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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 7513. Отображено 100.
29-03-2012 дата публикации

Bicyclic compounds and use as antidiabetics

Номер: US20120077812A1
Автор: Andrew J. Carpenter, Christopher R. Conlee, Gregory Peckham, Jing Fang, JUN TANG, Kien S. Du, Subba Reddy Katamreddy
Принадлежит: Individual

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.

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Номер записи: 1
17-05-2012 дата публикации

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

Номер: US20120122920A1
Автор: David Enrique MIGUEL CENTENO, Josep Castells Boliart, Marta Pascual Gilabert
Принадлежит: Institut Universitari de Ciencia i Tecnologia

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

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Номер записи: 2
30-08-2012 дата публикации

Selective calcium channel modulators

Номер: US20120220564A1
Автор: Eric Simonson, Hassan Pajouhesh, Michael E. Grimwood, Yongbao Zhu, Yuanxi Zhou
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I).

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Номер записи: 3
13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Автор: William J. Polvino, William R. Mann
Принадлежит: Helsinn Therapeutics Us Inc

The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

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Номер записи: 4
01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
Автор: Alexis Denis, Mayalen Oxoby, Sonia Escaich, Vincent Gerusz
Принадлежит: FAB PHARMA Sas

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

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Номер записи: 5
08-11-2012 дата публикации

[4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-fluoro-1-(2-methoxy-ethyl)-4-trifluoromethoxy-1h-indol-3-yl]-methanone as an inhibitor of mast cell tryptase

Номер: US20120283445A1
Автор: Adam W. Sledeski, Gregory Bernard Poli, John J. Shay, Jr., Nakyen Choy, Patrick Wai-Kwok Shum, Yong Mi Choi-Sledeski
Принадлежит: SANOFI SA

The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.

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Номер записи: 6
03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Автор: Andrew Stamford, Corey Strickland, Douglas W. Hobbs, Jared N. Cumming, Jeffrey F. Lowrie, Johannes H. Voight, Kurt W. Saionz, Samuel Chackalamannil, Suresh D. Babu, Tao Guo, Thuy X.H. Le, Ulrich Iserloh, Yan Xia, Ying Huang, Yusheng Wu
Принадлежит: Merck Sharp and Dohme LLC

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is R is —C(O)—N(R 27 )(R 28 ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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Номер записи: 7
14-03-2013 дата публикации

N-piperidinyl acetamide derivatives as calcium channel blockers

Номер: US20130065926A1
Автор: Hassan A. Pajouhesh, Jason Tan, Lingyun Zhang, Michael Edward Grimwood, Nagasree Chakka, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Yuanxi Zhou
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

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Номер записи: 8
04-04-2013 дата публикации

NOVEL BENZAMIDE DERIVATIVES

Номер: US20130085160A1
Автор: Cho Kang-Hun, Choi Sun-Ho, Choi Sung-Hak, Im Weon-Bin, Kim Mi-Yeon, Kim Soon-Hoe, Sohn Ju-Hee, Sohn Tae-Kyoung, Sung Hyun-Jung
Принадлежит:

The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HTreceptor agonist containing the same as an active ingredient. Benzamide derivatives of the present invention have a superior affinity for 5-HTreceptors, a capability to reduce a gastric emptying time and a low toxicity, and consequently are therapeutically effective for the treatment of a variety of diseases associated with -HTreceptors. 2. The compound of formula 1 of claim 1 , wherein m represents an integer of 1 to 5; and Q represents a heteroaromatic ring or phenyl wherein the heteroaromatic ring or phenyl is independently substituted by 0 claim 1 , 1 claim 1 , 2 or 3 substituents selected from among C-Calkyl claim 1 , C-Calkoxy claim 1 , hydroxy and halogen claim 1 , wherein the heteroaromatic ring is a C-Caromatic ring or C-Cbicyclic aromatic ring independently containing 1 to 4 hetero atoms selected from among N claim 1 , O and S.3. The compound of formula 1 of that is selected from among the following compounds:N-((1-(3-(1,2,4-triazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(tetrazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(indol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(2-methylimidazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(5-(indol-1-yl)pentyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(5-(1,2,3-triazol-1-yl)pentyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(1,2,3-triazol-1-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(3-(1,2,3-triazol-2-yl)propyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1-(pyridin-3-ylmethyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2-methoxybenzamide,N-((1((1-methylindol-3-yl)methyl)piperidin-4-yl)methyl)-4-amino-5-chloro-2- ...

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Номер записи: 9
02-05-2013 дата публикации

Chemical Compounds

Номер: US20130109701A1
Автор: Brown Alan Daniel, Rawson David James, Storer Robert Ian, Swain Nigel Alan
Принадлежит: PFIZER LIMITED

The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar, R, R, R, Rand Rare as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain. 2. A compound according to wherein X is —OCH—.3. A compound according to wherein X is —CHO—.4. A compound according to wherein Aris phenyl independently substituted by one to three Y.5. A compound according to wherein Arphenyl independently substituted by one or two Y.6. A compound according to wherein Aris phenyl meta-substituted by Y claim 1 , para-substituted by Y claim 1 , or meta- and para-substituted by independent Y.7. A compound according to wherein Y is F; Cl; CN; (C-C)alkyl claim 1 , optionally substituted by (C-C)cycloalkyl or one to three F; (C-C)cycloalkyl claim 1 , optionally substituted by one to three F; (C-C)alkyloxy claim 1 , optionally substituted by one to three F; or (C-C)cycloalkyloxy.8. A compound according to wherein Ris (C-C)alkyl or (C-C)cycloalkyl.9. A compound according to wherein Ris (C-C)alkyl or (C-C)cycloalkyl.10. A compound according to wherein R claim 1 , Rand Rare independently H claim 1 , F or Cl.11. A compound according to wherein Ris H; CN; F; Cl; (C-C)alkyl claim 1 , optionally substituted by one to three F; or (C-C)alkyloxy claim 1 , optionally substituted by one to three F.12. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof together claim 1 , as defined in claim 1 , with one or more pharmaceutically acceptable excipients.13. A pharmaceutical composition according to including one or more additional therapeutic agents.14. (canceled)15. (canceled)16. (canceled)17. ( ...

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Номер записи: 10
16-05-2013 дата публикации

DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

Номер: US20130123243A1
Автор: Arnaiz Damian O., Brown Greg, Claret Emmanuel, Cleve Arwed, Davey David, Guilford William, Khim Seok-Kyu, Kirkland Thomas, Kochanny Monica J., Liang Amy, Light David, Parkinson John, Vogel David, Wei Guo Ping, Ye Bin
Принадлежит:

This invention is directed to compounds of formula (I): 3. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, cyano, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each independently hydrogen or halo.'}4. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, optionally substituted phenyl, furanyl, thienyl, thiazolyl, or optionally substituted oxazolyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each hydrogen.'}6. A compound according to wherein R an optionally substituted heteroaryl.7. A compound according to wherein R is furanyl claim 6 , oxazoyl claim 6 , pyrazolyl claim 6 , pyridinyl claim 6 , triazolyl claim 6 , thiazolyl claim 6 , or benzothiazolyl claim 6 , each of which is optionally substituted.8. A compound according to wherein:{'sup': 2', '7', '5a', '5b', '5c, 'Rand R, together with the nitrogens to which they are attached and one of R, Rand R, form an optionally substituted 6- to 10-membered bridged N-heterocyclyl.'}10. A compound according to wherein:{'sup': 3', '12', '12', '12, 'Ris a direct bond, —O—, —R—O—, —O—R—, —O—R—O—, or an optionally substituted straight or branched alkylene chain;'}{'sup': 4', '12a, 'Ris a direct bond, —O—R— or an optionally substituted straight or branched alkylene chain;'}{'sup': 8', '13', '10', '13', '10', '13', '10', '11, 'Ris aralkyl optionally substituted with one or more substituents selected from the group consisting of —R—OR, —R—C(═O)ORand —R—C(═O)N(R)R;'}{'sup': 9', '10, 'each Ris independently alkyl, halo or —O—R;'}{'sup': '12', 'Ris an optionally substituted straight ...

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Номер записи: 11
23-05-2013 дата публикации

Flufenoxine derivatives for the treatment and prevention of amyloid pathologies

Номер: US20130131079A1
Автор: Ana Munoz Munoz, Carmen Pumar Duran, Francisco Ledo Gomez
Принадлежит: Faes Farma SA

The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).

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Номер записи: 12
30-05-2013 дата публикации

HISTONE DEMETHYLASE INHIBITORS AND METHODS FOR USING THE SAME

Номер: US20130137720A1
Автор: Wang Xiang, Xu Wenqing
Принадлежит: The Regents of the University of Colorado, a body corporated

The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an α-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an α-ketoglutarate mimic. 1. A compound of the formula: M-L-K , or a derivative or a prodrug thereof , wherein M is a methyllysine mimic , L is a linker , and K is an α-ketoglutarate mimic.3. The compound according to claim 2 , wherein Ris phenyl claim 2 , naphthyl claim 2 , benzyl claim 2 , or naphthylalkyl claim 2 , each of which is optionally substituted claim 2 , or fluorescein.4. The compound according to claim 2 , wherein X is NH.5. The compound according to claim 2 , wherein Y is O.6. The compound according to claim 2 , wherein Z is O.7. The compound according to claim 2 , wherein Ris C-Calkylene.8. The compound according to claim 2 , wherein Rand Rare methylene.9. The compound according to claim 2 , wherein Aris phenylene.10. The compound according to claim 2 , wherein Ris H or methyl.11. The compound according to claim 2 , wherein Ris alkyl or absent.13. The compound according to claim 12 , wherein Ris hydrogen or C-Calkyl.14. The compound according to claim 12 , wherein Xand Xare O.15. The compound according to claim 12 , wherein Yis —OR.16. The compound according to claim 12 , wherein Lis C-Calkylene or C-Calkenylene.17. A method for treating a clinic condition associated with activity of Jumonji C Domain-Containing Histone Demethylase comprising administering to the subject in need of such a treatment a therapeutically effective amount of a compound of .18. The method of claim 17 , wherein the clinical condition is a cancer or a mental retardation.19. A method for treating a clinic condition associated with overexpression of Jumonji C Domain-Containing Histone ...

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Номер записи: 13
06-06-2013 дата публикации

New piperidine derivatives, pharmaceutical compositions and uses thereof

Номер: US20130143876A1
Автор: Bernd Nosse, Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz
Принадлежит: Individual

The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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Номер записи: 14
06-06-2013 дата публикации

BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS

Номер: US20130143926A1
Автор: Donald Alastair David Graham, McDermott Joanne, Moffat David Festus Charles, Patel Sanjay Ratilal
Принадлежит:

The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R, R, R, R, R, Rand Rare as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90. 2. A compound as claimed in wherein Ris hydroxy.3. A compound as claimed in wherein R claim 1 , R claim 1 , Rand Rare the same or different and represent hydrogen or halogen atoms or hydroxy claim 1 , unsubstituted Calkyl or unsubstituted Calkoxy groups.4. A compound as claimed in wherein either:{'sup': 6', '7', '8', '9', '8', '9, 'sub': 3', '1-4', '1-4, '(i) Rrepresents —CH, Rrepresents —CRR-A wherein Rand Rare the same or different and represent a hydrogen or halogen atom or an unsubstituted Calkyl or Calkoxy group, and A represents a phenyl ring substituted with a group W; or'}{'sup': 6', '7, 'sub': 1-4', '1-4', '1-4', '1-4', '1-4', '1-2, '(ii) Rand R, together with the nitrogen atom to which they are bonded, form a pyrrolidinyl, piperidinyl or isoindolinyl group which is substituted with a group W and is optionally further substituted with 1 or 2 groups which are the same or different and are selected from halogen atoms and unsubstituted Calkyl, Calkoxy, hydroxyl, Chaloalkyl, Chaloalkoxy, Chydroxyalkyl, cyano, nitro, —SR′ and —NR′R″ groups where R′ and R″ are the same or different and represent hydrogen or unsubstituted Calkyl.'}5. A compound as claimed in wherein Alkrepresents a bond claim 1 , an unsubstituted Calkylene group claim 1 , or an unsubstituted —(Calkylene)-NH—(Calkylene)- group.6. A compound as claimed in wherein either:{'sup': 12', '13, 'sub': 1-6', '3-7', '6-10', '1-4', '6-10', '1-4', '3-7, '(i) Rand Rare the same or different and represent hydrogen, Calkyl, Ccarbocyclyl, Caryl, —(Calkyl)-(Caryl), or —(Calkyl)-(Ccarbocyclyl); or'}{'sup': 12', '13, 'sub': '3-7', '(ii) Rand R, together with the carbon atom to which they are bonded, ...

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Номер записи: 15
13-06-2013 дата публикации

HYDROBROMIDE SALT OF PRIDOPIDINE

Номер: US20130150406A1
Автор: FRØSTRUP Brian, Zimmermann Anne
Принадлежит: IVAX INTERNATIONAL GMBH

This invention relates to a new salt of Pridopidine, a drug substance currently in development for the treatment of Huntington's disease. More specifically the invention provides the pharmaceutically acceptable hydrobromide salt, pharmaceutical compositions comprising this salt, and uses of this salt as a drug substance. 1. A hydrobromide salt of 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine (Pridopidine).2. The hydrobromide salt of provided in an anhydrous form.3. The hydrobromide salt of provided in an anhydrous form and non-solvated form.4. The hydrobromide salt of provided in an anhydrous form which is in a substantially crystalline form.5. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 6.0 and 3.8.6. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 3.6 and 4.0.7. The hydrobromide salt of having an X-ray powder diffraction pattern with reflections corresponding to the d-spacing values 7.6 claim 1 , 6.9 claim 1 , 6.0 claim 1 , 5.4 claim 1 , 4.3 claim 1 , 4.2 claim 1 , 4.0 claim 1 , 3.8 claim 1 , 3.6 claim 1 , 3.1.8. The hydrobromide salt of having an x-ray powder diffraction pattern with reflections corresponding to the d-spacing values 10.8 claim 1 , 7.6 claim 1 , 6.9 claim 1 , 6.0 claim 1 , 5.7 claim 1 , 5.4 claim 1 , 5.3 claim 1 , 5.2 claim 1 , 4.7 claim 1 , 4.6 claim 1 , 4.3 claim 1 , 4.2 claim 1 , 4.0 claim 1 , 3.8 claim 1 , 3.7 claim 1 , 3.6 claim 1 , 3.5 claim 1 , 3.4 claim 1 , 3.3 claim 1 , 3.2 claim 1 , 3.1.9. The hydrobromide salt of characterized by having an endotherm with an onset of about 196° C. claim 1 , as obtained with DSC.10. The hydrobromide salt of characterized by having an IR spectrum with absorptions at about 2950 cm-1 claim 1 , 2700-2500 cm-1 claim 1 , 1550 cm-1 claim 1 , 1450 cm-1 claim 1 , 1300 cm-1 claim 1 , 1150 cm-1 claim 1 , 1100 cm-1 claim 1 , 950 cm-1 claim 1 , 900 cm-1 claim 1 , ...

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Номер записи: 16
27-06-2013 дата публикации

HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Номер: US20130165422A1
Автор: BARTSCH Regine, CHEURET Dorothee, EVEN Luc, Hoornaert Christian, Jeunesse Jean, MARGEUT Frank
Принадлежит: SANOFI

The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): 2. The compound of formula (I) according to claim 1 , wherein:{'sup': '1', 'Rrepresents a phenyl, naphthyl, indanyl, benzoxazole, benzisoxazole, benzimidazole, benzotriazole, oxadiazole, indazole, isoxazole, pyridine, pyrazine, pyrimidine, thienyl, thiazole, benzothiophene, indole, dihydrobenzodioxane, benzothiadiazole, pyrazole, dihydrobenzoxazine or indoline group;'}{'sup': '2', 'sub': 3', '3', '2', '2', '2', '2', '2, 'Rrepresents one or more groups chosen from a halogen atom or a methyl, trifluoromethyl, methoxy, trifluoromethoxy, cyano, oxo, CHNHCO, CHSO, NHCO, NHSOand pyrrolidine-SOgroup;'}{'sup': '3', 'Rrepresents a group chosen from a phenyl and an oxazole; and also the compound 2,2,2-trifluoro-1-(trifluoromethyl)ethyl 4-{[3-(2-methylpyrimidin-4-yl)benzenesulphonylamino]methyl}piperidine-1-carboxylate,'}in the form of the base or of an addition salt with an acid.3. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '3', '2, 'Z represents a bond or a CH, (CH), CH═CH, C≡C, OCHor OC(CH)group,'}in the form of the base or of an addition salt with an acid.4. The compound of formula (I) according to claim 1 , wherein:{'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '2, 'A represents a bond, an oxygen atom, a sulphur atom, an OCHgroup, an O—(CH)group, an NH, NHCHor NH(CH)group, an SOor CO group, a CONH group, a CONHCHor CONH(CH)group, an SONH group, an SONHCHor SONH(CH)group, an SONHCO, SONHCONH or SONHCONHCHgroup, an OCONH group, an NHCONH group, an NHCONHCHgroup, an N(CH)CONHCH, NHCONH(CH)or N(CH)CONH(CH)group or an SON(CH)CHgroup,'}in the form of the base or of an addition salt with an acid.5. The compound of formula (I) according claim 1 , wherein m and n represent 1 claim 1 , in the form of the base or of an addition salt with an ...

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Номер записи: 17
27-06-2013 дата публикации

PROSTAGLANDIN D SYNTHASE INHIBITORY PIPERIDINE COMPOUNDS

Номер: US20130165438A1
Автор: Aoki Shinichi, Kitade Makoto, Urade Yoshihiro, Yamanaka Hiroyoshi, Yamane Keiko
Принадлежит: TAIHO PHARMACEUTICAL CO., LTD.

The present invention provides a piperidine compound represented by Formula (I) 2. The piperidine compound or a salt thereof according to wherein{'sup': 1', '2', '3, 'Xis nitrogen, and Xand Xare the same or different and each represents CH; or'}{'sup': 1', '3', '1', '2, 'Xand Xare the same or different and each represents C—R, and Xis CH; and'}{'sup': '1', 'Ris halogen.'}3. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of at least one of the compounds according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.4. A prostaglandin D synthase inhibitor comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of the compound according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.5. An agent for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates claim 1 , the agent comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of the compound according to or a pharmaceutically acceptable salt thereof, and'}a pharmaceutically acceptable carrier.6. The agent according to claim 5 , wherein the disease in which prostaglandin D2 or a metabolite thereof participates is an allergic disease or an inflammatory disease.7. A method for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates claim 1 , comprising administering claim 1 , to a mammal claim 1 , the compound or a salt thereof according to in an amount effective for preventing or treating the disease.8. Use of the compound or a salt thereof according to for producing an agent for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates.9. The compound or a salt thereof according to for use in a method for preventing or treating a disease in which prostaglandin D2 or a metabolite thereof participates. The ...

