ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to novel compounds of general formula (1), which possess affinity for µ-opioid receptor and ORL1-receptor, to medications, containing said compounds, and to application of said compounds for obtaining medications, suitable for treating pain, fear, stress and other diseases or conditions. In general formula (1) Y 1 , Y 1 ', Y 2 , Y 2 ', Y 3 , Y 3 ', Y 4 and Y 4 ' stand for -H; R 1 and R 2 independently on each other stand for -H or -CH 3 ; on condition that R 1 and R 2 both simultaneously do not stand for -H; Q stands for: -C 6-16 -aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br or -I; or heteroaryl; R 3 stands for: -C 1-8 -alkyl, non-substituted or mono- or poly-substituted -OR 0 , where R 0 stands for non-substituted -C 1-3 -alkyl; non-substituted -C 3-6 -cycloalkyl-C 1-4 -alkyl; non-substituted -C 1-4 -alkyl-C 3-6 -cycloalkyl; -C 6-16 -aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br, -I, -CN, -R 0 or -OR 0 , where R 0 stands for non-substituted -C 1-8 -alkyl; or heteroaryl; n stands for 0; X stands for -NR A -; R A stands for -H or -R 0 ; where R 0 stands for non-substituted -C 1-4 -alkyl; and R B stands for -C(=O)R 0 ; where R 0 stands for non-substituted -C 2-8 -alkenyl-C 6-16 -aryl or non-substituted -C 1-8 -alkyl-(C 6-16 -aryl) 1-2 . EFFECT: obtaining compounds for obtaining medications, suitable for treatment of pain, fear, stress and other diseases or conditions. 10 cl, 14 tbl, 164 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 209/12 C07D 209/14 C07D 401/04 C07D 251/48 C07D 251/54 C07C 211/40 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 233/36 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 233/46 C07C 311/18 C07D 211/62 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 525 236 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D A61K A61K A61K A61P A61P 213/12 213/82 309/08 31/137 31/404 31/53 25/00 9/00 C2 (2006.01 ...

ФЕНИЛЭТИЛ- И ФЕНИЛПРОПИЛАМИНОВЫЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ

Описываются новые соединения формулы I, которые будут полезными при лечении психитрических нарушений, например шизофрении и других психозов, патологического страха, депрессии и маниакально-депрессивных психозов, в которой Z представляет собой насыщенную или ненасыщенную цепь с 3-6 атомами углерода, m является числом 2 или 3, R 1 представляет собой атом водорода или С 1 -C 4 -алкил нормального или разветвленного строения, R 2 , R 3 и R 13 находятся в орто-, мета- или параположении фенильного кольца, являются одинаковыми или разными и выбраны из следующих групп: Н, ОН, OR 14 , галогена, CO 2 R 9 , СN, СF 3 , NO 2 , СОСH 3 , OSO 2 CF 3 , OSO 2 СН 3 , CONR 10 R 11 , OCOR 12 , где R 9 , R 12 и R 14 представляют собой C 1 -C 4 -алкил нормального или разветвленного строения, R 10 и R 11 , одинаковые или разные, представляют собой водород или C 1 -C 6 -алкил нормального или разветвленного строения, в которой R представляет собой группу формулы Ia, в которой R 4 и R 5 являются одинаковыми или разными, и когда они разные, то представляют собой атом водорода, С 1 -C 5 -алкил нормального или разветвленного строения или замещенный или незамещенный циклоалкил, и когда они одинаковые, то представляют собой С 1 -C 5 -алкил нормального или разветвленного строения или R 4 и R 5 вместе образуют группу где n 1 является числом 3-7, или формулы II, в которой R 6 представляет собой атом водорода или C 1 -C 6 -алкил нормального или разветвленного строения, R 7 представляет собой замещенный или незамещенный циклоалкил или R 6 и R 7 вместе образуют группу , где n 2 является числом 3-6, или формулы III, в которой W представляет собой необязательно замещенное карбоциклическое кольцо (или кольца) или необязательно замещенную метиленовую группу, и R 8 представляет собой C 1 -C 5 -алкил нормального или разветвленного строения или фенил, n 3 является числом 0-2, или формулы IV, в которой W представляет собой необязательно замещенное карбоциклическое кольцо (кольца) или необязательно замещенную ...

НОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНЫХ, ИММУНОМОДУЛИРУЮЩИХ И ПРОТИВОПРОЛИФЕРАТИВНЫХ АГЕНТОВ

Соединение общей формулы (I) и его соли где А является неароматической кольцевой системой, содержащей пять атомов углерода, где кольцевая система содержит, по крайней мере, одну двойную связь и где один или более атомов углерода в кольце могут быть замещены на группу X, где Х выбран из группы, состоящей из S, О, N, NR4, SO или SO2 и где один или более атомов углерода в кольце могут иметь заместитель R1; D представлет собой О, S, SO2, NR4 или СН2; Z1 и Z независимо друг от друга являются О, S или NR5; R1 независимо является Н, галогеном, галогеналкилом, галогеналкилокси или алкилом; R2 является Н, OR6 или NHR7; R3 является Н, алкилом, циклоалкилом, арилом, арилалкилом, алкокси, O-арилом; O-циклоалкилом, галогеном, аминоалкилом, алкиламино, гидроксиламино, гидроксилалкилом, галогеналкилом, галогеналкилокси, гетероарилом, алкилтио, S-арилом или S-циклоалкилом; R4 является Н, алкилом, циклоалкилом, арилом или гетероарилом; R5 является Н, ОН, алкокси, O-арилом, алкилом или арилом; R6 является ...

Полиаминные аналоги в качестве цитотоксических агентов

... 1. Цитотоксический полиаминный аналог, имеющий структуру R1-X-R2, где R1 и R2 - независимо Н или радикал, выбранный из группы, включающей прямой или разветвленный C1-10 алифатический, алициклический, одно- или многокольцевой ароматический, одно- или многокольцевой арил-замещенный алифатический, алифатически замещенный одно- или многокольцевой ароматический, одно- или многокольцевой гетероциклический, одно- или многокольцевой гетероциклически замещенный алифатический и алифатически замещенный ароматический, а также их галогенированные формы; Х - полиамин с двумя концевыми аминогруппами, -(CH2)3-NH- или -СН2-Ph-СН2-, при этом R1 и R2 - не являются одновременно незамещенными бензиловыми радикалами. 2. Аналог по п.1, отличающийся тем, что Х выбирают из группы, содержащей путресцин, спермидин и спермин. 3. Аналог по п.1, отличающийся тем, что Х является путресцином. 4. Аналог по п.3, отличающийся тем, что указанная структура представляет собой соединение, которое выбрано из группы, включающей ...

PHENYLETHYL-UND PHENYLPROPYLAMINE

TETRAHYDROPHTHALIMID DERIVATE, ZWISCHENPRODUKTE ZU DEREN HERSTELLUNG, VERFAHREN ZUR HERSTELLUNG BEIDER SOWIE DIESE ALS WIRKSAME BESTANDTEILE ENTHALTENDE HERBIZIDE

ANILIDDERIVATE, DEREN HERSTELLUNG UND VERWENDUNG

1,3-DIAMINO 2-PROPANOLS AND PROCESS FOR THEIR PREPARATION

... 1399261 Cardiovascular medicines SCIENCE UNION ET CIE SOC FRANCAISE DE RECHERCHE MEDICALE 23 Jan 1973 [24 Jan 1972] 3237/72 Heading A5B [Also in Division C2] Pharmaceutical compositions having cardiovascular properties for oral, parenteral, sublingual or rectal administration comprise a compound of formula I wherein Y, Y' and Y" are independently H, halogen, optionally substituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy or CF 3 radical; R, which may be in the 5-, 10- or 11-position is a radical of general formula II wherein R, is H or an optionally substituted C 1 -C 6 alkyl, R 2 is H, optionally substituted C 1 -C 6 alkyl, C 2-10 alkenyl or benzyl radical, R 3 is optionally substituted C 1 -C 6 alkyl, C 2 -C 10 alkenyl, C 2 -C alkynyl or aryl-C 1 -C 6 alkyl radical or R 2 -N-R 3 represents a 5-7 membered heterocyclic ring which optionally contains a further hetero atom selected from O, N-S, the dotted line indicating an optional double bond, or acid addition salt thereof together with a pharmaceutically ...

New compounds

New compounds

New compounds

POLYAMINE-SIMILAR AS CYTOTOXIC ACTIVE SUBSTANCES

SUSTIUIERTE CYCLI CONNECTIONS, PROCEDURE FOR YOUR PRODUCTION AS WELL AS IT ABSTENTION PHARMACEUTICAL ZUSAMMESETZUNGEN

Novel potassium channel inhibitors

The present invention relates to novel compounds, pharmaceutical compositions comprising such compounds and their use for treating, alleviating or preventing diseases or disorders relating to the activity of potassium channels.

Labelled analogues of halobenzamides as radiopharmaceuticals

The present invention relates to the use of a compound of formula (I): in which R1 represents a radionuclide, Ar represents an aromatic nucleus, m is an integer varying from 2 to 4, R2 and R3 represent, independently of one another, a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6)alkenyl group or an aryl group chosen from a phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl group, and their addition salts with pharmaceutically acceptable acids, in the preparation of a radiopharmaceutical composition intended for the diagnosis and/or treatment of melanoma.

Enzymatic conjugation of polypeptides

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Farnesoid X receptor agonists and uses thereof

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Pharmaceutical composition for antagonizing ccr5 comprising anilide derivative

Activators of soluble guanylate cyclase

GLUCOCORTICOID-SELECTIVE AGENTS

Compounds having Formula (I) are useful for modulating the glucocorticoid receptor in a mammal. Also disclosed are pharmaceutical compositions comprising compounds of Formula (1) and methods of treating immune, autoimmune, inflammatory, adrenal imbalance, cognitive and behavioral diseases in a mammal.

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention concerne les composés de formule (I) : R-A-R' (I) dans laquelle : .cndot. A est tel que défini dans la description .cndot. R représente un groupement (voir formule), ou -NR'a R"a où R'a et R"a sont tels que définis dans la description, .cndot. R' représente un groupement -(CH2)T-R2 dans lequel t et R2 sont tels que définis dans la description. Les composés de la présente invention présentent des caractéristiques pharmacologiques très intéressantes concernant les récepteurs mélatoninergiques et peuvent être utilisés pour le traitement de pathologies liées au système mélatoninergique.

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention concerne les composés de formule (I): R-A-R' (I) dans laquelle: .cndot. A est tel que défini dans la description .cndot. R représente un groupement (voir formule I, II, III ou IV) où E, Q, R1, R2, R3, v et R4 sont tels que définis dans la description .cndot. R' représente un groupement -(CH2)t-R5 dans lequel t et R5 sont tels que définis dans la description. Les composés de la présente invention présentent des caractéristiques pharmacologiques très intéressantes concernant les récepteurs mélatoninergiques et peuvent être utilisés pour le traitement de pathologies liées au système mélatoninergique.

DERIVATIVES OF 1-(2-HALO-BIPHENYL-4-YL)- ALKANECARBOXYLIC ACIDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

The present invention concerns pro-drugs of 1-(2-halo-biphenyl-4-yl) alkanecarboxylic acids, pharmaceutical compositions thereof, a process for their preparation and their use for preventing and/or treating neurodegenerative diseases, improving cognitive function and treating cognitive impairment.

TETRAHYDROPHTHALAMIDE DERIVATIVE, INTERMEDIATE FOR PRODUCING THE SAME, PRODUCTION OF BOTH AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT

The present invention relates to 3,4,5,6-tetra-hydrophthalamide derivatives and 3,4,5,6-tetrahydroiso-phthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof. More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetra-hydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): (I) These tetrahydrophthalamide derlvatlves and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment. The tetrahydroisophthalimide derivatives ...

DERIVATIVES OF PHENOXYETHYLAMINE HAVING A HIGH AFFINITY FOR 5-HT1A RECEPTOR, THEIR PREPARATION PROCEDURE, THEIR APPLICATION AS MEDICATIONS AND PHARMACEUTICAL COMPOUNDS CONTAINING THEM

Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.

TRIS - AMIDE COMPOUNDS AND COMPOSITIONS, CONTAINING THEREOF

Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative

리신 진지페인의 억제제

... 본 발명은 일반적으로, 프로테아제 리신 진지페인 (Kgp)을 포함하여 세균 포르피로모나스 진지발리스를 표적으로 하는 치료법, 및 알츠하이머병과 같은 뇌 장애를 포함하여 P. 진지발리스 감염과 관련된 장애의 치료를 위한 이의 용도에 관한 것이다. 특정 구체예에서, 본 발명은 본원에 기재된 바와 같은 화학식 (I)에 따른 화합물, 및 이의 약제학적으로 허용가능한 염을 제공한다.

PHOTOSENSITIZERS FOR TARGETED PHOTODYNAMIC THERAPY

The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.

NOVEL COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS

The present invention relates to compounds of the general formula (I); or salts thereof, as anti-inflammatory, immunomodulatory and anti-proliferatory agents.

AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

置換された４−アミノシクロヘキサン誘導体

ИНГИБИТОРЫ ЛИЗИНСПЕЦИФИЧНОГО ГИНГИПАИНА

FIELD: pharmaceuticals.SUBSTANCE: invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof, wherein Z is halo-substituted phenoxymethylcarbonyl; A is -CH-; B and D are hydrogen; Rdenotes hydrogen; Ris hydrogen and Ris selected from a group consisting of cyclohexyl, cyclopentyl, morpholino, phenyl, piperidinyl, pyridinyl, tetrahydrofuranyl, tetrahydropyranyl, 1,2,3,4-tetrahydronaphthyl and thiazolyl, each of which is independently unsubstituted or independently substituted with 1–3 members selected from methyl, methoxy, trifluoromethyl, acetyl and -N; and Ris hydrogen..EFFECT: compounds of formula I are intended for inhibiting lysine-specific gingipain.8 cl, 10 dwg, 2 tbl, 37 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 233/62 (2006.01) C07D 277/28 (2006.01) C07D 277/64 (2006.01) C07D 277/24 (2006.01) C07D 417/12 (2006.01) C07D 409/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 213/50 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 213/53 (2006.01) A61K 31/4402 (2006.01) A61K 31/428 (2006.01) (12) (13) 2 728 785 C2 A61K 31/426 (2006.01) A61P 31/04 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 233/62 (2020.02); C07D 277/28 (2020.02); C07D 277/64 (2020.02); C07D 277/24 (2020.02); C07D 417/12 (2020.02); C07D 409/12 (2020.02); C07D 213/50 (2020.02); C07D 213/53 (2020.02); A61K 31/4402 (2020.02); A61K 31/428 (2020.02); A61K 31/426 (2020.02); A61P 31/04 (2020.02) 2017115726, 05.10.2015 (24) Дата начала отсчета срока действия патента: 05.10.2015 31.07.2020 (73) Патентообладатель(и): КОРТЕКСИМ, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: 06.10.2014 US 62/060,483 (43) Дата публикации заявки: 14.11.2018 Бюл. № 32 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 10.05.2017 (86) Заявка PCT: R U 2 7 2 8 7 8 5 US 2015/054050 (05.10.2015) (87) Публикация заявки PCT: WO 2016/057413 (14.04.2016) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) ...

НОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНЫХ, ИММУНОМОДУЛИРУЮЩИХ И ПРОТИВОПРОЛИФЕРАТИВНЫХ АГЕНТОВ

FIELD: organic chemistry, pharmaceuticals. SUBSTANCE: invention relates to compounds of general formula I and salt thereof, wherein F is non-aromatic ring system containing five carbon atoms and at least one double bond wherein one ring carbon atom is optionally substituted with X group, such as S, O, or SO 2 , and one or more ring carbon atoms are optionally substituted with R 1 ; D represents S, O, SO 2 , NR 4 , or CH 2 ; Z 1 and Z 2 are independently O; Y is steryl, mono- or polycyclic non-substituted ring system, containing one or more X group such as S, O, SO 2 , N; m, n, p, r and q = 0 or 1; meanings of the rest substituents are as defined in specification. Also invention relates to compounds of general formula I , wherein m, n, and q = 0; r = 1. Disclosed is pharmaceutical composition having inhibitory activity in relates to dihydroorotate dehydrogenase (DHODH) containing effective amount of said compound in free form or in form of pharmaceutically acceptable salts together with pharmaceutically acceptable diluents or carriers. Compounds of formula I are useful as drug inhibiting DHODH for treatment of disease or therapeutic condition in which inhibition of DHODH is beneficial. EFFECT: new compounds as anti-inflammatory, immunomodulating, and anti-proliferative agents. 13 cl, 1 tbl, 1 dwg, 76 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2 309 946 (13) C2 (51) ÌÏÊ C07C 233/60 C07C 233/58 C07C 233/59 C07C 233/62 C07C 255/60 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07D 335/12 ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07D 333/38 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ C07D 333/60 C07D 307/30 A61K 31/167 (12) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2004103741/04, 09.07.2002 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 09.07.2002 (30) Êîíâåíöèîííûé ïðèîðèòåò: 10.07.2001 (ïï.1-13) EP PCT/EP01/07948 (43) Äàòà ïóáëèêàöèè çà âêè: 20.06.2005 2 3 0 9 9 4 6 R U (56) ...

Patent RU2017115726A3

ВУ” 2017115726” АЗ Дата публикации: 08.05.2019 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017115726/04(027236) 05.10.2015 РСТ/О$2015/054050 05.10.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/060,483 06.10.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ИНГИБИТОРЫ ЛИЗИН-СПЕЦИФИЧНОГО ГИНГИПАИНА Заявитель: КОРТЕКСИМ, ИНК., (05 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 233/62 (2006.01) (070 417/12 (2006.01) Аб/1К 31/4402 (2006.01) (070 277/28 (2006.01) С07р 409/12 (2006.01) Аб/1К 31/428 (2006.01) (070 277/64 (2006.01) (070 213/50 (2006.01) Аб1К 31/426 (2006.01) (070 277/24 (2006.01) (070 213/53 (2006.01) Аб1Р 31/04 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 233/62, С07Ь 277/28, СО7О 277/64, С07О 277/24, С07Ь 417/12, С07О 409/12, С07О 213/53 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске ( ...

НИЗКОМОЛЕКУЛЯРНЫЕ МОДУЛЯТОРЫ АКТИВНОСТИ Trp-p8

... 1. Соединение формулы I: ! , ! где R1 выбирают из H, алкила, гетероалкила, арилалкила и арила, или R1 и R2 вместе с группой азота могут образовывать циклическую или гетероциклическую группу, самое большее, из 25 атомов; ! R2 выбирают из арила и арилалкила; ! R3 выбирают из алкила, гетероалкила и арилалкила; ! R4 выбирают из H, алкила, гетероалкила и арилалкила; и ! R3 и R4 вместе с группой азота образуют алифатический амин. ! 2. Соединение формулы I-A: ! , ! где A, B, C и D независимо выбирают из CR2 и N; где, по меньшей мере, один из A, B, C и D представляет собой CR2; где R2 представляет собой остаток, выбранный из H, алкила, гетероалкила, арила, галогена и арилалкила, R6O- и R6S-, где R6 представляет собой алкил; при этом, когда два соседних остатка A, B, C и D представляют собой CR2, два R2 могут объединяться с образованием единой арильной, циклоалкильной или гетероциклоалкильной группы; и ! R1 выбирают из H, алкила, гетероалкила, арила и арилалкила; ! R3 выбирают из алкила, гетероалкила ...

КЕТОНОВЫЕ ИНГИБИТОРЫ ЛИЗИН-СПЕЦИФИЧНОГО ГИНГИПАИНА

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

... 1. Соединение общей формулы (1)гдеY, Y', Y, Y', Y, Y', Yи Y' в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -Br, -I, -CN, -NO, -CHO, -R, -C(=O)R, -C(=O)H, -C(=O)-OH, -C(=O)OR, -C(=O)NH, -C(=O)NHR, C(=O)N(R), -ОН, -OR, -OC(=O)H, -OC(=O)R, -OC(=O)OR, -OC(=O)NHR, -OC(=O)N(R), -SH, -SR, -SOH, -S(=O)-R, -S(=O)NH, -NH, -NHR, N(R), -N(R), -N(R)O, -NHC(=O)R, -NHC(=O)OR, -NHC(=O)NH, NHC(=O)NHRи -NHC(=O)N(R); преимущественно в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -CN и -С-алифат; или Yи Y', или Yи Y', или Yи Y', или Yи Y' совместно означают =O;Q означает -R, -C(=O)-R, -C(=O)OR, -C(=O)NHR, -C(=O)N(R)или -C(=NH)-R;Rв каждом случае независимо означает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -С-алифат-С-циклоалифат, -C-алифат-арил, -C-алифат-гетероарил, -С-циклоалифат-С-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;Rи R, независимо друг от друга означают -Н или -R; или Rи Rсовместно образуют кольцо ...

NITRIERUNGS- ODER CARBOXYLIERUNGSKATALYSATOREN

CYCLOBUTAN-DERIVATE ALS INHIBITOREN DER SQUALEN-SYNTHETASE UND DER PROTEIN-FARNESYLTRANSFERASE

PHENOXYETHYLAMIN DERIVATIVES WITH HIGH AFFINITY FUR the 5-HT1A-REZEPTOR, PROCEDURE FOR ITS PRODUCTION, YOUR USE AS MEDICINES AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

INTERLACE-CASH MONOMERS AND COMPOSITION AS WELL AS INTERLACED POLYMERS

Novel polyamine analogues as therapeutic and diagnostic agents

Novel substituted cyclic compounds, preparation method and pharmaceutical compositions containing them

Anilide derivative, production and use thereof

Amide derivatives

The present invention provides a therapeutic agent useful in the treatment and/or prevention of conditions, including cancer, caused by enhanced OPN production, the therapeutic agent containing a compound represented by the formula (in the formula, R ...

NOVEL POTASSIUM CHANNEL INHIBITORS

The present invention relates to novel compounds, pharmaceutical compositions comprising such compounds and their use for treating, alleviating or preventing diseases or disorders relating to the activity of potassium channels.

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

NEW COMPOUNDS

This invention relates to compounds of formula (I) their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.

BISCATIONIC ACID AMIDE AND IMIDE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION

POLYHYDROXYBENZYLPXYPROPANOLAMINES

TITLE POLYHYDROXYBENZYLOXYPROPANOLAMINES Compounds of the present invention, are represented by the general formula wherein R1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R2, R3 and R4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents -NHCOR5, -NHCONR5R6, or -NHCOOR5 wherein R5 and R6 may be the same or different and represent hydrogen, alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, ...

ANILIDE DERIVATIVE, PRODUCTION AND USE THEREOF

This invention is provide a compound of formula (I) wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of formula (a) or (b) wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

AGONISTS FARNEZOIDNOGO X - RECEPTOR AND THEIR USE

NEW COMPOUNDS

СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ОФТАЛЬМОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ И РАССТРОЙСТВ

Описаны соединения и их фармацевтические композиции, а также способы лечения офтальмологических заболеваний и расстройств, таких как возрастная макулярная дегенерация и заболевание Штаргардта с использованием указанных соединений и композиций.

NEW COMPOSE CYCLIC SUBSTITUTE, THEIR METHOD OF PREPARATION AND LESCOMPOSITIONS PHARMACEUTICAL WHICH CONTAIN THEM

New hydrophobic/lipophobic perfluoroalkylated polyamide surfactants containing a polymeric hydrophilic group, useful in extinguishing foams

Hydrophobic or lipophobic perfluoroalkylated polyamide surfactant (I) containing a polymeric hydrophilic group, is new. Hydrophobic or lipophobic perfluoroalkylated surfactant (I) of formula A-B1-(D-Rf)r containing a polymeric hydrophilic group, is new. RfCnF2n+1; n : 4-20; A : X-E-CO-[NH-(CH2)m-N+>(R1)(R2)-CH2-CO]p-NH-(CH2)m-N+>(R1)(R2)- or ->OOC-CH2-[N+>(R1)(R2)-(CH2)m-N+>(R1)(R2)-(CH2)m-NHCO-CH2]p-N+>(R1)(R2)-(CH2)m-NH-; B1-CH2CH(OH)CH2OC2H4-, -CH2CH(OH)CH2(OC2H4)1-3SC2H4-, -CH2CH(OH)-CH2SC2H4-, -CH2CH(OH)-, -CH2CH(OH)-CH2-CH=CH-, -CH2CH(OH)-CH2-O-C3H6S-C2H4- or -CH2CH(OH)CH2-N=; E : absent, -(CH2)q-, 1,2-cyclohexadiyl, 1,2-benzen-diyl, 2,3-pyridin diyl or pyrazin-2,3-diyl; M+>alkaline ion or absent; m, p, q : 2-3; and R1, R2lower alkyl groups. Provided B1 is -CH2CH(OH)CH2OCH2CH(I)CH2- or -CH2CH(OH)CH2OCH2CH=CH-, when A is ->OOC-CH2-[N+>(R1)(R2)-(CH2)m-N+>(R1)(R2)-(CH2)m-NHCO-CH2]p-N+>(R1)(R2)-(CH2)m-NH-. Provided that D is -CH2CH(I)CH2 and/or -CH2CH=CH-, when B1 is -CH2CH(OH)-CH2-N= and absent in other cases. Provided that r is equal to 2 when B1 is -CH2CH(OH)CH2-N= and 1 in the other cases. Provided that X is alkyl or aryl, when E is absent and ->OOC- when E is present. An independent claim is included for the preparation of (I).

SPHINGOSINE KINASE INHIBITORS

The invention relates to substituted adamantane compounds of formula (I), pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, imflammatory disease, or angiogenic disease. © KIPO & WIPO 2008 ...

Substituted 4-aminocyclohexane derivatives

QUATERNARY AMMONIUM SALTS AND THEIR USE

L'invention concerne un composé permettant de contrarier CCR5, ce composé étant représenté par la formule (I), dans laquelle R1¿ représente un phényle éventuellement substitué ou un thiényle éventuellement substitué ; Y représente -CH¿2-, -S-, ou -O- ; et R2¿, R3¿, et R4¿ représentent indépendamment un groupe aliphatique hydrocarboné éventuellement substitué ou un groupe hétérocyclique alicyclique éventuellement substitué. Le composé de cette invention permet de prévenir et de traiter efficacement les infections à VIH.

