MX359471B - Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno. - Google Patents

Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno.

Info

Publication number
MX359471B
MX359471B MX2015010752A MX2015010752A MX359471B MX 359471 B MX359471 B MX 359471B MX 2015010752 A MX2015010752 A MX 2015010752A MX 2015010752 A MX2015010752 A MX 2015010752A MX 359471 B MX359471 B MX 359471B
Authority
MX
Mexico
Prior art keywords
compositions
estrogen receptor
compounds
selective estrogen
benzothiophene derivatives
Prior art date
Application number
MX2015010752A
Other languages
English (en)
Spanish (es)
Other versions
MX2015010752A (es
Inventor
Peukert Stefan
Elizabeth Burks Heather
A Dechantsreiter Michael
He Guo
Springer Clayton
Sun Yingchuan
Marie-France Thomsen Noel
Scott Tria George
Yu Bing
Nunez Jill
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 MX2015010752A publication Critical patent/MX2015010752A/es
Publication of MX359471B publication Critical patent/MX359471B/es

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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
MX2015010752A 2013-02-19 2014-02-12 Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno. MX359471B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361766439P 2013-02-19 2013-02-19
PCT/US2014/015938 WO2014130310A1 (en) 2013-02-19 2014-02-12 Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders

Publications (2)

Publication Number Publication Date
MX2015010752A MX2015010752A (es) 2015-11-30
MX359471B true MX359471B (es) 2018-09-28

Family

ID=50239942

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015010752A MX359471B (es) 2013-02-19 2014-02-12 Derivados de benzotiofeno y composiciones de los mismos como degradantes selectivos de los receptores de estrogeno.

Country Status (46)

