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公开(公告)号:US20240400528A1
公开(公告)日:2024-12-05
申请号:US18778172
申请日:2024-07-19
Applicant: Emory University , Neurop, Inc.
Inventor: Dennis Liotta , Stephen Traynelis , Lawrence Wilson , Yesim Altas Tahirovic , David Menaldino , Scott Myers , Kamalesh Poornachary
IPC: C07D295/135 , A61K31/495 , A61K31/496 , C07D209/34 , C07D215/22 , C07D295/096
Abstract: Compounds that selectively inhibit GluN2B-containing N-methyl-D-aspartic acid receptors (NMDARs) are disclosed. In some cases, the compounds selectively target GluN2B over GluN2A, GluN2C, and/or GluN2D. Generally, the compounds possess an enhanced potency to GluN2B at a pH that is more acidic compared to the physiological pH. Pharmaceutical formulations containing one or more of the compounds are also disclosed. Additionally, methods of treating a condition, disorder or disease using the compounds or their pharmaceutical formulations thereof are disclosed. Exemplary conditions, disorders, and diseases relevant to this disclosure include stroke, subarachnoid hemorrhage, cerebral ischemia, cerebral vasospasm, hypoxia, acute CNS injury, spinal cord injury, traumatic brain injury, coronary artery bypass graft, persistent or chronic cough, substance abuse disorder, opiate withdrawal, opiate tolerance, bipolar disorder, suicidal ideation, pain, fibromyalgia, depression, postpartum depression, resting tremor, dementia, epilepsy, seizure disorder, movement disorder, and neurodegenerative disease.
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公开(公告)号:US20240360075A1
公开(公告)日:2024-10-31
申请号:US18640931
申请日:2024-04-19
Applicant: ALCON INC.
Inventor: Heeren M. Gordhan , Mitchell A. deLong , Jill M. Sturdivant , David Archer Ellis , Cynthia L. Lichorowic
IPC: C07C233/60 , A61K9/00 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/175 , A61K31/192 , A61K31/27 , A61K31/277 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/4465 , A61K31/495 , A61K31/5375 , A61K31/69 , A61K47/12 , A61K47/18 , A61K47/38 , C07C231/02 , C07C233/58 , C07C233/59 , C07C233/62 , C07C233/63 , C07C235/14 , C07C235/56 , C07C237/24 , C07C271/20 , C07C271/24 , C07C279/22 , C07C315/04 , C07C317/30 , C07D205/04 , C07D207/09 , C07D209/54 , C07D211/58 , C07D213/75 , C07D213/79 , C07D231/40 , C07D239/42 , C07D263/04 , C07D263/56 , C07D265/36 , C07D275/03 , C07D277/46 , C07D295/088 , C07D295/135 , C07D295/32 , C07D305/06 , C07D305/08 , C07D305/14 , C07D307/22 , C07D307/94 , C07D309/14 , C07D311/58 , C07D335/02 , C07F5/02
CPC classification number: C07C233/60 , A61K9/0048 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/175 , A61K31/192 , A61K31/27 , A61K31/277 , A61K31/337 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/4465 , A61K31/495 , A61K31/5375 , A61K31/69 , A61K47/12 , A61K47/183 , A61K47/186 , A61K47/38 , C07C231/02 , C07C233/58 , C07C233/59 , C07C233/62 , C07C233/63 , C07C235/14 , C07C235/56 , C07C237/24 , C07C271/20 , C07C271/24 , C07C279/22 , C07C315/04 , C07C317/30 , C07D205/04 , C07D207/09 , C07D209/54 , C07D211/58 , C07D213/75 , C07D213/79 , C07D231/40 , C07D239/42 , C07D263/04 , C07D263/56 , C07D265/36 , C07D275/03 , C07D277/46 , C07D295/088 , C07D295/135 , C07D295/32 , C07D305/06 , C07D305/08 , C07D305/14 , C07D307/22 , C07D307/94 , C07D309/14 , C07D311/58 , C07D335/02 , C07F5/025 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/18 , C07C2602/38 , C07C2602/42 , C07C2602/50
Abstract: Described herein are modified monoterpene TRPM8 activating compounds. In particular, provided herein are compounds that affect the function of ion channels in a cell, and are useful as therapeutic agents or with therapeutic agents. The compounds provided herein are useful in the treatment of a variety of diseases and conditions including inflammatory eye diseases such as uveitis, cardiovascular diseases, inflammatory diseases, and diseases characterized by abnormal growth, such as cancers.