INHIBITORS OF HISTONE DEACETYLASE

The present invention relates to compounds of formula (I): 5. The compound of or a pharmaceutically acceptable salt claim 4 , hydrate claim 4 , solvate claim 4 , or prodrug thereof claim 4 , wherein Ris selected from phenyl claim 4 , 2-pyridinyl claim 4 , 3-pyridinyl claim 4 , 4-pyridinyl claim 4 , 2-pyrimidinyl claim 4 , 4-pyrimidinyl claim 4 , 5-pyrimidinyl claim 4 , 2-pyrazinyl claim 4 , oxazolyl claim 4 , thiazolyl claim 4 , and isoxazolyl.12. A pharmaceutical composition comprising an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof and a pharmaceutical carrier claim 1 , diluent claim 1 , or excipient.13. A method of treating claim 1 , alleviating claim 1 , and/or preventing a condition wherein said condition is associated with histone deacetylase activity in a subject comprising administering to the subject in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate or prodrug thereof.14. The method of claim 13 , wherein the condition is selected from a neurological disorder claim 13 , memory loss or impairment claim 13 , cognitive function disorder or impairment claim 13 , extinction learning disorder claim 13 , fungal disease or infection claim 13 , inflammatory disease claim 13 , hematological disease claim 13 , and neoplastic disease.15. The method of claim 14 , wherein the condition is selected from:a cognitive function disorder or impairment associated with Alzheimer's disease, Huntington's disease, seizure induced memory loss, schizophrenia, Rubinstein Taybi syndrome, Rett Syndrome, Fragile X, Lewy body dementia, vascular dementia, ADHD, dyslexia, bipolar disorder and social, cognitive and learning disorders associated with autism, traumatic head injury, or attention deficit disorder, anxiety disorder, conditioned fear response, panic disorder, obsessive compulsive disorder, posttraumatic stress ...

Aminoalcohol derivatives

The present invention relates to a compound formula (I) wherein X1 is bond or -O-CH2-, (II) or (III) R<1 >is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.

Substituted basic 2-aminotetralin in pharmaceuticals

For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula in which R1 represents hydrogen or alkyl, R2 represents hydrogen, alkyl or acyl, and R3 represents quinuclidine or a group of the formula -(CH2)a-R4, -CH2-CH=CH-(CH2)b-R4, -CH2-C 3BOND C-(CH2)b-R4, or wherein a denotes a number from 1 to 10, b denotes a number 0, 1, 2, 3 or 4, c denotes a number 0, 1 or 2, d denotes a number 2 or 3, and x denotes oxygen, sulphur or NR5, and their salts.

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds that have an affinity to the -opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

POLYAMINE ANALOGUES AS CYTOTOXIC AGENTS

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

CYCLOBUTANE DERIVATIVES AS INHIBITORS OF SQUALENE SYNTHETASE AND PROTEIN FARNESYLTRANSFERASE

ИНГИБИТОРЫ ЛИЗИН-СПЕЦИФИЧНОГО ГИНГИПАИНА

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

... 1. Соединение общей формулы (1)где Y, Y', Y, Y', Y, Y', Yи Y' означают -H;Q означает -арил или -гетероарил;Rи R, независимо друг от друга означают -Н или -СН; при условии, что Rи Rоба одновременно не означают -Н;Rозначает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -C-алифат-С-циклоалифат, -С-алифат-арил, -C-алифат-гетероарил, -С-циклоалифат-С-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;n означает 0;X означает -NR-;Rозначает -Н или -R; где Rозначает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -C-алифат-С-циклоалифат, -С-алифат-арил, -С-алифат-гетероарил, -С-циклоалифат-C-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;Rозначает -C(=O)R; где Rозначает -С-алифат-арил или -C-алифат-гетероарил;причем "алифат" в каждом случае представляет собой разветвленный или неразветвленный, насыщенный или моно- или многократно ненасыщенный, незамещенный или моно- или многократно замещенный, алифатический углеводородный остаток;"циклоалифат" в каждом случае представляет собой ...

ФЕНИЛЭТИЛ- И ФЕНИЛПРОПИАМИНОВЫЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ

Предложены соединения общей формулы Iв которой Z представляет собой насыщенную или ненасыщенную углеродную цепь с 3 - 6 атомами углерода, m является числом 2 или 3, Rпредставляет собой атом водорода или C-алкил нормального или разветвленного строения, R, Rи Rвыбраны из следующих групп: Н, ОН, OR, галогена, СOR, CN, CF, NO, NH, COCH, OSOCF, OSOCH, CONRRи OCOR, R представляет собой радикал формулы 123и 4в которой R, R, R, R, R, W, nи nимеют значения, указанные в формуле изобретения, способы их получения, фармацевтические препараты, содержащие их, и применение соединений для лечения психиатрических нарушений.

ПРОИЗВОДНЫЕ 1-(2-ГАЛОГЕНОБИФЕНИЛ-4-ИЛ) АЛКАНКАРБОНОВЫХ КИСЛОТ ДЛЯ ЛЕЧЕНИЯ НЕЙРОДЕГЕНЕРАТИВНЫХ ЗАБОЛЕВАНИЙ

1. Соединение общей формулы (I):,в которой Х представляет собой галоген, выбранный из группы F, Cl, Br и I;R и Rявляются идентичными и представляют собой (С-С)-алкил, в противном случае они образуют насыщенное кольцо от 3 до 6 атомов углерода с атомом углерода, с которым они связаны;Rпредставляет собой одну или более групп, независимо выбранных из атомов галогена;Q представляет собой группу Qили Qкак представлено ниже:,в которой R, Rи Rнезависимо выбраны из группы, состоящей из (C-C)-алкила, (C-C)-алканоила или связи, соединяющей группу Qили Qс остальной молекулой с условием, что один и только один из R, Rи Rпредставляет собой связь;Rи Rнезависимо выбраны из группы, состоящей из H, (C-C)-алкила и (C-C)-алканоила.2. Соединение по п. 1, в котором Х представляет собой фтор и любой Rпредставляет собой хлор.3. Соединение по п. 2, в котором R и Rобразуют 3 атомное углеродное кольцо с атомом углерода, с которым они связаны.4. Соединение по п. 2, в котором R и Rявляются идентичными и представляют собой метил.5. Соединение по п. 1, имеющее общую формулу (Iа),,в которой Q является таковым, как определено выше.6. Соединение по п. 5, имеющее формулу (Ib), в которой Rпредставляет собой связь.и в которой Rи Rявляются таковыми как определено выше.7. Соединение по п. 6, в котором Rи Rмогут быть идентичными или отличными друг от друга и независимо выбраны из (С-С)-алканоила, предпочтительно ацетила и (C-C)-алканоила, предпочтительно гексадеканоила.8. Соединение по п. 5, имеющее формулу (Ic), в которой Rпредставляет собой связьи в которой R, R, Rи Rявляются таковыми, как определено выше.9. Соединение по п. 8, в котором Rи Rмогут быть идентичными или отличными друг от друга и выбраны из (С-С)-алканоила, предпочтительно ацетила, тогда как Rи Rмогут быть идентичными или отличными друг от друга и независимо выбр РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 69/743 (13) 2014 139 971 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) ...

NITRIERUNGS- ODER CARBOXYLIERUNGSKATALYSATOREN

Compounds for treating ophthalmic diseases and disorders

SUBSTITUTED CYCLI CONNECTIONS, PROCEDURES FOR YOUR PRODUCTION AS WELL AS IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

PHENYLETHYL AND PHENYLPROPYLAMINE

NEW CONNECTIONS AS ENTZÜNDUNGSHEMMENDE ONES, IMMUNE-MODULATING AND ANTIPROLIFERATIVE MEANS

Labelled analogues of halobenzamides as radiopharmaceuticals

New terpenes and macrocycles

Novel polyamine analogues as therapeutic and diagnostic agents

Pharmaceutical composition for antagonizing CCR5 comprising anilide derivative

Tetrahydrophthalamide derivative, intermediate for producing the same, production of both, and herbicide containing the same as active ingredient

Novel substituted cyclic compounds, preparation method and pharmaceutical compositions containing them

Quaternary ammonium salts and their use

Modulators of the integrated stress pathway

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

NOVEL COMPOUNDS AS ANTI-INFLAMMATORY, IMMUNOMODULATORY AND ANTI-PROLIFERATORY AGENTS

The present invention relates to compounds of the general formula (I); or salts thereof, as anti-inflammatory, immunomodulatory and anti-proliferatory agents.

INHIBITORS OF HCV NS5B POLYMERASE

The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.

SUBSTITUTED 4-BENZYLOXY-PHENYLMETHYLAMIDE DERIVATIVES AS COLD MENTHOL RECEPTOR-1 (CMR-1) ANTAGONISTS FOR THE TREATMENT OF UROLOGICAL DISORDER

The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives of formula (I), processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

PROCEDE POUR LA PREPARATION DES NOUVEAUX DIBENZOCYCLOHEPTENES SU BSTITUES

META-DIAMIDE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS

Disclosed are compounds of Formula (1), N-oxides, and salts thereof, wherein Q, X, Y, A1, A2, L, R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the disclosure.

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

L'invention concerne les composés de formule (I): R-A-R' dans laquelle: A est tel que défini dans la description, R représente un groupement (V), -NR'aR''a où R'a et R''a sont tels que définis dans la description, ou R forme avec A une structure cyclique telle que défine dans la description; R' représente un groupement -(CH2)t-R2 dans lequel q, t et R2 sont tels que définis dans la description. Médicaments.

NOVEL POLYAMINE ANALOGUES AS THERAPEUTIC AND DIAGNOSTIC AGENTS

Novel "bispolyamine" inhibitor compounds of polyamine transport are disclosed. These compounds are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. These compounds display desirable activities both for diagnostic and research assays and therapy.

A NOVEL KCNQ POTASSIUM CHANNEL AGONIST, THE PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. (see above formula) ...

COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

BISCATIONIC ACID AMIDE AND IMIDE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION

The invention relates to biscationic acid amide and acid imide derivatives with an anion of formula (I), where R9 to R12 are aliphatic, iso- or heterocyclic aromatic residues or aralkyl residues, which may be substituted by alkyl (C1-C4) residues, alkoxy (C1-C4) residues, aryl residues or halogen atoms, or are fluorine atoms, and mixtures of these compounds and mixed crystals with mixed anions and/or cations. The invention also relates to a process for preparing them. The new compounds are excellent colourless charge controllers in toners and developers for electrophotographic recording and as charge-enhancers in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.

MONOMERS AND COMPOSITION WHICH CAN BE CROSSLINKED AND CROSSLINKED POLYMERS

The invention concerns compounds of formula (I) (A)n-B in which A is an extended cycloolefin group, B stands for a direct bond or an n-valent bridging group, and n is an integer from 2 to 8, with the exception of 1,2bisnorbornenyl ethane and norbornene carboxylic acid norbornene methylester. The compounds of formula (I) can be polymerized with single-component catalysts (ring-opening metathesis polymerization).

DERIVATIVES OF PHENOXYETHYLAMINE HAVING A HIGH AFFINITY FOR 5-HT1A RECEPTOR, THEIR PREPARATION PROCEDURE, THEIR APPLICATION AS MEDICATIONS AND PHARMACEUTICAL COMPOUNDS CONTAINING THEM

Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula(I), Ar is phenyl substituted by one or more substituents; and R is a C1-1- hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituent, and salts thereof.

Diacylethylenediamine compound

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

ENZYMATIC CONJUGATION OF POLYPEPTIDES

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions 1. An antibody or antibody fragment comprising a functionalized acceptor glutamine residue , the functionalized acceptor glutamine residue having Formula IVa ,{'br': None, 'sub': n', 'z', 'q', 'q', 'r, '(Q)-NH—(C)—X-L-(V—(Y—(Z))))\u2003\u2003Formula IVa'}or a pharmaceutically acceptable salt or solvate thereof,wherein:Q is glutamine residue present in an antibody or antibody fragment;{'sub': 'n', '(C)is a substituted or unsubstituted alkyl or heteroalkyl chain, optionally wherein any carbon of the chain is substituted with an alkoxy, hydroxyl, alkylcarbonyloxy, alkyl-S—, thiol, alkyl-C(O)S—, amine, alkylamine, amide, or alkylamide;'}n is an integer selected from among the range of 2 to 20;X is NH, O, S, absent, or a bond;L is independently absent, a bond or a continuation of a bond, or a carbon comprising framework of 5 to 200 atoms substituted at one or more atoms;r is an integer selected from among 1, 2, 3 or 4;q is an integer selected from among 1, 2, 3 or 4;z is an integer selected from among 1, 2, 3 or 4; andV is independently absent, a bond or a continuation of a bond, a non-cleavable moiety or a conditionally-cleavable moiety;Y is independently absent, a bond or a continuation of a bond, or a spacer system which is comprised of 1 or more spacers; andZ is a moiety that improves pharmacokinetic properties, a therapeutic moiety or a diagnostic moiety, wherein Z is an organic compound that is electrically negatively charged, hydrophobic and/or that has a molecular weight of at least 400 g/mol.2. The antibody of claim 1 , wherein n is an integer selected from among the range of 10 to 20.3. The antibody of claim 1 , wherein (C)is a heteroalkyl chain that comprises a (CH—CH—O—)group claim 1 , wherein x is ...

DERIVATIVES OF 1-(2-HALO-BIPHENYL-4-YL)-ALKANECARBOXYLIC ACIDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Pro-drugs of 1-(2-halo-biphenyl-4-yl)alkanecarboxylic acids are useful for preventing and/or treating neurodegenerative diseases, improving cognitive function and treating cognitive impairment. 2. A compound according to claim 1 , wherein X is fluorine and each Ris chlorine.3. A compound according to claim 2 , wherein R and R claim 2 , together with the carbon atom to which they are bonded claim 2 , form a 3 carbon atom ring.4. A compound according to claim 2 , wherein R and Rare both methyl.7. A compound according to claim 6 , wherein Rand Rare the same or different from each other claim 6 , and are independently selected from (C-C)-alkanoyl and (C-C)-alkanoyl.8. A compound according to claim 6 , wherein Rand Rare the same or different from each other claim 6 , and are independently selected from acetyl and hexadecanoyl.10. A compound according to claim 9 , wherein Rand Rare the same or different from each other claim 9 , and are independently selected from (C-C)-alkanoyl claim 9 , and Rand Rare the same or different from each other claim 9 , and are independently H or (C-C)-alkyl.11. A compound according to claim 9 , wherein Rand Rare both acetyl claim 9 , and Rand Rare the same or different from each other claim 9 , and are independently H or methyl.13. A compound according to claim 12 , wherein Rand Rare the same or different from each other claim 12 , and are independently selected from (C-C)-alkanoyl claim 12 , and Rand Rare the same or different from each other claim 12 , and are independently H or (C-C)-alkyl.14. A compound according to claim 12 , wherein Rand Rare both acetyl claim 12 , and Rand Rare the same or different from each other claim 12 , and are independently H or methyl.15. A pharmaceutical composition claim 1 , comprising a compound of formula (I) according to claim 1 , optionally in combination with one or more pharmaceutically acceptable carriers and/or excipients.16. A method for preventing and/or treating a neurodegenerative disease claim 1 ...