Country Link
US (5) US9321746B2 (OSRAM)
EP (2) EP2958907B1 (OSRAM)
JP (1) JP6364028B2 (OSRAM)
KR (1) KR102279999B1 (OSRAM)
CN (1) CN105008343B (OSRAM)
AP (1) AP2015008618A0 (OSRAM)
AR (1) AR094704A1 (OSRAM)
AU (1) AU2014219283C1 (OSRAM)
BR (1) BR112015018882B1 (OSRAM)
CA (1) CA2899030C (OSRAM)
CL (1) CL2015002098A1 (OSRAM)
CR (1) CR20150424A (OSRAM)
CU (1) CU24337B1 (OSRAM)
CY (1) CY1120155T1 (OSRAM)
DK (1) DK2958907T3 (OSRAM)
DO (1) DOP2015000202A (OSRAM)
EA (1) EA028032B1 (OSRAM)
ES (1) ES2671516T3 (OSRAM)
GE (1) GEP201706638B (OSRAM)
GT (1) GT201500233A (OSRAM)
HK (1) HK1251227A1 (OSRAM)
HR (1) HRP20180816T1 (OSRAM)
HU (1) HUE039052T2 (OSRAM)
IL (1) IL240131B (OSRAM)
JO (1) JO3494B1 (OSRAM)
LT (1) LT2958907T (OSRAM)
MA (1) MA38325B1 (OSRAM)
ME (1) ME03061B (OSRAM)
MX (1) MX359471B (OSRAM)
MY (1) MY174888A (OSRAM)
NI (1) NI201500106A (OSRAM)
NO (1) NO3077717T3 (OSRAM)
NZ (1) NZ710385A (OSRAM)
PE (1) PE20151428A1 (OSRAM)
PH (1) PH12015501832A1 (OSRAM)
PL (1) PL2958907T3 (OSRAM)
PT (1) PT2958907T (OSRAM)
RS (1) RS57106B1 (OSRAM)
SG (1) SG11201505697VA (OSRAM)
SI (1) SI2958907T1 (OSRAM)
TN (1) TN2015000323A1 (OSRAM)
TR (1) TR201806882T4 (OSRAM)
TW (1) TWI612040B (OSRAM)
UY (1) UY35334A (OSRAM)
WO (1) WO2014130310A1 (OSRAM)
ZA (1) ZA201505305B (OSRAM)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105008343B (zh) 2013-02-19 2017-12-08 诺华股份有限公司 作为选择性雌激素受体降解剂的苯并噻吩衍生物及其组合物
KR20170118687A (ko) 2015-02-19 2017-10-25 제이엔씨 주식회사 벤조티오펜을 가지는 액정성 화합물, 액정 조성물 및 액정 표시 소자
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
RU2747802C2 (ru) * 2015-12-09 2021-05-14 Зе Боард Оф Трастис Оф Зе Юниверсити Оф Иллинойс Бензотиофеновые селективные блокаторы эстрогеновых рецепторов
RU2738646C2 (ru) 2016-04-01 2020-12-15 РЕКЬЮРИУМ АйПи ХОЛДИНГС, ЛЛС Модуляторы эстрогеновых рецепторов
WO2018081168A2 (en) * 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
EA201991622A1 (ru) * 2017-01-06 2020-01-23 Г1 Терапьютикс, Инк. Комплексная терапия для лечения рака
EP3580223A4 (en) 2017-02-10 2021-01-06 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators
US11179365B2 (en) 2017-11-16 2021-11-23 Novartis Ag Pharmaceutical combination comprising LSZ102 and ribociclib
MX2020004756A (es) 2017-11-16 2020-08-20 Novartis Ag Terapias de combinacion.
US10695333B2 (en) 2017-12-01 2020-06-30 Novartis Ag Pharmaceutical combination comprising LSZ102 and alpelisib
IL304460B2 (en) 2018-01-22 2025-10-01 Radius Pharmaceuticals Inc Estrogen receptor modulators
JP7348665B2 (ja) 2018-02-06 2023-09-21 ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティ オブ イリノイ 選択的エストロゲン受容体分解剤としての置換ベンゾチオフェン類似体
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
AU2019321677A1 (en) * 2018-08-16 2021-03-11 G1 Therapeutics, Inc. Benzothiophene estrogen receptor modulators to treat medical disorders
BR112021011874A2 (pt) 2018-12-20 2021-09-08 Novartis Ag Regime de dosagem e combinação farmacêutica compreendendo derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona
WO2020165833A1 (en) 2019-02-15 2020-08-20 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
AU2020222346B2 (en) 2019-02-15 2021-12-09 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CA3136088A1 (en) 2019-05-20 2020-11-26 Matthew T. Burger Mcl-1 inhibitor antibody-drug conjugates and methods of use
KR20220044528A (ko) 2019-08-06 2022-04-08 리커리엄 아이피 홀딩스, 엘엘씨 돌연변이체를 치료하기 위한 에스트로겐 수용체 조절제
CN115175937A (zh) 2019-12-20 2022-10-11 诺华股份有限公司 用于治疗骨髓纤维化和骨髓增生异常综合征的抗TIM-3抗体MBG453和抗TGF-β抗体NIS793与或不与地西他滨或抗PD-1抗体斯巴达珠单抗的组合
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
CA3182346A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CN116096715A (zh) * 2020-07-06 2023-05-09 泰科根公司 用于精神障碍或精神增强的有益苯并噻吩组合物
US20230271940A1 (en) 2020-08-03 2023-08-31 Novartis Ag Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EP4251208A1 (en) 2020-11-24 2023-10-04 Novartis AG Mcl-1 inhibitor antibody-drug conjugates and methods of use
CR20230283A (es) 2020-11-24 2023-07-27 Novartis Ag Anticuerpos anti-cd48, conjugados de anticuerpo-fármaco, y usos de los mismos
JP2024502270A (ja) 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
IL304891A (en) 2021-02-02 2023-10-01 Servier Lab Selective Protech BCL-XL 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
JP2025517429A (ja) 2022-05-20 2025-06-05 ノバルティス アーゲー Ｍｅｔ ｂｃｌ－ｘｌ阻害剤抗体－薬物コンジュゲートおよびその使用の方法
AU2023271885A1 (en) 2022-05-20 2024-12-12 Les Laboratoires Servier Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
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
IL322700A (en) 2023-03-10 2025-10-01 Novartis Ag Antibody-drug conjugates that inhibit fennerase and methods of using them
WO2025111450A1 (en) 2023-11-22 2025-05-30 Les Laboratoires Servier Anti-cd74 antibody-drug conjugates and methods of use thereof
WO2025215536A1 (en) 2024-04-10 2025-10-16 Novartis Ag Macrocyclic panras inhibitors for the treatment of 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
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic 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 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
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
US5510357A (en) 1995-02-28 1996-04-23 Eli Lilly And Company Benzothiophene compounds as anti-estrogenic agents
EP1113013A1 (en) 1995-02-28 2001-07-04 Eli Lilly & Company Benzothiophene compounds, intermediates, compositions and methods
US5998441A (en) 1995-02-28 1999-12-07 Eli Lilly And Company Benzothiophene compounds, intermediates, compositions, and methods
US6417199B1 (en) 1995-03-10 2002-07-09 Eli Lilly And Company 3-benzyl-benzothiophenes
EP0842169B1 (en) * 1995-06-26 2001-01-03 Eli Lilly And Company Benzothiophene compounds
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
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.
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.
CA2331120A1 (en) 1998-05-12 1999-11-18 Iwan Gunawan Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
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
AU2001272098A1 (en) 2000-03-09 2001-09-17 Sanofi-Aventis Deutschland 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
WO2003064383A2 (en) 2002-02-01 2003-08-07 Ariad Gene Therapeutics, Inc. Phosphorus-containing compounds & uses thereof
HRP20040800B1 (en) 2002-03-05 2012-11-30 Merck Frosst Canada & Co Axys Cathepsin cysteine protease inhibitors
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
WO2004009086A1 (en) 2002-07-22 2004-01-29 Eli Lilly And Company Selective estrogen receptor modulators containing a phenylsulfonyl group
EP1641774B1 (en) 2003-06-10 2008-09-03 Eli Lilly And Company Pentafluoroalkanesulfinyl naphthalenes and related estrogen receptor modulators
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
DE602005017577D1 (de) 2004-01-22 2009-12-24 Lilly Co Eli Selektive östrogen-rezeptor-modulatoren
US20070111988A1 (en) 2004-01-22 2007-05-17 Eli Lilly And Company Selective estrogen receptor modulators
WO2005073190A1 (en) 2004-01-29 2005-08-11 Eli Lilly And Company Selective estrogen receptor modulators
KR20180122750A (ko) 2004-09-02 2018-11-13 제넨테크, 인크. 헤지호그 신호전달에 대한 피리딜 억제제
WO2006094235A1 (en) 2005-03-03 2006-09-08 Sirtris Pharmaceuticals, Inc. Fused heterocyclic compounds and their use as sirtuin modulators
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
KR20090112758A (ko) 2007-03-16 2009-10-28 일라이 릴리 앤드 캄파니 아르족시펜의 제조를 위한 방법 및 중간체
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
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
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
CA2819299A1 (en) 2010-12-24 2012-06-28 Merck Sharp & Dohme B.V. N-substituted azetidine derivatives
CN105008343B (zh) 2013-02-19 2017-12-08 诺华股份有限公司 作为选择性雌激素受体降解剂的苯并噻吩衍生物及其组合物

