen atom, methyl, etc., R 1 is trifluoromethyl, etc., R 2 is E-3a, etc., R 3 is hydrogen atom, etc., p is an integer of 0 to 2.

Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak)

Bisamide sarcomere activating compounds and uses thereof

本發明提供式(I)化合物或其醫藥學上可接受之鹽、包含本發明化合物之醫藥組合物、用於製造本發明化合物之方法及其治療用途。

Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3)

The invention relates to AKR1C3 inhibitors of the formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of menstrual complaints and endometriosis.

Compounds and Lubricating Compositions Containing the Compounds

An imidazoline compound comprising the reaction product of (i) a dicarbonyl, (ii) a primary amine moiety of a polyamine, and (iii) a hydrocarbyl carbonyl is disclosed. Lubricant and fuel additive compositions comprising the imidazoline compound are also disclosed.

Pyrrolo [2,3-d]pyrimidine derivatives as inhibitors of janus kinases (jak)

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Process for preparing a protected 4-aminomethyl-pyrrolidin-3-one

A process for preparing a compound of formula (1) in which P?1 and P2¿ are protecting groups; comprising a) reaction of a compound of formula (5) wherein P1 is as defined for formula (1); with a Raney-nickel catalyst in a solvent under hydrogen to produce a compound of formula (6) wherein P1 is as defined for formula (1); b) protecting the amino group to produce a compound of formula (7) wherein P?1 and P2¿ are as defined for formula (1); and c) selective reduction of the double bond to produce the compound of formula (1).

Process for the preparation of protected 4-aminomethyl-pyrrolidin-3-one.

Process for the preparation of a protected 4-aminomethyl-pyrrolidin-3-one

Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus- related kinases (jak)

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3)

The invention relates to AKR1C3 inhibitors of the formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of menstrual complaints and endometriosis.

Pyrrolo (2, 3 -d)pyrimidine derivatives as inhibitors of janus kinases (jak)

HYDRAZIDE COMPOSITE AND ITS USE IN PEST CONTROL

Reivindicacion 1: Un compuesto de hidrazida representado por la formula (1) en donde, G representa un grupo heterocíclico de 5 miembros representado por la las formulas (2), (3) o (4) en donde a Àl y b Àl representan cada uno un enlace y el b Àl está unido con el resto de formula (5) en la formula (1); R1 representa un grupo haloalquilo C1-4, Y1 representa un átomo de oxigeno, un átomo de azufre o un grupo NR7, Y2 representa un átomo de oxigeno, un átomo de azufre, un grupo NR7 o un grupo metileno, Y3 representa un átomo de oxígeno, un átomo de azufre, un grupo NR7 o un grupo metileno, R7 representa un grupo alquilo C1-6, un grupo alquenilo C2-6, un grupo alquinilo C2-6, un grupo cicloalquilo C3-6, un grupo cicloalquilalquilo C4-7, un grupo alquil C2-6-carbonilo, un grupo alcoxi C2-6-carbonilo, un grupo alquil C2-6-aminocarbonilo, un grupo dialquil C3-9-aminocarbonilo, un grupo fenilo, un grupo ciano, un grupo formilo o un átomo de hidrogeno, M representa un átomo de oxígeno o un átomo de azufre, Q1, Q2, Q3 y Q4 representan, de modo independiente, un átomo de nitrogeno o un grupo CR3; R3 representa un grupo alquilo C1-6 opcionalmente halogenado, un grupo alcoxi C1-4 opcionalmente halogenado, un grupo nitro, un grupo ciano, un átomo de halogeno o un átomo de H, m representa un numero entero de 0 a 5, R2 representa un grupo alquilo C1-6 opcionalmente halogenado, un grupo alcoxi C1-6 opcionalmente halogenado, un grupo alquil C1-6-tio, un grupo alquil C1-6-sulfinilo, un grupo alquil C1-6-sulfonilo, un grupo nitro, un grupo ciano o un átomo de halogeno, siempre que, cuando m es un numero entero de 2 a 5, R2 puedan ser iguales o diferentes entre sí, R5 y R6 representan, de modo independiente, un grupo hidrocarbonado de cadena C1-12 opcionalmente sustituido con un grupo seleccionado del grupo E1, un grupo benzoílo opcionalmente sustituido con un grupo seleccionado del grupo E2, un grupo alquil C2-6-carbonilo, un grupo alcoxi C2-6-carbonilo, un grupo cicloalquilo C3-12, un ...