INHIBITORS OF LYSINE GINGIPAIN

The present invention relates generally to therapeutics targeting the bacterium , including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. 145-. (canceled)47. The method of claim 46 , wherein Ris selected from the group consisting of cyclohexyl; 1-methylcyclohexyl; 1-methoxycyclohexyl; cyclopentyl; morpholin-2-yl; 4-acetylmorpholin-2-yl; phenyl; 2-trifluoromethylphenyl; 3-azidophenyl; piperidine-3-yl; 1-acetyl-piperidine-3-yl; pyridin-2-yl; pyridin-3-yl; pyridin-4-yl; 6-oxo-1 claim 46 ,6-dihydropyridin-2-yl; tetrahydrofuran-2-yl; tetrahydro-2H-pyran-2-yl; tetrahydro-2H-pyran-3-yl; tetrahydro-2H-pyran-4-yl; 1 claim 46 ,2 claim 46 ,3 claim 46 ,4-tetrahydronaphth-1-yl; 1 claim 46 ,2 claim 46 ,3 claim 46 ,4-tetrahydronaphth-2-yl; thiazol-5-yl; and thiazol-2-yl.49. The method of claim 48 , wherein Ris selected from the group consisting of cyclohexyl; 1-methylcyclohexyl; 1-methoxycyclohexyl; cyclopentyl; morpholin-2-yl; 4-acetylmorpholin-2-yl; phenyl; 2-trifluoromethylphenyl; 3-azidophenyl; piperidine-3-yl; 1-acetyl-piperidine-3-yl; pyridin-2-yl; pyridin-3-yl; pyridin-4-yl; 6-oxo-1 claim 48 ,6-dihydropyridin-2-yl; tetrahydrofuran-2-yl; tetrahydro-2H-pyran-2-yl; tetrahydro-2H-pyran-3-yl; tetrahydro-2H-pyran-4-yl; 1 claim 48 ,2 claim 48 ,3 claim 48 ,4-tetrahydronaphth-1-yl; 1 claim 48 ,2 claim 48 ,3 claim 48 ,4-tetrahydronaphth-2-yl; thiazol-5-yl; and thiazol-2-yl.52. The method of claim 46 , wherein Z is selected from the group consisting of pyridin-2-yl-carbonyl and thiazol-2-yl-carbonyl.55. The method of claim 46 , wherein the compound is administered as a pharmaceutical composition comprising the compound and a pharmaceutically acceptable excipient.56. The method of claim 46 , wherein the compound is ...

ADAMANTANE DERIVATIVES FOR THE TREATMENT OF FILOVIRUS INFECTION

Compounds of structural Formula I were developed for the treatment of infections by filoviruses including Ebolavirus and Marburgvirus, wherein, R, R, R, X and Y are defined in the specification. 119-. (canceled)21. The compound of claim 20 , wherein:{'sup': 4', '5, 'X is C-A-D and Y is CRR.'}23. The compound of claim 22 , wherein:{'sup': 2', '11a', '11b', '12, 'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10', '1', '10', '2', 'n, 'Ris selected from hydrogen, (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl, (Cto C) alkoxy, —(CH)C(O)N(RR), and —C(O)R, wherein'}{'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10', '1', '10, 'sup': '13', 'each of the said (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl, and (Cto C) alkoxy is optionally substituted with at least one Rgroup;'}{'sup': '3', 'sub': 1', '10', '1', '10', '1', '10', '3', '10', '5', '10, 'Ris selected from hydrogen, (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, and (Cto C) cycloalkenyl, wherein'}{'sub': 1', '10', '1', '10', '1', '10', '6', '10', '5', '10, 'sup': '13', 'each of the said (Cto C) alkyl, (Cto C) alkenyl, (Cto C) alkynyl, (Cto C) cycloalkyl, (Cto C) cycloalkenyl is optionally substituted with at least one Rgroup.'}24. The compound of claim 23 , wherein:{'sup': '3', 'Ris hydrogen.'}31. The method of claim 30 , wherein the infection is associated with filovirus selected from the group consisting of Ebolavirus and Marburgvirus.32. The method of claim 31 , where the filovirus is Ebolavirus.33. The method of claim 31 , including administering a therapeutic amount of a therapeutic agent selected from the group consisting of Ribavirin claim 31 , viral RNA-dependent-RNA polymeras inhibitors including favipiravir claim 31 , Triazavirin claim 31 , Remdesivir (GS-5734) claim 31 , monoclonal antibody therapies including claim 31 , ZMapp claim 31 , REGN3470-3471-3479 claim 31 , mAb 114 ...

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 1131-. (canceled)134. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:ring B is phenyl; orring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.136. The compound of claim 134 , or a pharmaceutically acceptable salt or solvate thereof claim 134 , wherein:ring D is phenyl; orring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl; or{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}138. The compound of claim 136 , or a pharmaceutically acceptable salt or solvate thereof claim 136 , wherein:{'sup': 3', '10, 'Lis absent, —O—, —S—, —CH═CH—, —C≡C—, or —NR—.'}139. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 3', '8, 'ring A is C-Ccycloalkyl'}140. The compound of claim 132 , or a pharmaceutically acceptable salt or solvate thereof claim 132 , wherein:{'sub': 2', '8, 'ring A is C-Cheterocycloalkyl.'}141. The compound of claim 140 , or a pharmaceutically acceptable salt or solvate thereof claim 140 , wherein:{'sub': 2', '8', '5', '8', '5', '8', '5', '8', '5', '8, 'ring A is a monocyclic C-Cheterocycloalkyl or a bicyclic C-Cheterocycloalkyl ...

KETONE INHIBITORS OF LYSINE GINGIPAIN

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium . Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Ccycloalkyl claim 1 , Calkyl claim 1 , Caryl claim 1 , and 5- to 12-membered heteroaryl each of which is optionally substituted with one or more Rsubstituents claim 1 , and each Ris independently selected from the group consisting of halogen claim 1 , —N claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , —N(R) claim 1 , —N(R) claim 1 , and —NRC(O)R.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl substituted with Calkoxy.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.67-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris Chaloalkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris 5- to 12-membered heteroaryl claim 1 , which is optionally substituted with one or more members independently selected from the group consisting of halogen and Calkyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —N(R) claim 1 , 5- to 12-membered heteroaryl claim 1 , and 3- to 12-membered heterocyclyl claim 1 , wherein:{'sub': 1-3', '1-3, '5- to 12-membered heteroaryl is optionally substituted with one or more members ...

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 4. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is phenyl.5. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring B is monocyclic 6-membered heteroaryl selected from pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.7. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is phenyl.8. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:ring D is monocyclic heteroaryl selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, and pyridazinyl.11. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sub': 2', '8, 'ring D is a monocyclic heterocycle that is a monocyclic C-Cheterocycloalkyl containing at least 1 N atom in the ring that is selected from aziridinyl, azetidinyl, pyrrolidinyl, pyrrolidinonyl, pyrrolidine-2,5-dionyl, piperidinyl, piperidin-2-onyl, piperazinyl, morpholinyl, thiomorpholinyl, and azepanyl.'}12. The compound of any one of - , or a pharmaceutically acceptable salt or solvate thereof , wherein:{'sup': 3', '2', '4', '4', '2, 'Lis —X-L- or -L-X—;'}{'sup': 2', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2, 'Xis absent, —O—, —S—, —S(═O)—, —S(═O)—, —S(═O)NR—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, or —NR—;'}{'sup': '4', 'sub': '2', 'Lis absent or —CH—.'}13. The compound of any one of - , or a pharmaceutically ...

Enzymatic conjugation of polypeptides

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

INHIBITORS OF HISTONE DEACETYLASE

The present invention relates to compounds of formula (I): 10. A pharmaceutical composition comprising an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , or prodrug thereof and a pharmaceutical carrier claim 1 , diluent claim 1 , or excipient.11. A method of treating claim 1 , alleviating claim 1 , and/or preventing a condition in a subject comprising administering to the subject in need thereof an effective amount of a compound of or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate or prodrug thereof.12. The method of claim 11 , wherein the condition is selected from a neurological disorder claim 11 , memory loss or impairment claim 11 , cognitive function disorder or impairment claim 11 , extinction learning disorder claim 11 , fungal disease or infection claim 11 , inflammatory disease claim 11 , hematological disease claim 11 , and neoplastic disease.13. The method of claim 11 , wherein the condition is selected from:a cognitive function disorder or impairment associated with Alzheimer's disease, Huntington's disease, seizure induced memory loss, schizophrenia, Rubinstein Taybi syndrome, Rett Syndrome, Fragile X, Lewy body dementia, vascular dementia, ADHD, dyslexia, bipolar disorder and social, cognitive and learning disorders associated with autism, traumatic head injury, or attention deficit disorder, anxiety disorder, conditioned fear response, panic disorder, obsessive compulsive disorder, posttraumatic stress disorder, phobia, social anxiety disorder, substance dependence recovery or Age Associated Memory Impairment (AAMI), or Age Related Cognitive Decline (ARCD);a hematological disease selected from acute myeloid leukemia, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syndromes, and sickle cell anemia;a cancer; andan extinction learning disorder selected from a fear extinction deficit and post-traumatic ...

NOVEL POTASSIUM CHANNEL INHIBITORS

The present invention relates to novel compounds, pharmaceutical compositions comprising such compounds and their use for treating, alleviating or preventing diseases or disorders relating to the activity of potassium channels. 4. The compound according to claim 3 , wherein{'sup': '9', 'Ris —C(H)— or —N—;'}{'sup': '10', 'Ris H or halogen;'}{'sup': '11', 'Ris H or halogen;'}{'sup': '12', 'sub': 3', '3, 'Ris —CX, —OCX, H or halogen; and'}X is halogen.5. The compound according to any one of the preceding claims claim 3 , wherein Rand Rare —H claim 3 , Rand Rare methyl claim 3 , and Rand Rare —H.11. The compound according to any one of the preceding claims claim 3 , wherein Ris —C(O)—OCalkyl.12. The compound according to any one of the preceding claims claim 3 , wherein Ris Calkyl.13. The compound according to any one of the preceding claims claim 3 , wherein Ris —CF claim 3 , —OCF claim 3 , or a halogen.14. The compound according to any one of the preceding claims claim 3 , wherein Ris —C(H)— claim 3 , Ris H claim 3 , Ris F and Ris —CF.15. The compound according to any one of the preceding claims claim 3 , wherein the compound is selected from the group consisting of:Methyl N-(2-(dimethylamino)ethyl)-N-(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl) carbamate;Methyl (2-amino-2-methylpropyl)(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl)carbamate;Methyl ((1-aminocyclopropyl)methyl)(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl) carbamate;Methyl 3-((1-(4-fluoro-3-(trifluoromethyl) phenyl) cyclopropyl) (methoxycarbonyl)amino)azetidine-1-carboxylate;Methyl azetidin-3-yl(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl)carbamate;N-(cyclopropylmethyl)-N-(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl)azetidin-3-amine;Methyl (2-aminoethyl)(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl)carbamate;N1-(cyclopropyl methyl)-N1-(1-(4-fluoro-3-(trifluoromethyl)phenyl)cyclopropyl)-2-methyl propane-1,2-diamine;N-(2-amino-2-methylpropyl)-N-(1-(4-fluoro-3-( ...

OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO

Compounds are provided having the structure of Formula (I): 1100-. (canceled)102. The compound of claim 101 , or a pharmaceutically acceptable isomer claim 101 , racemate claim 101 , hydrate claim 101 , solvate claim 101 , isotope claim 101 , or salt thereof claim 101 , wherein:ring A is phenyl, pyridinyl, or pyrazinyl;{'sub': 3', '7, 'sup': '7', 'ring C is a C-Ccycloalkyl or 3-7 membered heterocycloalkyl, substituted with 0-5 R;'}{'sup': 1', '2, 'Rand Rare each, independently, H, methyl, ethyl, isopropyl or cyclopropyl, substituted with 0-3 halo;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6, 'Rand Rare each, independently, H, (C-C)alkyl, (C-C)haloalkyl, or cyclopropylmethyl;'}{'sup': 5', '1', '2', '3', '5, 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently —C(O)NRR, —OH, halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle; or Rand one R, together with the atoms to which they are connected, form a 5-7 membered heterocycle;'}{'sup': '6', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '7', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '8', 'Ris H;'}m is 1-3; andn is 0-3.103. The compound of claim 102 , or a pharmaceutically acceptable isomer claim 102 , racemate claim 102 , hydrate claim 102 , solvate claim 102 , isotope claim 102 , or salt thereof claim 102 , wherein ring A is phenyl.104. The compound of claim 103 , or a pharmaceutically acceptable isomer claim 103 , racemate claim 103 , hydrate claim 103 , solvate claim 103 , isotope claim 103 , or salt thereof claim 103 , wherein ring B is phenyl claim 103 , indazolyl claim 103 , 2 claim 103 ,3-dihydrobenzoxazolyl claim 103 , benzoxazolonyl claim 103 , or pyrazolopyridinyl.105. The compound of claim 104 , or a pharmaceutically acceptable isomer claim 104 , racemate claim 104 , hydrate claim 104 , solvate claim 104 , isotope claim 104 , or ...

