AR094704A1 - Compuestos y composiciones como degradantes selectivos del receptor de estrógeno - Google Patents
Compuestos y composiciones como degradantes selectivos del receptor de estrógenoInfo
- Publication number
- AR094704A1 AR094704A1 ARP140100517A ARP140100517A AR094704A1 AR 094704 A1 AR094704 A1 AR 094704A1 AR P140100517 A ARP140100517 A AR P140100517A AR P140100517 A ARP140100517 A AR P140100517A AR 094704 A1 AR094704 A1 AR 094704A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- substituted
- hydrogen
- halo
- independently selected
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000008380 degradant Substances 0.000 title 1
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 10
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 7
- 229920006395 saturated elastomer Polymers 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical group C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361766439P | 2013-02-19 | 2013-02-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR094704A1 true AR094704A1 (es) | 2015-08-19 |
Family
ID=50239942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140100517A AR094704A1 (es) | 2013-02-19 | 2014-02-19 | Compuestos y composiciones como degradantes selectivos del receptor de estrógeno |
Country Status (46)
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112015018882B1 (pt) | 2013-02-19 | 2021-09-14 | Novartis Ag | Derivados de benzotiofeno e composições dos mesmos como degradadores de receptor de estrogênio seletivo |
| US10308871B2 (en) | 2015-02-19 | 2019-06-04 | Jnc Corporation | Liquid crystal compound having benzothiophene, liquid crystal composition and liquid crystal display device |
| 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 |
| SMT202300018T1 (it) * | 2015-12-09 | 2023-03-17 | Univ Illinois | Downregolatori del recettore degli estrogeni a base di benzotiofene |
| CN112745316A (zh) | 2016-04-01 | 2021-05-04 | 里科瑞尔姆Ip控股有限责任公司 | 雌激素受体调节剂 |
| WO2018081168A2 (en) * | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| EP3565558B1 (en) | 2017-01-06 | 2023-12-06 | G1 Therapeutics, Inc. | Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer |
| KR20190117582A (ko) | 2017-02-10 | 2019-10-16 | 쥐원 쎄라퓨틱스, 인크. | 벤조티오펜 에스트로겐 수용체 조정제 |
| CN111315378A (zh) | 2017-11-16 | 2020-06-19 | 诺华股份有限公司 | 包含lsz102和瑞博西尼的药物组合 |
| TW201922291A (zh) | 2017-11-16 | 2019-06-16 | 瑞士商諾華公司 | 組合療法 |
| WO2019106604A1 (en) | 2017-12-01 | 2019-06-06 | Novartis Ag | Pharmaceutical combination comprising lsz102 and alpelisib |
| IL276152B2 (en) | 2018-01-22 | 2023-12-01 | Radius Pharmaceuticals Inc | Estrogen receptor-modulating compounds |
| EP3749654B1 (en) * | 2018-02-06 | 2025-04-23 | The Board of Trustees of the University of Illinois | Substituted benzothiophene analogs as selective estrogen receptor degraders |
| 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 |
| CN112839646A (zh) * | 2018-08-16 | 2021-05-25 | G1治疗公司 | 用于治疗医学疾病的苯并噻吩雌激素受体调节剂 |
| KR20210106437A (ko) | 2018-12-20 | 2021-08-30 | 노파르티스 아게 | 3-(1-옥소이소인돌린-2-일)피페리딘-2,6-디온 유도체를 포함하는 투약 요법 및 약학적 조합물 |
| EP3924055B1 (en) | 2019-02-15 | 2024-04-03 | Novartis AG | Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof |
| 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 |
| KR20220024106A (ko) | 2019-05-20 | 2022-03-03 | 노파르티스 아게 | Mcl-1 억제제 항체-약물 접합체 및 사용 방법 |