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Номер записи: 18
27-06-2013 дата публикации

Piperidine Derivatives

Номер: US20130165444A1
Автор: Bernd Nosse, Gerald Juergen Roth, Martin Fleck, Thorsten Lehmann-Lintz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

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Номер записи: 19
04-07-2013 дата публикации

SUBSTITUTED ANILINES AS CCR(4) ANTAGONISTS

Номер: US20130172315A1
Автор: Charvat Trevor T., Fan Junfa, Lange Christorpher W., LELETI Manmohan Reddy, Li Yandong, MacMahon Jeffrey P., Mali Venkat Reddy, Powers Jay, Punna Sreenivas, Yang Ju
Принадлежит: ChemoCentryx, Inc.

Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. 2. A compound of claim 1 , wherein X and Y are not both N.3. A compound of claim 1 , wherein Ris H claim 1 , and each Ris a member independently selected from the group consisting of Calkyl claim 1 , Chaloalkyl claim 1 , halogen and —CN.5. A compound of claim 4 , wherein X is C or CH.8. A compound of claim 7 , wherein n is 1 claim 7 , and Ris hydrogen or methyl.10. A compound of claim 9 , wherein n is 1 claim 9 , and Ris hydrogen or methyl.12. A compound of claim 11 , wherein n is 1 claim 11 , and Ris hydrogen or methyl.14. A compound of claim 1 , wherein B is C(O).15. A compound of claim 1 , wherein the ring having Z as a ring vertex is selected from the group consisting of pyrrolidine and piperidine.16. A compound of claim 1 , wherein the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-2-yl and piperidin-2-yl claim 1 , and at least one of R claim 1 , Rand Ris other than hydrogen.17. A compound of claim 1 , wherein B is a bond.18. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidine claim 1 , piperidine and cyclohexane.19. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-1-yl claim 1 , pyrrolidin-2-yl claim 1 , piperidin-1-yl claim 1 , piperidin-2-yl claim 1 , piperidin-3-yl and cyclohexane.20. A compound of claim 1 , wherein B is a bond and the ring having Z as a ring vertex is selected from the group consisting of pyrrolidin-1-yl claim 1 , pyrrolidin-2-yl claim 1 , piperidin-1-yl claim 1 , piperidin-2-yl claim 1 , piperidin-3-yl and cyclohexane; and at least one of R claim 1 , Rand Ris other than hydrogen.21. A compound of claim 1 , wherein Z is CH or N.23. A pharmaceutical composition ...

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Номер записи: 20
04-07-2013 дата публикации

ANTHELMINTICS FOR PREVENTING PARASITIC INFECTIONS IN HUMANS AND ANIMALS

Номер: US20130172385A1
Автор: Harder Achim, Kruger Bernd-Wieland, Mehlhorn Heinz, Schmidt Jurgen, von Samson-Himmlstjerna Georg
Принадлежит: LANXESS DEUTSCHLAND GMBH

The present invention relates to compositions comprising certain active compounds which are suitable as repellents, and to their use for preventing an infection of humans or of animals by the infectious states of parasitic flatworms (platyhelminths). 2. Compositions for deterring helmintic parasites according to claim 1 , characterized in that they comprise at least one compound of the formula (I) in which{'sub': 1', '6, 'Y represents hydrogen, C-C-alkyl or the radical O—X,'}{'sup': 11', '13, 'X represents hydrogen, CORor R,'}{'sup': '1', 'sub': 3', '7', '3', '7', '1', '2', '3', '7', '1', '2', '3', '7', '1', '6', '1', '6, 'Rrepresents C-C-cycloalkyl, C-C-cycloalkenyl, C-C-alkyl-C-C-cycloalkyl, C-C-alkyl-C-C-cycloalkenyl, where the cycloalkyl or cycloalkenyl rings of the abovementioned radicals are optionally substituted up to three times by C-C-alkyl or by a C-C-dialkylene bridge, or'}{'sup': '1', 'sub': 1', '7', '2', 'r', '2', 'r, 'Rrepresents C-C-alkyl, C-Calkenyl or C-Calkinyl,'}{'sup': 2', '11', '13, 'sub': 1', '6, 'R, R, Rare identical or different and represent C-C-alkyl,'}{'sup': 3', '8', '2', '3', '3', '7', '3', '5', '5', '7, 'sub': 1', '6, 'Rto Rare identical or different and represent hydrogen or C-C-alkyl, where Rand Ror Rand Ror Rand Ror Rand Rtogether with the atoms to which they are attached may also form a 5- or 6- membered monocyclic ring and'}n represents 1 and m represents 0.4. (canceled)5. Process for preparing compositions for deterring helminthic parasites claim 1 , characterized in that compounds of the formula (I) according to are mixed with extenders and/or surfactants.7. The method according to claim 3 , wherein the effective amount is 0.03 to 1 mg of compounds according to formula (I) per cmof skin. This application is a continuation of U.S. patent application Ser. No. 10/311,41 8 filed Jun. 12, 2003, incorporated herein by reference.The present invention relates to compositions comprising certain active compounds which are suitable as ...

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Номер записи: 21
25-07-2013 дата публикации

CRYSTALLINE FORMS OF 4-[2-(4-METHYLPHENYLSULFANYL)-PHENYL] PIPERIDINE WITH COMBINED SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITION FOR THE TREATMENT OF NEUROPATHIC PAIN

Номер: US20130190352A1
Автор: Bang-Andersen Benny, Fajdt Andre, Lopez De Diego Heidi, Miller Silke, Stensbol Tine Bryan
Принадлежит: H. Lundbeck A/S

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain. 2. The compound according to claim 1 , which compound is the HBr addition salt.34-. (canceled)5. The compound according to claim 1 , which compound is the DL-lactic acid addition salt.67-. (canceled)8. The compound according to claim 1 , which compound is the glutaric acid addition salt (1:1).910-. (canceled)11. The compound according to claim 1 , which compound is the malonic acid addition salt (1:1).12. The compound according to claim 11 , which compound is characterized by peaks in an XRPD at 10.77° claim 11 , 16.70° claim 11 , 19.93° and 24.01°2θ claim 11 , or at 6.08° claim 11 , 10.11° claim 11 , 18.25° and 20.26°2θ.1310. The compound according to claim 11 , which compound is characterised by an XRPD as depicted in or .14. The compound according to which compound is L-aspartic acid addition salt (1:1) or L-aspartic acid addition salt hydrate (1:1).15. The compound according to which compound is glutamic acid addition salt (1:1) or glutamic acid addition salt monohydrate.16. (canceled)17. A pharmaceutical composition comprising a compound according to together with a pharmaceutically acceptable excipient.18. A method of treating a disease selected from chronic pain claim 1 , depression in partial responders claim 1 , treatment resistant depression claim 1 , Alzheimer's disease claim 1 , cognitive impairment claim 1 , ADHD claim 1 , melancholia claim 1 , PTSD claim 1 , hot flushes claim 1 , sleep apnea claim 1 , alcohol claim 1 , nicotine or carbohydrate craving claim 1 , substance abuse claim 1 , alcohol or drug abuse claim 1 , emesis claim 1 , eating disorders claim 1 , IBS claim 1 , affective disorders claim 1 , depression claim 1 , major depressive disorder claim 1 , postnatal depression claim 1 , depression associated with bipolar disorder claim 1 , Alzheimer's disease claim 1 , psychosis or Parkinson's disease claim ...

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Номер записи: 22
29-08-2013 дата публикации

SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN

Номер: US20130225621A1
Автор: Gunning Patrick, Turkson James
Принадлежит:

In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 5. The compound of claim 1 , wherein the compound exhibits inhibition of STAT with an ICof less than about 300 μM.6. The compound of claim 1 , wherein the compound exhibits inhibition with an Kof less than about 300 μM.7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of and a pharmaceutically acceptable carrier.12. The method of claim 8 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.13. The method of claim 8 , wherein the disorder is selected from psoriasis and pulmonary arterial hypertension.14. The method of claim 8 , wherein the disorder is a disease of uncontrolled cellular proliferation.15. The method of claim 14 , wherein the disease of uncontrolled cellular proliferation is a cancer selected from cancers of the head claim 14 , neck claim 14 , pancreas claim 14 , brain claim 14 , colon claim 14 , rectum claim 14 , skin claim 14 , ovary claim 14 , kidney claim 14 , prostate claim 14 , breast claim 14 , lung claim 14 , colon claim 14 , uterus claim 14 , and liver.18. The method of claim 16 , wherein the mammal has been diagnosed with a need for treatment of the disorder prior to the administering step.19. The method of claim 16 , wherein the disorder is a disease of uncontrolled cellular proliferation.20. The method of claim 19 , ...

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Номер записи: 23
29-08-2013 дата публикации

PROCESS FOR THE PREPARATION OF TRYPTASE INHIBITORS

Номер: US20130225825A1
Автор: GRAF Claus-Dieter, SLEDESKI Adam W., TAPPERTZHOFEN Christoph
Принадлежит: SANOFI-AVENTIS DEUTSCHLAND GMBH

This invention is directed to processes for the preparation of a compound of the formula I or salt thereof, 2. A process according to for the preparation of 4-[3-(tert-butoxycarbonylaminomethyl)phenyl]piperidine or its salt claim 1 ,comprisinga) treating 3-bromobenzylamine hydrochloride or 3-iodobenzylamine hydrochloride with 1,2-bis(chlorodimethylsilyl)ethane in a halogenated aliphatic hydrocarbon in the presence of a tertiary amine to provide the corresponding 1-(3-halobenzyl)-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane, where halo is bromo or iodo;b) treating the 1-(3-halobenzyl)-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane in an ether with an alkyllithium compound and 1-benzyl-4-piperidone at a temperature of from about −80° C. to about −40° C. to provide 1-[3-(1-benzyl-4-hydroxypiperidin-4-yl)benzyl]-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane;c) treating the 1-[3-(1-benzyl-4-hydroxypiperidin-4-yl)benzyl]-2,2,5,5-tetramethyl-1-aza-2,5-disilacyclopentane with an inorganic acid in a halogenated hydrocarbon to provide 3-(1-benzyl-4-hydroxypiperidin-4-yl)benzylamine as the salt of the inorganic acid;d) treating the 3-(1-benzyl-4-hydroxypiperidin-4-yl)benzylamine with a concentrated, non-oxidizing acid at a temperature of from about 70° C. to about 150° C., followed by alkalinization to provide 3-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)benzylamine; ande) treating the 3-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)benzylamine with di-tert-butyl dicarbonate in an aliphatic alcohol, ethyl acetate, an ether, a halogenated hydrocarbon, a mixture of two or more of such solvents or a mixture of one or more of such solvents with water, in the presence of an alkali metal hydroxide, carbonate or alcoholate or a tertiary amine to provide 3-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)benzylcarbamic acid tert-butyl ester.3. A process according to claim 1 , further comprising treating the amine of the formula XII with hydrogen in a solvent in the presence of a palladium ...

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Номер записи: 24
12-09-2013 дата публикации

Intermediates useful for the synthesis of fexofenadine, processes for their preparation and for the preparation of fexofenadine

Номер: US20130237709A1
Автор: Graziano Castaldi, Marco Baratella, Mauro Gaboardi
Принадлежит: CHEMELECTIVA Srl

Intermediates useful for the synthesis of fexofenadine, processes for their preparation and processes for the synthesis of fexofenadine are described.

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Номер записи: 25
19-09-2013 дата публикации

ACRYLOMIDO DERIVATIVES USEFUL AS INHIBITORS OF THE MITOCHONDRIAL PERMEABILITY TRANSITION

Номер: US20130245019A1
Автор: Ballarini Marco, CAPPA Anna, CARENZI Giacomo, Fancelli Daniele, Minucci Saverio, PAIN Gilles, PLYTE Simon, Varasi Mario, VILLA Manuela
Принадлежит: CONGENIA SRL

Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R′, R″, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them. 110-. (canceled)12. The method according to claim 11 , for the prevention and/or treatment of a diseases resulting from ischemia/reperfusion damage or oxidative damage claim 11 , age-related diseases claim 11 , degenerative and neurodegenerative diseases.13. The method according to claim 12 , for the prevention and/or treatment of acute myocardial infarction claim 12 , heart failure claim 12 , organ ischemia claim 12 , ischemic and traumatic brain damage claim 12 , Duchenne muscular dystrophy claim 12 , Uilrich congenital muscular dystrophy claim 12 , Bentham myopathy claim 12 , amyotrophic lateral sclerosis claim 12 , Huntington's disease claim 12 , Alzheimer's disease claim 12 , Parkinson's disease claim 12 , diabetes type I and type II claim 12 , diabetic complications claim 12 , hyperglycemic tissue damage claim 12 , hypoglycemic tissue damage claim 12 , cholestasis claim 12 , or alcohol-induced damage.1415-. (canceled) The present invention relates to acrylamido derivatives and to their use as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising ...

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Номер записи: 26
07-11-2013 дата публикации

GGA AND GGA DERIVATIVES COMPOSITIONS THEREOF AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES INCLUDING PARALYSIS INCLUDING THEM

Номер: US20130296323A1
Автор: Argade Ankush B., Datwani Akash, Ermini Florian, Pan Yonghua, Serizawa Hiroaki, Spencer Natalie
Принадлежит: COYOTE PHARMACEUTICALS, INC.

This invention relates to geranylgeranyl acetone (GGA) derivatives and the use of GGA, its isomers, and GGA derivatives in methods for inhibiting neural death, increasing neural activity, increasing axon growth and cell viability, and increasing the survival rate of subjects administered the GGA or GGA derivatives. 3. A novel compound of Table 1 or a pharmaceutically acceptable salt thereof.4. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.5. A pharmaceutical composition comprising a sufficient amount of 5E claim 1 , 9E claim 1 , 13E geranylgeranyl acetone or a GGA derivative of claim 1 , and optionally at least one pharmaceutical excipient claim 1 , wherein the sufficient amount is an amount which provides for a dosing of about 1 mg/kg/day to about 12 mg/kg/day to the patient.6. The pharmaceutical composition of claim 5 , wherein the 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone is synthetic 5E claim 5 , 9E claim 5 , 13E geranylgeranyl acetone.7. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing pathogenic protein aggregates associated with AD or ALS claim 5 , said composition comprising a protein aggregate inhibiting amount of GGA or a GGA derivative.8. A composition for increasing the expression and/or release of one or more neurotransmitters from a neuron at risk of developing extracellular pathogenic protein aggregates claim 5 , said composition comprising an extracellular protein aggregate inhibiting amount of GGA or a GGA derivative.10. The method of claim 10 , wherein said pre-contacted neuron exhibits one or more of:(i) a reduction in the axon growth ability,(ii) a reduced expression level of one or more neurotransmitters,(iii) a reduction in the formation of synapses, and(iv) a reduction in electrical excitability.11. The method of claim 9 , wherein the neurostimulation comprises one or more of:(i) enhancing or inducing ...

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Номер записи: 27
28-11-2013 дата публикации

C5aR ANTAGONISTS

Номер: US20130317028A1
Автор: Horoko Tanaka, Jay Powers, JU Yang, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Pingchen Fan, Yandong Li, Yibin Zeng
Принадлежит: Chemocentryx Inc

Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

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Номер записи: 28
05-12-2013 дата публикации

Novel (aza)Benzhydryl Ether Derivatives, Their Process of Preparation and Their Use as H4-Receptor Ligands for Therapeutical Applications

Номер: US20130324507A1
Автор: Berrebi-Bertrand Isabelle, Billot Xavier, Calmels Thierry, Capet Marc, Krief Stéphane, Labeeuw Olivier, Lecomte Jeanne-Marie, Levoin Nicolas, Ligneau Xavier
Принадлежит: BIOPROJET

The present invention concerns novel (aza)benzhydryl ether derivatives which exhibit H4-receptor binding activity. The present invention also concerns their process of preparation and their therapeutical uses. 4. Compounds according to claim 1 , wherein R1 represents a methyl.5. Compounds according to claim 1 , wherein Het represents a piperidine.6. Compounds according to claim 1 , wherein A represents a single bond.7. Compounds according to claim 1 , wherein each R2 claim 1 , R3 claim 1 , R4 claim 1 , R5 claim 1 , R6 identical or different is independently chosen from:hydrogenhalo; hydroxy;alkyl; alkoxy; alkenyl;whose alkyl, alkenyl, alkynyl part can be substituted with one or more of halo, amino, alkoxycarbonylamino,where at least one of R2, R3, R4, R5, R6 is different from H;12. Process of preparation of the compounds of formula (I) according to comprising functionally modifying a corresponding compound of formula (I) as defined in .13. The process according to further comprising the additional step of isolating the desired compound.14. A pharmaceutical composition comprising a compound of formula (I) according to with a pharmaceutically acceptable excipient.15. A method for treating and/or preventing a disease associated with Hdysfunction comprising administering a compound according to .16. The method according to for treating or preventing respiratory diseases such as respiratory inflammatory diseases claim 1 , adult respiratory distress syndrome claim 1 , acute respiratory distress syndrome claim 1 , bronchitis claim 1 , chronic bronchitis claim 1 , chronic obstructive pulmonary disease claim 1 , cystic fibrosis claim 1 , asthma claim 1 , emphysema claim 1 , rhinitis claim 1 , chronic sinusitis claim 1 , allergy claim 1 , allergy induced airway responses claim 1 , allergic rhinitis claim 1 , viral rhinitis claim 1 , non-allergic rhinitis claim 1 , perennial and seasonal rhinitis claim 1 , conjunctivitis claim 1 , nasal congestion claim 1 , allergic congestion ...

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Номер записи: 29
05-12-2013 дата публикации

Protease Activated Receptor 2 (PAR2) Antagonists

Номер: US20130324556A1
Автор: Boyd Joe William, Higginbottom Michael, MEO Paul, Mountford David Mark, Savory Edward Daniel, Simpson Iain
Принадлежит:

A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof 2. A compound according to wherein Rand Rare independently selected from H claim 1 , Calkyl claim 1 , or cyclopropyl claim 1 , each of which Calkyl claim 1 , or cyclopropyl being optionally substituted with one or more substituents independently selected from fluoro and Calkoxy4. A compound according to wherein the ring comprising Z and Y is optionally substituted with one more substituents independently selected from fluoro claim 1 , C-alkyl claim 1 , C-alkoxy claim 1 , fluoro-C-alkyl and fluoro-C-alkoxy.7. A compound according to any wherein Ris hydrogen.8. A compound according to wherein W is an optionally substituted phenyl ring.9. A compound according to wherein the Rsubstituent is optionally substituted with one or more fluoro substituents10. A compound according to wherein Ris H.11. A compound according to wherein Ris H or methyl.12. A compound according to wherein Ris H or methyl.14. (canceled)15. A compound according to wherein U═O.16. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , —N(R)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.17. A compound according to wherein Q is independently selected from —O— claim 1 , —S— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)(OH)— claim 1 , —(CHR)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.18. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , or —N(R).19. A compound according to wherein Q is independently selected from —O— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)OH)— claim 1 , —(CHR)—.20. A compound as claimed in selected from:(4-{[(4-Benzylpiperidin-1-yl)carbonylamino]methyl}phenyl)methanaminium chloride;2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(4-methoxyphenyl)methyl]piperidine-1-carboxamide:2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(3- ...