NOVEL KCNQ POTASSIUM CHANNEL AGONIST, AND PREPARATION METHOD THEREFOR AND USE THEREOF

The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window. 2. The method according to claim 1 , wherein claim 1 ,{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}4. The method according to claim 3 , wherein claim 3 ,{'sub': '1', 'Ris H or fluorine;'}{'sub': 2', '3', '2', '3, 'Rand Rare each independently selected from a group consisting of H and D, or Rand Rtogether with the carbon atom to which they attached form cyclopropyl;'}{'sub': 4', '5', '1', '4', '1', '4, 'one of Rand Ris C-Calkyl, and the other is H or C-Calkyl.'}8. The method according to claim 1 , wherein one of Rand Ris methyl claim 1 , and the other is H or methyl.9. The method according to claim 1 , wherein the pharmaceutical acceptable salt is a salt formed by reacting the compound with an acid.10. The method according to claim 9 , wherein the acid is selected from a group consisting of maleic acid claim 9 , succinic acid claim 9 , citric acid claim 9 , tartaric acid claim 9 , fumaric acid claim 9 , formic acid claim 9 , acetic acid claim 9 , propanoic acid claim 9 , propandioic acid claim 9 , oxalic acid claim 9 , benzoic acid claim 9 , phthalic acid claim 9 , methanesulfonic acid claim 9 , ...

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections.X is selected from the group consisting of O and H;R1 is selected from (C6 to C10) aryl and (C2 to C9) heteroaryl, andR2 is selected from (C1 to C10) alkyl, (C1 to C10) alkenyl, (C1 to C10) alkynyl, (C3 to C10) cycloalkyl, and (C5 to C10) cycloalkenyl, andNR3aR3b is defined in the specification.These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions. 198.-. (canceled)100. The compound of wherein claim 99 ,{'sup': 42', '40', '9', '10', '19', '9', '10, 'sub': 1', '5, 'G is selected from —N(R)C(═O)—R; and Rand Rare each independently selected from hydrogen, halogen, C-Calkyl, or —OR; or Rand Rform an oxo.'}101. The compound of wherein claim 99 ,{'sup': 42', '40', '9', '19', '10, 'sub': 1', '5, 'G is selected from —N(R)C(═O)—R; and Ris —OR; and Ris selected from hydrogen, halogen, or C-Calkyl.'}102. The compound of wherein claim 99 ,{'sup': 42', '40', '9', '10, 'G is selected from —N(R)C(═O)—R; and Rand Rform an oxo.'}103. The compound of wherein claim 100 ,{'sup': 11', '12, 'Rand Rare each hydrogen; and n is 0.'}104. The compound of wherein claim 101 ,{'sup': 11', '12, 'Rand Rare each hydrogen; and n is 0.'}105. The compound of wherein claim 102 ,{'sup': 11', '12, 'Rand Rare each hydrogen; and n is 0.'}106. The compound of wherein claim 103 ,{'sup': 16', '17, 'sub': 1', '5, 'Rand Rare each independently selected from hydrogen or C-Calkyl; and'}{'sup': '18', 'sub': 1', '5, 'Ris selected from hydrogen, C-Calkyl, alkoxy, or hydroxyl.'}107. The compound of wherein claim 104 ,{'sup': 16', '17, 'sub': 1', '5, 'Rand Rare each independently selected from hydrogen, C-Calkyl; and'}{'sup': '18', 'sub': 1', '5, 'Ris selected from hydrogen, C-Calkyl, alkoxy, or hydroxyl.'}108. The compound of wherein claim 105 ,{'sup': 16', '17, 'sub': 1', '5, 'Rand Rare each independently selected from hydrogen, C-Calkyl; and'}{'sup': '18', 'sub': 1', '5, 'Ris selected from hydrogen, C-Calkyl, alkoxy, or hydroxyl.'}109. The compound of wherein claim 99 ,{'sup': 42', '42', '42', '40', '9', '10', '19', '9', '10, 'sub': 1', '5, 'G is selected from —N(R)—C(R)(R)—R; and Rand Rare each independently selected from hydrogen, ...

ORGANIC COMPOUNDS, LIGHT MODULATING COMPOSITION AND LIGHT MODULATING DEVICES EMPLOYING THE SAME

An organic compound, a light modulating composition and a light modulating device are provided. The organic compound has a chemical structure represented by formula (I): 2. The organic compound as claimed in claim 1 , wherein Ris a C1-8 alkyl group.3. The organic compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , a C1-8 alkyl group claim 1 , or a C1-8 alkoxy group.4. The organic compound as claimed in claim 1 , wherein Ris hydrogen claim 1 , a C1-8 alkyl group claim 1 , or a C1-8 alkoxy group.9. A light modulating composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a first oxidizable compound, wherein the first oxidizable compound is as claimed in ;'}a reducible compound;an electrolyte; anda solvent.10. The light modulating composition as claimed in claim 9 , wherein the electrolyte is an organic ammonium salt or an inorganic lithium salt.11. The light modulating composition as claimed in claim 9 , wherein the oxidizable compound and the electrolyte have a mole ratio of 1:1 to 1:20 claim 9 , and the reducible compound and the electrolyte have a mole ratio of 1:1 to 1:20.12. The light modulating composition as claimed in claim 9 , wherein the concentration of the electrolyte is between 0.01M and 1.5M.15. A light modulating device claim 9 , comprising:a pair of electrodes, comprising:a first transparent substrate with a first transparent conductive layer on a surface of the transparent substrate; anda second transparent substrate with a second transparent conductive layer on a surface of the transparent substrate, disposed by arranging the first transparent conductive layer and the second transparent conductive layer to face each other;an isolating unit, inserted between the first and second transparent conductive layers to form a cell; anda light modulating composition filled in the cell, wherein the light modulating composition comprises:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a first oxidizable compound, ...

ENZYMATIC CONJUGATION OF ANTIBODIES

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions. 1. A human or humanized antibody comprising one or more solvent-exposed glutamine residues in a variable region and at least one acceptor glutamine residue in its constant region or in a sequence fused to a variable or constant region , wherein said one or more solvent-exposed glutamine residues are present in a light chain variable domain (VL) CDR at a Kabat position selected from the group consisting of 27 , 55 , and a combination thereof ,{'sub': 'n', 'wherein said antibody is conjugated via said acceptor glutamine residue to one or more moieties-of-interest (Z) through a linker that comprises a NH—(C)— moiety,'}wherein{'sub': 'n', '(C)is a substituted or unsubstituted alkyl or heteroalkyl chain, optionally wherein any carbon of the chain is substituted with an alkoxy, hydroxyl, alkylcarbonyloxy, alkyl-S—, thiol, alkyl-C(O)S—, amine, alkylamine, amide, or alkylamide, and n is an integer selected from among the range of 2 to 20; and'}Z is a reactive moiety or a moiety that improves the pharmacokinetic properties, a therapeutic moiety or a diagnostic moiety.2. The antibody of claim 1 , wherein the antibody is a tetrameric antibody and said constant region is a heavy chain constant region.34-. (canceled)5. The antibody of claim 1 , wherein the antibody comprises:a heavy chain framework region 1 (FR-H1) comprising a glutamine residue at Kabat position 1, 3, 5, 6, 10, 11, 12, 13 and/or 16;a heavy chain framework region 2 (FR-H2) comprising a glutamine residue at Kabat position 38, 39, 43 and/or 45;a heavy chain framework region 3 (FR-H3) comprising a glutamine residue at Kabat position 66, 75, 77, 81 and/or 85;a heavy chain framework region 1 (CDR-H1) comprising a glutamine residue at Kabat position 26 and/ ...

KETONE INHIBITORS OF LYSINE GINGIPAIN

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium . Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Ccycloalkyl claim 1 , Calkyl claim 1 , Caryl claim 1 , 5- to 12-membered heteroaryl claim 1 , and 3- to 12-membered heterocyclyl claim 1 , each of which is optionally substituted with one or more Rsubstituents.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently selected from the group consisting of halogen claim 1 , —N claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , —N(R) claim 1 , —N(R) claim 1 , and —NRC(O)R.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —O-phenyl claim 1 , wherein phenyl is substituted with 1-5 halogens.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of 2 claim 1 ,3 claim 1 ,6-trifluorophenoxy; 2 claim 1 ,3 claim 1 ,5-trifluorophenoxy; 2 claim 1 ,3 claim 1 ,4-trifluorophenoxy; 3 claim 1 ,4 claim 1 ,5-trifluorophenoxy; 2 claim 1 ,3-difluorophenoxy; 2 claim 1 ,4-difluorophenoxy; 2 claim 1 ,5-difluorophenoxy; 2 claim 1 ,6-difluorophenoxy; 3 claim 1 ,4-difluorophenoxy; 3 claim 1 ,5-difluorophenoxy; 2-fluorophenoxy; 3-fluorophenoxy; and 4-fluorophenoxy.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O ...

NEW DERIVATES OF DHAA WITH ELECTROSTATIC TUNING

Dehydroabietic acid derivatives according to Formula Ia or Formula Ib and all stereoisomers thereof, having a linker chain A of 1 to 10 atoms selected from carbon, nitrogen and oxygen to a group X capable of being negatively charged at a physiological pH and covalently attached to the linker chain A, selected from carboxyl, sulfate, sulfonate and phosphate groups. The Dehydroabietic acid derivatives are useful for therapeutic treatment of hyperexcitability diseases

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring B is a bicyclic heterocyle or a bicyclic carbocycle.3. The compound of claim 2 , or a pharmaceutically acceptable salt or solvate thereof claim 2 , wherein:ring B is an 8-, 9- or 10-membered bicyclic heterocycle that is quinolinyl, isoquinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, naphthyridinyl, pteridinyl, indolizinyl, azaindolizinyl, indolyl, azaindolyl, indazolyl, azaindazolyl, benzimidazolyl, azabenzimidazolyl, benzotriazolyl, azabenzotriazolyl, benzoxazolyl, azabenzoxazolyl, benzisoxazolyl, azabenzisoxazolyl, benzofuranyl, azabenzofuranyl, benzothienyl, azabenzothienyl, benzothiazolyl, azabenzothiazolyl, or purinyl.4. The compound of claim 2 , or a pharmaceutically acceptable salt or solvate thereof claim 2 , wherein:ring B is an 8-, 9- or 10-membered bicyclic heterocycle with at least one N atom in the ring.8. The compound of claim 2 , or a pharmaceutically acceptable salt or solvate thereof claim 2 , wherein:ring B is a bicyclic carbocycle that is indanyl, indenyl, or naphthyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring B is a 5-membered heteroarylene containing 1-4 N atoms, 0 or 1 O or S atom or a 5-membered heteroarylene containing 0-4 N atoms, 1 O or S atom.10. The compound of claim 9 , or a pharmaceutically acceptable salt or solvate thereof claim 9 , wherein:ring B is a 5-membered heteroarylene selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazolyl, tetrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, and thiadiazolyl ...

TRISAMIDE COMPOUNDS AND COMPOSITIONS COMPRISING THE SAME

Provided are trisamide compounds and compositions containing the same. In an embodiment, the trisamides are represented by the following formula: 2. The trisamide compound of claim 1 , wherein Ris selected from the group consisting of C-Calkyl groups unsubstituted or substituted by one or more hydroxy; C-Calkenyl groups unsubstituted or substituted by one or more hydroxy; C-Calkyl groups interrupted by oxygen or sulfur; C-Calkyl groups substituted by one or more halogens; halogens; trimethylsilyl; and cyano.3. The trisamide compound of claim 1 , wherein Ris selected from the group consisting of C-Calkyl groups; branched C-Calkyl groups unsubstituted or substituted by one or more hydroxy; C-Calkyl groups substituted by one or more halogens; halogens; trimethylsilyl; and cyano.4. The trisamide compound of claim 1 , wherein Ris selected from the group consisting of C-Calkyl groups; branched C-Calkyl groups; fluorine claim 1 , chlorine; and trimethylsilyl.5. The trisamide compound of claim 1 , wherein Ris selected from the group consisting of branched C-Calkyl groups.6. The trisamide compound of claim 1 , wherein Xand Xare independently selected from the group consisting of:{'sub': 1', '20, 'C-Calkyl groups unsubstituted or substituted by one or more hydroxy;'}{'sub': 2', '20, 'C-Calkenyl groups unsubstituted or substituted by one or more hydroxy;'}{'sub': 2', '20, 'C-Calkyl groups interrupted by oxygen or sulfur;'}{'sub': 3', '12', '1', '20, 'C-Ccycloalkyl groups unsubstituted or substituted by one or more C-Calkyl groups;'}{'sub': 3', '12', '1', '10', '1', '20, '(C-Ccycloalkyl)-C-Calkyl groups unsubstituted or substituted by one or more C-Calkyl groups;'}{'sub': 3', '12', '1', '10', '1', '20, 'bis[C-Ccycloalkyl]-C-Calkyl groups unsubstituted or substituted by one or more C-Calkyl groups;'}{'sub': 1', '20, 'bicyclic or tricyclic hydrocarbon groups with 5 to 20 carbon atoms unsubstituted or substituted by one or more C-Calkyl groups;'}{'sub': 1', '20', '1', '20', '1', ' ...

