公开(公告)号：US20240174611A1

公开(公告)日：2024-05-30

申请号：US18273476

申请日：2022-02-07

申请人： Rappta Therapeutics Oy

发明人： George L. Trainor ,  Maria Obdulia Rabal Gracia ,  Laura Fourmois ,  Olga Gherbovet ,  Frederic Cachoux

IPC分类号： C07D211/96 ,  C07C311/29 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D207/14 ,  C07D207/48 ,  C07D209/52 ,  C07D211/28 ,  C07D211/56 ,  C07D211/58 ,  C07D211/76 ,  C07D231/56 ,  C07D261/10 ,  C07D309/14 ,  C07D311/68 ,  C07D311/96 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D451/04

CPC分类号： C07D211/96 ,  C07C311/29 ,  C07D205/04 ,  C07D205/12 ,  C07D207/09 ,  C07D207/14 ,  C07D207/48 ,  C07D209/52 ,  C07D211/28 ,  C07D211/56 ,  C07D211/58 ,  C07D211/76 ,  C07D231/56 ,  C07D261/10 ,  C07D309/14 ,  C07D311/68 ,  C07D311/96 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  C07D451/04 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/74

摘要： The present disclosure relates in part to chemical modulators of protein phosphatase 2A (PP2A). The compounds of the present disclosure are useful in treating, preventing, and/or ameliorating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease, and cardiac hypertrophy.

公开(公告)号：US20230250104A1

公开(公告)日：2023-08-10

申请号：US17944782

申请日：2022-09-14

申请人： CELLTAXIS, LLC

发明人： Damian O. Arnaiz ,  Greg Brown ,  Emmanuel Claret ,  Arwed Cleve ,  David Davey ,  William Guilford ,  Seock-Kyu Khim ,  Thomas Kirkland ,  Monica J. Kochanny ,  Amy Liang ,  David Light ,  John Parkinson ,  Guo Ping Wei ,  Bin Ye

IPC分类号： C07D487/08 ,  C07C217/58 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D207/09 ,  C07D211/26 ,  C07D263/32 ,  C07D295/096 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07C229/08 ,  C07D263/14 ,  C07D401/12 ,  C07D207/16 ,  C07D211/34 ,  C07D277/22 ,  C07D277/68 ,  C07D451/02

CPC分类号： C07D487/08 ,  C07C217/58 ,  C07C229/38 ,  C07C233/78 ,  C07C255/57 ,  C07C271/20 ,  C07D207/04 ,  C07D211/58 ,  C07D243/08 ,  C07D295/04 ,  C07D295/16 ,  C07D451/04 ,  C07D207/09 ,  C07D211/26 ,  C07D263/32 ,  C07D295/096 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07C229/08 ,  C07D263/14 ,  C07D401/12 ,  C07D207/16 ,  C07D211/34 ,  C07D277/22 ,  C07D277/68 ,  C07D451/02 ,  C07C2601/14 ,  C07B2200/07

摘要： This invention is directed to compounds of formula (I):




where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

公开(公告)号：US20180291024A1

公开(公告)日：2018-10-11

申请号：US16005366

申请日：2018-06-11

申请人： JANSSEN PHARMACEUTICA NV

发明人： Bart DeCorte ,  Jacob Cornelis Russcher ,  Menno Cornelis Franciscus Monnee

IPC分类号： C07D471/18 ,  C07D451/00

CPC分类号： C07D471/18 ,  C07D451/00 ,  C07D451/04 ,  C07D451/06 ,  C07D451/10 ,  C07D451/12

摘要： The invention provides compounds of Formula 1: and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

公开(公告)号：US20180244653A1

公开(公告)日：2018-08-30

申请号：US15558986

申请日：2016-03-24

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  THE SCRIPPS RESEARCH INSTITUTE ,  MAHIDOL UNIVERSITY

发明人： Palmer TAYLOR ,  John YAMAUCHI ,  Todd T. TALLEY ,  Kuntarat ARUNRUNGVICHIAN ,  Opa VAJRAGUPTA ,  Valery FOKIN

IPC分类号： C07D403/04 ,  A61K31/439 ,  A61K31/454 ,  A61K31/5377 ,  C07D451/14 ,  A61K31/46 ,  A61K31/496 ,  C07D401/14 ,  A61K31/4192 ,  A61K31/55

CPC分类号： C07D403/04 ,  A61K31/4192 ,  A61K31/439 ,  A61K31/454 ,  A61K31/46 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  C07D249/06 ,  C07D401/14 ,  C07D405/04 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D473/34

摘要： In alternative embodiments, provided are selective agonists having a high affinity for the alpha7 nicotinic acetylcholine receptor (α7 nAChR), assays for selectivity of nicotinic receptor subtype and ligand-gated ion channel subtype based on receptor occupation and response, behavioral assessments for reversing cognitive impairment after scopolamine treatment, enhancing memory retention over time, pharmaceutical compositions and formulations and devices comprising them, and methods for making and using them, including characterizing and efficiently assaying them for receptor subtype selectivity. In alternative embodiments, provided are substituted anti 1,2,3-triazoles compounds with high affinity, and selective binding, for the alpha7 nicotine acetylcholine receptor (α7 nAChR), as exemplified by 5-(1-(2-(Piperidin-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND1”), 5-((quinuclid-3-yl)-1H-1,2,3-triazol-4-yl)-1H-indole (“IND8”) and 3-(4-hydroxyphenyl-1,2,3-triazol-1-yl) quinuclidine (“QND8”). In alternative embodiments, provided are products of manufacture such as pumps, devices, syringes and the like comprising a compound, pharmaceutical composition or formulation as provided herein.

公开(公告)号：US09975890B2

公开(公告)日：2018-05-22

申请号：US15595107

申请日：2017-05-15

申请人： Heptares Therapeutics Limited

发明人： Giles Albert Brown ,  Julie Elaine Cansfield ,  Miles Stuart Congreve ,  Mark Pickworth ,  Benjamin Gerald Tehan

IPC分类号： C07D401/04 ,  C07D451/04 ,  C07D401/08

CPC分类号： C07D451/04 ,  A61K31/439 ,  A61K31/4439 ,  C07B59/002 ,  C07B2200/05 ,  C07D401/04 ,  C07D401/08

摘要： This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.

公开(公告)号：US09944601B2

公开(公告)日：2018-04-17

申请号：US15271772

申请日：2016-09-21

申请人： Oryzon Genomics, S.A.

发明人： Alberto Ortega Muñoz ,  Matthew Colin Thor Fyfe ,  Marc Martinell Pedemonte ,  Maria de los Àngeles Estiarte Martinez ,  Nuria Valls Vidal ,  Guido Kurz ,  Julio Cesar Castro Palomino Laria

IPC分类号： C07D211/58 ,  C07D309/04 ,  C07D309/14 ,  C07D215/42 ,  C07D221/20 ,  C07D223/12 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D451/04 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D209/96 ,  C07D211/26 ,  C07D211/56 ,  C07D335/02

CPC分类号： C07D211/58 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D209/96 ,  C07D211/26 ,  C07D211/56 ,  C07D215/42 ,  C07D221/20 ,  C07D223/12 ,  C07D309/04 ,  C07D309/14 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D451/04

摘要： 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.

公开(公告)号：US09914702B2

公开(公告)日：2018-03-13

申请号：US15366513

申请日：2016-12-01

申请人： Bionomics Limited ,  Merck Patent GmbH

发明人： Andrew Harvey ,  Agnes Bombrun ,  Rachel Cooke ,  Isabelle Jeanclaude-Etter ,  Nathan Kuchel ,  Jerome Molette ,  Jorgen Mould ,  Dharam Paul ,  Rajinder Singh ,  Cristina Donini ,  Veronique Colovray ,  Thomas Avery ,  Julia Crossman ,  Justin Ripper

IPC分类号： A61K31/497 ,  C07D213/40 ,  C07D309/14 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D401/12 ,  C07D237/08 ,  C07D239/24 ,  C07D405/12 ,  C07D411/12 ,  C07C217/90 ,  C07D413/12 ,  C07D241/12 ,  C07D209/52 ,  C07D211/16 ,  C07D211/26 ,  C07D211/38 ,  C07D213/16 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D241/18 ,  C07D451/04 ,  C07D239/34

CPC分类号： C07D213/40 ,  C07C217/90 ,  C07D209/52 ,  C07D211/16 ,  C07D211/26 ,  C07D211/38 ,  C07D213/16 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/89 ,  C07D231/12 ,  C07D233/56 ,  C07D237/08 ,  C07D239/24 ,  C07D239/34 ,  C07D241/12 ,  C07D241/18 ,  C07D309/14 ,  C07D401/12 ,  C07D405/12 ,  C07D411/12 ,  C07D413/12 ,  C07D451/04

摘要： The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.

公开(公告)号：US20170355695A1

公开(公告)日：2017-12-14

申请号：US15510586

申请日：2015-09-09

申请人： EPIZYME, INC.

发明人： Megan Alene Cloonan FOLEY ,  Kevin Wayne KUNTZ ,  James Edward John MILLS ,  Lorna Helen MITCHELL ,  Michael John MUNCHHOF ,  Darren Martin HARVEY

IPC分类号： C07D451/04 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D237/24 ,  C07D211/34 ,  C07D401/14 ,  C07D205/04 ,  C07C271/18 ,  C07D249/04 ,  C07D417/14 ,  C07D231/14 ,  C07D401/12

CPC分类号： C07D451/04 ,  C07C271/18 ,  C07D205/04 ,  C07D209/08 ,  C07D211/34 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/90 ,  C07D237/24 ,  C07D241/26 ,  C07D249/04 ,  C07D261/10 ,  C07D263/34 ,  C07D275/03 ,  C07D277/56 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D417/14

摘要： The present disclosure provides carboxamides and sulfonamides having Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, Y, B, X, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.

公开(公告)号：US20170183355A1

公开(公告)日：2017-06-29

申请号：US15301815

申请日：2015-04-03

申请人： SYROS PHARMACEUTICALS, INC.

发明人： Kevin Sprott ,  Jason J. Marineau ,  Darby Schmidt ,  Michael Bradley ,  Stephane Ciblat ,  M. Arshad Siddiqui ,  Anzhelika Kabro ,  Melissa Leblanc ,  Serge Leger ,  Stephanie Roy ,  Dana K. Winter ,  Tom Miller ,  Amy Ripka ,  Dansu Li

IPC分类号： C07D487/10 ,  A61K31/506 ,  C07D403/04 ,  C07D401/14 ,  C07D471/10 ,  C07D487/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/5377 ,  C07D451/04 ,  A61K31/551 ,  C07D405/04 ,  C07D409/04 ,  C07D417/04 ,  A61K45/06 ,  C07D403/14

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D409/04 ,  C07D411/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D451/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10

摘要： The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：US09624229B2

公开(公告)日：2017-04-18

申请号：US14243579

申请日：2014-04-02

申请人： Rigel Pharmaceuticals, Inc.

发明人： Somasekhar Bhamidipati ,  Jeffrey Clough ,  Ankush Argade ,  Rajinder Singh ,  Vadim Markovtsov ,  Pingyu Ding ,  Jiaxin Yu ,  Andy Atuegbu ,  Hui Hong ,  Ihab Darwish ,  Sambaiah Thota

IPC分类号： C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

CPC分类号： C07D487/08 ,  C07D451/00 ,  C07D451/04 ,  C07D491/08 ,  C07D519/00

摘要： This invention is directed to methods of treating diseases or conditions associated with JAK2 activity in a mammal comprising the administration of a compound of formula (I): where n, m, Y, R1, R2, R3, R4 and R5 are disclosed herein, or a pharmaceutically acceptable salt.