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1. WO2019050988 - VASOPRESSIN RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO

Publication Number WO/2019/050988
Publication Date 14.03.2019
International Application No. PCT/US2018/049607
International Filing Date 05.09.2018
IPC
C07D 487/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
C07D 519/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
A61P 25/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 9/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
A61K 31/538 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
538ortho- or peri-condensed with carbocyclic ring systems
A61K 31/4439 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
CPC
A61K 31/4439
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/538
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
538ortho- or peri-condensed with carbocyclic ring systems
A61K 31/554
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
55having seven-membered rings, e.g. azelastine, pentylenetetrazole
554having at least one nitrogen and one sulfur as ring hetero atoms, e.g. chlothiapine, diltiazem
A61P 15/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
A61P 15/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
02for disorders of the vagina
A61P 15/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
15Drugs for genital or sexual disorders
08for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
Applicants
  • BLACKTHORN THERAPEUTICS, INC. [US]/[US]
Inventors
  • CHAMBERS, Mark
  • HARDICK, David
  • TIERNEY, Jason
  • KNIGHT, Chris
  • LOCK, Chris
  • BRANDT, Gary
  • JONES, Robert, M.
  • URBANO, Mariangela
Agents
  • COOPER, Michael, P.
  • OBEIDAT, Baha, A.
  • KUMABE, Blake, K.
  • SOLTANI, Bobby, B.
  • ZENTZ, Bradley, J.
  • SARGEANT, Brooke
  • QUIST, Brooke, W.
  • ROTH, Carol, J.
  • EIDT, Chandra, E.
  • YAO, Cong
  • WITTKOPP, Cristina, J.
  • O'BRIEN, Daniel
  • CARLSON, David, V.
  • STARK, Duncan
  • TARLETON, E., Russell
  • SUN, Eileen, S.
  • HARWOOD, Eric, A.
  • CHAN, Frieda, K.
  • GERTZ, Glenda, A.
  • HAN, Hai
  • TALBERT, Hayley, J.
  • WHITE, James, A. D.
  • BARRETT, Jared, M.
  • PEPE, Jeffrey, C.
  • DANLEY, Jeffrey, E.
  • SAKOI, Jeffrey, M.
  • BAUNACH, Jeremiah, J.
  • ZHANG, Jianping
  • KARLEN, John, R.
  • MORGAN, John, A.
  • WAKELEY, John, J.
  • COE, Justin, E.
  • HENCKEL, Karen, M.
  • HEFTER, Karl, A.
  • HERMANNS, Karl, R.
  • MORGAN, Kevan, L.
  • COSTANZA, Kevin, S.
  • RUSYN, Paul
  • LIN, Qing
  • HALLER, Rachel, A.
  • IANNUCCI, Robert
  • KOVELMAN, Robert, L.
  • WEBB, Samuel, E.
  • LEEK, Shoko, I.
  • ROSENMAN, Stephen, J.
  • ABEDI, Syed
  • SATAGAJ, Thomas, J.
  • SHEWMAKE, Thomas, A.
  • BOLLER, Timothy, L.
  • LIGON, Toby, J.
  • CANTRELL, Tyler, C.
  • FERRON, William, O., Jr.
Priority Data
62/554,45205.09.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) VASOPRESSIN RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO
(FR) ANTAGONISTES DU RÉCEPTEUR DE LA VASOPRESSINE, PRODUITS ET PROCÉDÉS ASSOCIÉS
Abstract
(EN)
Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: (I) wherein Q1, Q2, Q3, R2a, R2b, R3 and X are as defined herein.
(FR)
L'invention concerne des composés qui sont des antagonistes du récepteur de la vasopressine, en particulier des produits du récepteur V1a contenant de tels composés, ainsi que des procédés d'utilisation et de synthèse de ceux-ci. Les composés selon l'invention sont représentés par la formule (I), ou un isomère, racémate, hydrate, solvate, isotope ou sel pharmaceutiquement acceptables de ceux-ci : (I) dans la formule Q1, Q2, Q3, R2a, R2b, R3 et X sont tels que définis dans la description.
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