Synthesis of Cyclohexane Carboxamide Derivatives Useful as Sensates in Consumer Products

Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product. The present invention relates to the synthesis of cyclohexane-based derivatives useful as sensates. In particular the present synthetic route can be used to prepare various isomers of cyclohexane-based carboxamide coolants.Oral care products, such as dentifrice and mouthwash, are routinely used by consumers as part of their oral care hygiene regimens. It is well known that oral care products can provide both therapeutic and cosmetic hygiene benefits to consumers. Therapeutic benefits include caries prevention, which is typically delivered through the use of various fluoride salts; gingivitis prevention, by the use of an antimicrobial agent such as stannous fluoride, triclosan, essential oils; or hypersensitivity control through the use of ingredients such as strontium chloride or potassium nitrate. Cosmetic benefits provided by oral care products include the control of plaque and calculus formation, removal and prevention of tooth stain, tooth whitening, breath freshening, and overall improvements in mouth feel impression, which can be broadly characterized as mouth feel aesthetics. Calculus and plaque along with behavioral and environmental factors lead to formation of dental stains, significantly affecting the aesthetic appearance of teeth. Behavioral and environmental factors that contribute to teeth staining propensity include regular use of coffee, tea, cola or tobacco products, and also the use of certain oral products containing ingredients that promote staining, such as cationic antimicrobials and metal salts.Thus daily oral care at home requires products with multiple ingredients working by different mechanisms to provide the complete range of therapeutic and aesthetic benefits, including anticaries, antimicrobial, antigingivitis, antiplaque, anticalculus and anti-erosion ...

INHIBITORS OF LYSINE GINGIPAIN

The present invention relates generally to therapeutics targeting the bacterium , including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. 145-. (canceled)47. The method of claim 46 , wherein Z is halogen-substituted phenoxymethyl carbonyl.48. The method of claim 46 , wherein Ris selected from the group consisting of cyclohexyl claim 46 , cyclopentyl claim 46 , morpholino claim 46 , phenyl claim 46 , piperidinyl claim 46 , pyridinyl claim 46 , tetrahydrofuranyl claim 46 , tetrahydropyranyl claim 46 , 1 claim 46 ,2 claim 46 ,3 claim 46 ,4-tetrahydronaphthyl claim 46 , and thiazolyl claim 46 , each of which is optionally substituted with 1-3 members selected from the group consisting of methyl claim 46 , methoxy claim 46 , trifluoromethyl claim 46 , acetyl claim 46 , and —N.50. The method of claim 49 , wherein{'sup': '3', 'Ris selected from the group consisting of cyclohexyl, cyclopentyl, morpholino, phenyl, piperidinyl, pyridinyl, tetrahydrofuranyl, tetrahydropyranyl, 1,2,3,4-tetrahydronaphthyl, and thiazolyl,'}{'sub': '3', 'each of which is optionally substituted with 1-3 members selected from the group consisting of methyl, methoxy, trifluoromethyl, acetyl, and —N.'}55. The method of claim 46 , wherein Ris selected from the group consisting of Calkyl and Chaloalkyl.58. The method of claim 46 , wherein the compound is administered to the subject for at least one month.59. The method of claim 46 , wherein the subject is a human claim 46 , a canine claim 46 , or a feline. The present application is a continuation of U.S. patent application Ser. No. 15/996,660, filed on Jun. 4, 2018; which is a continuation of U.S. patent application Ser. No. 15/683,348 filed on Aug. 22, 2017, now U.S. Pat. No. 9,988,375 ...

INHIBITORS OF LYSINE GINGIPAIN

The present invention relates generally to therapeutics targeting the bacterium , including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. 3. The compound of claim 1 , wherein Ris selected from the group consisting of Caryl claim 1 , 5-to-12 membered heteroaryl claim 1 , Ccycloalkyl claim 1 , 5-to-12 membered saturated heterocyclyl claim 1 , and -L-R.5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein{'sup': '3', 'Ris selected from the group consisting of cyclohexyl, cyclopentyl, morpholino, phenyl, piperidinyl, pyridinyl, tetrahydrofuranyl, tetrahydropyranyl, 1,2,3,4-tetrahydronaphthyl, and thiazolyl,'}{'sub': '3', 'each of which is optionally substituted with 1-3 members selected from the group consisting of methyl, methoxy, trifluoromethyl, acetyl, and —N.'}8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , whereinZ is selected from the group consisting of pyridin-2-yl-carbonyl and thiazol-2-yl-carbonyl, and{'sup': '3', 'sub': 6-10', '3-8, 'Ris selected from the group consisting of Caryl and Ccycloalkyl.'}11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Calkyl and Chaloalkyl.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.19. The method of claim 13 , wherein the disease or condition is selected from a brain disorder claim 13 , periodontal disease claim 13 , diabetes claim 13 , a cardiovascular disease claim 13 , arthritis claim 13 , elevated risk of preterm birth claim 13 , pneumonia claim 13 , cancer claim 13 , a kidney disease claim 13 , a liver disease claim 13 , a retinal disorder claim ...

INHIBITORS OF LYSINE GINGIPAIN

The present invention relates generally to therapeutics targeting the bacterium , including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof. 145-. (canceled)47. The pharmaceutical composition of claim 46 , wherein Z is halogen-substituted phenoxymethyl carbonyl.48. The pharmaceutical composition of claim 46 , wherein Ris selected from the group consisting of cyclohexyl claim 46 , cyclopentyl claim 46 , morpholino claim 46 , phenyl claim 46 , piperidinyl claim 46 , pyridinyl claim 46 , tetrahydrofuranyl claim 46 , tetrahydropyranyl claim 46 , 1 claim 46 ,2 claim 46 ,3 claim 46 ,4-tetrahydronaphthyl claim 46 , and thiazolyl claim 46 , each of which is optionally substituted with 1-3 members selected from the group consisting of methyl claim 46 , methoxy claim 46 , trifluoromethyl claim 46 , acetyl claim 46 , and —N.50. The pharmaceutical composition of claim 49 , wherein{'sup': '3', 'Ris selected from the group consisting of cyclohexyl, cyclopentyl, morpholino, phenyl, piperidinyl, pyridinyl, tetrahydrofuranyl, tetrahydropyranyl, 1,2,3,4-tetrahydronaphthyl, and thiazolyl,'}{'sub': '3', 'each of which is optionally substituted with 1-3 members selected from the group consisting of methyl, methoxy, trifluoromethyl, acetyl, and —N.'}55. The pharmaceutical composition of claim 46 , wherein Ris selected from the group consisting of Calkyl and Chaloalkyl.59. The pharmaceutical composition of claim 58 , wherein Ris selected from the group consisting of cyclohexyl; 1-methylcyclohexyl; 1-methoxycyclohexyl; cyclopentyl; morpholin-2-yl; 4-acetylmorpholin-2-yl; phenyl; 2-trifluoromethylphenyl; 3-azidophenyl; piperidine-3-yl; 1-acetyl-piperidine-3-yl; pyridin-2-yl; pyridin-3-yl; pyridin-4-yl; 6-oxo-1 claim 58 ,6- ...

Modulators of the integrated stress pathway

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

AMIDE DERIVATIVE

The present invention provides a useful medicament for the treatment and/or prophylaxis of a disease associated with the enhancement of OPN production including cancer, which comprises a compound of formula: 3. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris Ccycloalkyl claim 1 , Cheterocycloalkyl claim 1 , Caryl claim 1 , or 5- to 10-membered heteroaryl wherein the Ccycloalkyl claim 1 , Cheterocycloalkyl claim 1 , Caryl claim 1 , and 5- to 10-membered heteroaryl may be optionally substituted with one group or the same or different two or more groups selected independently from the group consisting of halogen claim 1 , hydroxy claim 1 , amino claim 1 , mono- or di-Calkylamino claim 1 , Cacyl claim 1 , Cacylamino claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , and Chaloalkoxy at any replaceable positions;{'sup': '2', 'Ris hydrogen atom, amino, or hydroxy which is linked at the 2-position of the benzene ring;'}{'sup': 3', '3, 'sub': 1-6', '1-6', '1-6', '1-6, 'ORis linked at the 3-position of the benzene ring, and Ris phenyl which may be optionally substituted with one group or the same or different two or more groups selected independently from the group consisting of halogen, hydroxy, Calkyl, Chaloalkyl, Calkoxy, and Chaloalkoxy at any replaceable positions; and'}{'sup': '4', 'Ris hydrogen atom, halogen, or amino.'}4. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris Ccycloalkyl claim 1 , tetrahydropyranyl claim 1 , pyridyl claim 1 , thienyl claim 1 , or phenyl wherein the Ccycloalkyl claim 1 , tetrahydropyranyl claim 1 , pyridyl claim 1 , thienyl claim 1 , and phenyl may be optionally substituted with one group or the same or different two or more groups selected independently from the group consisting of halogen claim 1 , hydroxy claim 1 , amino claim 1 , Cacyl claim 1 , Cacylamino claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , and Chaloalkoxy at any ...

Substituted 4-benzyloxy-phenylmethylamide derivatives as cold menthol receptor-1 (cmr-1) antagonists for the treatment of urological disorder

The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives of formula (I), processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

Imaging and therapeutic compositions

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging and therapeutic agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

폴리아미노폴리아미드

하기식(I)의 폴리아미노플리아미드는, 바람직하기로는 저온에서 에폭시 수지를 경화시키는데 적합하다: 상기식에서, n은 1내지 4의 정수이고, A와 D는 동일하거나 상이하며 각각 독립적으로 하기식의 기타 라디칼이거나 : 또는 일반식 또는 의 두 라디칼의 이성질체 혼합물이며, E는 일반식 또는 의 라디칼이고, R은 수소 원자 또는 일반식 -CO-NH-A-HH 2 또는 -CO-NH-D-NH 2 의 라디칼이며, R1은 일반식의 -CO-NH-A-NH 2 , 또는 -CO-NH-D-NH 2 의 라디칼이고, m은 2내지 12의 정수이다.

新的萜类和大环类化合物

本发明涉及的新的萜类和大环类化合物是TGR5的激活剂，且能用于预防和/或治疗2型糖尿病、肥胖、神经病和/或肾病。

Substituted derivatives of 4-aminocyclohexane

FIELD: chemistry. SUBSTANCE: invention relates to novel compounds of general formula (1), which possess an affinity to the µ-opiod receptor and the ORL1-receptor. The invention also relates to the application of the said compounds for obtaining medications, which can be used in treatment of fear, stress and associated with stress syndromes, depressions, epilepsy, Alzheimer's disease, senile dementia, general cognitive dysfunctions, learning and memory disorders (as nootropic), withdrawal syndromes, alcohol and/or drug abuse and/or abuse of medications and/or alcohol, narcotic and medication addiction, etc. In general formula (1) (1) Y 1 , Y 1   ' , Y 2 , Y 2   ' , Y 3 , Y 3   ' , Y 4 and Y 4   ' in each case stand for -H; Q stands for -R 0 , -C(=O)-R 0 , -C(=O)OR 0 , -C(=O)NHR 0 , -C(=O)N(R 0 ) 2 or-C(=NH)-R 0 ; R 0 in each case stands for -C 1-8 -aliphate, -C 3-12 -cycloaliphate, -aryl, -heteroaryl, -C 1-8 -aliphate-C 3-12 -cycloaliphate, -C 1-8 -aliphate-aryl, -C 1-8 -aliphate-heteroaryl, -C 3-8 -cycloaliphate-C 1-8 -aliphate, -C 3-8 -cycloaliphate-aryl or -C 3-8 -cycloaliphate-heteroaryl; R 1 and R 2 independently on each other stand for -C- 1-8 -aliphate; R 3 stands for -C 1-8 -aliphate, -aryl, -heteroaryl or -C 1-8 -aliphate-C 3-12 -cycloaliphate; n stands for 0; X stands for -NR A -;R A stands for -C 1-8 -aliphate; R B stands for -C 1-8 -aliphate; on condition that R 1 , R 2 , R A and R B simultaneously do not stand for the non-substituted-C 1-8 -aliphate. EFFECT: increased efficiency of the application of the compounds. 9 cl, 11 tbl, 164 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 209/12 C07D 209/14 C07D 401/04 C07D 251/48 C07C 211/40 C07C 233/36 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 233/46 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 311/18 C07D 211/62 C07D 213/12 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 532 545 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D A61K A61K A61K A61P A61P 213/ ...

