[go: up one dir, main page]

MA38325A3 - Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes - Google Patents

Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes

Info

Publication number
MA38325A3
MA38325A3 MA38325A MA38325A MA38325A3 MA 38325 A3 MA38325 A3 MA 38325A3 MA 38325 A MA38325 A MA 38325A MA 38325 A MA38325 A MA 38325A MA 38325 A3 MA38325 A3 MA 38325A3
Authority
MA
Morocco
Prior art keywords
compositions
estrogen receptor
selective estrogen
compounds
degradation agents
Prior art date
Application number
MA38325A
Other languages
English (en)
Other versions
MA38325B1 (fr
MA38325A2 (fr
Inventor
Heather Elizabeth Burks
Michael A Dechantsreiter
Guo He
Jill Nunez
Stefan Peukert
Clayton Springer
Yingchuan Sun
Noel Marie-France Thomsen
George Scott Tria
Bing Yu
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MA38325A2 publication Critical patent/MA38325A2/fr
Publication of MA38325A3 publication Critical patent/MA38325A3/fr
Publication of MA38325B1 publication Critical patent/MA38325B1/fr

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/64—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/66—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne des composés répondant à la formule i : dans laquelle n, m, x, y1, r1, r2, r3, r4 et r5 sont définis dans le résumé de l'invention ; qui sont capables d'être à la fois de puissants antagonistes et des agents de dégradation des récepteurs des œstrogènes. L'invention concerne en outre un procédé de préparation des composés de l'invention, des préparations pharmaceutiques comprenant de tels composés et des procédés d'utilisation de tels composés et compositions dans la prise en charge de maladies ou de troubles associés à une activité aberrante des récepteurs des œstrogènes.
MA38325A 2013-02-19 2014-02-12 Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes MA38325B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361766439P 2013-02-19 2013-02-19
PCT/US2014/015938 WO2014130310A1 (fr) 2013-02-19 2014-02-12 Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes

Publications (3)

Publication Number Publication Date
MA38325A2 MA38325A2 (fr) 2016-12-30
MA38325A3 true MA38325A3 (fr) 2018-05-31
MA38325B1 MA38325B1 (fr) 2019-03-29

Family

ID=50239942

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38325A MA38325B1 (fr) 2013-02-19 2014-02-12 Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes

Country Status (46)