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Номер записи: 30
02-01-2014 дата публикации

DIMETHYL-BENZOIC ACID COMPOUNDS

Номер: US20140005222A1
Автор: BLANCO-PILLADO Maria-Jesus, Fisher Matthew Joseph, Kuklish Steven Lee, VETMAN Tatiana Natali
Принадлежит:

The present invention provides a compound of the Formula II: 3. A compound or salt according to wherein Ris CH.4. A compound or salt according to wherein X is N.5. A compound or salt according to wherein Ris H and Ris OH.8. Hydrated compound according to .9. The hydrated compound according to characterized by a substantial peak in the X-ray diffraction spectrum claim 8 , at diffraction angle 2-theta claim 8 , of 9.0° claim 8 , in combination with two or more peaks at diffraction angle 2-theta selected from the group consisting of 5.8° claim 8 , 8.5° claim 8 , 9.8° claim 8 , 11.6° claim 8 , 11.8° claim 8 , 17.5° claim 8 , and 24.2°.10. A method of treating osteoarthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to .11. A method of treating rheumatoid arthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound or pharmaceutically acceptable salt thereof claim 1 , according to .12. A method of treating pain associated with osteoarthritis or rheumatoid arthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound or a pharmaceutically acceptable salt thereof claim 1 , according to .13. A pharmaceutical composition claim 1 , comprising a compound or a pharmaceutically acceptable salt thereof according to in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients. The present invention relates to novel dimethyl-benzoic acid compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders, and to intermediates and processes useful in the synthesis of the compounds.The present invention is in the field of treatment of inflammatory conditions, such as arthritis, ...

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Номер записи: 31
16-01-2014 дата публикации

Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto

Номер: US20140018371A1
Автор: Han Sangdon, Jones Robert M., Lehmann Juerg, Thoresen Lars
Принадлежит: ARENA PHARMACEUTICALS, INC.

The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto. 2. The compound according to claim 1 , wherein:{'sub': 1', '6', 'n', '2', '1', '6', '1', '6, 'sup': 6', '6', '7', '6', '7', '6', '7, 'Ar is selected from: phenyl, a 5-membered heteroaryl, and a 6-membered heteroaryl, each optionally substituted with 1, 2, or 3 substituents selected independently from: C-Calkyl, cyano, halogen, a 5-membered heteroaryl, a 6-membered heteroaryl, heterocyclyl, S(O)R, S(O)NRR, and C(O)NRR; wherein said C-Calkyl and said heterocyclyl are each optionally substituted with 1 or 2 substituents selected from: C-Calkylsulfonyl, cyano, hydroxyl, and C(O)NRR; and'}{'sup': 1', '8', '8', '8', '8, 'Ris selected from: C(O)R, C(O)OR, C(S)OR, and C(O)SR; or'}{'sup': '1', 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '3', '6', '1', '6', '3', '6', '1', '6', '1', '6, 'Ris selected from: C-C-alkylene-C-C-cycloalkyl, a 5-membered heteroaryl, and a 6-membered heteroaryl, each optionally substituted with 1 substituent selected from: C-Calkoxy, C-Calkyl, C-Ccycloalkyl, halogen, and C-Chaloalkyl; wherein said C-Ccycloalkyl is optionally substituted with 1 or 2 substituents selected from: C-Chaloalkyl and C-Calkyl.'}3. The compound according to claim 1 , wherein is a single bond.4. The compound according to claim 1 , wherein is a double bond.5. The compound according to claim 1 , wherein:{'sup': 1', '8', '8, 'sub': 1', '6, 'Ris C(O)OR, wherein Ris C-Calkyl.'}6. The compound according to claim 1 , wherein:{'sup': '1', ' ...

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Номер записи: 32
16-01-2014 дата публикации

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

Номер: US20140018393A1
Автор: Johnson Neil W., Kasparec Jiri
Принадлежит:

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer. 122-. (canceled)25. A pharmaceutical composition comprising the compound or pharmaceutically acceptable salt thereof according to and a pharmaceutically acceptable excipient.26. A pharmaceutical composition comprising the compound according to and a pharmaceutically acceptable excipient. This invention relates to novel cyclopropylamines which are inhibitors of Lysine-specific demethylase 1 (LSD1; also known as BHC110), to pharmaceutical compositions containing them, and to their use in therapy for the treatment of cancers.Chromatin modification plays an essential role in transcriptional regulation (T. Kouzarides, 2007, 128: 693-705). These modifications, which include DNA methylation, histone acetylation and histone methylation, are disregulated in tumors. This epigenetic disregulation plays an important role in the silencing of tumor suppressors and overexpression of oncogenes in cancer (M. Esteller, 2008, 358:1148-59. P. Chi et al, 2010, 10:457-469.). The enzymes that regulate histone methylation are the histone methyl transferases and the histone demethylases.Lysine-specific demethylase 1 (LSD1; also known as BHC110) is a histone lysine demethylase reported to demethylate H3K4mel/2 (Y. Shi et al., 2004, 119: 941-953) and H3K9mel/2 (R. Schüe et al., 2005, 437: 436-439). LSD1 is overexpressed in multiple human cancers, including prostate where it is associated with more frequent relapse (P. Kahl et al., 2006, 66: 11341-11347), breast (J. Kirfel et al., 2010, 31: 512-520) neuroblastoma (J. Kirfel et al., 2009, 69: 2065-2071. G. Sun et al., 2010, 28: 1997-2000). LSD1 is essential for transcriptional regulation mediated by a number of nuclear hormone receptors, including androgen receptor in prostate cancer ...

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Номер записи: 33
13-02-2014 дата публикации

CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL) PHENYL]PIPERIDINE COMPOUND

Номер: US20140045892A1
Автор: Chao Robert S., Patterson Lori Jean, Rapta Miroslav
Принадлежит: THERAVANCE, INC.

The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases. 1. (canceled)2. The method of claim 13 , where the crystalline hydrochloride salt is characterized by having one or more additional diffraction peaks at 2θ values selected from 8.11±0.20 claim 13 , 13.18±0.20 claim 13 , 16.06±0.20 claim 13 , 18.38±0.20 claim 13 , 23.76±0.20 claim 13 , 26.32±0.20 claim 13 , 27.24±0.20 claim 13 , 29.60±0.20 claim 13 , and 31.94±0.20.3. The method of claim 13 , where the crystalline hydrochloride salt is characterized by a powder x-ray diffraction pattern in which the peak positions are substantially in accordance with the peak positions of the pattern shown in .4. The method of claim 13 , where the crystalline hydrochloride salt is characterized by a differential scanning calorimetry trace which has a melting point of about 196.9° C.5. The method of claim 13 , where the crystalline hydrochloride salt is characterized by a differential scanning calorimetry trace substantially in accordance with that shown in .612-. (canceled)13. A method of treating a patient that is suffering from a disease or disorder selected from a pain disorder claim 13 , a depressive disorder claim 13 , an affective disorder claim 13 , attention deficit hyperactivity disorder claim 13 , a cognitive disorder claim 13 , stress urinary incontinence claim 13 , chronic fatigue syndrome claim 13 , obesity claim 13 , or vasomotor symptoms associated with menopause claim 13 , comprising administering a therapeutically effective amount of a crystalline hydrochloride salt of 4-[2-(2 claim 13 ,4 claim 13 ,6-trifluorophenoxymethyl)phenyl]-piperidine claim 13 , characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values ...

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Номер записи: 34
20-02-2014 дата публикации

Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial Cystitis

Номер: US20140051702A1
Автор: Gupta Sandeep, Laping Nicholas James, Priestley Tony
Принадлежит: Endo Pharmaceuticals Inc.

The present application provides methods of using the aminoindane compounds of formula (I) or (II) in treating an overactive bladder or interstitial cystitis by administering one or more of the compounds to a patient. 2. The method according to claim 1 , wherein two hydrogen atoms attached to a carbon atom are replaced with a double bond to an oxygen atom to form a carbonyl.3. The method according to claim 1 , wherein said compound contains at least 1 chiral center.4. The method according to claim 1 , wherein said compound is a mixture of enantiomers.5. The method according to claim 1 , wherein said compound is an R-enantiomer.6. The method according to claim 1 , wherein said compound is an S-enantiomer.8. The method according to claim 1 , wherein said compound is selected from the group consisting of(S)-1,1-dimethyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(R)-1,1-dimethyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(S)-1,1-diethyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(R)-1,1-diethyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(S)-1,1-dipropyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(R)-1,1-dipropyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]piperidinium iodide,(S)-1,1-dimethyl-2-[((indan-2-yl)(phenyl)amino)methyl]piperidinium iodide,(R)-1,1-dimethyl-2-[((indan-2-yl)(phenyl)amino)methyl]piperidinium iodide,(S)-1,1-dimethyl-2-[2-((indan-2-yl)(2-methylphenyl)amino)ethyl]piperidinium iodide,(R)-1,1-dimethyl-2-[2-((indan-2-yl)(2-methylphenyl)amino)ethyl]piperidinium iodide,1,1-dimethyl-2-[((indan-2-yl)(phenyl)amino)methyl]piperidinium iodide,1,1-dimethyl-2-[2-((indan-2-yl)(phenyl)amino)ethyl]pyrrolidinium iodide,1,1-diethyl-2-[((indan-2-yl)(phenyl)amino)methyl]piperidinium iodide,1,1-dimethyl-2-[2-((2-fluorophenyl)(indan-2-yl)amino)ethyl]piperidinium iodide,1,1-dimethyl-2-[2-((3-fluorophenyl)(indan-2-yl)amino)ethyl]piperidinium iodide,1,1-dimethyl-2-[2-((4-fluorophenyl)(indan-2-yl)amino) ...

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Номер записи: 35
27-02-2014 дата публикации

SUBSTITUTED CYCLOPROPLY COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT

Номер: US20140057893A1
Автор: Anand Rajan, Chang Lehua, Colandrea Vincent J., DeMong Duane E., Edmondson Scott, Geiss William B., Guo Zhiqiang, Harris Joel M., Hu Zhiyong, Huang Yong, Kar Nam Fung, Liu Ping, Macala Megan, Maletic Milana, Miller Michael W., Morriello Gregori J., Stamford Andrew W., Sun Wanying, Szewczyk Jason W., Wang Bowei, Wang Liping, Wood Harold B., Zhao Kake, Zhu Cheng, Zhu Yuping
Принадлежит: Merck Sharp & Dohme Corp.

Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included 2. The compound of claim 1 , wherein ring A is phenyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , pyridazinyl claim 1 , or pyrazinyl.3. The compound of claim 1 , wherein ring A is phenyl or pyrimidine.4. The compound of claim 1 , wherein ring A is a pyridine ring.8. The compound of claim 1 , wherein B is C(O)R claim 1 , or C(O)OR.10. The compound of claim 1 , wherein Rrepresents a member selected from the group consisting of 3- to 6-membered heterocyclyl claim 1 , containing 1-3 O claim 1 , S claim 1 , or N claim 1 , optionally substituted by oxo; 5-membered heteroaryl claim 1 , containing 1-4 O claim 1 , S claim 1 , or N claim 1 , optionally substituted by Calkyl; aryl; C(O)Calkyl; C(O)Ccycloalkyl; SOCalkyl; SOCcycloalkyl; CN; C(O)NRR; and CHC(O)NRR.11. The compound of claim 10 , wherein R′ is 5-membered heteroaryl claim 10 , containing 1-4 O claim 10 , S claim 10 , or N claim 10 , optionally substituted by Calkyl.12. The compound of claim 11 , wherein Ris SOCalkyl claim 11 , or SOCcycloalkyl.13. The compound of claim 12 , wherein Ris C(O)NRRor CHC(O)NRR.14. The compound of claim 1 , wherein each Ris methyl claim 1 , chloro claim 1 , fluoro claim 1 , CN claim 1 , or methoxy.17. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.1821-. (canceled)22. A method for the treatment of a condition selected from the group consisting of obesity and diabetes comprising administering to an individual a pharmaceutical composition comprising the compound of . The present invention relates to G-protein coupled receptor agonists. ...

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Номер записи: 36
27-02-2014 дата публикации

4-[2-(2-FLUOROPHENOXY METHYL)PHENYL]PIPERIDINE COMPOUNDS

Номер: US20140057944A1
Автор: LONG Daniel D., Patterson Lori Jean, Stangeland Eric L., Zipfel Sheila
Принадлежит: THERAVANCE, INC.

The invention relates to compounds of formula I: 1. (canceled)2. The method of claim 34 , where Ris hydrogen claim 34 , fluoro claim 34 , chloro claim 34 , or methyl.3. The method of claim 34 , where Ris hydrogen claim 34 , fluoro claim 34 , chloro claim 34 , or bromo.4. The method of claim 34 , where Ris hydrogen or fluoro.5. The method of claim 34 , where Ris hydrogen claim 34 , fluoro claim 34 , chloro claim 34 , or bromo.6. The method of claim 34 , where a is 0.7. The method of claim 6 , where Ris hydrogen claim 6 , fluoro claim 6 , chloro claim 6 , or methyl; Ris hydrogen claim 6 , fluoro claim 6 , chloro claim 6 , or bromo; Ris hydrogen or fluoro; and Ris hydrogen claim 6 , fluoro claim 6 , chloro claim 6 , or bromo.8. The method of claim 34 , where a is 0 claim 34 , Rand Rare hydrogen claim 34 , and Rand Rare fluoro.9. The method of claim 34 , where a is 1.10. The method of claim 9 , where Ris 3-fluoro claim 9 , 4-fluoro claim 9 , 5-fluoro claim 9 , 5-trifluoromethyl claim 9 , or 6-fluoro.11. The method of claim 9 , where Ris hydrogen or fluoro; Ris hydrogen or fluoro; Ris hydrogen or fluoro; and Ris hydrogen claim 9 , fluoro or chloro.12. The method of claim 34 , where a is 2.13. The method of claim 12 , where Ris 4 claim 12 ,5-difluoro claim 12 , 4 claim 12 ,6-difluoro claim 12 , or 5 claim 12 ,6-difluoro.14. The method of claim 12 , where Ris hydrogen or fluoro; Ris hydrogen or fluoro; Ris hydrogen or fluoro; and Ris hydrogen claim 12 , fluoro or chloro.15. (canceled)17. The method of claim 16 , where Rand Rare hydrogen claim 16 , and:{'sup': 4', '6, '(i) Ris fluoro, Ris fluoro, and a is 0;'}{'sup': 4', '6', '1, '(ii) Ris fluoro, Ris fluoro, a is 1, and Ris 4-fluoro, 5-fluoro, 5-trifluoromethyl, or 6-fluoro;'}{'sup': 4', '6', '1, '(iii) Ris fluoro, Ris fluoro, a is 2, and Ris 4,5-difluoro, 4,6-difluoro, or 5,6-difluoro;'}{'sup': 4', '6, '(iv) Ris fluoro, Ris chloro, and a is 0;'}{'sup': 4', '6, '(v) Ris chloro, Ris fluoro, and a is 0; or'}{'sup': 4', '6, ...

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Номер записи: 37
13-03-2014 дата публикации

Process for the preparation of substituted pyrimidine derivatives

Номер: US20140073795A1
Автор: Cesco-Cancian Sergio, Chen Hongfeng, Grimm Jeffrey S., Mani Neelakandha S., Mapes Christopher M., Palmer David C., Pippel Daniel J., Sorgi Kirk L., Xiao Tong
Принадлежит: Janssen Pharmaceutica NV

The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine Hreceptor modulators, and to intermediates in H4 modulator synthesis. 138.-. (canceled)40. A compound as in claim 39 , wherein Z is CH.42. A compound as in claim 41 , wherein each Ris selected from the group consisting of hydrogen and benzyloxycarbonyl (CBz); and wherein the two Rgroups are the same. This application is a divisional application of U.S. patent application Ser. No. 13/844,227, filed on Mar. 15, 2013, which is a divisional application of U.S. patent application Ser. No. 13/663,233, filed on Oct. 29, 2012, which is a divisional application of U.S. patent application Ser. No. 12/459,229, filed on Jun. 29, 2009, now U.S. Pat. No. 8,309,720, which claims the benefit of U.S. Provisional Application 61/076,752, filed on Jun. 30, 2008, all of which are incorporated by reference herein in their entirety.The present invention is directed to novel processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine Hreceptor modulators, and to novel intermediates in Hmodulator synthesis.The present invention is directed to a process for the preparation of compounds of formula (I)whereinLis CN;Ris selected from the group consisting of H, methyl, ethyl, propyl, isopropyl, —CF, cyclopropyl, and cyclobutyl;Ris hydrogen;Ris selected from the group consisting of hydrogen and Calkyl;Z is selected from the group consisting of N and CH;n is 1 or 2;R, Rand Rare each independently selected from the group consisting of hydrogen and Calkyl;and pharmaceutically acceptable salts thereof; comprisingreacting a compound of formula (V) wherein PGand PGare each independently a nitrogen protecting group, with a compound of formula (VI), wherein LGis a leaving group, in a first organic solvent; and when LGis —OH, in the presence of a coupling agent system; to yield the ...

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Номер записи: 38
20-03-2014 дата публикации

identification of compounds that disperse tdp-43 inclusions

Номер: US20140080780A1
Автор: Benjamin Wolozin
Принадлежит: Individual

Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.

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Номер записи: 39
02-01-2020 дата публикации

4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS

Номер: US20200000792A1
Автор: Patterson Lori Jean, Stangeland Eric L.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention relates to compounds of formula I: 137-. (canceled)39. The pharmaceutical composition of claim 38 , wherein the pharmaceutical composition comprises about 1 mg to about 15 mg of the compound or a pharmaceutically acceptable salt thereof.40. The pharmaceutical composition of claim 38 , wherein the pharmaceutical composition comprises about 5 mg to about 20 mg of the compound or a pharmaceutically acceptable salt thereof.41. The pharmaceutical composition of claim 38 , wherein the pharmaceutical composition comprises about 7.5 mg to about 15 mg of the compound or a pharmaceutically acceptable salt thereof.42. The pharmaceutical composition of claim 38 , wherein the pharmaceutical composition comprises about 1 mg to about 10 mg of the compound or a pharmaceutically acceptable salt thereof.43. The pharmaceutical composition of claim 38 , wherein the pharmaceutical composition comprises about 10 mg of the compound or a pharmaceutically acceptable salt thereof.44. The pharmaceutical composition of any one of to claim 38 , wherein the pharmaceutical composition is a solid dosage form.45. The pharmaceutical composition of any one of to claim 38 , wherein the pharmaceutical composition is in the form of a capsule claim 38 , tablet or pill.46. The pharmaceutical composition of any one of to claim 38 , wherein the pharmaceutical composition is in the form of a tablet.48. The pharmaceutical composition of claim 47 , wherein the pharmaceutical composition comprises about 1 mg to about 15 mg of the hydrochloride salt of the compound.49. The pharmaceutical composition of claim 47 , wherein the pharmaceutical composition comprises about 5 mg to about 20 mg of the hydrochloride salt of the compound.50. The pharmaceutical composition of claim 47 , wherein the pharmaceutical composition comprises about 7.5 mg to about 15 mg of the hydrochloride salt of the compound.51. The pharmaceutical composition of claim 47 , wherein the pharmaceutical composition comprises about 1 ...