含六元环的化合物,其制备方法及其作为药物的用途

描述了新颖化合物。这些化合物一般包含有酸性基团,碱性基团,取代的氨基或N－酰基和具有选择性羟基化的链烷部分的基团。还描述了包含本发明抑制剂的药物组合物。还描述了在可能含有神经氨酸酶的试样中抑制神经氨酸酶的方法。还描述了带标记的本发明化合物的抗原材料、聚合物、抗体、共轭物及检测神经氨酸酶活性的测定方法。

Замещенные производные 4-аминоциклогексана

Изобретение относится к новым производным 4-аминоциклогексана, которые обладают сродством к µ-опиоидному рецептору и ORL1-рецептору. В формуле (1) Y 1 , Y 1 ', Y 2 , Y 2 ', Y 3 , Y 3 ', Y 4 и Y 4 ' означают -Н; Q означает -R 0 , -C(=O)-R 0 или -C(=NH)-R 0 ; R 0 и R 3 в каждом случае независимо означает -C 1-8 -алифат, -арил, -гетероарил, -C 1-8 -алифат-С 5 -циклоалифат, -C 1-8 -алифат-арил; R 1 и R 2 , независимо означают незамещенный -C 1-8 -алифат; -C 1-8 -алифат-C 5 -циклоалифат, -C 1-8 -алифат-арил; n означает 0; Х означает -NR A -; R A означает незамещенный -C 1-8 -алифат; R B означает незамещенный -C 1-8 -алифат; «алифат» представляет собой неразветвленный, насыщенный, незамещенный или моно- или многократно замещенный атомами -F углеводородный остаток; «циклоалифат» представляет собой насыщенный, незамещенный моноциклический углеводородный остаток, с 5 атомами углерода в цикле; «арил» означает фенил, который может быть замещенным -F, -R 0 и -OR 0 ; «гетероарил» означает 5-членный циклический ароматический остаток, который содержит 1 гетероатом, причем гетероатом представляет собой N или S, и гетероцикл может быть замещенным -F, -R 0 и -OR 0 ; гетероцикл может быть частью бициклической системы, включающей фенил. Изобретение также относится к лекарственному средству, содержащему указанные соединения, и к применению соединений для получения лекарственного средства для лечения: боли, стресса, эпилепсии, нарушений обучения и памяти, медикаментозной зависимости, сердечно-сосудистых заболеваний, нарушений приема пищи, локомоторных расстройств. 4 н. и 5 з.п. ф-лы, 10 табл., 164 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 503 660 (13) C2 (51) МПК C07D C07C C07D A61K A61K A61K ФЕДЕРАЛЬНАЯ СЛУЖБА A61K ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P A61P A61P (12) ОПИСАНИЕ 209/04 (2006.01) 211/40 (2006.01) 333/10 (2006.01) 31/135 (2006.01) 31/132 (2006.01) 31/381 (2006.01) 31/404 (2006.01) 25/00 (2006.01) 1/00 (2006.01) 9/00 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы ...

三酰胺化合物和包含所述三酰胺化合物的组合物

本发明提供三酰胺化合物和包含所述三酰胺的组合物。在一种实施方案中，三酰胺由式(I)表示： 其中R 1 表示除氢之外的单价基团，并且X 1 和X 2 独立地表示经选择的单价基团。

用作抗炎、免疫调节及抗增殖药剂的新化合物

本发明涉及用作抗炎、免疫调节及抗增殖药剂的通式(I)的化合物或其盐。

Sphyngosine kinase inhibitors

FIELD: medicine, pharmaceutics. SUBSTANCE: present invention refers to new compounds of formula I or their pharmaceutically acceptable salts showing an ability to inhibit sphingosine kinase, to a based pharmaceutical composition, to a method of inhibiting sphingosine kinase and a method of treating diseases specified in breast cancer, diabetic retinopathy, arthritis and colitis. , wherein X represents -C(R 3 ,R 4 )N(R 5 )-, -C(O)N(R 4 )-; R 1 represents phenyl unsubstituted or substituted by 1 or 2 halogens. The values of R 2 , R 3 , R 4 , R 5 substitutes are such as specified in the patent claim. EFFECT: preparation of new compounds. 17 cl, 24 dwg, 9 tbl, 26 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 447 060 (13) C2 (51) МПК C07C C07C C07C C07C C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИC07D C07D C07D 233/57 255/44 317/32 323/23 317/58 207/02 295/13 295/32 213/24 265/30 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D C07D C07D C07D C07D A61K A61K A61K 233/54 (2006.01) 277/46 (2006.01) 263/58 (2006.01) 277/82 (2006.01) 257/04 (2006.01) 209/88 (2006.01) 473/34 (2006.01) 31/33 (2006.01) 31/16 (2006.01) 31/13 (2006.01) (см. прод.) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ Приоритет(ы): (30) Конвенционный приоритет: 17.06.2005 US 60/691,563 (73) Патентообладатель(и): ЭПОУДЖИ БИОТЕКНОЛОДЖИ КОРПОРЕЙШН (US) 2 4 4 7 0 6 0 (43) Дата публикации заявки: 27.07.2009 Бюл. № 21 2 4 4 7 0 6 0 R U (56) Список документов, цитированных в отчете о поиске: US 4053509 А, 11.10.1977. US 5595995 А, 21.01.1997. US 4332806 А, 01.06.1982. US 3663565 A, 16.05.1972. US 4349552 A, 14.09.1982. US 6649600 B1, 18.11.2003. US 3657273 A, 18.04.1972. WO 99/26927 A2, 03.06.1999. WO 2004/089470 A2, 21.10.2004. SU 1574586 A1, 30.06.1990. SU 1367194 A1, 10.04.1996. RU 2197467 C2, 27.01.2003. SU 451691 A, 09.07.1975. (см. прод.) C 2 C 2 (45) Опубликовано: 10.04.2012 Бюл. № 10 (85) Дата начала рассмотрения заявки PCT на ...

Efficient isotactic polypropylene beta-crystal form nucleating agent and preparation method and application thereof

本发明公开了一类高效等规聚丙烯β晶型成核剂及其制备方法和应用，本发明制备的成核剂在添加量为等规聚丙烯质量的0.05～0.20wt％时，等规聚丙烯β晶型的相对含量可达85～99％；经本发明制备的成核剂改性后的聚丙烯样品与未改性的聚丙烯样品相比，其热变形温度提高了15～19℃，冲击性能和断裂伸长率均提高3～4倍；与经对称取代酰胺类β晶型成核剂DCHT改性后的等规聚丙烯样品相比，其β晶型的相对含量提高了5～16％，热变形温度提高了2～6℃，冲击性能提高了12～39％，断裂伸长率提高了12～37％。经本发明制备的成核剂改性后的聚丙烯样品具有较好的耐热性能和力学性能，拓展了等规聚丙烯的应用领域，极具工业应用前景。

Trisamide compound and composition containing it

Inhibitors of protein farnesyltransferase and squalene synthase

The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

Sigma receptor ligands

The present invention concerns phenylcyclopentylacetamides and phenylcyclopropylcarboxamides and analogues thereof, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Small­molecule modulators of trp­p8 activity

본 발명은 Trp-p8 작용제 및 Trp-p8 길항제를 포함하는, 소-분자 Trp-p8 조절자, 및 소-분자 Trp-p8 작용제를 포함하는 조성물을 비롯한 신규한 소-분자 Trp-p8 조절자를 확인하고 특성을 결정하기 위한 방법 및 Trp-p8 발현 세포의 생존도를 감소시키고/시키거나 상기 세포의 성장을 억제시키기 위한 방법, Trp-p8-매개성 양이온 유입을 활성화시키기 위한 방법, 아폽토시스 및/또는 괴사를 자극하기 위한 방법을 제공하며, Trp-p8 발현과 관련된, 암, 예컨대 폐암, 유방암, 대장암, 및/또는 전립선암을 비롯한 기타 질병, 예컨대 양성 전립선 비대증을 포함하는, 질병의 치료를 위한 관련 방법과 관련이 있다.

Hepatitis C virus inhibitors

The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Hepatitis c virus inhibitors

Hepatitis c virus inhibitors

The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents

본 발명은 다음 화학식 1의 화합물 또는 이의 염에 관한 것이다: The present invention relates to a compound of formula (I) or a salt thereof: 상기 식에서, Where A는 5개의 탄소원자를 함유하는 비방향족 환 시스템이고, 여기에서 이러한 환 시스템은 하나 이상의 이중 결합을 포함하고, 이 환에서 탄소원자중의 하나 이상은 그룹 X 에 의해 치환될 수 있으며, X 는 S, O, N, NR 4 , SO 또는 SO 2 로 이루어진 그룹으로부터 선택되고, 이 환의 탄소원자중의 하나 이상은 치환체 R 1 을 수반할 수 있고, A is a non-aromatic ring system containing five carbon atoms, wherein such ring system comprises at least one double bond, wherein at least one of the carbon atoms in the ring may be substituted by group X, X is S, Is selected from the group consisting of O, N, NR 4 , SO or SO 2 , at least one of the carbon atoms of this ring may carry a substituent R 1 , D 는 O, S, SO 2 , NR 4 또는 CH 2 이고, D is O, S, SO 2 , NR 4 or CH 2 , Z 1 및 Z 2 는 서로 독립적으로 O, S 또는 NR 5 이고, Z 1 and Z 2 are independently of each other O, S or NR 5 , R 1 은 독립적으로 H, 할로겐, 할로알킬, 할로알킬옥시 또는 알킬이고, R 1 is independently H, halogen, haloalkyl, haloalkyloxy or alkyl, R 2 는 H 또는 OR 6 이고, R 2 is H or OR 6 , R 3 은 H, 알킬, 사이클로알킬, 아릴, 알콕시, O-아릴, O-사이클로알킬, 할로겐, 아미노알킬, 알킬아미노, 하이드록실알킬, 할로알킬옥시, 헤테로아릴, 알킬티오, S-아릴, S-사이클로알킬, 아릴알킬 또는 할로알킬이다. R 3 is H, alkyl, cycloalkyl, aryl, alkoxy, O-aryl, O-cycloalkyl, halogen, aminoalkyl, alkylamino, hydroxylalkyl, haloalkyloxy, heteroaryl, alkylthio, S-aryl, S -Cycloalkyl, arylalkyl or haloalkyl. 소염제, 면역조절물질, 세포 증식, 류마티즘, 면역학적 질환, 디하이드로오로테이트 데하이드로제나제, 피리미딘 생합성, 생리학적으로 관능성인 유도체 Anti-inflammatory agents, immunomodulators, cell proliferation, rheumatism, immunological disorders, dehydroorotate dehydrogenase, pyrimidine biosynthesis, physiologically functional derivatives

Iron death inhibitors diarylamine para-acetamides

本发明提供了抑制铁死亡活性、或调节或抑制与铁死亡调节异常相关的疾病诸如神经病、缺血再灌注损伤、急性肾衰竭和癌症的化合物，包括相应的磺酰胺类，及其药学上可接受的盐、水合物和立体异构体。将化合物用于药物组合物以及制备和使用方法中，包括用有效量的化合物或组合物治疗有此需要的人，并检测由此产生的所述人的健康或病症的改善。

DERIVATIVES OF BENZENE AND THEIR PHARMACEUTICAL USE

Substituted Benzyloxy-Phenylmethylamide Derivatives

The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives, processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

Substituted 4-benzyloxy-phenylmethylamide derivatives as cold menthol receptor-1 (cmr-1) antagonits for the treatment of urological disorders

The present invention relates to novel substituted benzyloxy-phenylmethylamide derivatives of formula (I), processes for their preparation, and their use in medicaments, especially for the prophylaxis and treatment of diseases associated with Cold Menthol Receptor 1 (CMR-1) activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor overactivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

SUBSTITUTED BASIC 2-AMINOTETRALINE

Substituted basic 2-aminotetralines

Enzymatic conjugation of polypeptides

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

A kind of kcnq potassium channel agonist, preparation method and use

本发明提供了一种具有以下通式Ⅰ的结构的化合物或其药学上可接受的盐，其制备方法以及所述化合物或其药学上可接受的盐在制备治疗神经性类疾病如癫痫、惊厥、神经性疼痛、急性局部缺血性中风以及神经退行性疾病的药物中的用途。与瑞替加滨相比，本发明所述的化合物具有更好的脑组织吸收。并且，本发明所提供化合物不仅药效大大提高，而且神经毒副作用远低于瑞替加滨，因此具有更宽的安全窗口。

Enzymatic conjugation of polypeptides

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Enzymatic conjugation of polypeptides

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Enzymatic conjugation of antibodies

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Enzymatic conjugation of antibodies

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Enzymatic conjugation of antibodies

The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs. Also disclosed herein are linking reagents, functionalized antibodies, pharmaceutical compositions, and method of treating disease and/or conditions.

Anilide derivative, production and use thereof

本发明提供式(Ⅰ)化合物或其盐,其中R 1 是选择性取代的5至6元环;W是式(a)或(b)的二价基团,其中环A是选择性取代的5至6元芳香族环,X是选择性取代的C、N或O原子,环B是选择性取代的5至7元环:Z是化学键或二价基团;R 2 是(1)其中的氮原子可以形成季铵盐的选择性取代的氨基等;这些化合物可以拮抗MCP－1受体。

Patent RU2019111188A3

`” ВУ“? 2019111188” АЗ Дата публикации: 14.01.2021 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2019111188/04(02 1741) 15.09.2017 РСТЛ52017/051912 15.09.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/395,938 16.09.2016 05 2. 62/459,456 15.02.2017 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) КЕТОНОВЫЕ ИНГИБИТОРЫ ЛИЗИН-СПЕЦИФИЧНОГО ГИНГИПАИНА Заявитель: КОРТЕКСИМ, ИНК., 05 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) Аб/1К 31/16 (2006.01) А6б1К 45/06 (2006.01) С07С 323/42 (2006.01) Аб/1К 31/165 (2006.01) Аб1Р 25/00 (2006.01) С07С 381/00 (2006.01) Аб1К 31/167 (2006.01) Аб1Р 31/4 (2006.01) С07В 59/00 (2006.01) Аб/1К 31/41 (2006.01) С07С 233/62 (2006.01) (070 213/70 (2006.01) Аб1К 31/42 (2006.01) С07С 233/78 (2006.01) (070 213/65 (2006.01) Аб/1К 31/44 (2006.01) С07С 235/10 (2006.01) (070 213/68 (2006.01) Аб1К 31/4402 (2006.01) С07С 235/50 (2006.01) (070 213/651 (2006.01) Аб1К 31/4406 (2006.01) С07С 237/42 (2006.01) (070 213/82 (2006.01) Аб/1К 31/4409 (2006.01) ...