(E) -alpha, beta-unsaturated amide compound, preparation method and application thereof

本发明提供一类新的由式I所表示的(E)‑α,β‑不饱和酰胺化合物，还涉及这类化合物的制备方法及其制药用途。所述化合物具有保护神经细胞的作用和免疫调节活性。式I中R 1 、R 2 和R 3 的定义见说明书。

Hydrazide compound,its use,pest- controlling composition,and method for controlling pest

Method of enantiometrically selective nucleophilic addition reaction to carbonyl of enamide and method of synthesizing optically active alpha-hydroxy-gamma-keto acid ester and hydroxydiketone

A method of enantiometrically selective nucleophilic addition reaction to carbonyl, which enables asymmetric synthesis of optically active α-hydroxy-Ϝ-keto acid esters, optically active α-hydroxy-Ϝ-amino acid esters, hydroxydiketone compounds, etc. being useful as a raw material or synthetic intermediate for the production of pharmaceutical products, agricultural chemicals, perfumes, functional polymers, etc. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (-OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.

Pyrrolo [2,3-d]pyrimidine derivatives as inhibitors of janus-related kinases (jak)

피롤로{2,3-d}피리미딘 유도체, 야누스 키나아제(JAK) 억제제로서의 이의 용도, 및 이를 함유하는 약학 조성물.

Method for producing olefin

Pyrrolo [2,3-d] pyrimidine derivatives as Janus-associated kinase (JAK) inhibitors

Claimed are pyrrolo[2,3-d]pyrimidine derivatives of Formula I, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

METHOD OF OBTAINING PROTECTED 4-AMINOMETHYLPROLIDIN-3-SHE

Способ получения соединения формулы (1), в которой Pи P- защитные группы; включающий a) взаимодействие соединения формулы (5), где P- такой, как определено для формулы (1); с катализатором никель Ренея в растворителе в атмосфере водорода с получением соединения формулы (6), где P- такой, как определено для формулы (1); b) защиту аминогруппы с получением соединения формулы (7), где Pи P- такие, как определено для формулы (1); и c) селективное восстановление двойной связи с получением соединения формулы (1).Международная заявка была опубликована вместе с отчетом о международном поиске. A method for preparing a compound of formula (1), wherein Pi and P are protecting groups; comprising a) reacting a compound of formula (5), wherein P is as defined for formula (1); with a Raney nickel catalyst in a solvent under a hydrogen atmosphere to produce a compound of formula (6), where P is as defined for formula (1); b) protecting the amino group to give a compound of formula (7), where Pi and P- are as defined for formula (1); and c) selective restoration of a double bond to produce a compound of formula (1). The international application was published along with an international search report.

Bisamide sarcomere activating compounds and uses therof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

METHOD OF ENANTIOMETRICALLY SELECTIVE NUCLEOPHILIC ADDITION REACTION TO CARBONYL OF ENAMIDE AND METHOD OF SYNTHESIZING OPTICALLY ACTIVE α-HYDROXY-Ϝ-KETO ACID ESTER AND HYDROXYDIKETONE

A method of enantiometrically selective nucleophilic addition reaction to carbonyl, which enables asymmetric synthesis of optically active α-hydroxy-Ϝ-keto acid esters, optically active α-hydroxy-Ϝ-amino acid esters, hydroxydiketone compounds, etc. being useful as a raw material or synthetic intermediate for the production of pharmaceutical products, agricultural chemicals, perfumes, functional polymers, etc. In this method, the nucleophilic addition reaction of enamide compound accompanied by hydroxyl (-OH) formation to carbonyl is carried out in the presence of a chiral catalyst with copper or nickel.