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Номер записи: 40
04-01-2018 дата публикации

CYCLOPROPYLAMINES AS LSD1 INHIBITORS

Номер: US20180000805A1
Автор: Johnson Neil W., Kasparec Jiri
Принадлежит:

This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer. 2. The method of wherein said hematologic cancer is myelodysplastic syndrome.3. The method of claim 1 , further comprising administering an additional therapeutic agent selected from the group consisting of tretinoin claim 1 , azacitidine claim 1 , and decitabine.4. The method of claim 3 , wherein said additional therapeutic agent is tretinoin.5. The method of claim 3 , wherein said additional therapeutic agent is azacitidine.6. The method of claim 3 , wherein said additional therapeutic agent is decitabine.7. The method of claim 3 , wherein said hematologic cancer is myelodysplastic syndrome.8. The method of claim 4 , wherein said hematologic cancer is myelodysplastic syndrome.9. The method of claim 5 , wherein said hematologic cancer is myelodysplastic syndrome.10. The method of claim 6 , wherein said hematologic cancer is myelodysplastic syndrome.11. The method of claim 3 , wherein said hematologic cancer is acute myeloid leukemia.12. The method of claim 4 , wherein said hematologic cancer is acute myeloid leukemia.13. The method of claim 5 , wherein said hematologic cancer is acute myeloid leukemia.14. The method of claim 6 , wherein said hematologic cancer is acute myeloid leukemia. This invention relates to novel cyclopropylamines which are inhibitors of Lysine-specific demethylase 1 (LSD1; also known as BHC110), to pharmaceutical compositions containing them, and to their use in therapy for the treatment of cancers.Chromatin modification plays an essential role in transcriptional regulation (T. Kouzarides, 2007128: 693-705). These modifications, which include DNA methylation, histone acetylation and histone methylation, are disregulated in tumors. This epigenetic disregulation plays an important ...

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Номер записи: 41
05-01-2017 дата публикации

4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide Derivatives as Potent and Selective Inhibitors of 12-Lipoxygenase

Номер: US20170001955A1
Автор: Holinstat Michael, Holman Theodore, Jadhav Ajit, LUCI Diane K., Maloney David J., Nadler Jerry L., Simeonov Anton, Taylor-Fishwick David, YASGAR Adam
Принадлежит:

Human lipoxygenases (LOXs) are a family of iron-containing enzymes involved in catalyzing the oxidation of polyunsaturated fatty acids to provide the corresponding bioactive hydroxyeicosatetraenoic acid (HETE) metabolites. These eicosanoid signaling molecules are involved in a number of physiologic responses such as platelet aggregation, inflammation, and cell proliferation. Platelet-type 12-(S)-LOX (12-LOX) is of particular interest because of its demonstrated role in skin diseases, diabetes, platelet hemostasis, thrombosis, and cancer. Disclosed herein is the identification and medicinal chemistry optimization of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold. The compounds display nM potency against 12-LOX and excellent selectivity over related lipoxygenases and cyclooxygenases. In addition to possessing favorable ADME properties, the compounds also inhibit PAR-4 induced aggregation and calcium mobilization in human platelets, and reduce 12-HETE in mouse/human beta cells. The compounds can also be used in methods for treating or preventing a 12-lipoxygenase mediated disease or disorder. 2. The compound of claim 1 , wherein Ris selected from the group consisting of methoxy and Cl when Ris H;{'sub': 2', '1, 'Ris selected from the group consisting of Br, and Cl when Ris H; and'}{'sub': '3', 'Ris selected from the group consisting of thiazole, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 4-methyl-2-benzothiazole, thiophene, 4-methyl-2-thiazole, 5-methyl-2-thiazole, 4, 5-methyl-2-thiazole, phenyl, 1-naphthalene, 2-naphthalene, 1, 4-bi-phenyl, 3-piperazine-phenyl, 4-piperidine-phenyl, 4-piperazine-3-pyridine, 6-methyl-3-pyridine, 3-quinoline, 8-isoquinoline, 2-pyridine, 3-pyridine, 3-tertbutyl-phenyl, 6-methoxy-2-benzothiazole, 6-fluro-2-benzothiazole, 4-phenyl-2-thiazole, 3-morpholine-phenyl, 4N-boc-piperidine-3-phenyl, 3-piperidine-phenyl, 3-isopropyl-phenyl, and 4-bi-phenyl;'}or a pharmaceutically acceptable salt thereof, enantiomers ...

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Номер записи: 42
05-01-2017 дата публикации

N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

Номер: US20170002017A1
Автор: ANDREZ Jean-Christophe, Chowdhury Sultan, DECKER Shannon Marie, DEHNHARDT Christoph Martin, FOCKEN Thilo, GRIMWOOD Michael Edward, HEMEON Ivan William, Jia Qi, LI JUN, Ortwine Daniel F., SAFINA Brian, SHENG Tao, Sun Shaoyi, Sutherlin Daniel P., WILSON Michael Scott, ZENOVA Alla Yurevna
Принадлежит:

The invention provides novel compounds having the general formula: 3. The compound of wherein B is N and Ris absent.4. The compound of wherein B is C.5. The compound of wherein R claim 1 , Rand Rare each independently selected from H claim 1 , F claim 1 , or Cl.6. The compound of wherein Ris H claim 1 , F or Cl; Rand Rare each H; and Ris an optionally substituted group selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CN claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl claim 1 , and Calkoxy.7. The compound of wherein Ris Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl or —NRR.8. The compound of claim 7 , wherein Ris selected from the group consisting of methyl claim 7 , ethyl claim 7 , propyl claim 7 , trifluoromethyl claim 7 , difluoromethyl claim 7 , monofluoromethyl claim 7 , isopropyl and cyclopropyl.11. The compound of wherein Ris selected from the group consisting of: methyl claim 1 , ethyl claim 1 , tert-butyl claim 1 , dimethylamino claim 1 , methylamino claim 1 , amino claim 1 , morpholino claim 1 , azetidino claim 1 , imidazolyl claim 1 , 3-hydroxyazetidino claim 1 , 3-fluoroazetidino claim 1 , cyclopropyl claim 1 , pyrrolidinyl claim 1 , 3 claim 1 ,3-difluoroazetidino claim 1 , tert-butyl claim 1 , ethyl claim 1 , 2-methoxyethyl claim 1 , 3-methoxyazetidino claim 1 , 2-hydroxyethyl claim 1 , 3-hydroxypyrrolidinyl claim 1 , and N-methylimidazolyl.12. The compound of wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is an optionally substituted group selected from the group consisting of Calkylene claim 1 , Calkenylene or Calkynylene.13. The compound of claim 1 , wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is selected from the group consisting of —CH— claim 1 , —C(═O)— claim 1 , —C(H)(CH)— claim 1 , —CH—CH— claim 1 , —CH—C(H)(CH)— claim 1 , —C(H)(CH)—C(H)— claim 1 , —CHCHCH— claim 1 , —CH—C(H)(CH)—CH— or —CHCHCHCH—.14. The compound of claim 13 , ...

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Номер записи: 43
03-01-2019 дата публикации

SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN

Номер: US20190002443A1
Автор: ALMANSA-ROSALES Carmen, CHRISTMANN Ule, Garcia-Lopez Monica, GARRIGA-SANAHUJA Lourdes, LLORENTE-FERNANDEZ Ana Virginia
Принадлежит:

The present invention relates to substituted amide derivatives having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. 116-. (canceled)19. The compound according to claim 18 , wherein W is nitrogen.21. The compound according to claim 17 , whereinX is a bond, C═O, —C(O)O— or —O—.22. The compound according to claim 21 , wherein X is a bond or —O—.23. The compound according to claim 17 , wherein{'sub': 1', '1-6', '2-6', '2-6, 'Ris selected from the group consisting of substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted monocyclic heterocyclyl.'}24. The compound according to claim 23 , wherein Ris substituted or unsubstituted ethyl claim 23 , substituted or unsubstituted isobutyl claim 23 , substituted or unsubstituted phenyl claim 23 , substituted or unsubstituted pyridine and substituted or unsubstituted thiazole.25. The compound according to claim 17 , wherein{'sub': Z', '1-6', '2-6', '2-6, 'Ris selected from the group consisting of substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl.'}26. The compound according to claim 25 , wherein Ris selected from the group consisting of substituted or unsubstituted methyl claim 25 , substituted or unsubstituted ethyl claim 25 , substituted or unsubstituted isopropyl claim 25 , substituted or unsubstituted isobutyl claim 25 , —CF claim 25 , —CHCF claim 25 , substituted or unsubstituted phenyl claim 25 , substituted or unsubstituted pyridine claim 25 , substituted or ...

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Номер записи: 44
20-01-2022 дата публикации

Formulations of t-type calcium channel modulators and methods of use thereof

Номер: US20220017465A1
Автор: Gabriel Maurice Belfort, Kiran Reddy, Mahesh Padval, Margaret S. Lee, Marion WITTMANN, Randall Wagner, Sapna Makhija Garad
Принадлежит: Praxis Precision Medicines Inc

Described herein, in part, are dosage forms and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel.

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Номер записи: 45
12-01-2017 дата публикации

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Номер: US20170008844A1
Автор: CASTRO PALOMINO LARIA Julio Cesar, ESTIARTE MARTINEZ Maria de los Àngeles, Fyfe Matthew Colin Thor, KURZ Guido, MARTINELL PEDEMONTE Marc, ORTEGA MUÑOZ Alberto, VALLS VIDAL Nuria
Принадлежит:

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 6. The compound of claim 2 , wherein D is a 3- to 7-membered monocyclic saturated heterocyclic ring containing 1 or 2 heteroatoms independently selected from N claim 2 , O and S claim 2 ,wherein D is linked to the remainder of the compound of Formula I through a ring C atom,wherein one or more ring C atoms in ring D are optionally oxidized to form CO groups,{'sub': '2', 'wherein one or more S atoms in ring D, if present, are optionally oxidized to form independently SO groups or SOgroups, and'}{'sup': '3', 'wherein ring D is optionally substituted with one or more R.'}7. The compound of claim 2 , wherein D is a 3- to 7-membered monocyclic saturated heterocyclic ring containing 1 or 2 heteroatoms independently selected from O and S claim 2 ,wherein D is linked to the remainder of the compound of Formula I through a ring C atom,wherein one or more ring C atoms in ring D are optionally oxidized to form CO groups,{'sub': '2', 'wherein one or more S atoms in ring D, if present, are optionally oxidized to form independently SO groups or SOgroups, and'}{'sup': '3', 'wherein ring D is optionally substituted with one or more R.'}8. The compound of claim 2 , wherein D is a 3- to 7-membered monocyclic saturated heterocyclic ring containing 1 heteroatom selected from N claim 2 , O and S claim 2 ,wherein D is linked to the remainder of the compound of Formula I through a ring C atom,wherein one or more ring C atoms in ring D are optionally oxidized to form CO groups,{'sub': '2', 'wherein one S atom in ring D, if present, is optionally oxidized to form an SO group or an SOgroup, and'}{'sup': '3', 'wherein ring D is optionally substituted with one or more R.'}9. The compound of claim 2 , ...

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Номер записи: 46
27-01-2022 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20220023280A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит:

This invention provides a composition comprising pridopidine or pharmaceutically acceptable salt thereof and at least one of compounds 1-8: 2. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of Huntington disease claim 1 , wherein the Huntington disease is an early stage Huntington disease.3. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of ALS.4. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of dystonia claim 1 , wherein the dystonia is a severe dystonia.5. The method of claim 1 , wherein the method treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of Rett Syndrome.6. The method of claim 1 , wherein the method comprises treating claim 1 , slowing the progression claim 1 , lessening the decline claim 1 , delaying onset of symptoms or slowing the progression of symptoms of a mitochondrial disease or dysfunction claim 1 , wherein the mitochondrial disease or dysfunction is Lysosomal Storage Disease (LSD) claim 1 , leukodystrophies or a vanishing white matter (VWM) disease.7. The method of claim 1 , wherein the composition comprises pridopidine or a pharmaceutically acceptable salt thereof and at least one of compound 1 claim 1 , compound 4 claim 1 , pharmaceutically acceptable salt thereof or combination thereof.8. The method of claim 1 , wherein the composition comprises pridopidine or a pharmaceutically acceptable salt thereof and compound 1 or pharmaceutically acceptable salt thereof.9. The method of ...

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Номер записи: 47
11-01-2018 дата публикации

THERAPEUTIC COMPOUNDS AND USES THEREOF

Номер: US20180009735A1
Автор: Albrecht Brian K., Audia James Edmund, CÔTÉ Alexandre, Duplessis Martin, Gehling Victor S., Good Andrew Charles, Harmange Jean-Christophe, LEBLANC Yves, Nasveschuk Christopher G., Taylor Alexander M., Vaswani Rishi G.
Принадлежит:

Provided herein are compounds of formula I: 23-. (canceled)4. The compound of claim 1 , wherein X is —CH— claim 1 , —CHCH— or —CHCHCH—.79-. (canceled)11. The compound of claim 1 , wherein X is or —N(R)C(R)—.1214-. (canceled)15. The compound of claim 1 , wherein Ris hydrogen claim 1 , halo claim 1 , heteroaryl claim 1 , —OR claim 1 , CN claim 1 , —C(O)—N(R)or —C(O)—OR claim 1 , wherein any heteroaryl of Ris optionally substituted with one or more Rgroups.1618-. (canceled)2022-. (canceled)2425-. (canceled)27. (canceled)2933-. (canceled)36. (canceled)40. (canceled)42. (canceled)43. A method of treating cancer in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .44. A method of treating an LSD1-mediated disorder in an animal comprising administering to the animal in need thereof a compound of formula I or a pharmaceutically acceptable salt thereof as described in .4549-. (canceled)50. A method of increasing efficacy of a cancer treatment comprising a cytotoxic agent in an animal comprising administering to the animal an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof as described in .51. (canceled)52. A method of delaying or preventing development of cancer resistance to a cytotoxic agent in an animal claim 1 , comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof as described in .53. A method of extending the duration of response to a cancer therapy in an animal claim 1 , comprising administering to the animal undergoing the cancer therapy a compound of formula I or a pharmaceutically acceptable salt thereof claim 1 , as described in claim 1 , wherein the duration of response to the cancer therapy when the compound of formula I is administered is extended over the duration of response to the cancer therapy in the absence of the administration of the compound of formula I or ...

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Номер записи: 48
11-01-2018 дата публикации

Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same

Номер: US20180009783A1
Автор: Diego Broggini, Guangrong Tang, Lucie Lovelle, Matteo Conza, Oliver FLÖGEL, Stefan Horns, Susanne Lochner, Zhaobin Wang
Принадлежит: Janssen Pharmaceutica NV

The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including

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Номер записи: 49
10-01-2019 дата публикации

Compounds and uses thereof for the modulation of hemoblogin

Номер: US20190010121A1
Автор: II Stephen L. Gwaltney, Qing Xu, Zhe Li
Принадлежит: Global Blood Therapeutics Inc

Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

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Номер записи: 50
17-01-2019 дата публикации

DEUTERATED ANALOGS OF PRIDOPIDINE USEFUL AS DOPAMINERGIC STABILIZERS

Номер: US20190015401A1
Автор: Sonesson Clas
Принадлежит: Teva Pharmaceuticals International GmbH

The present invention provides novel deuterated analogs of Pridopidine, i.e. 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine. Pridopidine is a drug substance currently in clinical development for the treatment of Huntington's disease. 2. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '2, 'R-Rrepresent deuterium (D); and'}{'sup': 3', '23, 'all of R-Rrepresent hydrogen (H).'}3. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '7, 'at least one of R-Rrepresents deuterium (D); and'}{'sup': 1', '23, 'the remaining of R-Rrepresent hydrogen (H).'}4. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', '7, 'all of R-Rrepresent deuterium (D); and'}{'sup': 8', '23, 'all of R-Rrepresent hydrogen (H).'}5. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 8', '9', '10', '11, 'R, R, Rand Rrepresent deuterium (D); and'}{'sup': 1', '7', '12', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}6. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '12', 'Rrepresents deuterium (D); and'}{'sup': 1', '11', '13', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}7. The deuterated analog according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 17', '20, 'R-Rrepresent deuterium (D); and'}{'sup': 1', '16', '21', '23, 'all of R-Rand R-Rrepresent hydrogen (H).'}8. A pharmaceutical composition claim 1 , comprising a therapeutically effective amount of a deuterated analog of 4-(3-methanesulfonyl-phenyl)-1-propyl-piperidine according to any one of - claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , together with at least one pharmaceutically acceptable carrier claim 1 , excipient or diluent.9. The deuterated ...

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Номер записи: 51
18-01-2018 дата публикации

Process for the synthesis of difluoromethyl ether-based compounds

Номер: US20180016227A1
Автор: Abdelmalik Slassi, Peter Dove
Принадлежит: Trillium Therapeutics ULC

The present application relates to a novel process for the preparation of difluoromethyl ether-based derivatives from, for example, aliphatic and aromatic hydroxyl precursors, compositions comprising these compounds and their use, in particular as precursors for medicines for the treatment of diseases, disorders or conditions. In particular, the present application includes the process of preparing compounds of Formula (I), and compositions and uses thereof:

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Номер записи: 52
18-01-2018 дата публикации

SOLID SUPPORTS AND PHOSPHORAMIDITE BUILDING BLOCKS FOR OLIGONUCLEOTIDE CONJUGATES

Номер: US20180016232A1
Автор: Gogoi Khirud, GUZAEV Andrei Pavel, VVEDENSKIY Vladimir V.
Принадлежит: AM Chemicals LLC

Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest. 2. The compound of wherein one of R and Ris selected from tris-(4-methoxyphenyl)methyl protecting group claim 1 , bis-(4-methoxyphenyl)phenylmethyl protecting group claim 1 , 9-phenylxanthen-9-yl protecting group claim 1 , or 9-(4-methoxyphenyl)xanthen-9-yl protecting group and the other of R and Ris selected from a residue of succinic acid optionally further attached to a solid phase material W via the second carboxylic function or a residue of diglycolic acid optionally further attached to a solid phase material W via the second carboxylic function.3. The compound of wherein one of R and Ris selected from tris-(4-methoxyphenyl)methyl protecting group claim 1 , bis-(4-methoxyphenyl)phenylmethyl protecting group claim 1 , 9-phenylxanthen-9-yl protecting group claim 1 , or 9-(4-methoxyphenyl)xanthen-9-yl protecting group and the other of R and Ris a phosphoramidite moiety PA.4. The compound of wherein each Rand Ris isopropyl group or Rand Rtogether with the nitrogen they are attached to form a cycle so that R+R=—(CH)— claim 3 , R+R=—(CH)— claim 3 , or R+R=—(CH)—O—(CH)—.5. The compound of wherein each A and Ais independently selected from —CH— or —(CH)—.6. The compound of wherein each E and Eis independently selected from —CH— claim 1 , —OCH— claim 1 , —(CH)— claim 1 , or —O(CH)—.7. The compound of wherein G is selected from an atom of hydrogen claim 1 , an alkyl group claim 1 , a trifluoroacetyl group claim 1 , (9H-fluoren-9-yl)methoxycarbonyl (Fmoc) group claim 1 , 6-( ...