| CA3148221A1 (en) | 2019-08-06 | 2021-02-11 | Recurium Ip Holdings, Llc | Estrogen receptor modulators for treating mutants |
| MX2022007759A (es) | 2019-12-20 | 2022-07-19 | Novartis Ag | Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico. |
| 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 |
| CN115916199A (zh) | 2020-06-23 | 2023-04-04 | 诺华股份有限公司 | 包含3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物的给药方案 |
| CA3182412A1 (en) * | 2020-07-06 | 2022-01-13 | Mathew BAGGOTT | Advantageous benzothiophene compositions for mental disorders or enhancement |
| 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 |
| US20240042051A1 (en) | 2020-11-24 | 2024-02-08 | Francesca Rocchetti | Mcl-1 inhibitor antibody-drug conjugates and methods of use |
| CA3200858A1 (en) | 2020-11-24 | 2022-06-02 | Novartis Ag | Anti-cd48 antibodies, antibody drug conjugates, and uses thereof |
| EP4267578A4 (en) | 2020-12-23 | 2024-11-20 | Recurium IP Holdings, LLC | ESTROGEN RECEPTOR MODULATORS |
| CN117794929A (zh) | 2021-02-02 | 2024-03-29 | 法国施维雅药厂 | 选择性bcl-xl protac化合物及使用方法 |
| 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 |
| US20250339547A1 (en) | 2022-05-20 | 2025-11-06 | Novartis Ag | Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof |
| IL317102A (en) | 2022-05-20 | 2025-01-01 | Novartis Ag | EPHA2 BCL-XL inhibitor antibody-drug conjugates and methods of using them |
| 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 |
| AU2024234194A1 (en) | 2023-03-10 | 2025-08-07 | Novartis Ag | Panras inhibitor antibody-drug conjugates and methods of use thereof |
| PY24103486A (es) | 2023-11-22 | 2025-06-06 | Servier Lab | Conjugados de anticuerpo anti-cd74-fármaco y métodos de uso de los mismos |
| WO2025215536A1 (en) | 2024-04-10 | 2025-10-16 | Novartis Ag | Macrocyclic panras inhibitors for the treatment of cancer |
Family Cites Families (57)
| 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 |
| UA44710C2 (uk) * | 1995-02-28 | 2002-03-15 | Елі Ліллі Енд Компані | Похідні бензотіофену, спосіб їх одержання (варіанти), проміжні сполуки, фармацевтична композиція |
| 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 |
| JPH11508269A (ja) * | 1995-06-26 | 1999-07-21 | 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 |
| 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. |
| 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. |
| ZA982818B (en) | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Prevention of breast cancer using selective estrogen receptor modulators. |
| AU3791799A (en) | 1998-05-12 | 1999-11-29 | American Home Products Corporation | 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 |
| KR20020081424A (ko) | 2000-03-09 | 2002-10-26 | 아벤티스 파마 도이칠란트 게엠베하 | Ppar 매개인자의 치료학적 용도 |
| 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 |
| JP4547911B2 (ja) | 2002-02-01 | 2010-09-22 | アリアド・ファーマシューティカルズ・インコーポレイテッド | リン含有化合物およびその用途 |
| US7375134B2 (en) | 2002-03-05 | 2008-05-20 | Axys Pharmaceuticals, Inc. | Cathepsin cysteine protease inhibitors |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| ATE433322T1 (de) | 2002-07-22 | 2009-06-15 | Lilly Co Eli | Selektive östrogenrezeptor modulatoren, die eine phenylsulfonyl-gruppe enthalten |