Combination of pyrrolo [2,3-d] pyrimidine derivatives with one or more additional agents such as janus kinase inhibitors (JAK)

Un compuesto de fórmula IA que tiene la estructura:**Fórmula** o una sal farmacéuticamente aceptable del mismo, en la que Y es -A-R5, en el que A es un enlace, --(CH2)k-- o --(CD2)k-- y R5 es un alquilo cadena de cadena lineal o ramificada C1-C6, cicloalquilo C3-C6, arilo o --NRa'Rb', o es una estructura de anillo monocíclico o bicíclico, insaturado, saturado o parcialmente saturado que contiene un total de cinco a once átomos que tiene de uno a tres heteroátomos seleccionados independientemente entre el grupo que consiste en oxígeno, nitrógeno y azufre, en el que dicho alquilo, cicloalquilo C3-C6, arilo o estructura de anillo monocíclico o bicíclico además se sustituye opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en deuterio, halo, alquilo de cadena lineal o ramificada C1-C6, CN, hidroxilo, CF3, --ORe, --NReRf, --S(O)pRe y cicloalquilo C3- C6, en los que dicho alquilo y cicloalquilo pueden sustituirse opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en halo, CN, hidroxilo, CONH2 y SO2CH3, en el que (a) Ra' y Rb' son independientemente hidrógeno, deuterio, alquilo de cadena lineal o ramificada C1-C6, cicloalquilo C3-C6, arilo, (alquilo de cadena lineal o ramificada C1-C6)arilo, heteroarilo o (alquilo de cadena lineal o ramificada C1- C6)heteroarilo, en el que dicho alquilo y cicloalquilo pueden sustituirse opcionalmente con uno o más Rc', o (b) Ra' y Rb' juntos forman una cadena que comprende --(CRc'Rd')y--, en el que Rc' y Rd' son independientemente hidrógeno, deuterio, alquilo de cadena lineal o ramificada C1-C6, arilo, (alquilo de cadena lineal o ramificada C1- C6)arilo, heteroarilo, (alquilo de cadena lineal o ramificada C1-C6)heteroarilo, halo, CN, hidroxilo, CF3, CONH2, -- 20 ORe, --NReRf o --S(O)pRe; en el que Re y Rf son independientemente hidrógeno, deuterio, alquilo de cadena lineal o ramificada C1-C6 o cicloalquilo C3-C6, en los que dicho ...

Compositions for organ preservation

Composition for organ preservation

本发明涉及保存器官或组织活性的领域，所述器官或组织待移植到需要这种移植的接受者中。特别地，本发明涉及sigma 1受体激动剂化合物在保藏溶液中的用途以及包含sigma 1受体激动剂化合物的保藏溶液。

Pyrrolo [2,3-d] pyrimidine derivatives

EN LA PRESENTE, SE DESCRIBEN DERIVADOS DE PIRROLO [2,3-D]PIRIMIDINA, SU USO COMO INHIBIDORES DE LA QUINASA JANUS (JAK) Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. THEREOF, PIRROLO [2,3-D] PYRIMIDINE, ITS USE AS INHIBITORS OF THE JANUS KINASE (JAK) AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM ARE DESCRIBED.

ESTRA-1, 3,5 (10), 16 TETRAENE-3-CARBOXAMIDS FOR THE INHIBITION OF THE 17B-HYDROXIESTEROID DEHYDROGENASE (AKR1 C3)

Inhibidores de AKR1C3 de fórmula (I) útiles en el tratamiento y/o profilaxis de enfermedades, en especial de trastornos de sangrado y endometriosis

Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (akr1 c3)

The invention relates to AKR1C3 inhibitors of the formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of menstrual complaints and endometriosis.

Pyrrolo[2,3-D]pyrimidine derivatives

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

As pyrrolo- [2,3 D] pyrimidine derivatives of Zhan Nasi associated kinases (JAK) inhibitor

本申请中描述的是吡咯并{2,3‑d}嘧啶衍生物、它们作为詹纳斯激酶(JAK)抑制剂的用途以及包含它们的药物组合物。

Compositions for organ preservation

The invention relates to the field of preserving the viability of organs or tissues to be transplanted into a recipient in need of such a transplantation. In particular, the invention relates to use of a sigma 1 receptor agonist compound in preservation solutions and preservation solutions comprising a sigma 1 receptor agonist compound.