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Номер записи: 53
18-01-2018 дата публикации

INHIBITORS OF HISTONE DEACETYLASE

Номер: US20180016282A9
Автор: Haggarty Stephen J., Holson Edward, Tsai Li-Huei, Wagner Florence Fevrier, Weiwer Michel, ZHANG YAN-LING
Принадлежит:

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 ...

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Номер записи: 54
25-01-2018 дата публикации

Novel glp-1 receptor modulators

Номер: US20180021346A1
Автор: Adam R. Yeager, Andrew Novak, Daniel Glynn, Enugurthi Brahmachary, Esther Martinborough, Junko Tamiya, Liming Huang, Manisha Moorjani, Marcus F. Boehm, Mark Mills, Michael Knaggs, Premji Meghani, Thomas Fowler
Принадлежит: Celgene International II SARL

Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ ” represents either or both the R and S form of the compound): where A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

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Номер записи: 55
26-01-2017 дата публикации

PROCESS FOR PREPARING PRIDOPIDINE

Номер: US20170022158A1
Автор: Barel Offir, Bergh Anders Olof Ingemar, Gottesfeld Ronen, Lidor-Hadas Ramy, Mizrahi Orel Yosef, Nguyen Ba-Vu
Принадлежит: Teva Pharmaceuticals International GmbH

This invention provides a pridopidine base in a solid form, a method of preparing the solid pridopidine base, and a composition comprising the pridopidine base including a pharmaceutical composition. 1. Pridopidine base in a solid form.2. A composition comprising the pridopidine base of .3. A composition comprising the pridopidine base of claim 1 , wherein the composition is free of isopropyl alcohol.4. The composition of claim 2 , wherein the composition is free of chloride or free of pridopidine hydrochloride.5. (canceled)6. A process for preparing solid pridopidine base comprisinga) obtaining a solution comprising pridopidine base, andb) precipitating pridopidine base from the solution to form solid pridopidine base.7. The process of further comprising precipitating pridopidine base with a volume of one or more alkanes claim 6 , preferably wherein the alkane is n-heptane.8. (canceled)9. The process of claim 6 ,(a) wherein the solution comprises one or more organic solvents or water, or a mixture thereof,(b) wherein the solution is a mixture of toluene and water,(c) further comprising adding a strong base to the solution, preferably NaOH, more preferably wherein the strong base is added until the pH of the solution is pH 8-14, pH 11-14 or about pH 13,(d) wherein the solution comprises an aqueous layer and an organic layer, and the process further comprises separating the organic layer from the aqueous layer and washing the organic layer with water, or(e) wherein the step of washing the organic layer with water removes Compound 1 from the organic layer.1015-. (canceled)16. The process of claim 6 , wherein the process further comprises (a) forming the pridopidine base with a chemical purity in which the weight percent of Compound 1 is less than 0.2% or less than 0.15% of the total amount of pridopidine base and Compound 4 and/or (b) removing an amount of the organic solvent under vacuum distillation to obtain a mixture comprising a volume of the organic solvent ...

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Номер записи: 56
26-01-2017 дата публикации

Substituted 3-phenylpropylamine derivatives for the treatment of ophthalmic diseases and disorders

Номер: US20170022180A1
Автор: Feng Hong, Mark W. Orme, Ryo Kubota, Vladimir A. Kuksa
Принадлежит: Acucela Inc

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

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Номер записи: 57
17-04-2014 дата публикации

Benzamides

Номер: US20140107340A1
Автор: Chen Bin, Eldemenky Eman Mohammed, Hopper Allen T., Jessing Mikkel, Jiang Yu, Kilburn John Paul, Rasmussen Lars Kyhn
Принадлежит: H. Lundbeck A/S

The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor 2. The compound of claim 1 , wherein Ris optionally substituted phenyl.3. The compound of claim 1 , wherein Ris optionally substituted pyridyl.4. The compound of claim 1 , wherein Ris optionally substituted pyrazinyl.5. The compound of claim 1 , wherein Ris optionally substituted pyrimidyl.6. The compound of claim 1 , wherein Ris optionally substituted 5 membered heteroaryl.7. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperazinyl.8. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted piperidinyl.9. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted morpholinyl.10. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolidinyl.11. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted pyrrolo.12. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted imidazo.13. The compound of anyone of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homomorpholinyl14. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperidinyl15. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted homopiperazinyl16. The compound of claim 1 , wherein Rand Rcombine with the nitrogen to which they are attached to form optionally substituted azetidinyl.17. The compound of claim 1 , wherein Ris chlorine claim 1 , methyl or trifluorormethyl.18. The compound of claim 1 ...

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Номер записи: 58
22-01-2015 дата публикации

1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes

Номер: US20150025110A1
Автор: Hans Richter, Henrietta Dehmlow, Patrizio Mattei, Rainer E. Martin, Ulrike Obst Sander
Принадлежит: Hoffmann La Roche Inc

This invention relates to novel 1-cycloalkyl- or 1-heterocyclyl-hydroxyimino-3-phenyl-propanes of the formula wherein R 1 to R 7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.

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Номер записи: 59
24-01-2019 дата публикации

DOPAMINE D2 RECEPTOR LIGANDS

Номер: US20190023656A1
Автор: Holson Edward, Lewis Michael C., Palmer Michelle, Pan Jennifer Q., Scolnick Edward, Wagner Florence Fevrier, Weiwer Michel, Xu Qihong, ZHANG YAN-LING
Принадлежит:

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopaminergic activity. 2. (canceled)6. (canceled)10. (canceled)11. The compound of claim 1 , or a stereoisomer claim 1 , racemate claim 1 , tautomer claim 1 , polymorph claim 1 , hydrate claim 1 , or solvate thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Cy claim 1 , Cyor Cyis independently C-Caryl claim 1 , heteroaryl comprising one or two 5- or 6-membered rings and one to four heteroatoms selected from N claim 1 , O claim 1 , and S claim 1 , C-Ccycloalkyl claim 1 , or C-Cbicyclic group claim 1 , wherein the aryl claim 1 , heteroaryl claim 1 , cycloalkyl claim 1 , and bicyclic group are each independently optionally substituted with one or more substituents independently selected from halogen claim 1 , CHF claim 1 , CHF claim 1 , CF claim 1 , C-Calkyl claim 1 , OH claim 1 , O—C-Calkyl claim 1 , OCF claim 1 , OCHF claim 1 , OCHF claim 1 , and NRR.12. (canceled)13. The compound of claim 1 , or a stereoisomer claim 1 , racemate claim 1 , tautomer claim 1 , polymorph claim 1 , hydrate claim 1 , or solvate thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.14. (canceled)15. The compound of claim 1 , or a stereoisomer claim 1 , racemate claim 1 , tautomer claim 1 , polymorph claim 1 , hydrate claim 1 , or solvate thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A-B is C(O)—NRor CRR—NR.1618-. (canceled)19. The compound of claim 1 , or a stereoisomer claim 1 , racemate claim 1 , tautomer claim 1 , polymorph claim 1 , hydrate claim 1 , or solvate thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein B-A-Zform a 3- to 6-membered ring optionally comprising one to ...

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Номер записи: 60
28-01-2021 дата публикации

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20210024462A1
Автор: Last Stefaan Julien, Raboisson Pierre Jean-Marie Bernard, ROMBOUTS Geert, Vandyck Koen, Verschueren Wim Gaston
Принадлежит:

Inhibitors of HBV replication of Formula (I) 2. The compound according to claim 1 , wherein Rrepresents a 3-7 membered saturated ring claim 1 , containing one or more heteroatoms each independently selected from the group consisting of O claim 1 , S and N claim 1 , such 3-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , C-Calkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF;{'sub': 1', '2', '1', '4', '1', '3', '1', '4', '2', '2', '3, 'Or RRtogether with the Nitrogen to which they are attached form a 5-7 membered saturated ring, optionally containing one or more additional heteroatoms each independently selected from the group consisting of O, S and N, such 5-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halo, CCalkyloxy, oxo, C(═O)—C-Calkyl, C-Calkyl, OH, CN, CFH, CFH and CF.'}3. The compound according to wherein Rrepresents a 4-7 membered saturated ring containing carbon and one or more oxygen atoms claim 1 , such 4-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , CCalkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.4. The compound according to claim 1 , wherein B represents phenyl or thiophene claim 1 , optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.5. The compound according to claim 1 , wherein Rrepresents C-Calkyl-Ror a 4-7 membered saturated ring consisting of carbon atoms and one or more heteroatoms each independently ...

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Номер записи: 61
28-01-2021 дата публикации

Cyclopropylamines as lsd1 inhibitors

Номер: US20210024487A1
Автор: Bo Shen, Chunhong He, Ding-Quan Qian, Fenglei Zhang, Joel R. Courter, Leah C. Konkol, Liangxing Wu, Wenqing Yao
Принадлежит: Incyte Corp, Incyte Holdings Corp

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

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Номер записи: 62
31-01-2019 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20190030016A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит: TEVA PHARMACEUTICAL INDUSTRIES LTD.

This invention provides an isolated compound having the structure: 17. A pharmaceutical composition comprising an amount of pridopidine and at least one of Compound 1 , Compound 2 , Compound 3 , Compound 4 , Compound 5 , Compound 6 , and Compound 7 whereina) Compound 1 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orb) Compound 2 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orc) Compound 3 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, ord) Compound 4 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, ore) Compound 5 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orf) Compound 6 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, org) Compound 7 is present in the pharmaceutical composition in an amount not more than 10 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method.18. The pharmaceutical composition of claim 17 , whereina) Compound 1 is present in the pharmaceutical composition in an amount not more than 0.15 area-% relative to the concentration of pridopidine, based on a determination by an HPLC method, orb) Compound 2 is present in the pharmaceutical composition in an amount not more than 0.15 area-% relative to the concentration of pridopidine, based on a determination by an HPLC ...

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Номер записи: 63
30-01-2020 дата публикации

ANALOGS OF PRIDOPIDINE, THEIR PREPARATION AND USE

Номер: US20200030308A1
Автор: Kaljuste Kalle, Laos Marit, Maasalu Ants, Päri Malle, Schmidt Malle
Принадлежит:

This invention provides an isolated compound having the structure: 2. The composition of claim 1 , wherein the composition comprises pridopidine and at least one of compound 1 claim 1 , compound 4 or combination thereof.3. The composition of claim 1 , wherein the composition comprises pridopidine salt claim 1 , wherein the salt is hydrochloride claim 1 , hydrobromide claim 1 , nitrate claim 1 , perchlorate claim 1 , phosphate claim 1 , sulphate claim 1 , formate claim 1 , acetate claim 1 , aconate claim 1 , ascorbate claim 1 , benzenesulphonate claim 1 , benzoate claim 1 , cinnamate claim 1 , citrate claim 1 , embonate claim 1 , enantate claim 1 , fumarate claim 1 , glutamate claim 1 , glycolate claim 1 , lactate claim 1 , maleate claim 1 , malonate claim 1 , mandelate claim 1 , methane-sulphonate claim 1 , naphthalene-2-sulphonate claim 1 , phthalate claim 1 , salicylate claim 1 , sorbate claim 1 , stearate claim 1 , succinate claim 1 , tartrate or toluene-p-sulphonate salt.4. The composition of claim 1 , in the form of a capsule claim 1 , a tablet claim 1 , a pill claim 1 , a powder claim 1 , a granule claim 1 , a liquid solution or a liquid suspension.5. The composition of claim 1 , in an oral dosage unit form.6. The composition of claim 5 , wherein the oral dosage unit form comprises between 22.5-315 mg pridopidine.7. The composition of claim 6 , wherein the oral dosage unit form comprises between 45-250 mg pridopidine.8. The composition of claim 7 , wherein the oral dosage unit form comprises between 45-135 mg pridopidine.9. The composition of claim 8 , wherein the oral dosage unit form comprises between 90-315 mg pridopidine.10. The composition of claim 6 , wherein the oral dosage unit form comprises about 22.5 mg pridopidine claim 6 , about 45 mg pridopidine claim 6 , about 67.5 mg pridopidine claim 6 , about 90 mg pridopidine claim 6 , about 100 mg pridopidine claim 6 , about 112.5 mg pridopidine claim 6 , about 125 mg pridopidine claim 6 , about 135 mg ...

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Номер записи: 64
31-01-2019 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20190031607A1
Автор: ANDREZ Jean-Christophe, BERGERON Philippe, BICHLER Paul Robert, Chowdhury Sultan, DEHNHARDT Christoph Martin, FOCKEN Thilo, GONG WEI, GRIMWOOD Michael Edward, HASAN Abid, HEMEON Ivan William, Jia Qi, SAFINA Brian Salvatore, Sun Shaoyi, WILSON Michael Scott, ZENOVA Alla Yurevna
Принадлежит:

The invention provides compounds having the general Formula (I); 3. The compound or pharmaceutically acceptable salt of claim 1 , wherein Ris selected from the group consisting of F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CN claim 1 , —OH claim 1 , —NH claim 1 , Calkyl and Chaloalkyl.5. The compound or pharmaceutically acceptable salt of claim 1 , wherein ring “A” is a Cheterocycle and is selected from the group consisting of azetidine claim 1 , pyrrolidine claim 1 , piperidine claim 1 , morpholine claim 1 , homopiperazine claim 1 , piperazine and 8-azabicyclo[3.2.1]octane claim 1 , and is optionally substituted.16. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sup': 'o', 'sub': '1-6', 'Ris hydrogen or Calkyl;'}{'sup': 1', '2, 'sub': '1-8', 'Rand Rare each independently selected from the group consisting of hydrogen and Calkyl;'}{'sup': '3', 'Ris selected from the group consisting of hydrogen and F;'}{'sup': 4', '1', '4, 'sub': '1-4', 'Ris selected from the group consisting of hydrogen or Calkyl; or Rand Rare combined to form a 3- to 7-membered heterocycle ring as described above;'}{'sup': '5', 'sub': 1-8', '3-8, 'Ris selected from the group consisting of F, Cl, Calkyl, and Ccycloalkyl;'}{'sub': '1-6', 'L is Calkylene;'}the subscript m represents the integer 0 or 1;{'sup': 1', '2', '1', '2, 'Xand Xare each independently selected from the group consisting of absent and —O—, and wherein if the subscript m is 0 then one of Xor Xis absent;'}the ring “A” in is selected from the group consisting of:{'sub': '2-11', 'claim-text': [{'sup': 'AA', 'sub': 1-8', '1-8', '1-8, 'Ris independently selected from the group consisting of Calkyl, Chaloalkyl, Cheteroalkyl, F, Cl, Br and I;'}, 'n is an integer from 0 to 5;', {'sup': A', 'RA', 'RA', 'A', 'RA', 'RA', 'RAi', 'RA, 'sub': 6-10', '1-2', '1-2', '6-10', '1-4', '1-4', '1-4', '2', '1-4, 'Ris selected from the group consisting of (Caryl)-(X)—, and (5- to 10-membered heteroaryl)-(X)—, wherein said ...

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Номер записи: 65
04-02-2021 дата публикации

SALTS OF AN LSD1 INHIBITOR

Номер: US20210032203A1
Автор: Cao Ganfeng, Frietze William, Han Wayne, Jia Zhongjiang, Li Qun, Pan Yongchun, Sharief Vaqar, Zhou Jiacheng
Принадлежит:

The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer. 1. A method of treating cancer comprising administering to a patient in need thereof a therapeutically effective amount of a salt which is a p-toluenesulfonic acid salt of 1-((4-(methoxymethyl)-4-(((1R ,2S)-2-phenylcyclopropylamino)methyl)piperidin-1-yl)methyl)cyclobutanecarboxylic acid bis(4-methylbenzenesulfonate) or a hydrate or solvate thereof.25.-. (canceled)6. The salt of claim 1 , having Form I.7. The salt of claim 6 , wherein the salt exhibits a differential scanning calorimetry thermogram having an endotherm with an onset temperature of about 94.6° C. and a peak temperature of about 103.1° C.8. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 3.6±0.3 degrees 2-theta.9. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 4.9±0.3 degrees 2-theta.10. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 6.2±0.3 degrees 2-theta.11. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 7.7±0.3 degrees 2-theta.12. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 22.7±0.3 degrees 2-theta.13. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising at least two characteristic peaks selected from about 3.6±0.3 claim 6 , about 4.9±0.3 claim 6 , about 6.2±0.3 claim 6 , about 7.7±0.3 and about 22.7±0.3 degrees 2-theta.14. The salt of claim 13 , wherein the salt ...

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Номер записи: 66
04-02-2021 дата публикации

COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9

Номер: US20210032214A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Pandey Anjali
Принадлежит:

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I). 2. (canceled)4. (canceled)5. (canceled)6. (canceled)7. The compound of claim 1 , wherein m is 1.8. The compound of claim 1 , wherein m is 0 or 1.9. The compound of claim 1 , wherein Ris hydrogen.10. (canceled)11. The compound of any preceding claim claim 1 , wherein Ris hydrogen or Calkyl optionally substituted with halo or hydroxy.12. (canceled)13. The compound of claim 1 , wherein Ris halo claim 1 , Calkyl claim 1 , or aryl claim 1 , wherein Calkyl or aryl is optionally substituted with 1 to 3 halo.14. The compound of claim 1 , wherein Ris chlorine or fluorine.15. The compound of claim 1 , wherein Ris CF.16. (canceled)17. (canceled)19. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of .21. A method of treating a disease or condition mediated claim 18 , at least in part claim 18 , by PCSK9 claim 18 , the method comprising administering to a patient in need thereof a compound of .22. The method of claim 20 , wherein the disease or condition is a cardiovascular disease claim 20 , a metabolic disease claim 20 , or hypocholesterolemia.23. The method of claim 22 , wherein the cardiovascular disease is coronary disease claim 22 , hypertension claim 22 , hypercholesterolemia claim 22 , or atherosclerosis.24. The method of claim 22 , the metabolic disease is diabetes.25. The method of claim 24 , wherein the patient has elevated plasma levels of low density lipoprotein cholesterol.26. (canceled)27. A method of inhibiting the activity of PCSK9 claim 1 , the method comprising binding a compound of to PCSK9 claim 1 , thereby inhibiting the activity of PCSK9. This application is a continuation of U.S. application Ser. No. 16/078,578, filed Aug. 21, 2018, which is the U.S. National Stage of ...