Country Link
US (5) US8877801B2 (fr)
EP (2) EP2958907B1 (fr)
JP (1) JP6364028B2 (fr)
KR (1) KR102279999B1 (fr)
CN (1) CN105008343B (fr)
AP (1) AP2015008618A0 (fr)
AR (1) AR094704A1 (fr)
AU (1) AU2014219283C1 (fr)
BR (1) BR112015018882B1 (fr)
CA (1) CA2899030C (fr)
CL (1) CL2015002098A1 (fr)
CR (1) CR20150424A (fr)
CU (1) CU24337B1 (fr)
CY (1) CY1120155T1 (fr)
DK (1) DK2958907T3 (fr)
DO (1) DOP2015000202A (fr)
EA (1) EA028032B1 (fr)
ES (1) ES2671516T3 (fr)
GE (1) GEP201706638B (fr)
GT (1) GT201500233A (fr)
HK (1) HK1251227A1 (fr)
HR (1) HRP20180816T1 (fr)
HU (1) HUE039052T2 (fr)
IL (1) IL240131B (fr)
JO (1) JO3494B1 (fr)
LT (1) LT2958907T (fr)
MA (1) MA38325B1 (fr)
ME (1) ME03061B (fr)
MX (1) MX359471B (fr)
MY (1) MY174888A (fr)
NI (1) NI201500106A (fr)
NO (1) NO3077717T3 (fr)
NZ (1) NZ710385A (fr)
PE (1) PE20151428A1 (fr)
PH (1) PH12015501832B1 (fr)
PL (1) PL2958907T3 (fr)
PT (1) PT2958907T (fr)
RS (1) RS57106B1 (fr)
SG (1) SG11201505697VA (fr)
SI (1) SI2958907T1 (fr)
TN (1) TN2015000323A1 (fr)
TR (1) TR201806882T4 (fr)
TW (1) TWI612040B (fr)
UY (1) UY35334A (fr)
WO (1) WO2014130310A1 (fr)
ZA (1) ZA201505305B (fr)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2671516T3 (es) 2013-02-19 2018-06-06 Novartis Ag Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrógeno
WO2016132998A1 (fr) * 2015-02-19 2016-08-25 Jnc株式会社 Composé cristallin liquide comprenant du benzothiophène, composition de cristaux liquides et élément d'affichage à cristaux liquides
TWI708770B (zh) 2015-06-08 2020-11-01 日商捷恩智股份有限公司 具有苯并噻吩的液晶性化合物、液晶組成物及液晶顯示元件
WO2017100715A1 (fr) * 2015-12-09 2017-06-15 The Board Of Trustees Of The University Of Illinois Composés régulateurs à la baisse des récepteurs des œstrogènes sélectifs à base de benzothiophène
WO2017172957A1 (fr) 2016-04-01 2017-10-05 Kalyra Pharmaceuticals, Inc. Modulateurs du récepteur des œstrogènes
WO2018081168A2 (fr) * 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Répresseurs du récepteur oestrogénique sélectifs mixtes à base de benzothiophène
MX2019008158A (es) 2017-01-06 2019-12-09 G1 Therapeutics Inc Terapia de combinacion para el tratamiento del cancer.
TW201835064A (zh) * 2017-02-10 2018-10-01 美商G1治療公司 苯并噻吩雌激素受體調節劑
US11179365B2 (en) 2017-11-16 2021-11-23 Novartis Ag Pharmaceutical combination comprising LSZ102 and ribociclib
CA3081602A1 (fr) 2017-11-16 2019-05-23 Novartis Ag Polytherapies
CN111386113A (zh) 2017-12-01 2020-07-07 诺华股份有限公司 包含lsz102和阿培利司的药物组合
AU2019210129B2 (en) 2018-01-22 2023-09-28 Radius Pharmaceuticals, Inc. Estrogen receptor-modulating compounds
KR102765922B1 (ko) * 2018-02-06 2025-02-11 더 보오드 오브 트러스티스 오브 더 유니버시티 오브 일리노이즈 선택적인 에스트로겐 수용체 분해제로서의 치환된 벤조티오펜 유사체
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
WO2020037251A1 (fr) * 2018-08-16 2020-02-20 G1 Therapeutics, Inc. Modulateurs de récepteur d'oestrogène à base de benzothiophène pour le traitement de troubles médicaux
EP3897637A1 (fr) 2018-12-20 2021-10-27 Novartis AG Schéma posologique et combinaison pharmaceutique comprenant des dérivés de 3-(1-oxoisoindoline-2-yl) pipéridine-2,6-dione
CN113490528B (zh) 2019-02-15 2024-12-03 诺华股份有限公司 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
ES2982474T3 (es) 2019-02-15 2024-10-16 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidin-1,6-diona sustituidos y usos de estos
US20230081720A1 (en) 2019-05-20 2023-03-16 Novartis Ag Mcl-1 inhibitor antibody-drug conjugates and methods of use
AU2020326691A1 (en) 2019-08-06 2022-03-03 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants
IL293889A (en) 2019-12-20 2022-08-01 Novartis Ag Uses of anti-tgf-beta antibodies and checkpoint inhibitors for the treatment of proliferative diseases
CN111057065B (zh) * 2019-12-24 2021-04-23 沈阳药科大学 噻吩并嘧啶类化合物的制备方法和用途
CN111646972B (zh) * 2020-06-12 2021-06-29 上海皓元医药股份有限公司 一种选择性雌激素受体降解剂及其中间体的制备方法
WO2021260528A1 (fr) 2020-06-23 2021-12-30 Novartis Ag Schéma posologique comprenant des dérivés de 3-(1-oxoisoindoline-2-yl) pipéridine-2,6-dione
AU2021305165A1 (en) 2020-07-06 2023-02-02 Tactogen Inc Advantageous benzothiophene compositions for mental disorders or enhancement
WO2022029573A1 (fr) 2020-08-03 2022-02-10 Novartis Ag Dérivés de 3-(1-oxoisoindolin-2-yl)pipéridine-2,6-dione substitués par hétéroaryle et leurs utilisations
CA3202759A1 (fr) 2020-11-24 2022-06-02 Novartis Ag Conjugues anticorps-medicament inhibiteurs de mcl-1 et procedes d'utilisation
MX2023006010A (es) 2020-11-24 2023-06-08 Novartis Ag Anticuerpos anti-cd48, conjugados de anticuerpo-farmaco, y usos de los mismos.
WO2022140744A1 (fr) 2020-12-23 2022-06-30 Recurium Ip Holdings, Llc Modulateurs du récepteur des œstrogènes
US20240376094A2 (en) 2021-02-02 2024-11-14 Les Laboratoires Servier Selective bcl-xl protac compounds and methods of use
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
CN116265458A (zh) * 2021-12-17 2023-06-20 中国科学院上海药物研究所 苯并噻吩类衍生物、及其制备方法和用途
GB2617173B (en) 2022-03-31 2024-11-20 Iceye Oy Detecting and suppressing ambiguities in synthetic aperture radar data and images
CA3256012A1 (fr) 2022-05-20 2023-11-23 Les Laboratoires Servier Conjugués anticorps-médicament inhibiteurs de met bcl-xl et leurs procédés d'utilisation
KR20250027281A (ko) 2022-05-20 2025-02-25 노파르티스 아게 Epha2 bcl-xl 억제제 항체-약물 접합체 및 그의 사용 방법
CN115710248B (zh) * 2022-11-18 2024-06-21 南京中医药大学 新型选择性雌激素受体下调剂化合物、制备方法及用途
KR20250160354A (ko) 2023-03-10 2025-11-12 노파르티스 아게 Panras 억제제 항체-약물 콘쥬게이트 및 이의 사용 방법
TW202540185A (zh) 2023-11-22 2025-10-16 法商施維雅藥廠 抗cd74抗體藥物結合物及其使用方法
WO2025215536A1 (fr) 2024-04-10 2025-10-16 Novartis Ag Inhibiteurs de panras macrocycliques pour le traitement du cancer