Novel compound having skin-whitening, anti-oxidizing and ppar activities and medical use therefor

The present invention relates to a novel compound having skin-whitening, anti-oxidizing and PPAR activities and to a medical use therefor. Compounds according to the present invention can be used to advantage in skin-whitening pharmaceutical compositions or cosmetics as they have a skin-whitening activity whereby tyrosinase is inhibited, and can be used to advantage in the prevention or treatment of skin ageing or the like as they have an anti-oxidizing activity, and can also be used as pharmaceutical compositions or health foods which are useful in preventing and treating obesity, metabolic disease or cardiovascular disease as they have PPAR activity and, more particularly, PPARα and PPARγ activity.

Cyclic lipids and methods of use thereof

The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

Conjugated diynes and their use as flavor modifiers

The present disclosure generally provides conjugates diynes, particularly 6,8-diyne amides, and the use of such compounds and related compounds as flavor modifiers. In some aspects, the disclosure provides compositions that include such conjugated diynes, such as compositions that include such conjugated diynes and one or more additional compounds, such as a sweetener, salt, a glutamate, an arginate, and the like. In some other aspects, the disclosure provides methods of reducing or eliminating the amount of sweetener, salt, glutamate, or arginate in a food or beverage product.

Compuestos de bisamida que activan el sarcomero y sus usos.

La presente invención provee un compuesto de fórmula (I) o una sal farmacéuticamente aceptable de este, composiciones farmacéuticas que comprenden un compuesto de la invención, un método para fabricar compuestos de la invención y usos terapéuticos de estos. (ver Fórmula).

Bisamide sarcomere activating compounds and uses thereof

共役ジイン、及びフレーバー改質剤としてのその使用

本開示は、概して、共役ジイン、特に６，８－ジインアミド、並びにかかる化合物及び関連化合物のフレーバー改質剤としての使用を提供する。いくつかの態様において、本開示は、かかる共役ジインを含む特定の組成物、例えばかかる共役ジインと１つ以上の追加の化合物、例えば甘味料、塩、グルタメート、アルギネートなどとを含む組成物を提供する。他のいくつかの態様において、本開示は、食品又は飲料製品における甘味料、塩、グルタメート、又はアルギネートの量を低減又は除去する方法を提供する。

Cyclic lipids and methods of use thereof

The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

Verfahren zur herstellung eines geschützten 4- aminomethyl-pyrrolidin-3-ons

環狀脂質及其使用方法

本發明詳述用於遞送核酸序列、多肽或肽以用於針對傳染原進行疫苗接種之各種脂質、組合物及/或最佳化系統及遞送載體的方法。

化合物、包含该化合物的组合物、成型体、染色物和光学层

本发明的目的在于提供一种新型化合物，其有效地吸收可见光区域的光，同时具有良好的耐候性，并且本发明提供一种包含具有包含由下式(I)表示的部分结构的阳离子的化合物以及包含该化合物的组合物、成型体、染色物和光学层。

Novel compound having skin-whitening, anti-oxidizing and ppar activities and medical use therefor

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

皮膚美白、抗酸化及びｐｐａｒ活性を有する新規化合物及びその医学的用途

本発明は、皮膚美白、抗酸化及びＰＰＡＲ活性を有する新規化合物及びその医学的用途に関するものであって、本発明による化合物は、チロシナーゼを抑制する皮膚美白活性を有するので、皮膚美白用薬学組成物または化粧品に有用に使われ、抗酸化活性を有するので、皮膚老化などの予防及び治療に有用に使われ、また、ＰＰＡＲ活性、特に、ＰＰＡＲα及びＰＰＡＲγ活性を有するので、肥満、代謝性疾患または心血関係疾患の予防及び治療に有用な薬学組成物または健康食品として使われる。

Novel compound having skin-whitening, anti-oxidizing and ppar activities and medical use thereof

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

Bisamide sarcomere activating compounds and uses thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

Bisamide sarcomere activating compounds and uses thereof

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

Cyclic lipids and methods of use thereof

The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

화합물과, 이를 포함하는 조성물, 성형체, 염색물 및 광학층

본 발명은 가시광 영역의 빛을 효율적으로 흡수하고, 동시에 양호한 내후성을 갖는 신규 화합물을 제공하는 것을 목적으로 하여, 하기 식 (I)로 표시되는 부분 구조를 포함하는 양이온을 갖는 화합물과, 이를 포함하는 조성물, 성형체, 염색물 및 광학층을 제공한다.