Diacylethylenediamine compound

本发明提供一种可用作抗肥胖药的化合物。本发明人对有望用作用于治疗肥胖、II型糖尿病、脂肪肝、以及由它们引起的相关疾病的药物组合物的有效成分、并且具有DGAT1抑制作用的化合物进行了研究，发现本发明的二酰基乙二胺化合物具有优异的DGAT1抑制作用，从而完成本发明。即，本发明的二酰基乙二胺化合物具有DGAT1抑制作用，可用作肥胖、II型糖尿病、脂肪肝、以及相关疾病的预防剂和/或治疗剂。

Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents

The present invention relates to compounds of the general formula (I), wherein A is a non-aromatic ring system containing 4 to 8 carbon atoms, wherein the ring system comprises at least one double bond and wherein one or more of the carbon atoms in the ring can be substituted by a group X, wherein X is selected from the group consisting of S, O, N, NH, NHR4, SO or SO¿2?, and wherein one or more of the carbon atoms of the ring can carry a substituent R?1¿; D is O, S, SO¿2?, NH, NHR?4¿, or CH¿2; R?1 is independently H, halogen, CF¿3?, OCF3, or C1-C5-alkyl; R?2¿ is H, OH, OR6, NH2, NHR7; R6 is H, alkyl, cycloalkyl, aryl, arylalkyl, alkylaryl, alkoxyalkyl, acylmethyl, (acyloxy)alkyl, non-symmetrical(acyloxy)alkyldiester, dialkylphosphate; R7 is H, alkyl, aryl, O-alkyl, O-aryl, cycloalkyl or O-cycloalkyl; R8 is hydrogen or alkyl; R3 is H, cycloalkyl, aryl, O-alkyl, O-aryl or O-cycloalkyl; R4 is C1-C5-alkyl or an unsaturated or saturated carbocycle selected from the group consisting of cyclopentyl, cyclohexyl or aryl; Z?1 and Z2¿ are independent from each other O, S, NH or NR5; R5 is OH, O-alkyl, O-aryl, alkyl or aryl; Ar is a monocyclic or polycyclic substituted or unsubstituted ring system which may contain one or more groups X and which contains at least one aromatic ring; Y is hydrogen, halogen, CF¿3?, OCF3, substituted or unsubstituted alkyl; substituted or unsubstituted cycloalkyl, Ar, O-substituted or unsubstituted Ar, O-substituted or unsubstituted alkylaryl, O-substituted or unsubstituted arylalkyl or (Formula); m is 0 or 1; and q is 0 to 10; with the proviso that when ring A is an unsubstituted carbocyclus containing five carbon atoms and one double bond between the CZ?1 and CZ2-¿substituents with Z1 = Z2 = O and R2 = OH, the following compounds are excluded: q = 0; Y = hydrogen; Ar = phenylene or naphthylene, phenylene substituted with one or two chlorine atoms or with 2-methyl, 4-methyl, 4-methoxy, 4-ethoxy, 2, 6-diethyl, 2-chloro-4-methyl, 4-bromo, 4-cyano, 2 ...

Fine-celled polystyrene foam and method for producing same

本发明涉及一种由苯乙烯聚合物组分(S)和式(I)添加剂生产小孔泡沫的方法，其中Z表示C 1 ‑C 5 亚烷基或氧或硫原子，R1和R2表示C 3 ‑C 12 烷基、C 3 ‑C 12 环烷基或苄基；并且R3、R4、R5和R6表示氢或C 1 ‑C 6 烷基，该方法包括以下步骤：加热至少一种苯乙烯聚合物组分(S)以获得熔融的聚合物模塑化合物，将发泡剂(T)引入熔融模塑化合物中以形成可发泡组合物(Z)，以及使可发泡组合物发泡以获得发泡模塑制品，所述熔融聚合物模塑化合物包含至少一种通式(I)的羧酸衍生物。

ANALOGUES OF HALOGENOBENZAMIDES BRANDED AS RADIOPHARMACEUTICALS

La présente invention concerne l'utilisation d'un composé de formule (I): dans laquelleR1 représente un radionucléide,Ar représente un noyau aromatique,m est un entier variant de 2 à 4,R2 et R3 représentent, indépendamment l'un de l'autre, un atome d'hydrogène, un groupe (C1-C6)alkyle, un groupe (C1-C6)alkényle ou un groupe aryle choisi parmi un groupe phényle, benzyle, imidazolyle, pyridyle, pyrimidinyle, pyrazinyle, indolyle, indazolyle, furyle et thiényle,ainsi que leurs sels d'addition à des acides pharmaceutiquement acceptable, pour la préparation d'une composition radiopharmaceutique destinée au diagnostic et/ou au traitement du mélanome. The present invention relates to the use of a compound of formula (I): wherein R1 represents a radionuclide, Ar represents an aromatic ring, m is an integer ranging from 2 to 4, R2 and R3 represent, independently of one another, other, a hydrogen atom, a (C1-C6) alkyl group, a (C1-C6) alkenyl group or an aryl group selected from phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl, as well as their pharmaceutically acceptable acid addition salts, for the preparation of a radiopharmaceutical composition for the diagnosis and / or treatment of melanoma.

N- [3- [2 - [(2,3-DIHYDRO-1H-INDEN-2-YL) ALKYLAMINO] - ETHYL] PHENYL] CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Novel phenylethyl and phenyl-propyl-amine

Sphingosine kinase inhibitors

Compuesto de fórmula**Fórmula** o una sal farmaceuticamente aceptable, hidrato o solvato del mismo, en la que: Y es -N(R4)-; R1 es fenilo, sustituido con 1 ó 2 halogenos, R2 es arilo, -alquilarilo, heterocicloalquilo, -alquil-heterocicloalquilo, heteroarilo o -alquil-heteroarilo opcionalmente sustituido; R3 es H, alquilo u oxo; en la que la parte de alquilo y anillo de cada uno de los grupos R2 y R3 anteriores esta opcionalmente sustituida con hasta 5 grupos que son independientemente alquilo (C1-C6), halógeno, haloalquilo, -0C(0)(alquilo C1-C6), -C(0)0(alquilo C1-C6), -CONR'R", -0C(0)NR' R", -NR'C(0)R", -CF3, -0CF3, -OH, alcoxilo hidroxialquilo, -CN, -CO2H, -SH, -S-alquilo, -SOR'R", -SO2R', -NO2 o NR'R", en la que R' y R" son independientemente H o alquilo (C1-C6), y en la que cada parte de alquilo de un sustituyente esta opcionalmente sustituida adicionalmente con 1, 2 1:5 3 grupos seleccionados independientemente de halógeno, CN, OH y NH2; y R4 es H o alquilo (C1-C6). Compound of formula ** Formula ** or a pharmaceutically acceptable salt, hydrate or solvate thereof, in which: Y is -N (R4) -; R1 is phenyl, substituted with 1 or 2 halogens, R2 is aryl, -alkylaryl, heterocycloalkyl, -alkyl-heterocycloalkyl, heteroaryl or -alkyl-heteroaryl optionally substituted; R3 is H, alkyl or oxo; wherein the alkyl and ring portion of each of the above R2 and R3 groups is optionally substituted with up to 5 groups that are independently (C1-C6) alkyl, halogen, haloalkyl, -0C (0) (C1-C6 alkyl ), -C (0) 0 (C1-C6 alkyl), -CONR'R ", -0C (0) NR 'R", -NR'C (0) R ", -CF3, -0CF3, -OH, hydroxyalkyl alkoxy, -CN, -CO2H, -SH, -S-alkyl, -SOR'R ", -SO2R ', -NO2 or NR'R", in which R' and R "are independently H or (C1 alkyl) -C6), and in which each alkyl part of a substituent is optionally further substituted with 1, 2 1: 5 3 groups independently selected from halogen, CN, OH and NH2; and R4 ...

Diacylethylenediamine compound

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

Biscationic acid amide and acid imide derivatives as charge controllers

ABSTRACT Biscationic acid amide and acid imide derivatives as charge controllers Use of biscationic acid amide and acid imide derivatives whose anion is the stoichiometric equivalent of one or more organic or inorganic, mixed or non-mixed anions, the compounds also being able to exist as mixed crystals with different cations, individually or in combination, as charge controllers for toners and developers employed for electrophotographic copying or multicopying of originals and for printing electronically, optically or magnetically stored data or in color proofing, and as charge controllers for powders and powder paints.

NEW DIBENZOCYCLOHEPTENES, THEIR PROCESS FOR OBTAINING AND THEIR APPLICATION AS A MEDICINAL PRODUCT

Method for producing substituted dibenzocycloheptenes

Substituted 4-aminocyclohexane derivatives

Labelled analogues of halobenzamides as radiopharmaceuticals

The present invention relates to the use of a compound of formula (I): in which R 1 represents a radionuclide, Ar represents an aromatic nucleus, m is an integer varying from 2 to 4, R 2 and R 3 represent, independently of one another, a hydrogen atom, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkenyl group or an aryl group chosen from a phenyl, benzyl, imidazolyl, pyridyl, pyrimidinyl, pyrazinyl, indolyl, indazolyl, furyl and thienyl group, and their addition salts with pharmaceutically acceptable acids, in the preparation of a radiopharmaceutical composition intended for the diagnosis and/or treatment of melanoma.

Bis:cationic acid amide and imide cpds. - used as charge transfer agents in toner and charge controllers for powder and powder paint

Charge transfer agents for toners and developers used in electrophotographic copying and printing of data stored in an electronic, optical or magnetic system or in colour proofing and charge control agents for powder and powder paints are bis-cationic acid amide and imide derivs. of formula (I), (II) and/or (III): R1-8 independently = H or a hydrocarbon gp., opt. contg. a hetero-atom; KR1R2 and K'R4R5 may = a ring system; if R1R2, R4 or R5 is connected to K or K' by a double bond, R3 or R6 is absent and/or one of R1-3 with R7 or R4-6 with or R8 = a 2-5C aliphatic bridge; A, A' and W1 = divalent, W2 = a tetravalent and W3 = a trivalent bridge based on a hydrocarbon, opt. contg. hetero-atoms, and W1 may also = a direct bond; K and K' independently = N, P, As or Sb; X(-) the stoichiometric equiv. of (in)organic or (un)mixed anion(s). USE/ADVANTAGE - (I), (II) and (III) are colourless. The claims include their use in powders and paints for coating metals, wood, plastics, glass, ceramics, cement concrete, textiles, paper or rubber, esp. in triboelectric or electrokinetic spray powder paints. They have high and constant charge control properties, excellent temp. stability and very good dispersibility. They can be synthesised more economically than the usual charge control agents.

The inhibitor of lysine porphyromonas mycoproteinase

本发明总体上涉及靶向细菌—牙龈卟啉单胞菌(包括其蛋白酶—赖氨酸牙龈卟啉菌蛋白酶(Kgp))的治疗学，以及其治疗与牙龈卟啉单胞菌感染相关的病症的用途，所述病症包括诸如阿尔茨海默氏病的脑部病症。在某些实施方案中，本发明提供了如本文所述的式I的化合物及其药物可接受的盐。

Novel phenylethyl and phenylpropylamines

Compounds of general formula (I) wherein Z is a saturated or unsaturated 3 to 6 carbon chain, m is 2 or 3, R1 is a hydrogen atom, or a straight or branched C1-4 alkyl group, R2, R3 and R13 are selected from the following groups: H, OH, OR14, halogen, CO2R9, CN, CF3, NO2, NH2, COCH3, OSO2CF3, OSO2CH3, CONR10R11 and OCOR12, R is (1), (2), (3) or (4) wherein R4, R5, R6, R7, R8, W, n3 and n4 have the definitions of the claims, processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment of psychiatric disorders.

Metadiamide compounds for controlling invertebrate pests

公开了式(1)的化合物、其N‑氧化物和盐， 其中Q、X、Y、A 1 、A 2 、L、R 1 、R 2 、R 3 、R 4 、R 5 、R 6a 、R 6b 、R 7 和R 8 如本公开中所定义。还公开了包含式(1)的化合物的组合物和用于防治无脊椎害虫的方法，所述方法包括使所述无脊椎害虫或其环境与生物学有效量的本公开的化合物或组合物接触。

Imaging and therapeutic compositions

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging and therapeutic agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

Anilide derivative, production and use thereof

This invention is provide a compound of formula (I) wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of formula (a) or (b) wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

Patent US4880802B1

Inhibitors of histone deacetylase

The present invention relates to compounds of formula (I): (I) or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.

Substituted acetylenic compounds useful for the treatment of diseases

The invention relates to novel compounds according to formula Ia and Ib; (Formula Ia and Ib) wherein A represents substituted or unsubstituted C1-10heteroaryl, C6-14aryl or C6- 10heterocycloalkylaryl; R1 is C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C3-6 cycloalkyl, or C1-6heterocycloalkyl, each of which are optionally substituted; X represents -CR3R4-(CR5R6)n-(CR7=CR8)m-(C6-14aryl)r-(C1-10heteroaryl)s-(CR9R10)p- (CR11 = CR12)q, R2 represents C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6hydroxyalkyl, C1-6haloalkyl, C1-6amino, C1-12alkylsilyl, C6-30alkylarylsilyl, C1-10heteroaryl, C6-14aryl, C1-10heterocycloalkyl, C1-10heterocycloalkenyl, C1-8cycloalkyl, C1-18cycloalkenyl, each of which is optionally substituted, or R2 represents hydrogen, carboxy, or hydroxy; or a pharmaceutically acceptable salt, solvate, or ester thereof; to processes for the preparation thereof, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, wherein said compounds being useful, e.g. in the treatment of diseases associated with disturbances of CaSR activity, such as hyperparathyroidism.

Opioid receptor modulators and products and methods related thereto

Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R3, R4, R5, R6, R8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.

Enzymatic conjugation of polypeptides

Novel amide derivatives and medicinal use thereof

The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action (see formula 1) wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.