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH445129A (fr) 1964-04-29 1967-10-15 Nestle Sa Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453259A (en) 1967-03-22 1969-07-01 Corn Products Co Cyclodextrin polyol ethers and their oxidation products
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 １，２‐ジアミノシクロヘキサン異性体のシス白金（２）錯体
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
ZA822247B (en) * 1981-04-03 1983-11-30 Lilly Co Eli Benzothiophene compounds and process for preparing them
US4418068A (en) 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
US4737323A (en) 1986-02-13 1988-04-12 Liposome Technology, Inc. Liposome extrusion method
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
EP0647450A1 (fr) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Prodrogues améliorées pour activation médiée par enzyme
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
US6562862B1 (en) * 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
IL115849A0 (en) 1994-11-03 1996-01-31 Merz & Co Gmbh & Co Tangential filtration preparation of liposomal drugs and liposome product thereof
US5589482A (en) 1994-12-14 1996-12-31 Pfizer Inc. Benzo-thiophene estrogen agonists to treat prostatic hyperplasia
US5998441A (en) 1995-02-28 1999-12-07 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
JP3989569B2 (ja) 1995-02-28 2007-10-10 イーライ リリー アンド カンパニー ベンゾチオフェン化合物、中間体、組成物および方法
US6417199B1 (en) 1995-03-10 2002-07-09 Eli Lilly And Company 3-benzyl-benzothiophenes
ATE198477T1 (de) * 1995-06-26 2001-01-15 Lilly Co Eli Benzothiophenderivate
US5731342A (en) 1996-02-22 1998-03-24 Eli Lilly And Company Benzothiophenes, formulations containing same, and methods
US5827876A (en) * 1996-04-09 1998-10-27 American Home Products Corporation Inhibition of bone loss by 3-(4-acrylamidobenzoyl) benzo b!-thiophenes
US5886025A (en) 1997-03-06 1999-03-23 Baylor University Anti-mitotic agents which inhibit tubulin polymerization
ZA982819B (en) 1997-04-09 1999-10-04 Lilly Co Eli Treatment or prophylaxis of prostatic cancer and benign prostatic hyperplasia with selective estrogn receptor modulators.
ZA982877B (en) 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
ZA982818B (en) 1997-04-09 1999-10-04 Lilly Co Eli Prevention of breast cancer using selective estrogen receptor modulators.
EP1077965A1 (fr) 1998-05-12 2001-02-28 American Home Products Corporation Acides phenyl-oxo-acetiques utiles dans le traitement de l'insulinoresistance et de l'hyperglycemie
US6166069A (en) 1998-05-12 2000-12-26 American Home Products Corporation Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
NZ521225A (en) 2000-03-09 2004-08-27 Aventis Pharma Gmbh Therapeutic uses of PPAR mediators
US7091240B2 (en) 2000-03-10 2006-08-15 Oxigene, Inc. Tubulin binding ligands and corresponding prodrug constructs
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7425565B2 (en) 2002-05-09 2008-09-16 Cedars-Sinai Medical Center Use of benzothiopenes to treat and prevent prostate cancer
EP2407473A3 (fr) 2002-02-01 2012-03-21 ARIAD Pharmaceuticals, Inc Procédé de préparation de composés contenant du phosphore
IL163748A0 (en) 2002-03-05 2005-12-18 Merck Frosst Canada Inc Cathepsin cysteine protease inhibitors
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
DE60327931D1 (de) 2002-07-22 2009-07-23 Lilly Co Eli Selektive östrogenrezeptor modulatoren, die eine phenylsulfonyl-gruppe enthalten
DE602004016331D1 (de) 2003-06-10 2008-10-16 Lilly Co Eli Pentafluoroalkylsulfin-naphthaline und und darauf bezogene modulatoren des östrogenrezeptors
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
WO2005073206A1 (fr) 2004-01-22 2005-08-11 Eli Lilly And Company Modulateurs selectifs du recepteur des oestrogenes
US20070111988A1 (en) 2004-01-22 2007-05-17 Eli Lilly And Company Selective estrogen receptor modulators
EP1713770A1 (fr) 2004-01-29 2006-10-25 Eli Lilly And Company Modulateurs selectifs du recepteur des oestrogenes
CN102964294A (zh) 2004-09-02 2013-03-13 遗传技术研究公司 Hedgehog信号转导的吡啶基抑制剂
CA2599987A1 (fr) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Composes heterocycliques liquefies et leur utilisation comme modulateurs de sirtuine
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2681478A1 (fr) 2007-03-16 2008-09-25 Eli Lilly And Company Procede et intermediaires pour preparer l'arzoxifene
PE20090678A1 (es) 2007-09-12 2009-06-27 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso
US20090069380A1 (en) 2007-09-12 2009-03-12 Protia, Llc Deuterium-enriched aroxifene
JP5348725B2 (ja) 2007-10-25 2013-11-20 ジェネンテック， インコーポレイテッド チエノピリミジン化合物の製造方法
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
CN102477033A (zh) * 2010-11-23 2012-05-30 苏州波锐生物医药科技有限公司 苯并噻酚类化合物及其在制备预防和/或治疗乳腺癌骨质疏松症药物中的用途
WO2012084711A1 (fr) 2010-12-24 2012-06-28 Msd Oss B.V. Dérivés d'azétidine n-substitués
ES2671516T3 (es) 2013-02-19 2018-06-06 Novartis Ag Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrógeno

Also Published As

Publication number Publication date
AR094704A1 (es) 2015-08-19
MA38325B1 (fr) 2019-03-29
EP2958907B1 (fr) 2018-02-28
GEP201706638B (en) 2017-03-10
EA201591537A1 (ru) 2015-12-30
HRP20180816T1 (hr) 2018-06-29
MX2015010752A (es) 2015-11-30
ES2671516T3 (es) 2018-06-06
CU24337B1 (es) 2018-04-03
CR20150424A (es) 2015-10-19
IL240131A0 (en) 2015-09-24
EP3360870A1 (fr) 2018-08-15
US20170112805A1 (en) 2017-04-27
NI201500106A (es) 2015-10-20
US20160184265A1 (en) 2016-06-30
US20150361065A1 (en) 2015-12-17
BR112015018882A2 (pt) 2017-07-18
UY35334A (es) 2014-09-30
US8877801B2 (en) 2014-11-04
MY174888A (en) 2020-05-20
US9561211B2 (en) 2017-02-07
PT2958907T (pt) 2018-03-23
LT2958907T (lt) 2018-04-25
CN105008343A (zh) 2015-10-28
PE20151428A1 (es) 2015-09-24
CA2899030C (fr) 2021-03-09
GT201500233A (es) 2016-01-21
TW201443034A (zh) 2014-11-16
PH12015501832A1 (en) 2015-11-09
AU2014219283B2 (en) 2015-10-29
NO3077717T3 (fr) 2018-07-21
ME03061B (fr) 2019-01-20
JO3494B1 (ar) 2020-07-05
CN105008343B (zh) 2017-12-08
IL240131B (en) 2018-11-29
PH12015501832B1 (en) 2015-11-09
KR20150119385A (ko) 2015-10-23
KR102279999B1 (ko) 2021-07-22
DK2958907T3 (en) 2018-06-06
DOP2015000202A (es) 2015-11-30
US20180169063A1 (en) 2018-06-21
US20140235660A1 (en) 2014-08-21
EA028032B1 (ru) 2017-09-29
HK1211941A1 (en) 2016-06-03
SG11201505697VA (en) 2015-09-29
TR201806882T4 (tr) 2018-06-21
CL2015002098A1 (es) 2015-11-13
HUE039052T2 (hu) 2018-12-28
US10058534B2 (en) 2018-08-28
ZA201505305B (en) 2016-09-28
PL2958907T3 (pl) 2018-07-31
US9321746B2 (en) 2016-04-26
BR112015018882B1 (pt) 2021-09-14
SI2958907T1 (en) 2018-05-31
CA2899030A1 (fr) 2014-08-28
TN2015000323A1 (en) 2017-01-03
TWI612040B (zh) 2018-01-21
HK1251227A1 (en) 2019-01-25
JP6364028B2 (ja) 2018-07-25
AU2014219283A1 (en) 2015-08-13
EP2958907A1 (fr) 2015-12-30
US9931317B2 (en) 2018-04-03
JP2016509022A (ja) 2016-03-24
MA38325A2 (fr) 2016-12-30
WO2014130310A1 (fr) 2014-08-28
NZ710385A (en) 2016-10-28
AU2014219283C1 (en) 2016-10-27
RS57106B1 (sr) 2018-06-29
CY1120155T1 (el) 2018-12-12
MX359471B (es) 2018-09-28
CU20150090A7 (es) 2016-04-25
AP2015008618A0 (en) 2015-07-31

Similar Documents

Publication Publication Date Title
MA38325A2 (fr) Dérivés de benzothiophène et compositions correspondantes en tant qu'agents de dégradation sélectifs des récepteurs des œstrogènes
MA35187B1 (fr) Composés ayant une activité antagoniste d'un récepteur muscarinique et agoniste d'un récepteur béta2 adrénergique
MA38147A1 (fr) Composés ayant une activité antagoniste du récepteur muscarinique et agoniste du récepteur bêta2 adrénergique
MA42230B1 (fr) Dérivés bicycliques, leur procédé de préparation, et compositions pharmaceutiques les contenant
MA50240B1 (fr) Modulateurs de la protéine régulatrice de la conductance transmembranaire de la fibrose kystique et procédés d'utilisation
MA35275B1 (fr) Composés de tétrahydropyridopyridine et tétrahydropyridopyrimidine et utilisation de ceux-ci en tant que modulateurs de récepteur c5a
MA30991B1 (fr) Utilisation de dérivés du benzamide comme agonistes des récepteurs ep4
EP2614860A4 (fr) Composition pharmaceutique pour le traitement de l'oeil sec
WO2019007696A1 (fr) Nouveaux composés et compositions pharmaceutiques de ceux-ci destinés au traitement de la fibrose
MA31521B1 (fr) Dérivés de 2,3-dihydrobenzo[1,4] dioxin-2-ylméthyle utilisés en tant qu'antagonistes des alpha2c pour traiter des maladies des systèmes nerveux périphérique et central
MA38260A1 (fr) Nouveaux dérivés de cyclohexyl et quinuclidinyl carbamate ayant une activité d'agoniste adrénergique beta2 et une activité d'antagoniste muscarinique m3
MA33132B1 (fr) Derives pyrazole utilises comme antagonistes du recepteur ccr4
MA37888B1 (fr) Composition pharmaceutique enrobée contenant du régorafenib
TN2016000014A1 (fr) Nouveaux dérivés d'indolizine, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent
MA35893B1 (fr) Dérivés d'amide hétérocyclique comme antagonistes du récepteur p2x7
MA28435B1 (fr) Composes d'indazole-carboxamide en tant qu'agonistes de recepteur 5-ht4
MA37990B1 (fr) Benzamides
MA47469B1 (fr) Dérivés 2-(3-(1h-benzo[d]imidazol-1-yl)propyl)pipéridin-3-ol et composés similaires en tant q'inhibiteurs prs pour le traitement du cancer
MA38679B1 (fr) Modulateurs du récepteur de cxcr7
MA43913A (fr) Modulateurs allostériques positifs du récepteur m1 muscarinique
MA39229A1 (fr) Pyrrolidines, térahydrofuranes et cyclopentanes substitués utiles en tant qu'antagonistes des récepteurs des orexines
MA43250B1 (fr) Composés d'oxadiazaspiro pour le traitement de l'abus et la dépendance aux drogues
MA34910B1 (fr) Dérivés de 2-methoxy-pyridin-4-yl
MA38011B1 (fr) Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5
MA39054A1 (fr) Dérivés pyridyle bicycliques à anneaux fusionnés utilisés en tant qu'inhibiteurs de fgfr4