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公开(公告)号:US12060339B2
公开(公告)日:2024-08-13
申请号:US17631212
申请日:2021-07-28
Applicant: Vivozon Inc.
Inventor: Dae Kyu Choi , Hyo Jin Kim , Mi Seon Bae , Jin Choi , Hyun Jin Heo , Yong Seok Lee , Geon Ho Lee , Mi Yon Shim , Jin Sun Park , Han Mi Lee
IPC: C07D295/135 , A61P25/04 , C07C233/66 , C07C233/70 , C07C233/72 , C07C233/78 , C07C233/86 , C07C237/34 , C07D213/40 , C07D213/56 , C07D305/06 , C07D307/14 , C07D309/06 , C07D309/14 , C07D319/12
CPC classification number: C07D295/135 , A61P25/04 , C07C233/66 , C07C233/70 , C07C233/72 , C07C233/78 , C07C233/86 , C07C237/34 , C07D213/40 , C07D213/56 , C07D305/06 , C07D307/14 , C07D309/06 , C07D309/14 , C07D319/12
Abstract: Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain.
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公开(公告)号:US20240199564A1
公开(公告)日:2024-06-20
申请号:US18546560
申请日:2022-02-16
Applicant: Concentric Analgesics, Inc.
Inventor: Craig HUSFELD
IPC: C07D295/135 , A61K31/166 , A61K31/40 , A61K31/4465 , A61K31/451 , A61K31/472 , A61K31/4965 , A61K31/5375 , C07C233/62 , C07C235/10 , C07C237/10 , C07D211/46 , C07D213/40 , C07D217/02 , C07D295/185
CPC classification number: C07D295/135 , A61K31/166 , A61K31/40 , A61K31/4465 , A61K31/451 , A61K31/472 , A61K31/4965 , A61K31/5375 , C07C233/62 , C07C235/10 , C07C237/10 , C07D211/46 , C07D213/40 , C07D217/02 , C07D295/185 , C07C2601/16
Abstract: Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential melastatin 8 receptor (TRPM8) activity.
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公开(公告)号:US11957687B2
公开(公告)日:2024-04-16
申请号:US17622454
申请日:2020-07-01
Applicant: REGENERON PHARMACEUTICALS, INC.
Inventor: Joseph Vacca
IPC: A61K31/5377 , A61K31/4412 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/513 , A61P1/16 , C07D213/82 , C07D239/36 , C07D239/56 , C07D295/135 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D498/04 , C07D513/04
CPC classification number: A61K31/5377 , A61K31/4412 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/513 , A61P1/16 , C07D213/82 , C07D239/36 , C07D239/56 , C07D295/135 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D498/04 , C07D513/04
Abstract: The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.
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公开(公告)号:US11697636B2
公开(公告)日:2023-07-11
申请号:US17096438
申请日:2020-11-12
Applicant: Hoffmann-La Roche Inc.
Inventor: Katrin Groebke Zbinden , Roger Norcross , Phillippe Pfileger
IPC: C07D207/09 , C07D207/10 , C07D207/12 , C07D211/26 , C07D241/04 , C07D263/32 , C07D265/30 , C07D267/08 , C07D267/10 , C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K9/20 , C07D495/04
CPC classification number: C07D207/09 , A61K9/2018 , C07D207/10 , C07D207/12 , C07D211/26 , C07D241/04 , C07D263/32 , C07D265/30 , C07D267/08 , C07D267/10 , C07D295/135 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D495/04
Abstract: The invention relates to compounds of formula
wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof.
Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.-
7.