Also Published As

Publication number Publication date
CR20150424A (es) 2015-10-19
AU2014219283A1 (en) 2015-08-13
US20150361065A1 (en) 2015-12-17
UY35334A (es) 2014-09-30
MY174888A (en) 2020-05-20
AR094704A1 (es) 2015-08-19
PT2958907T (pt) 2018-03-23
LT2958907T (lt) 2018-04-25
ZA201505305B (en) 2016-09-28
US20160184265A1 (en) 2016-06-30
RS57106B1 (sr) 2018-06-29
MA38325B1 (fr) 2019-03-29
TWI612040B (zh) 2018-01-21
IL240131B (en) 2018-11-29
GEP201706638B (en) 2017-03-10
US9321746B2 (en) 2016-04-26
ES2671516T3 (es) 2018-06-06
KR20150119385A (ko) 2015-10-23
PH12015501832B1 (en) 2015-11-09
HUE039052T2 (hu) 2018-12-28
US8877801B2 (en) 2014-11-04
US20170112805A1 (en) 2017-04-27
EP2958907A1 (en) 2015-12-30
US9561211B2 (en) 2017-02-07
HK1251227A1 (en) 2019-01-25
NO3077717T3 (OSRAM) 2018-07-21
CL2015002098A1 (es) 2015-11-13
EA028032B1 (ru) 2017-09-29
CU20150090A7 (es) 2016-04-25
HK1211941A1 (en) 2016-06-03
JP6364028B2 (ja) 2018-07-25
JO3494B1 (ar) 2020-07-05
US20180169063A1 (en) 2018-06-21
BR112015018882A2 (pt) 2017-07-18
JP2016509022A (ja) 2016-03-24
TN2015000323A1 (en) 2017-01-03
WO2014130310A1 (en) 2014-08-28
NI201500106A (es) 2015-10-20
KR102279999B1 (ko) 2021-07-22
EP2958907B1 (en) 2018-02-28
CA2899030C (en) 2021-03-09
GT201500233A (es) 2016-01-21
PL2958907T3 (pl) 2018-07-31
NZ710385A (en) 2016-10-28
HRP20180816T1 (hr) 2018-06-29
EA201591537A1 (ru) 2015-12-30
US20140235660A1 (en) 2014-08-21
AU2014219283C1 (en) 2016-10-27
MA38325A2 (fr) 2016-12-30
PH12015501832A1 (en) 2015-11-09
AU2014219283B2 (en) 2015-10-29
CY1120155T1 (el) 2018-12-12
DOP2015000202A (es) 2015-11-30
CU24337B1 (es) 2018-04-03
CN105008343B (zh) 2017-12-08
EP3360870A1 (en) 2018-08-15
CA2899030A1 (en) 2014-08-28
CN105008343A (zh) 2015-10-28
SG11201505697VA (en) 2015-09-29
DK2958907T3 (en) 2018-06-06
MX2015010752A (es) 2015-11-30
IL240131A0 (en) 2015-09-24
AP2015008618A0 (en) 2015-07-31
US10058534B2 (en) 2018-08-28
MA38325A3 (fr) 2018-05-31
PE20151428A1 (es) 2015-09-24
TW201443034A (zh) 2014-11-16
BR112015018882B1 (pt) 2021-09-14
SI2958907T1 (en) 2018-05-31
US9931317B2 (en) 2018-04-03
TR201806882T4 (tr) 2018-06-21
ME03061B (me) 2019-01-20