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Номер записи: 67
11-02-2016 дата публикации

BENZYL UREA DERIVATIVES FOR ACTIVATING TGF-BETA SIGNALING

Номер: US20160039756A1
Автор: Tanga Mary Jean
Принадлежит: The Board of Trustees of the Leladn Stanford Junior University

Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-B signaling are described. In particular, the compositions and methods are useful for reducing or eliminating the pathologies associated with Alzheimer's disease. The compositions include urea derivatives containing a piperidine, piperidinium, or a piperidin-4-yl methyl; cycloalkyl, aryl, and fluorobenzyl moieties. 125-. (canceled)27. The composition of claim 26 , wherein Ris a phenyl substituted with at least one halogen.28. The composition of claim 27 , wherein Ris phenyl substituted with at least one fluorine.29. The composition of claim 26 , wherein the agonist is protonated at the N-piperidine and the pharmaceutically acceptable salt is a chloride claim 26 , tosylate claim 26 , or trifuoroacetate.31. The composition of claim 26 , wherein said composition is a pharmaceutical composition comprising a therapeutically effective amount of the TGF-β signaling agonist and at least one of a pharmaceutically acceptable excipient and a pharmaceutically acceptable carrier.32. The composition of claim 30 , wherein said composition is a pharmaceutical composition comprising a therapeutically effective amount of the TGF-β signaling agonist and at least one of a pharmaceutically acceptable excipient and a pharmaceutically acceptable carrier.35. The method of claim 33 , wherein the composition comprising the effective dose of the TGF-β signaling agonist further comprises a pharmaceutically acceptable carrier and is formulated for delivery of the agonist to a cell or population of cells of a mammalian subject.36. The method of claim 35 , wherein the method further comprises the step of administering the composition to a mammalian subject.37. The method of claim 34 , wherein the composition comprising the effective dose of the TGF-β signaling agonist further comprises a pharmaceutically acceptable carrier and is formulated for delivery of the agonist to a cell or ...

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Номер записи: 68
09-02-2017 дата публикации

CRYSTALLINE FORMS OF 4-[2-(4-METHYLPHENYLSULFANYL)-PHENYL] PIPERIDINE

Номер: US20170037006A1
Автор: Bang-Andersen Benny, Faldt André, Lopez De Diego Heidi, Miller Silke, Stensbol Tine Bryan
Принадлежит:

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided, e.g., for the treatment of neuropathic pain. 2. The compound of claim 1 , wherein the compound is the HBr addition salt. This is a continuation of U.S. application Ser. No. 14/542,210, filed Nov. 14, 2014, which is a continuation of U.S. application Ser. No. 13/660,718, filed Oct. 25, 2012, which is continuation of U.S. application Ser. No. 12/303,449, filed Jun. 1, 2009, now U.S. Pat. No. 8,299,095, which is a U.S. National Phase application under 35 U.S.C. §371 of International Patent Application No. PCT/DK2007/050076, filed Jun. 15, 2007, which claims the benefit of U.S. Provisional Application No. 60/805,009, filed Jun. 16, 2006; Danish Patent Application No. PA 2006 00816, filed Jun. 16, 2006; and Danish Patent Application No. PA 2007 00423, filed Mar. 20, 2007, all of which are incorporated by reference herein. The International Application published in English on Dec. 21, 2007 as WO 2007/144006 under PCT Article 21(2).The perception of pain is more complicated than a direct transmission of signals from an injured part of the body to specific receptors in the brain, and wherein the pain perceived is proportional to the injury. Rather, damage to peripheral tissue and injury to nerves may cause alterations in the central neural structures involved in pain perception affecting subsequent pain sensitivity. This neuroplasticity may bring about a central sensitization in response to longer lasting noxious stimuli, which may manifest itself as e.g. chronic pain, i.e. that the perception of pain remains even after the noxious stimulus has stopped, or as hyperalgesia, i.e. an increased response to a stimulus, which is normally painful. On of the more mysterious and dramatic examples of this is the “phantom limb syndrome”, i.e. the persistence of pain that existed in a limb prior to its amputation. For a recent review of central neuroplasticity and pain see Melzack et al ...

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Номер записи: 69
24-02-2022 дата публикации

PHACETOPERANE FOR TREATING OF ATTENTION DEFICIT HYPERACTIVITY DISORDER

Номер: US20220054471A1
Автор: Figadere Bruno, KONOFAL Eric
Принадлежит:

The invention relates to the treatment of an attention deficit hyperactivity disorder (ADHD) with alpha-phenyl(piperidin-2-yl)methanol, or the pharmaceutically acceptable salts and esters thereof, in particular the acetate derivative, more particularly dextrophacetoperane. The invention additionally provides a method of synthesis of the (S,S) enantiomer of alpha-phenyl(piperidin-2-yl)methanol as well as a method of synthesis of dextrophacetoperane. 110-. (canceled)11. A pharmaceutical composition comprising a therapeutically effective amount of levophacetoperane , or a pharmaceutically acceptable salt thereof , for the treatment of attention deficit hyperactivity disorder (ADHD) and a pharmaceutical acceptable excipient.12. The pharmaceutical composition of claim 11 , wherein the therapeutically effective amount for the treatment of ADHD ranges from about 5 mg to about 20 mg.13. The pharmaceutical composition of claim 12 , wherein the therapeutically effective amount for the treatment of ADHD ranges from about 5 mg to about 10 mg.14. A tablet comprising the pharmaceutical composition of . The invention relates to the treatment of attention deficit hyperactivity disorder.Attention deficit hyperactivity disorder (ADHD) is a combination of behavioural hyperactivity, inattentiveness, and impulsiveness. Diagnosis is based on clinical criteria defined in the Diagnostic and Statistical Manual of Mental Disorders (DSM-IV TR). ADHD is first and foremost the exaggerated, permanent and continual expression of behavioural manifestations that are not due to educational, pedagogical or socio-economic deprivation.This disorder is a frequent reason for consultation in child psychopathology. According to studies, its prevalence in the general child population is from 2 to 5%. The signs of inattentiveness may persist beyond childhood and are responsible for social, relational and affective difficulties. Up to 60% of children with ADHD continue to present characteristic symptoms at ...

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Номер записи: 70
24-02-2022 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20220055977A1
Автор: HEMEON Ivan William, SAFINA Brian, SUTHERLIN Daniel
Принадлежит:

The invention provides a method of treating a disease or condition in a mammal by administering a compound having the general formula I: 5. The method of claim 1 , wherein ring “B” is selected from the group consisting of cyclobutyl claim 1 , cyclopentyl claim 1 , and cyclohexyl.14. The method of claim 1 , wherein wherein n is 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5.15. The method of claim 1 , wherein ring “A” is a 6-15 membered carbocycle claim 1 , a 6-10 membered aryl claim 1 , or a 4-6 membered heterocycle.18. The method of claim 1 , wherein Xis absent; Xis —O—; m is 1; and -(L)- is an optionally substituted Calkylene.19. The method of claim 1 , wherein wherein:ring “A” is a 6-15 membered carbocycle, a 6-10 membered aryl, or a 4-6 membered heterocycle;{'sup': '1', 'Xis absent;'}{'sup': '2', 'Xis —O—;'}m is 1; and{'sub': '1-4', '-(L)- is an optionally substituted Calkylene.'} This application is a divisional of U.S. application Ser. No. 16/685,335, filed 15 Nov. 2019, which is a continuation of U.S. application Ser. No. 15/896,970, filed 14 Feb. 2018, now abandoned, which is a continuation of International Application No. PCT/US2016/048477, filed 24 Aug. 2016, which claims the benefit of U.S. Provisional Application No. 62/210,891, filed 27 Aug. 2015. The entire content of the applications referenced above are hereby incorporated by reference.The present invention relates to organic compounds useful for therapy in a mammal, and in particular to inhibitors of sodium channel (e.g., NaV1.7) that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the modulation of sodium channels.Voltage-gated sodium channels are transmembrane proteins that initiate action potentials in nerve, muscle and other electrically excitable cells, and are a necessary component of normal sensation, emotions, thoughts and movements (Catterall, W. A., Nature (2001), Vol. 409, pp. 988-990). These channels ...

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Номер записи: 71
12-02-2015 дата публикации

PROCESSES FOR THE PREPARATION OF PERIPHERAL OPIOID ANTAGONIST COMPOUNDS AND INTERMEDIATES THERETO

Номер: US20150045556A1
Автор: Dolle Roland E., Le Bourdonnec Bertrand, Martin Pierre, Moessner Christian Steffen, Spielvogel Dirk Jost, Spindler Felix Herbert
Принадлежит:

Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability. 2. The process according to claim 1 , wherein the N-alkylpiperidine is a compound of Formula IIa′.4. The process according to claim 3 , wherein Ris Calkyl.5. The process according to claim 4 , wherein Ris methyl.6. The process according to claim 3 , further comprising contacting the compound of Formula Ia″ with NHCHCOH for a time and under conditions effective to provide (+)-2-[(S)-benzyl-3-[4(R)-(3-hydroxyphenyl)-3(R) claim 3 ,4-dimethylpiperidin-1-yl] propionamidolacetic acid (alvimopam) claim 3 , or a pharmaceutically acceptable salt thereof.7. The process according to claim 1 , wherein the Group VIII transition metal catalyst comprises rhodium claim 1 , ruthenium claim 1 , or iridium.8. The process according to claim 7 , wherein the Group VIII transition metal catalyst comprises rhodium.9. The process according to claim 8 , wherein the catalyst is [Rhnbd)]BF.10. The process according to claim 7 , wherein the catalyst is [Ru(cod)(OOCCF)].11. The process according to claim 1 , wherein the chiral phosphorus-containing ligand is a chiral tertiary diphosphine.16. The process according to claim 6 , wherein the chiral phosphorus-containing ligand is a chiral tertiary diphosphine. This application is a national stage entry of International Application No. PCT/US2012/047082, filed Jul. 17, 2012, which claims priority to and the benefit under 35 U.S.C. §119(e) of U.S. ...

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Номер записи: 72
06-02-2020 дата публикации

Chemical Process for Preparing Pyrimidine Derivatives and Intermediates Thereof

Номер: US20200039935A1
Автор: Davis Mark Clinton, Gong Baoqing, Har Denis, KAPFERER Tobias, Zheng Xuchun
Принадлежит:

The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib. 2. The process for preparing a compound of formula (C2-1) according to claim 1 , wherein T is Br and X1 is ZnI.5. The process for preparing a compound of formula (C2) claim 4 , or a salt thereof claim 4 , according to claim 4 , wherein the reaction is performed in acetic acid in the presence of Pd/Al and hydrogen at 60° C. and a pressure of 80 bar.6. The process for preparing a compound of formula (C2) claim 4 , or a salt thereof claim 4 , according to claim 4 , wherein the reaction is performed in the presence of Pt/C and hydrogen at 10 to 50° C. and a pressure of 1 to 10 bar.8. The process for preparing the compound of formula (C) claim 7 , or a salt thereof claim 7 , according to claim 7 , wherein Y is Cl or Br; B(X)is B(OH)or B(OC(CH)C(CH)O) and Xis B(X).11. The process for preparing a compound of formula (C3) according to claim 10 , wherein the process is carried out in ethyl acetate claim 10 , in the presence of CHCOH as a solution in CHCOH claim 10 , at the temperature between 20-40° C.12. The process for preparing a compound of formula (C3) according to claim 10 , wherein the process is carried out in methanol claim 10 , in the presence of HOand NaWO claim 10 , at the temperature between 20 and 70° C. The present disclosure is in the field of organic synthesis and is directed to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, methods for further preparing pharmaceuticals and pharmaceutical compositions from ceritinib or from intermediates, the use of intermediates for preparing ceritinib and ...

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Номер записи: 73
06-02-2020 дата публикации

N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE

Номер: US20200039951A1
Автор: Bennett David Jonathan, Brnardic Edward J., Han Yongxin, Liverton Nigel J., Meng Zhaoyang, Rudd Michael T., Stachel Shawn J., Tempest Paul, Wai Jenny, Xu Xuewang, Zhu Jiuxiang
Принадлежит: Merck Sharp & Dohme Corp.

In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is N.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is CH.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from H claim 1 , methyl claim 1 , F claim 1 , and Cl.5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris selected from H claim 4 , Cl claim 4 , cyano claim 4 , cyclopropyl claim 4 , —CH claim 4 , and —OCH.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris H claim 5 , —CH claim 5 , or chloro.7. The compound of claim 6 , or a pharmaceutically acceptable salt thereof claim 6 , wherein L is —C(O)—.8. The compound of claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Ris —N(R)(R) claim 7 , wherein:{'sup': 'N1', 'sub': 1', '6, 'Ris selected from H and —(C-C)alkyl; and'}{'sup': 'N2', 'sub': 1', '6', '1', '6', '1', '6, 'claim-text': —OH, halogen, —CN,', {'sub': 1', '4', '1', '4, 'optionally substituted phenyl, (wherein said optional substitutents on said phenyl are 1 to 3 groups independently selected from OH, CN, —(C-C)alkyl, —(C-C)alkoxyl),'}, {'sub': 1', '6', '1', '4, 'optionally substituted heteroaryl, (wherein said optional substituents on said heteroaryl are 1 to 3 groups independently selected from —(C-C)alkyl, —(C-C)alkoxyl, and cyclopropyl),'}, {'sub': 1', '6, 'optionally substituted cyclopropyl (wherein said optional substituents on said cyclopropyl are 1 to 3 groups independently selected from —(C-C)alkyl), and'}, {'sub': 1', '6, 'optionally substituted heterocycloalkyl (wherein said optional substitutents on said heterocycloalkyl are 1 to 3 groups independently selected from halogen, —OH, oxo, CN, and —(C-C) ...

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Номер записи: 74
06-02-2020 дата публикации

AROMATIC COMPOUND

Номер: US20200039957A1
Автор: AIDA Jumpei, Furukawa Hideki, Hirata Yasuhiro, Hitomi Yuko, KASAl Shizuo, KOBAYASHI Toshitake, Maekawa Tsuyoshi, Miwatashi Seiji, Miyamoto Yasufumi, NAKAYAMA Yayoi, NOGUCHI Naoyoshi, Okawa Tomohiro, SHIBUYA Akita, Takakura Nobuyuki, Takami Kazuaki, Tokunaga Norihito, WATANABE Koji
Принадлежит: Takeda Pharmaceutical Company Limited

Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): 4. 3-Cyclopropyl-3-(2-((trans-4-(5-methoxy-2-(1-(2 ,2 ,2-trifluoroethyl)piperidin-4-yl)phenoxy)cyclohexyl)oxy)pyridin-4-yl)propanoic acid or a salt thereof.5. 3-Cyclopropyl-3-(2-((trans-4-(5-methoxy-2-(2-(2 ,2 ,2-trifluoroethoxy)pyrimidin-5-yl)phenoxy)cyclohexyl)oxy)pyridin-4-yl)propanoic acid or a salt thereof.6. (3S)-3-cyclopropyl-3-(2-((1-(2-methoxy-5-(1-(2 ,2 ,2-trifluoroethyl)piperidin-4-yl)pyridin-4-yl)piperidin-4-yl)methoxy)pyridin-4-yl)propanoic acid or a salt thereof.7. (3S)-3-cyclopropyl-3-(2-((1-(2-methoxy-5-((2 ,2 ,3 ,3 ,3-pentafluoropropyl)amino)pyridin-4-yl)piperidin-4-yl)methoxy)pyridin-4-yl)propanoic acid or a salt thereof.8. 3-Cyclopropyl-3-(2-((trans-4-(5-methoxy-2-(6-methoxypyridin-3-yl)phenoxy)cyclohexyl)oxy)pyridin-4-yl)propanoic acid or a salt thereof.9. A medicament comprising the compound according to or a salt thereof.10. The medicament according to claim 9 , which is a GPR40 receptor function regulator.11. The medicament according to claim 9 , which is a prophylactic or therapeutic agent for diabetes.12. A method for regulating GPR40 receptor function in a mammal claim 1 , comprising administering an effective amount of the compound according to or a salt thereof to the mammal.13. A method for preventing or treating obesity or diabetes in a mammal claim 1 , comprising administering an effective amount of the compound according to or a salt thereof to the mammal.14. Use of the compound according to or a salt thereof for the production of an agent for the prophylaxis or treatment of obesity or diabetes.15. The compound according to or a salt thereof for use for the prophylaxis or treatment of obesity or diabetes. The present invention relates to a novel aromatic ring compound which may have a GPR40 agonist activity and GLP-1 secretagogue action.Patent document 1 describes the following ...

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Номер записи: 75
16-02-2017 дата публикации

SALTS OF AN LSD1 INHIBITOR

Номер: US20170044101A1
Автор: Cao Genfeng, Frietze William, Han Wayne, Jia Zhongjiang, Li Qun, Pan Yongchun, Sharief Vaqar, Zhou Jiacheng
Принадлежит:

The present disclosure relates to tosylate salts 1-{[4-(methoxymethyl)-4-({[(1R,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the LSD1-associated or mediated diseases such as cancer. 1. A salt which is a p-toluenesulfonic acid salt of 1-((4-(methoxymethyl)-4-(((1R ,2S)-2-phenylcyclopropylamino)methyl)piperidin-1-yl)methyl)cyclobutanecarboxylic acid or a hydrate or solvate thereof.2. The salt of claim 1 , or a hydrate or solvate thereof claim 1 , wherein the salt is 1-{[4-(methoxymethyl)-4-({[(1R claim 1 ,2S)-2-phenylcyclopropyl]amino}methyl)piperidin-1-yl]methyl}cyclobutanecarboxylic acid bis(4-methylbenzenesulfonate).3. The salt of claim 1 , wherein the salt is substantially crystalline.4. The salt of claim 1 , wherein the salt is crystalline.5. The salt of claim 1 , which is a hydrate.6. The salt of claim 1 , having Form I.7. The salt of claim 6 , wherein the salt exhibits a differential scanning calorimetry thermogram having an endotherm with an onset temperature of about 94.6° C. and a peak temperature of about 103.1° C.8. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 3.6±0.3 degrees 2-theta.9. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 4.9±0.3 degrees 2-theta.10. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 6.2±0.3 degrees 2-theta.11. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 7.7±0.3 degrees 2-theta.12. The salt of claim 6 , wherein the salt has an X-ray powder diffraction pattern comprising a characteristic peak at about 22.7±0.3 degrees 2-theta.13. The salt of claim 6 , wherein the salt has an X-ray ...

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Номер записи: 76
15-02-2018 дата публикации

DEUTERATED DIAMINOPYRIMIDINE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SUCH COMPOUNDS

Номер: US20180044323A1
Автор: CAO Benwen, Li Chengwei, Lv Binhua, PANG Xudong
Принадлежит:

Deuterated diaminopyrimidine compounds, and intermediates thereof are described. In particular, disclosed are deuterated diaminopyrimidine compounds of formula (I), and pharmaceutical compositions containing such compounds or crystal forms, pharmaceutically acceptable salt, hydrates or solvates thereof. The disclosed deuterated diaminopyrimidine compounds can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like. 2. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently deuterium or hydrogen.3. The compound of claim 1 , wherein R claim 1 , Rand Rare independently deuterium or hydrogen.4. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently deuterium or hydrogen.5. The compound of claim 1 , wherein Ris deuterium.6. The compound of claim 1 , wherein each of R claim 1 , R claim 1 , Rand Ris deuterium.8. The compound of claim 7 , wherein R claim 7 , R claim 7 , R claim 7 , R claim 7 , R claim 7 , Rand Rare each independently deuterium or hydrogen.9. The compound of claim 7 , wherein Ris chlorine.11. The method of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , Rand Rare each independently deuterium or hydrogen.12. The method of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , Rand Rare each independently deuterium or hydrogen.13. The method of claim 10 , wherein R claim 10 , Rand Rare each independently deuterium or hydrogen.14. The method of claim 10 , wherein R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , R claim 10 , Rand Rare each independently deuterium or hydrogen.15. The method of claim 10 , wherein Ris chlorine.16. The method of claim 10 , wherein Ris deuterium.17. The method of claim 10 , wherein R claim 10 , R claim 10 ...