2-azacycloalkylmethyl-substituierte vinylencarbinole und -ketone, verfahren zu deren herstellung und deren verwendung

مركبات تنشيط القسيم العضلي ثنائي الأميد واستخداماتها

يتعلق الاختراع الحالي بتوفير مركب له الصيغة (I) أو ملح منه مقبول صيدليًا، تركيبات صيدلية تشتمل على مركب الاختراع، طريقة تصنيع مركبات الاختراع واستخدامات علاجية لها. (I).

Cyclic lipids and methods of use thereof

The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

화합물과, 이를 포함하는 조성물, 성형체, 염색물 및광학층

본 발명은 가시광 영역의 빛을 효율적으로 흡수하고, 동시에 양호한 내후성을 갖는 신규 화합물을 제공하는 것을 목적으로 하여, 하기 식 (I)로 표시되는 부분 구조를 포함하는 양이온을 갖는 화합물과, 이를 포함하는 조성물, 성형체, 염색물 및 광학층을 제공한다.

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2-azacycloalkylmethyl, substituted vinylene carbinols and ketones

2-azacycloalkylmethyl substituted vinylene carbinols and ketones

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2-azacycloalkylmethyl substituted vinylene carbinols and ketones

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Cyclic lipids and methods of use thereof

The present disclosure details various lipids, compositions, and/or methods of optimized systems and delivery vehicles for the delivery of nucleic acid sequences, polypeptides or peptides for use in vaccinating against infectious agents.

신규 펩티드 데포르밀라제 저해제 화합물 및 그 제조방법

본 발명은 우수한 항균활성을 가지는 신규 펩티드 데포르밀라제(PDF, peptide deformylase) 저해제 또는 약제학적으로 허용 가능한 염, 이의 제조 방법 및 이를 유효 성분으로 포함하는 약제학적 조성물에 관한 것이다.

環状脂質及びその使用方法

本開示は、感染性物質に対して免疫する際に使用するための核酸配列、ポリペプチドまたはペプチドの送達のための最適化システム及び送達ビヒクルの様々な脂質、組成物、及び／または方法を詳述する。【選択図】なし

2-azacycloalkylmetnyl substituted phenyl carbinols and ketones

化合物、包含该化合物的组合物、成型体、染色物和光学层

本发明的目的在于提供一种新型化合物，其有效地吸收可见光区域的光，同时具有良好的耐候性，并且本发明提供一种包含具有包含由下式(I)表示的部分结构的阳离子的化合物以及包含该化合物的组合物、成型体、染色物和光学层。

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2-azacycloalkylmethyl substituted phenyl carbinols and ketones

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共轭二炔及其作为风味改良剂的用途

本公开概括而言提供了共轭二炔，特别是6,8‑二炔酰胺，以及此类化合物和相关化合物作为风味改良剂的用途。在一些形态中，本公开提供了包含此类共轭二炔的组合物，例如包含此类共轭二炔和一种或多种额外化合物如甜味剂、盐、谷氨酸盐、精氨酸盐等的组合物。在一些其他形态中，本公开提供了减少或消除食物或饮料产品中甜味剂、盐、谷氨酸盐或精氨酸盐的量的方法。

双酰胺肌节活化化合物及其用途

本发明提供式(I)化合物或其药学上可接受的盐、包含本发明化合物的药物组合物、用于制造本发明化合物的方法、及其治疗用途。

(E)-α,β-不饱和酰胺化合物及其制备方法和用途

本发明提供一类新的由式I所表示的(E)‑α,β‑不饱和酰胺化合物，还涉及这类化合物的制备方法及其制药用途。所述化合物具有保护神经细胞的作用和免疫调节活性。式I中R 1 、R 2 和R 3 的定义见说明书。

用于器官保藏的组合物

本发明涉及保存器官或组织活性的领域，所述器官或组织待移植到需要这种移植的接受者中。特别地，本发明涉及sigma 1受体激动剂化合物在保藏溶液中的用途以及包含sigma 1受体激动剂化合物的保藏溶液。

Compound having skin-whitening, anti-oxidizing and PPAR activities and medical use thereof

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)

The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.

Pyrrolo[2,3-D]pyrimidine derivatives

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.

Pyrrolo[2,3-D]pyrimidine derivatives

Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.