公开(公告)号:US20230146507A1
公开(公告)日:2023-05-11
申请号:US17913490
申请日:2021-03-23
Inventor: Rolf W. Hartmann , Jelena Konstantinovic , Jörg Haupenthal , Anna K. Hirsch , Andreas M. Kany , Cansu Kaya , Samir Yahiaoui , Thomas Wichelhaus , Eugen Proschak
IPC: A61K31/196 , A61K31/407 , C07C323/41 , C07C311/08 , C07C311/46 , C07C311/58 , C07C311/64 , C07D295/26 , C07D295/135 , A61K31/18 , A61K31/167 , A61K31/245 , A61K31/64 , A61K31/5375 , A61K31/495 , A61P31/04
CPC classification number: A61K31/196 , A61K31/407 , C07C323/41 , C07C311/08 , C07C311/46 , C07C311/58 , C07C311/64 , C07D295/26 , C07D295/135 , A61K31/18 , A61K31/167 , A61K31/245 , A61K31/64 , A61K31/5375 , A61K31/495 , A61P31/04
Abstract: The present invention related to novel inhibitors of metallo-β3-lactamases of formula (I)
wherein R1 is an optionally substituted aryl group of an optionally substituted heteroaryl group, and the use thereof in the treatment of bacterial infections, especially in combination with β-lactam antibiotics.-
公开(公告)号:US20230064417A1
公开(公告)日:2023-03-02
申请号:US17295335
申请日:2019-11-22
Applicant: GREY WOLF THERAPEUTICS LIMITED
Inventor: Martin QUIBELL , Anil Lallubhai PATEL , Jason John SHIERS , Michael SPARENBERG , Peter Ian JOYCE
IPC: A61K39/39 , A61K39/395 , C07D295/135 , C07D211/14 , C07D498/08 , C07D487/04 , C07D211/38 , C07D471/08 , C07D491/107 , C07D211/48 , C07D211/44 , C07D205/04 , C07D207/12 , C07D209/44 , A61K31/451 , A61K31/55 , A61K31/407 , A61K31/439 , A61K31/397 , A61K31/402 , A61K31/4035 , A61K31/553 , A61K31/495 , A61K31/438 , A61K31/4985 , A61K31/454 , A61K31/501 , A61K31/41 , A61K31/497
Abstract: The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is —NHSO2— or —SO2NH—; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H, Cl and F; R5 is selected from H, alkyl, alkynyl, alkenyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, Cl, F, SO2-alkyl, SO2NR13R14, optionally substituted heteroaryl and alkyl; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H, C1-C3-alkyl, or halo; R10 and R11, together with the nitrogen to which they are attached, form an azepanyl group, wherein (a) said azepanyl group is substituted by one or more substituents, or (b) one or two carbons in said azepanyl group are replaced by a group selected from O, NH, S and CO, and said azepanyl group is optionally further substituted; or R10 and R11, together with the nitrogen to which they are attached, form an azetidinyl, pyrrolidinyl or piperidinyl group wherein (a) said azetidinyl, pyrrolidinyl or piperidinyl group is substituted by one or more substituents, or (b) one or two carbons in said azetidinyl, pyrrolidinyl or piperidinyl group are replaced by a group selected from NH, S and CO; or R10 and R11, together with the nitrogen to which they are attached, form an 8, 9 or 10-membered bicyclic heterocycloalkyl group, wherein one or two carbons in the bicyclic heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic heterocycloalkyl group is optionally substituted; or R10 and R11, together with the nitrogen to which they are attached, form a 6 to 12-membered bicyclic group containing a spirocyclic carbon atom, wherein one or two carbons in the bicyclic group are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic group is optionally substituted, or said bicyclic group is optionally fused to a 5 or 6-membered aryl or heteroaryl group; R13 and R14 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.
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公开(公告)号:US11547679B2
公开(公告)日:2023-01-10
申请号:US16670326
申请日:2019-10-31
Applicant: LUNELLA BIOTECH, INC.
Inventor: Michael P. Lisanti , Federica Sotgia
IPC: A61K31/55 , C07D403/04 , A61P31/00 , A61P35/00 , A61K31/137 , C07D295/135 , C07C217/74 , C07D223/04 , C07D401/04 , C07C235/46 , C07D491/107 , C07C275/24 , C07D513/04 , C07D207/06 , A61P15/16 , A61K31/14 , A61K31/155 , A61K31/66 , G16C20/50 , A61K9/00 , A61K31/40 , A61K31/436 , A61K31/519 , A61K31/5513
Abstract: The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed.
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公开(公告)号:US20220396556A1
公开(公告)日:2022-12-15
申请号:US17769858
申请日:2020-10-19
Inventor: Michael Mitchell , Margaret Billingsley
IPC: C07D295/135 , A61K39/00 , A61K9/127 , C12N15/87
Abstract: The present invention relates to lipids and compositions thereof. In various aspects of the invention, the compositions are lipid nanoparticle compositions used to deliver various nucleic acid molecules and/or therapeutic agents to selected targets, such as cells for gene delivery, and/or to prevent or treat diseases or disorders in a subject in need thereof.
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