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Номер записи: 77
03-03-2022 дата публикации

5-ht2a agonists for use in treatment of depression

Номер: US20220062257A1
Автор: Anders Asbjørn Jensen, Emil MÄRCHER-RØRSTED, Jesper Langgaard Kristensen, Sebastian Leth-Petersen
Принадлежит: Lophora ApS

The present invention relates to agonists of the 5-HT 2A serotonin receptors and their medical uses. In one aspect the invention relates to 5-HT 2A agonists of formula (I). In second aspect, the invention relates to selective 5-HT 2A agonists of formula (II). In another aspect, the invention relates to mixed 5-HT 2A /5-HT 2C agonists of formula (III). In yet another aspect, the invention relates to 5-HT 2A agonists for use in the treatment of a depressive disorder, more particular a 5-HT 2A agonist for the use in the treatment of treatment-resistant depression.

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Номер записи: 78
25-02-2016 дата публикации

Novel chalcone derivatives having an anti-allergic activity

Номер: US20160052881A1
Автор: Ahcene Boumendjel, Charles Dumontet, Guillaume Monneret
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Hospices Civils de Lyon HCL, Universite Claude Bernard Lyon 1 UCBL

The present invention relates to the compounds of formula (I): wherein: R 2 , R 4 and R 6 , either identical or different, represent a hydrogen, chlorine bromine, iodine or fluorine atom, or a group —OH or —O-alkyl comprising from 1 to 6 carbon atoms; R 2 ′ and R 4 ′, either identical or different, represent a hydrogen atom, or a group —OH or —O-alkyl comprising from 1 to 6 carbon atoms; with R 2 ′ and/or R 4 ′ which represent a methoxy group; n is equal to 1, 2, 3; X═CH 2 , O, S or N(R 7 ); and R 7 represents a hydrogen atom or an alkyl group comprising from 1 to 6 carbon atoms; as well as pharmaceutically acceptable hydrates, solvates and salts thereof.

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Номер записи: 79
22-02-2018 дата публикации

4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS

Номер: US20180050024A1
Автор: LONG Daniel D., Patterson Lori Jean, Stangeland Eric L., Zipfel Sheila
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention relates to compounds of formula I: 14-. (canceled)6. The method of claim 5 , wherein the compound is administered as a hydrochloride salt.7. The method of claim 5 , wherein the mammal is a human.9. The method of claim 8 , wherein the compound is administered as a hydrochloride salt.10. The method of claim 8 , wherein the mammal is a human.11. The method of claim 8 , wherein the pharmaceutical composition contains about 1 milligram to about 20 milligrams of the compound or a pharmaceutically acceptable salt thereof.12. The method of claim 8 , wherein the pharmaceutical composition contains about 1 milligram to about 15 milligrams of the compound or a pharmaceutically acceptable salt thereof.13. The method of claim 8 , wherein the pharmaceutical composition contains about 1 milligram to about 10 milligrams of the compound or a pharmaceutically acceptable salt thereof.14. The method of claim 8 , wherein the pharmaceutical composition is administered orally. The present invention relates to 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compounds having activity as serotonin (5-HT) and norepinephrine (NE) reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat a pain disorder, such as neuropathic pain, and other ailments.Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage (International Association for the Study of Pain (IASP), Pain Terminology). Chronic pain persists beyond acute pain or beyond the expected time for an injury to heal (American Pain Society. “Pain Control in the Primary Care Setting.” 2006:15). Neuropathic pain is pain initiated or caused by a primary lesion or dysfunction in the nervous system. Peripheral neuropathic pain occurs when the lesion or dysfunction affects the peripheral nervous system and ...

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Номер записи: 80
25-02-2021 дата публикации

Spirocyclic ror-gamma modulators

Номер: US20210053976A1
Автор: Jason Harris, John Nuss, Raju Mohan, Shendong Yuan
Принадлежит: Escalier Biosciences BV

Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing NROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

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Номер записи: 81
25-02-2021 дата публикации

Pyrimidine-fused cyclic compound, preparation method therefor and application thereof

Номер: US20210053989A1
Автор: Bin Zou, Lanzhen LIU, Rui Zhang, Shichao Ma, Shuaijie XU, Wencheng FU, Xianlei FU
Принадлежит: Shanghai Blueray Biopharma Co ltd

Disclosed in the present disclosure are a pyrimidine-fused cyclic compound or a pharmaceutically acceptable salt, hydrate, prodrug, stereoisomer, solvate or isotope labeled compound thereof. Also provided in the present disclosure are a preparation method for the compound, a composition comprising the compound and a use of the compound for the preparation of a medicament for the prevention and/or treatment of a disease or condition associated with abnormal SHP2 activity.

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Номер записи: 82
08-05-2014 дата публикации

NOVEL MODULATORS OF CORTICAL DOPAMINERGIC- AND NMDA-RECEPTOR-MEDIATED GLUTAMATERGIC NEUROTRANSMISSION

Номер: US20140128360A1
Автор: Karlsson Jonas, Sonesson Clas, Svensson Peder
Принадлежит: Integrative Research Laboratories Swenden AB

The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. 2. The phenoxy-ethyl-amine derivative according to claim 1 , a stereoisomer or a mixture of its stereoisomers claim 1 , or an N-oxide thereof claim 1 , or a fully or partially deuterated analog thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rrepresents CHor CF.3. The phenoxy-ethyl-amine derivative according to claim 1 , a stereoisomer or a mixture of its stereoisomers claim 1 , or an N-oxide thereof claim 1 , or a fully or partially deuterated analog thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of C-C-alkyl claim 1 , allyl claim 1 , CHCHOCH claim 1 , C(CH)CHCH claim 1 , CH-cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , CHCHCHF claim 1 , CHCHCHF claim 1 , CHCHF claim 1 , 3 claim 1 ,3 claim 1 ,3-trifluoropropyl and 4 claim 1 ,4 claim 1 ,4-trifluorobutyl.4. The phenoxy-ethyl-amine derivative according to claim 1 , a stereoisomer or a mixture of its stereoisomers claim 1 , or an N-oxide thereof claim 1 , or a fully or partially deuterated analog thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of H and CH.5. The phenoxy-ethyl-amine derivative according to claim 1 , a stereoisomer or a mixture of its stereoisomers claim 1 , or an N-oxide thereof claim 1 , or a fully or partially deuterated analog thereof claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether form CH(CH)CHor CH(CH)CH.6. The phenoxy-ethyl-amine derivative according to claim 1 , a ...

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Номер записи: 83
08-05-2014 дата публикации

SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT

Номер: US20140128368A1
Автор: Basu Kallol, Dai Xing, DeMong Duane, DUBOIS BYRON GABRIEL, Edmondson Scott D., Garfunkle Joie, Hu Zhiyong, Liu Ping, Miller Michael, Moyes Christopher, Stamford Andrew, Sun Wanying, Wood Harold B.
Принадлежит: Merck Sharp & Dohme Corp.

Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. 3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is pyridyl.4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is phenyl.5. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein B represents (b) COR claim 1 , wherein Ris{'sub': '1-6', 'Calkyl, or'}{'sub': '3-6', 'Ccycloalkyl,'}wherein the alkyl and cycloalkyl are optionally substituted with 1-3 substituents independently selected from:halogen,{'sub': '1-6', 'Calkyl,'}{'sub': '3-6', 'or Ccycloalkyl.'}6. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein B is pyrimidine claim 1 , optionally substituted with 1-3 substituents independently selected from:halogen;hydroxyl;{'sub': '1-6', 'Calkyl;'}{'sub': '1-6', 'C(O)OCalkyl;'}C═O;CN;{'sub': '1-6', 'Calkoxy;'}{'sub': '3-6', 'Ccycloalkyl;'}{'sub': n', '1-6, 'C(═O)—(O)—R′, wherein n is an integer from 0-3 and R′ is Calkyl or H;'}5-6 membered heteroaryl ring containing 1-4 heteroatoms independently selected from nitrogen or oxygen;{'sup': f', 'f, 'C(═O)—R, wherein Ris a 5-6 membered heteroaryl ring containing 1-4 heteroatoms independently selected from nitrogen or oxygen;'}{'sub': '1-6', 'or haloCalkoxy;'}wherein the alkyl moiety is optionally substituted with 1-3 substituents independently selected from:halogen,hydroxy,{'sub': '1-6', 'Calkyl, or'}{'sub': '1-6', 'Calkoxy.'}7. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein B is 1 claim 1 ,2 claim 1 ,4-oxadiazol optionally substituted with 1-3 substituents independently selected from{'sub': '1-6', 'Calkyl;'}{'sub': '1-6', ' ...

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Номер записи: 84
13-02-2020 дата публикации

SUBSTITUTED BENZAMIDES

Номер: US20200048194A1
Автор: Groebke Zbinden Katrin, Norcross Roger, Pfileger Phillippe
Принадлежит:

The invention relates to compounds of formula 2. The compound of claim 1 , wherein X is NR′ and R′ is hydrogen.3. The compound of claim 2 , selected from the group consisting of(RS)-1-(4-Butyl-2-methyl-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;1-(3,4-Dichloro-phenyl)-3-[4-(4-methyl-piperazin-1-yl)-phenyl]-urea;(RS)-1-(3,4-Dichloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(4-Chloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-Phenyl-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(2,4-Dichloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(3-Chloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(4-Pyrrolidin-3-yl-phenyl)-3-(4-trifluoromethyl-phenyl)-urea;(RS)-1-(5-Chloro-pyridin-2-yl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(6-Chlor-pyridin-3-yl)-3-(4-piperidin-3-yl-phenyl)-urea;(RS)-1-(5-Chloro-pyridin-2-yl)-3-(4-piperidin-3-yl-phenyl)-urea; and(RS)-1-(5-Chloro-pyridin-2-yl)-3-[4-(2-pyrrolidin-3-yl-ethyl)-phenyl]-urea.4. The compound of claim 2 , selected form the group consisting of(RS)-1-(4-Chloro-phenyl)-3-[4-(2-pyrrolidin-3-yl-ethyl)-phenyl]-urea;(RS)-1-(4-Chloro-phenyl)-3-[4 (2-piperidin-3-yl-ethyl)-phenyl]-urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-(trifluoromethyl)phenyl)urea;(RS)-1-(4-Chiorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-p-tolylurea;(RS)-1-(6-Chloropyridin-3-yl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(3-Chlorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-m-tolylurea;(RS)-1-(2-Chlorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-Methylbenzyl)-3-(4-(morpholin-2-yl)phenyl)urea;(R)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-(trifluoromethyl)phenyl)urea; and(S)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-(trifluoromethyl)phenyl)urea.5. The compound of claim 1 , wherein X is a bond.6. The compound of claim 5 , selected from the group consisting of(RS)—N-(4-Pyrrolidin-3-yl-phenyl)-benzamide;(RS)-4-Chloro-N-(4-pyrrolidin-3-yl-phenyl)-benzamide;(RS)—N-(4-Pyrrolidin-3-yl-phenyl)-4- ...

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Номер записи: 85
22-02-2018 дата публикации

CATIONIC LIPID

Номер: US20180051285A1
Автор: KASUYA Yuji, Koizumi Makoto, NIWA Takako, Onishi Yoshiyuki, Tamura Masakazu
Принадлежит:

The present invention provides a compound represented by the formula (Ia) as a novel cationic lipid that forms a lipid particle and also provides a lipid particle comprising the compound. The present invention further provides a nucleic acid lipid particle containing the lipid particle, and a pharmaceutical composition containing the nucleic acid lipid particle as an active ingredient. 2. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Rand Rare each independently a C-Calkyl group.3. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein both Rand Rare methyl groups.4. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Ris a C-Calkyl group.5. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Ris a methyl group.6. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein{'sup': '1', 'sub': 17', '19', '1', '7', '17', '19', '1', '7, 'Lis a C-Calkyl group optionally substituted with a C-Calkanoyloxy group or a C-Calkenyl group optionally substituted with a C-Calkanoyloxy group.'}7. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Lis a heptadecenyl group claim 1 , an octadecenyl group claim 1 , a nonadecenyl group claim 1 , a heptadecadienyl group claim 1 , an octadecadienyl group claim 1 , a nonadecadienyl group claim 1 , a heptadecatrienyl group claim 1 , an octadecatrienyl group claim 1 , or a nonadecatrienyl group optionally substituted with a C-Calkanoyloxy group.8. The lipid of or a pharmacologically acceptable salt thereof claim 1 , wherein Lis a (R)-11-acetyloxy-cis-8-heptadecenyl group claim 1 , a cis-9-octadecenyl group (oleyl group) claim 1 , a cis-8 claim 1 ,11-heptadecadienyl group claim 1 , a cis-9 claim 1 ,12-octadecadienyl group (linoleyl group) claim 1 , a cis-10 claim 1 ,13-nonadecadienyl group claim 1 , or a cis-6 claim 1 ,9 claim 1 ,12-octadecatrienyl group (linolenyl group).9. The lipid of or a ...

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Номер записи: 86
13-02-2020 дата публикации

RESIST COMPOSITION AND PATTERNING PROCESS

Номер: US20200050105A1
Автор: Fujiwara Takayuki, Hatakeyama Jun, OHASHI Masaki
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

A resist composition comprising a base polymer and a quencher in the form of an amine compound having an iodized aromatic ring bonded to the nitrogen atom via a divalent hydrocarbon group offers a high sensitivity and minimal LWR or improved CDU, independent of whether it is of positive or negative tone. 1. A resist composition comprising a base polymer and a quencher , the quencher being an amine compound having an iodine-substituted aromatic ring bonded to the nitrogen atom via a C-Cdivalent hydrocarbon group which may contain at least one moiety selected from ester bond and ether bond.3. The resist composition of claim 1 , further comprising an acid generator capable of generating a sulfonic acid claim 1 , imide acid or methide acid.4. The resist composition of claim 1 , further comprising an organic solvent.6. The resist composition of which is a chemically amplified positive resist composition.7. The resist composition of wherein the base polymer is free of an acid labile group.8. The resist composition of which is a chemically amplified negative resist composition.10. The resist composition of claim 1 , further comprising a surfactant.11. The resist composition of claim 1 , further comprising a quencher other than the amine compound.12. A process for forming a pattern comprising the steps of applying the resist composition of onto a substrate claim 1 , baking to form a resist film claim 1 , exposing the resist film to high-energy radiation claim 1 , and developing the exposed resist film in a developer.13. The process of wherein the high-energy radiation is ArF excimer laser radiation of wavelength 193 nm or KrF excimer laser radiation of wavelength 248 nm.14. The process of wherein the high-energy radiation is EB or EUV of wavelength 3 to 15 nm. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2018-150050 filed in Japan on Aug. 9, 2018, the entire contents of which are hereby incorporated by reference.This ...

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Номер записи: 87
23-02-2017 дата публикации

CURVED LIQUID CRYSTAL DISPLAY AND METHOD OF MANUFACTURING THE SAME

Номер: US20170052412A1
Автор: BAE Ji Hong, OH Keun Chan, PARK Heung Shik
Принадлежит:

A curved liquid crystal display comprises, a first curved substrate; a second curved substrate facing the first curved substrate; a liquid crystal layer disposed between the first curved substrate and the second curved substrate; a first curved liquid crystal alignment layer disposed between the liquid crystal layer and the first curved substrate and containing a light stabilizer; and a second curved liquid crystal alignment layer disposed between the liquid crystal layer and the second curved substrate. 1. A curved liquid crystal display comprising:a first curved substrate;a second curved substrate facing the first curved substrate;a liquid crystal layer disposed between the first curved substrate and the second curved substrate;a first curved liquid crystal alignment layer disposed between the liquid crystal layer and the first curved substrate and containing a light stabilizer; anda second curved liquid crystal alignment layer disposed between the liquid crystal layer and the second curved substrate.2. The curved liquid crystal display of claim 1 , wherein the second curved liquid crystal alignment layer does not contain the light stabilizer.3. The curved liquid crystal display of claim 2 , wherein the second curved liquid crystal alignment layer comprises a reactive mesogen and an amount of the reactive mesogen is higher in the second curved liquid crystal alignment layer than an amount in the first curved liquid crystal alignment layer.4. The curved liquid crystal display of claim 2 , wherein the second curved liquid crystal alignment layer has a multilayer structure including a 2-1curved liquid crystal alignment layer and a 2-2curved liquid crystal alignment layer comprising a reactive mesogen claim 2 , and an amount of the reactive mesogen in the 2-2curved liquid crystal alignment layer is higher than an amount in the 2-1curved liquid crystal alignment layer.6. The curved liquid crystal display of claim 5 , wherein in the Chemical Formula 1 claim 5 , Z1 to Z3 ...

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Номер записи: 88
10-03-2022 дата публикации

FORMULATIONS OF T-TYPE CALCIUM CHANNEL MODULATORS AND METHODS OF USE THEREOF

Номер: US20220073463A1
Автор: BELFORT Gabriel Maurice, GARAD Sapna Makhija, Lee Margaret S., PADVAL Mahesh, REDDY Kiran, WAGNER Randall
Принадлежит:

Described herein, in part, are dosage forms and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel. 1137-. (canceled)139. The crystalline anhydrous Form C hydrochloride of claim 138 , wherein the XRPD pattern comprises one or more of the following peaks at the diffraction angle 2θ: 26.6±0.2 claim 138 , 16.2±0.2 claim 138 , and 17.4±0.2.140. The crystalline anhydrous Form C hydrochloride of claim 138 , wherein the XRPD pattern comprises a peak at the diffraction angle 2θ of 26.6±0.2.141. The crystalline anhydrous Form C hydrochloride of claim 140 , wherein the XRPD pattern further comprises one or more of the following peaks at the diffraction angle 2θ: 16.2±0.2 claim 140 , 17.4±0.2 claim 140 , 22.6±0.2 claim 140 , and 11.5±0.2.142. The crystalline anhydrous Form C hydrochloride of claim 140 , wherein the XRPD pattern further comprises peaks at the diffraction angle 2θ of 16.2±0.2 and 17.4±0.2.143. The crystalline anhydrous Form C hydrochloride of claim 142 , wherein the XRPD pattern further comprises peaks at the diffraction angle 2θ of 22.6±0.2 and 11.5±0.2.144. The crystalline anhydrous Form C hydrochloride of claim 138 , wherein the XRPD pattern further comprises one or more of the following peaks at the diffraction angle 2θ: 23.9±0.2 claim 138 , 18.3±0.2 claim 138 , 19.2±0.2 claim 138 , 18.5±0.2 claim 138 , and 20.0±0.2.145. The crystalline anhydrous Form C hydrochloride of claim 138 , wherein the XRPD pattern comprises peaks at the diffraction angle 2θ of 26.6±0.2 claim 138 , 16.2±0.2 claim 138 , 17.4±0.2 claim 138 , 22.6±0.2 claim 138 , 11.5±0.2 ...