| US7462647B2 (en) | 2003-06-10 | 2008-12-09 | Eli Lilly And Company | Pentalfluoroalkanesulfinyl naphthalenes and related estrogen receptor modulators |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| ATE448215T1 (de) * | 2004-01-22 | 2009-11-15 | Lilly Co Eli | Selektive östrogen-rezeptor-modulatoren |
| WO2005073205A1 (en) | 2004-01-22 | 2005-08-11 | Eli Lilly And Company | Selective estrogen receptor modulators |
| EP1713770A1 (en) | 2004-01-29 | 2006-10-25 | Eli Lilly And Company | Selective estrogen receptor modulators |
| DK1789390T3 (da) | 2004-09-02 | 2012-02-27 | Genentech Inc | Pyridyl-inhibitorer af hedgehog-signalering |
| AU2006218403A1 (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 |
| EA200970863A1 (ru) | 2007-03-16 | 2010-02-26 | Эли Лилли Энд Компани | Способ и промежуточные соединения для получения арзоксифена |
| AU2008298948B2 (en) | 2007-09-12 | 2014-09-04 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| US20090069380A1 (en) | 2007-09-12 | 2009-03-12 | Protia, Llc | Deuterium-enriched aroxifene |
| US8354528B2 (en) | 2007-10-25 | 2013-01-15 | 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 |
| BR112015018882B1 (pt) | 2013-02-19 | 2021-09-14 | Novartis Ag | Derivados de benzotiofeno e composições dos mesmos como degradadores de receptor de estrogênio seletivo |
-
2014
- 2014-02-12 BR BR112015018882-6A patent/BR112015018882B1/pt not_active IP Right Cessation
- 2014-02-12 WO PCT/US2014/015938 patent/WO2014130310A1/en not_active Ceased
- 2014-02-12 AP AP2015008618A patent/AP2015008618A0/xx unknown
- 2014-02-12 MA MA38325A patent/MA38325B1/fr unknown
- 2014-02-12 MY MYPI2015702659A patent/MY174888A/en unknown
- 2014-02-12 CN CN201480009342.8A patent/CN105008343B/zh active Active
- 2014-02-12 LT LTEP14708992.4T patent/LT2958907T/lt unknown
- 2014-02-12 PT PT147089924T patent/PT2958907T/pt unknown
- 2014-02-12 HR HRP20180816TT patent/HRP20180816T1/hr unknown
- 2014-02-12 PL PL14708992T patent/PL2958907T3/pl unknown
- 2014-02-12 US US14/178,652 patent/US8877801B2/en active Active
- 2014-02-12 EP EP18156411.3A patent/EP3360870A1/en not_active Withdrawn
- 2014-02-12 SG SG11201505697VA patent/SG11201505697VA/en unknown
- 2014-02-12 DK DK14708992.4T patent/DK2958907T3/en active
- 2014-02-12 CA CA2899030A patent/CA2899030C/en active Active
- 2014-02-12 AU AU2014219283A patent/AU2014219283C1/en not_active Ceased
- 2014-02-12 GE GEAP201413917A patent/GEP201706638B/en unknown
- 2014-02-12 ME MEP-2018-102A patent/ME03061B/me unknown
- 2014-02-12 SI SI201430679T patent/SI2958907T1/en unknown
- 2014-02-12 US US14/768,341 patent/US9321746B2/en active Active
- 2014-02-12 KR KR1020157025506A patent/KR102279999B1/ko not_active Expired - Fee Related
- 2014-02-12 JP JP2015558090A patent/JP6364028B2/ja active Active
- 2014-02-12 HU HUE14708992A patent/HUE039052T2/hu unknown
- 2014-02-12 MX MX2015010752A patent/MX359471B/es active IP Right Grant
- 2014-02-12 ES ES14708992.4T patent/ES2671516T3/es active Active
- 2014-02-12 NZ NZ710385A patent/NZ710385A/en not_active IP Right Cessation
- 2014-02-12 RS RS20180412A patent/RS57106B1/sr unknown
- 2014-02-12 CU CUP2015000090A patent/CU24337B1/es unknown
- 2014-02-12 PE PE2015001768A patent/PE20151428A1/es unknown
- 2014-02-12 EP EP14708992.4A patent/EP2958907B1/en active Active
- 2014-02-12 EA EA201591537A patent/EA028032B1/ru not_active IP Right Cessation
- 2014-02-12 TR TR2018/06882T patent/TR201806882T4/tr unknown