Similar Documents

Publication Publication Date Title
PH12015501832B1 (en) Benzothiophene derivatives and compositions thereof as selective estrogen receptor degraders
MX2015017861A (es) Derivados de benzotiofeno como inhibidores del receptor de estrogeno.
MX2021007432A (es) Compuestos y composiciones para inhibir la actividad de shp2.
PH12014502540B1 (en) Benzimidazole-proline derivatives
BR112015031903A2 (pt) composto, sal farmaceuticamente aceitável do composto, composição farmacêutica e utilização de um composto
PH12014501057A1 (en) New cyclohexylamine derivatives having beta 2 adrenergic agonist and m3 muscarinic antagonist activities
PH12014501056A1 (en) New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
EA201500651A1 (ru) НОВЫЕ ПРОИЗВОДНЫЕ ЦИКЛОГЕКСИЛ- И ХИНУКЛИДИНИЛКАРБАМАТА, ОБЛАДАЮЩИЕ АГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К β2 АДРЕНЕРГИЧЕСКОМУ РЕЦЕПТОРУ И АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К МУСКАРИНОВОМУ РЕЦЕПТОРУ М3
MX2017002775A (es) Derivados de pirrolopirimidina como antagonistas del receptor de n-metil-d-aspartato (nmda), subunidad nr2b.
PH12014501195A1 (en) Novel 2h-indazoles as ep2, receptor antagonists
PH12015502632A1 (en) Cxcr7 receptor modulators
MX2015008733A (es) Derivados de 1,2,3-triazol-4-amina para el tratamiento de enfermedades y transtornos relacionados con receptores sigma.
IN2014MN01765A (OSRAM)
MX2013005169A (es) Derivados biciclicos sustituidos de carboxamida y urea como ligandos de receptor vanilloide.
MX2015014516A (es) Compuestos triazolicos triciclicos como ligandos de receptores sigma.
PH12014500934A1 (en) Nicotinic receptor non-competitive modulators
PH12013501453A1 (en) Nicotinic receptor non-competitive antagonists
UA108104C2 (uk) ПОХІДНІ ЦИКЛОГЕКСИЛАМІНУ, ЩО МАЮТЬ АГОНІСТИЧНУ АКТИВНІСТЬ ПО ВІДНОШЕННЮ ДО β2 АДРЕНЕРГІЧНОГО РЕЦЕПТОРА І АНТАГОНІСТИЧНОЇ АКТИВНОСТІ ПО ВІДНОШЕННЮ ДО M3 МУСКАРИНОВОГО РЕЦЕПТОРА
GR1008039B (el) Σταθερο ενεσιμο φαρμακευτικο σκευασμα ενος αγωνιστη των υποδοχεων της βιταμινης d και μεθοδος για την παρασκευη αυτου

Legal Events

Date Code Title Description
FG Grant or registration