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Номер записи: 89
01-03-2018 дата публикации

CRYSTALLINE FORM OF A 4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUND

Номер: US20180055830A1
Автор: Chao Robert S., Patterson Lori Jean, Rapta Miroslav
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases. 117-. (canceled)18. A method of inhibiting norepinephrine reuptake in a mammal , the method comprising administering to the mammal a norepinephrine transporter-inhibiting amount of a crystalline hydrochloride salt of 4-[2-(2 ,4 ,6-trifluorophenoxymethyl)-phenyl]piperidine characterized by (a) a powder x-ray diffraction pattern comprising diffraction peaks at 20 values of 4.44±0.20 , 10.22±0.20 , 17.16±0.20 , and 21.78±0.20; or (b) a differential scanning calorimetry trace which has a melting point of about 196.9° C.19. The method of claim 18 , wherein the crystalline hydrochloride salt of 4-[2-(2 claim 18 ,4 claim 18 ,6-trifluorophenoxymethyl)phenyl]piperidine is characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 20 values of 4.44±0.20 claim 18 , 10.22±0.20 claim 18 , 17.16±0.20 claim 18 , and 21.78±0.20.20. The method of claim 19 , wherein the crystalline hydrochloride salt of 4-[2-(2 claim 19 ,4 claim 19 ,6-trifluorophenoxymethyl)phenyl]piperidine is characterized by having one or more additional diffraction peaks at 20 values selected from 8.11±0.20 claim 19 , 13.18±0.20 claim 19 , 16.06±0.20 claim 19 , 18.38±0.20 claim 19 , 23.76±0.20 claim 19 , 26.32±0.20 claim 19 , 27.24±0.20 claim 19 , 29.60±0.20 claim 19 , and 31.94±0.20.21. The method of claim 19 , wherein the crystalline hydrochloride salt of 4-[2-(2 claim 19 ,4 claim 19 ,6-trifluorophenoxymethyl)phenyl]piperidine is characterized by a powder x-ray diffraction pattern in which the peak positions are substantially in accordance with the peak positions of the pattern shown in .22. The method of claim 18 , wherein the crystalline hydrochloride salt of 4-[ ...

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Номер записи: 90
01-03-2018 дата публикации

METHODS FOR TREATING NEUROGENIC ORTHOSTATIC HYPOTENSION

Номер: US20180055831A1
Автор: Hegde Sharathchandra S.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention relates to methods for treating neurogenic orthostatic hypotension and symptoms thereof using 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine or a pharmaceutically-acceptable salt thereof. 2. The method of claim 1 , wherein administration of the compound to the patient results in one or more of: (a) an increase in the patient's seated systolic blood pressure; (b) an increase in the patient's standing time; and (c) a decrease in dizziness or lightheadedness experienced by the patient.3. The method of or claim 1 , wherein the compound is 4-[2-(2 claim 1 ,4 claim 1 ,6-trifluorophenoxymethyl)phenyl]piperidine hydrochloride.4. The method of or claim 1 , wherein the compound is a crystalline hydrochloride salt of 4-[2-(2 claim 1 ,4 claim 1 ,6-trifluorophenoxymethyl)phenyl]piperidine characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 4.44±0.20 claim 1 , 10.22±0.20 claim 1 , 17.16±0.20 and 21.78±0.20.5. The method of claim 4 , wherein the crystalline hydrochloride salt of 4-[2-(2 claim 4 ,4 claim 4 ,6-trifluorophenoxymethyl)phenyl]piperidine is further characterized by having one or more additional diffraction peaks at 2θ values selected from 8.11±0.20 claim 4 , 13.18±0.20 claim 4 , 16.06±0.20 claim 4 , 18.38±0.20 claim 4 , 23.76±0.20 claim 4 , 26.32±0.20 claim 4 , 27.24±0.20 claim 4 , 29.60±0.20 and 31.94±0.20.6. The method of or claim 4 , wherein the compound is a crystalline hydrochloride salt of 4-[2-(2 claim 4 ,4 claim 4 ,6-trifluorophenoxymethyl)phenyl]piperidine characterized by a differential scanning calorimetry trace having a melting point of about 197±2° C.7. The method of or claim 4 , wherein the patient has multiple system atrophy claim 4 , pure autonomic failure claim 4 , or Parkinson's disease.8. The method of or claim 4 , wherein the patient has multiple system atrophy.9. The method of or claim 4 , wherein the compound is administered in an amount ranging from about 0.5 mg/day to about 20 mg/ ...

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Номер записи: 91
15-05-2014 дата публикации

PIPERIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AND ITS USE

Номер: US20140135314A1
Автор: CHOI Jong-Gil, Chung Coo-Min, JUN Hyung-Jin, KIM Hongwook, Kim Hui-Ho, KIM Jin-Sung, Kim Yong-Gil, MIN Hye-Kyung
Принадлежит: SK BIOPHARMACEUTICALS CO., LTD.

Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided. 116-. (canceled)18. The method of claim 17 , wherein the gastrointestinal disease is selected from irritable bowel syndrome claim 17 , gastric motility disorder claim 17 , constipation and visceral pain.19. The method of claim 17 , wherein the gastrointestinal disease is irritable bowel syndrome.21. The method of claim 20 , wherein the compound is selected from the group consisting of:4-amino-5-chloro-N-[[1-(2-hydroxy-2-phenylethyl)piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-(4-fluorophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-hydroxy-2-(4-methylphenyl)ethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-hydroxy-2-(4-methoxyphenyl)ethyl]piperidin-4-yl]-methyl]-2-methoxybenzamide4-amino-5-chloro-N-[[1-[2-(4-cyanophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-(4-chlorophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-hydroxy-2-(4-phenylphenyl)ethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-hydroxy-2-(2-methoxyphenyl)ethyl]piperidin-4-yl]-methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-hydroxy-2-(3-methoxyphenyl)ethyl]piperidin-4-yl]-methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-(3,4-dichlorophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-(2,4-difluorophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4-amino-N-[[1-[2-(4-tert-butylphenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-5-chloro-2-methoxybenzamide,4-amino-5-chloro-N-[[1-[2-(2-chlorophenyl)-2-hydroxyethyl]piperidin-4-yl]methyl]-2-methoxybenzamide,4- ...

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Номер записи: 92
15-05-2014 дата публикации

Aryl Derivatives And Uses Thereof

Номер: US20140135360A1
Автор: Heffernan Gavin David, Jacobus David Penman, Schiehser Guy Alan, Shieh Hong-Ming, Zhao Wenyi
Принадлежит: Jacobus Pharmaceutical Company, Inc

The present invention relates to antimalarial compounds and their use against protozoa of the genus , including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds. 2. The compound according to wherein A is CH.3. The compound according to wherein Rand Rare H.4. The compound according to wherein Ris tert-butyl or 1-methylcyclobutyl and Ris H.5. The compound according to wherein Ris tert-butyl claim 1 , Caryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 Ror heteroaryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 R.6. The compound according to wherein Ris tert-butyl.7. The compound according to wherein Ris phenyl substituted with 1 claim 1 , 2 claim 1 , or 3 groups of R; Ris halo claim 1 , cyano claim 1 , CFor OCF.8. The compound according to wherein:{'sup': 1', '5, 'Ris phenyl substituted with 1-3 groups of R,'}A is CH;{'sup': 3', '3a, 'Rand Rare H;'}{'sup': 4', '4a, 'Ris tert-butyl or 1-methylcyclobutyl and Ris H;'}{'sup': 2', '5', '5, 'sub': '6-10', 'Ris tert-butyl, Caryl optionally substituted with 1, 2, or 3 Ror heteroaryl optionally substituted with 1, 2, or 3 R.'}9. The compound according to wherein:{'sup': 1', '5, 'Ris phenyl substituted with 1, 2, or 3 groups of R;'}A is CH;{'sup': 3', '3a, 'Rand Rare H;'}{'sup': 4', '4a, 'Ris tert-butyl and Ris H;'}{'sup': '2', 'Ris tert-butyl.'}12. The compound according to claim 11 , wherein Rand Rare claim 11 , independently claim 11 , hydrogen or Calkyl or Rand R claim 11 , together with the nitrogen atom through which they are attached claim 11 , form a heterocyclic ring of 4 to 7 ring atoms.13. The compound according to claim 11 , wherein Ris unsubstituted naphthyl.14. The compound according to claim 11 , wherein Ris substituted with 1 claim 11 , 2 claim 11 , or 3 of R claim 11 , wherein each Ris independently —CF claim 11 , —OCF claim 11 , —SOCalkyl claim 11 , F claim 11 , Cl claim 11 , Br claim 11 , — ...

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Номер записи: 93
01-03-2018 дата публикации

COMPOUNDS USEFUL AS IMMUNOMODULATORS

Номер: US20180057455A1
Автор: Frennesson David B., Grant-Young Katharine A., Hewawasam Piyasena, Langley David R., Meng Zhaoxing, Mull Eric, Saulnier Mark G., Scola Paul Michael, Sun Li-Qiang, WANG TAO, Yeung Kap-Sun, Zhang Zhongxing, Zhu Juliang
Принадлежит:

The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases. 2. A compound of wherein Ris hydrogen.3. A compound of wherein Rand Rare selected from —CHand halo.4. A compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein:{'sup': 2', '3', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b, 'sub': 2', 'm', '2', 'm', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '2', 'm', '2', 'm', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '1', '3', '1', '3', '1', '3', '1', '3', '3', '6', '2', 'm', '2', '2, 'one of Rand Ris hydrogen and the other is selected from —O(CH)Ph, —(CH)OPh, —O(CH)NRR, —S(O)NH(CH)NRR, —S(O)NH(CH)COH, —O(CH)pyridinyl, —(CH)NH(CH)NRR, —C(O)NH(CH)NRR, —NHC(O)(CH)NRR, —NHC(O)NH(CH)NRR; and —NHC(O)NH(CH)COH; wherein each piperidinyl group is optionally substituted with a C-Calkyl group; and wherein the pyridinyl group is optionally substituted with a cyano group; and wherein each Ph group is optionally substituted with one, two, or three groups independently selected from C-Calkoxy, C-Calkyl, C-Calkylcarbonyl, amino, carboxy, (C-Ccycloalkyl)alkoxy, cyano, halo, hydroxy, hydroxymethyl, —CHO, —C(O)NRR, —(CH)NRR, —OCHphenyl wherein the phenyl is optionally substituted with one or two halo groups, and —OCHpyridinyl optionally substituted with a cyano group, aminocarbonyl group, or a pyrazole ring; and'}{'sup': 6', '7', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b, 'sub': 2', 'm', '2', 'm', '2', 'n', '2', '2', 'n', '2', '2', 'n', '2', '2', 'm', '2', 'm', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', '1', '3', '1', '3', '1', '3', ...

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Номер записи: 94
01-03-2018 дата публикации

Chemical Process for Preparing Pyrimidine Derivatives and Intermediates Thereof

Номер: US20180057457A1
Автор: Davis Mark Clinton, Gong Baoqing, Har Denis, KAPFERER Tobias, Zheng Xuchun
Принадлежит: NOVARTIS AG

The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib. 161-: (canceled)631. The process for preparing a compound of formula (C2-1) according to claim , wherein T is Br and X1 is ZnI.664. The process for preparing a compound of formula (C2) , or a salt thereof , according to claim , wherein the reaction is performed in acetic acid in the presence of Pd/Al and hydrogen at 60° C. and a pressure of 80 bar.674. The process for preparing a compound of formula (C2) , or a salt thereof , according to claim , wherein the reaction is performed in the presence of Pt/C and hydrogen at 10 to 50° C. and a pressure of 1 to 10 bar.697. The process for preparing the compound of formula (C) , or a salt thereof , according to claim , wherein Y is Cl or Br; B(X)is B(OH)or B(OC(CH)C(CH)O) and Xis B(X).7210. The process for preparing a compound of formula (C3) according to claim , wherein the process is carried out in ethyl acetate , in the presence of CHCOH as a solution in CHCOH , at the temperature between 20-40° C.7310. The process for preparing a compound of formula (C3) according to claim , wherein the process is carried out in methanol , in the presence of HOand NaWO , at the temperature between 20 and 70° C.75. The process for preparing ceritinib , or a salt thereof , wherein the compound of formula (C2) , or a salt thereof , is reacted with the compound of formula (C3) in a solvent , in the absence of a base , wherein the solvent is selected from 1 ,4-dioxane , tetrahydrofuran (THF) , 2-methyl tetrahydrofuran , diethyl ether , toluene , N-methyl-2-pyrrolidone (NMP) , 1-butyl-2-pyrrolidone (NBP) , acetonitrile , acetone , dimethylcarbonate , ethylacetate , isopropylacetate , tertbutylacetate , water , ...

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Номер записи: 95
01-03-2018 дата публикации

Derivatives of sobetirome

Номер: US20180057472A1
Автор: Andrew PLACZEK, James Matthew MEINIG, Sky Ferrara, Tapasree BANERJI, Thomas S. Scanlan
Принадлежит: Oregon Health Science University

Ester derivatives of sobetirome with enhanced CNS distribution are disclosed.

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Номер записи: 96
20-02-2020 дата публикации

BENZAMIDES-CONTAINING COMPOUNDS AND THEIR USE IN THE TREATMENT OF DEPRESSION

Номер: US20200054630A1
Автор: Chen Bin, Eldemenky Eman Mohamed, Hopper Allen T., Jessing Mikkel, Jiang Yu, Kilburn John Paul, Rasmussen Lars Kyhn
Принадлежит:

The present invention is directed to benzamide-containing compounds of formula I 118-. (canceled)20. The method of claim 19 , wherein the depression is major depressive disorder (MDD) including mild claim 19 , moderate and severe depression.21. The method of claim 19 , wherein the depression is treatment-resistant depression.22. The method of claim 19 , wherein the depression is catatonic depression claim 19 , melancholic depression claim 19 , atypical depression claim 19 , psychotic depression claim 19 , postpartum depression. bipolar depression claim 19 , mild claim 19 , moderate or severe depression claim 19 , wherein bipolar depression includes bipolar I and bipolar II.23. The method of claim 19 , wherein the depression is associated with inflammatory disease.24. The method of claim 19 , wherein the compound is 2-chloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide or a pharmaceutically acceptable salt thereof.25. The method of claim 24 , wherein the depression is major depressive disorder (MDD) including mild claim 24 , moderate and severe depression.26. The method of claim 24 , wherein the depression is treatment-resistant depression.27. The method of claim 24 , wherein the depression is catatonic depression claim 24 , melancholic depression claim 24 , atypical depression claim 24 , psychotic depression claim 24 , postpartum depression. bipolar depression claim 24 , mild claim 24 , moderate or severe depression claim 24 , wherein bipolar depression includes bipolar I and bipolar II.28. The method of claim 24 , wherein the depression is associated with inflammatory disease.29. The method of claim 19 , wherein the compound is (−)2-chloro-N-[3-cyclopropyl-2-[2-(trifluoromethyl)pyrimidin-5-yl]propyl]benzamide or a pharmaceutically acceptable salt thereof.30. The method of claim 29 , wherein the depression is major depressive disorder (MDD) including mild claim 29 , moderate and severe depression.31. The method of claim 29 , wherein the ...

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Номер записи: 97
04-03-2021 дата публикации

SUBSTITUTED BENZAMIDES

Номер: US20210061760A1
Автор: Groebke Zbinden Katrin, Norcross Roger, Pfileger Phillippe
Принадлежит:

The invention relates to compounds of formula 132-. (canceled)34. The method according to claim 33 , wherein X is NR′ and R′ is hydrogen.35. The method according to claim 33 , wherein X is a bond.36. The method according to claim 33 , wherein X is —(CH)—O—.37. The method according to claim 33 , wherein X is —O(CHR″)—.38. The method according to claim 33 , wherein X is —CHR″—.39. The method according to claim 33 , wherein X is —CHCH—.40. The method according to claim 33 , wherein said compound is selected from the group consisting of:(RS)-1-(4-Butyl-2-methyl-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;1-(3,4-Dichloro-phenyl)-3-[4-(4-methyl-piperazin-1-yl)-phenyl]-urea;(RS)-1-(3,4-Dichloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(4-Chloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-Phenyl-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(2,4-Dichloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(3-Chloro-phenyl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(4-Pyrrolidin-3-yl-phenyl)-3-(4-trifluoromethyl-phenyl)-urea;(RS)-1-(5-Chloro-pyridin-2-yl)-3-(4-pyrrolidin-3-yl-phenyl)-urea;(RS)-1-(6-Chloro-pyridin-3-yl)-3-(4-piperidin-3-yl-phenyl)-urea;(RS)-1-(5-Chloro-pyridin-2-yl)-3-(4-piperidin-3-yl-phenyl)-urea;(RS)-1-(5-Chloro-pyridin-2-yl)-3-[4-(2-pyrrolidin-3-yl-ethyl)-phenyl]-urea;(RS)-1-(4-Chloro-phenyl)-3-[4-(2-pyrrolidin-3-yl-ethyl)-phenyl]-urea;(RS)-1-(4-Chloro-phenyl)-3-[4-(2-piperidin-3-yl-ethyl)-phenyl]-urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-(trifluoromethyl)phenyl)urea;(RS)-1-(4-Chlorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-p-tolylurea;(RS)-1-(6-Chloropyridin-3-yl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(3-Chlorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-(Morpholin-2-yl)phenyl)-3-m-tolylurea;(RS)-1-(2-Chlorophenyl)-3-(4-(morpholin-2-yl)phenyl)urea;(RS)-1-(4-Methylbenzyl)-3-(4-(morpholin-2-yl)phenyl)urea;(R)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-(trifluoromethyl)phenyl)urea;(S)-1-(4-(Morpholin-2-yl)phenyl)-3-(4-( ...

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Номер записи: 98
28-02-2019 дата публикации

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF

Номер: US20190062277A1
Автор: Douglas Karensa L., Govek Steven P., Smith Nicholas D.
Принадлежит:

Described herein are compounds that are famesoid 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 famesoid X receptor activity. 2. The compound of claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:{'sub': 3', '10, 'ring A is C-Ccycloalkyl that is selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, and cyclooctyl.'}4. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:{'sup': 1', '2', '2', '1, 'L is —X-L-, -L-X—;'}{'sup': 1', '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': '2', 'sub': '2', 'Lis absent or —CH—.'}5. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:{'sup': 1', '10', '10', '10', '10', '10', '10, 'sub': 2', '2', '2', '2', '2', '2, 'Lis absent, —O—, —S—, —S—CH—, —CH—S—, —CH—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —C(═O)NR—, —NRC(═O)—, —NRS(═O)—, —NR—, —NR—CH—, or —CH—NR—.'}9. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring C is monocyclic carbocycle, or bicyclic carbocycle.10. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring C is monocyclic carbocycle selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and phenyl.11. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring C is phenyl.12. The compound of any one of - claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , wherein:ring C is ...

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Номер записи: 99
28-02-2019 дата публикации

Cyclopropylamines as lsd1 inhibitors

Номер: US20190062301A1
Автор: Bo Shen, Chunhong He, Ding-Quan Qian, Fenglei Zhang, Joel R. Courter, Leah C. Konkol, Liangxing Wu, Wenqing Yao
Принадлежит: Incyte Corp, Incyte Holdings Corp

The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.

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Номер записи: 100