- 2014-02-18 JO JOP/2014/0038A patent/JO3494B1/ar active
- 2014-02-18 UY UY0001035334A patent/UY35334A/es not_active Application Discontinuation
- 2014-02-18 TW TW103105338A patent/TWI612040B/zh not_active IP Right Cessation
- 2014-02-19 AR ARP140100517A patent/AR094704A1/es unknown
- 2014-10-06 NO NO14795784A patent/NO3077717T3/no unknown
-
2015
- 2015-07-21 ZA ZA2015/05305A patent/ZA201505305B/en unknown
- 2015-07-23 IL IL240131A patent/IL240131B/en active IP Right Grant
- 2015-07-27 CL CL2015002098A patent/CL2015002098A1/es unknown
- 2015-07-31 TN TN2015000323A patent/TN2015000323A1/en unknown
- 2015-08-13 NI NI201500106A patent/NI201500106A/es unknown
- 2015-08-19 PH PH12015501832A patent/PH12015501832B1/en unknown
- 2015-08-19 DO DO2015000202A patent/DOP2015000202A/es unknown
- 2015-08-19 GT GT201500233A patent/GT201500233A/es unknown
- 2015-08-19 CR CR20150424A patent/CR20150424A/es unknown
-
2016
- 2016-03-10 US US15/066,425 patent/US9561211B2/en active Active
-
2017
- 2017-01-05 US US15/399,562 patent/US9931317B2/en active Active
-
2018
- 2018-02-17 US US15/898,561 patent/US10058534B2/en active Active
- 2018-04-27 CY CY20181100447T patent/CY1120155T1/el unknown
- 2018-08-17 HK HK18110605.6A patent/HK1251227A1/en unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR094704A1 (es) | Compuestos y composiciones como degradantes selectivos del receptor de estrógeno | |
| AR129635A2 (es) | Moduladores de tetrahidropiridopirazina de gpr6 | |
| AR113964A1 (es) | Carbamoíl ciclohexil ácidos ligados a n de triazol como antagonistas de lpa | |
| AR119018A1 (es) | Inhibidores de proteína quinasas dependientes de adn | |
| AR114793A1 (es) | Moduladores de enzimas modificadoras de metilo, composiciones y usos de los mismos | |
| AR095311A1 (es) | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante | |
| AR106301A1 (es) | Composiciones de pirrolpirimidina como inhibidores de quinasas | |
| AR104178A1 (es) | Derivados de imidazolilmetilo 5-sustituidos | |
| AR109179A1 (es) | Inhibidores de diacilglicerol aciltransferasa 2 | |
| AR107032A1 (es) | Inhibidores bicíclicos de pad4 | |
| AR103990A1 (es) | Ureas cíclicas como inhibidoras de rock | |
| AR090191A1 (es) | Derivados del acido fenil alcanoico como agonistas gpr | |
| AR109709A1 (es) | Inhibidores de la fosfatidilinositol 3-quinasa | |
| AR100033A1 (es) | Compuestos y composiciones para inhibir la actividad de shp2 | |
| AR099228A1 (es) | Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos | |
| AR100808A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR090760A1 (es) | Compuestos de benzotiazol y su uso contra el virus de hiv | |
| AR098666A1 (es) | Compuestos de biarilacetamida y sus métodos de uso | |
| AR088828A1 (es) | DERIVADOS DE CICLOHEXILAMINA QUE TIENEN ACTIVIDAD COMO AGONISTAS ADRENERGICOS b2 Y COMO ANTAGONISTAS MUSCARINICOS M3 | |
| AR089143A1 (es) | Triazolopiridinas sustituidas con actividad inhibidora de ttk | |
| AR111808A1 (es) | Derivados de pirimidina como moduladores del receptor de pge2 | |
| AR091185A1 (es) | Derivados de 1,2,4-triazol | |
| AR112468A1 (es) | Carboxamidas como inhibidores de proteasa específicos de ubiquitina | |
| AR091781A1 (es) | Antagonistas del receptor de 5-ht3 | |
| AR096152A1 (es) | Derivados de purina |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |