AR077430A1 - Dihidropirrolo[2, 1-alfa]isoquinolina anillada de anillo como activadores de fshr - Google Patents
Dihidropirrolo[2, 1-alfa]isoquinolina anillada de anillo como activadores de fshrInfo
- Publication number
- AR077430A1 AR077430A1 ARP100102726A ARP100102726A AR077430A1 AR 077430 A1 AR077430 A1 AR 077430A1 AR P100102726 A ARP100102726 A AR P100102726A AR P100102726 A ARP100102726 A AR P100102726A AR 077430 A1 AR077430 A1 AR 077430A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- hydroxy
- halogen
- 4alkyl
- Prior art date
Links
- 102100027627 Follicle-stimulating hormone receptor Human genes 0.000 title 1
- 101000862396 Homo sapiens Follicle-stimulating hormone receptor Proteins 0.000 title 1
- 239000012190 activator Substances 0.000 title 1
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical group C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 10
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 4
- 229910052731 fluorine Inorganic materials 0.000 abstract 4
- 239000011737 fluorine Substances 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000004366 heterocycloalkenyl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 abstract 1
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- MVHPKFQBHWGTQH-UHFFFAOYSA-N cyano(nitro)carbamic acid Chemical group OC(=O)N(C#N)[N+]([O-])=O MVHPKFQBHWGTQH-UHFFFAOYSA-N 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- AQYSYJUIMQTRMV-UHFFFAOYSA-N hypofluorous acid Chemical compound FO AQYSYJUIMQTRMV-UHFFFAOYSA-N 0.000 abstract 1
- 208000000509 infertility Diseases 0.000 abstract 1
- 230000036512 infertility Effects 0.000 abstract 1
- 231100000535 infertility Toxicity 0.000 abstract 1
- 125000002183 isoquinolinyl group Chemical class C1(=NC=CC2=CC=CC=C12)* 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Reproductive Health (AREA)
- Pregnancy & Childbirth (AREA)
- Endocrinology (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
El compuesto puede ser usado para el tratamiento de la infertilidad. Reivindicacion 1: Un derivado de dihidropirrolo[2,1-alfa]isoquinolina anillado de anillo de acuerdo con la formula 1 o una sal farmacéuticamente aceptable de él, caracterizado porque R1 es fenilo, heteroarilo C2-5, cicloalquilo C3-6, alquilo C1-6, heterocicloalquilo C2-5 o heterocicloalquenilo C2-5, cada uno opcionalmente sustituidos por uno o más alquilo C1-3 o halogeno; o R1 es halogeno; R2 es H o alquil C1-4; R3 es hidroxilo, alcoxi C1-3; alquiltio C1-3 o alquilo C1-4; R4 es heteroarilo C1-5, heterocicloalquilo C2-5 o heterocicloalquenilo C2-5, cada uno opcionalmente sustituidos por uno o más hidroxi, ciano, halogeno, alcoxi C1-3 o alquilo C1-6, el grupo alquilo opcionalmente sustituido por uno o más hidroxi o fluor; o R4 es halogeno, nitro, ciano, amino, ácido carboxílico o N-hidroxi-imidamida; o R4 es alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6, alcoxi C1-6, alquiltio C1-6, alquilo C1-6C(O)alquilo C1-6, cada uno opcionalmente sustituido por uno o más hidroxi, oxo, ciano o fluor; o R4 es -NH(CO)R6, -NHSO2R6, -NHR6, -C(O)N(R7)R8, -C(O)OR6, -S(O)R6 o -SO2R6; R5 es H o halogeno; R6 es alquilo C1-6, alquenilo C2-6 o heteroarilo C2-5, cada uno opcionalmente sustituido por uno o más alquilo C1-3, alcoxi C1-3, hidroxi o halogeno; o R6 es (di)[alquil C1-4]aminoalquilo C1-4, (di)[alquil C1-4]aminoC(O)alquilo C1-4 o heterocicloalquilalquilo C2-5 alquilo C1-4, el grupo heterocicloalquilo opcionalmente sustituido por uno o más alquil C1-4, oxo, hidroxi, fluor o (di)[alquil C1-4]amino-alquilo C1-4; Y es un enlace, Y es (CH2)n o Y es X(CH2)m, donde uno o más de los átomos de hidrogeno en los grupos (CH2)n o (CH2)m en Y pueden estar opcionalmente sustituidos por alquilo C1-3, fluor o hidroxi; X es O, S o NR9; R7 es H o alquilo C1-6, opcionalmente sustituido por uno o más grupos hidroxilo; R8 es H, o alquilo C1-6, alquenilo C1-6 o heteroarilo C2-5, cada uno opcionalmente sustituido por uno o más alquilo C1-3, alcoxi C1-3, hidroxi o halogeno; o R8 es heterocicloalquil C2-5 alquilo C1-4, el grupo heterocicloalquilo opcionalmente sustituido por alquilo C1-4 o (di)[alquil C1-4]amino-alquil C1-4; o R7 y R8 pueden formar, junto con el nitrogeno interconector, un grupo heterocicloalquilo C2-5, opcionalmente sustituido por hidroxi, alcoxicarbonilo C1-6 o alquilo C1-6, el grupo alquilo opcionalmente sustituido por uno o más hidroxi o fluor; R9 es hidrogeno o R10-carbonilo; R10 es alquilo C1-3, opcionalmente sustituido por halogeno; n es 0-4; m es 2 o 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09166740 | 2009-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077430A1 true AR077430A1 (es) | 2011-08-24 |
Family
ID=41066233
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102726A AR077430A1 (es) | 2009-07-29 | 2010-07-28 | Dihidropirrolo[2, 1-alfa]isoquinolina anillada de anillo como activadores de fshr |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP2459560B1 (es) |
| JP (1) | JP5723364B2 (es) |
| AR (1) | AR077430A1 (es) |
| AU (1) | AU2010277620B2 (es) |
| CA (1) | CA2769056A1 (es) |
| ES (1) | ES2548389T3 (es) |
| TW (1) | TW201116531A (es) |
| WO (1) | WO2011012600A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106967076A (zh) * | 2017-03-30 | 2017-07-21 | 河南师范大学 | 一种具有6h‑二苯并吡喃结构化合物及其制备方法 |
| CN106977523A (zh) * | 2017-03-30 | 2017-07-25 | 河南师范大学 | 具有苯基并四氢吡咯结构的fshr拮抗剂及其制备方法 |
| EP3728277B1 (de) | 2017-12-19 | 2022-11-23 | Wacker Chemie AG | Oxamidoester-gruppen aufweisende silane |
| TW202435866A (zh) | 2023-03-08 | 2024-09-16 | 荷蘭商菲林公司 | 小分子ｆｓｈ受體調節劑 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU212427B (en) | 1991-12-19 | 1996-06-28 | Gyogyszerkutato Intezet | Process for producing dl-, d- and l-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acids and their derivatives containing urethane-type n-protecting groups |
| IL141063A (en) | 1998-08-07 | 2005-06-19 | Applied Research Systems | Derivatives of pyrrolidine-2-carboxylic acid and piperidine-2-carboxylic acids and pharmaceutical compositions comprising said derivatives for treating infertility |
| WO2002009706A1 (en) | 2000-07-27 | 2002-02-07 | Smithkline Beecham Corporation | Agonists of follicle stimulating hormone activity |
| JP4523273B2 (ja) | 2001-07-02 | 2010-08-11 | ナームローゼ・フエンノートチヤツプ・オルガノン | テトラヒドロキノリン誘導体 |
| GB0218816D0 (en) * | 2002-08-13 | 2002-09-18 | Pharma Mar Sa | Antitumoral analogs of lamellarins |
| ES2399047T3 (es) | 2002-09-20 | 2013-03-25 | Merck Serono Sa | Derivados de piperazina y procedimiento de uso |
| TWI306855B (en) * | 2002-12-20 | 2009-03-01 | Organon Nv | Tetrahydroquinoline derivatives |
| WO2005087765A1 (en) | 2004-03-04 | 2005-09-22 | Arena Pharmaceuticals, Inc. | Ligands of follicle stimulating hormone receptor and methods of use thereof |
| UA92009C2 (ru) | 2005-05-04 | 2010-09-27 | Н.В. Органон | Производные 4-фенил-5-оксо-1,4,5,6,7,8-гексагидрохинолина для лечения бесплодия |
| CA2606521C (en) | 2005-05-04 | 2012-09-18 | N.V. Organon | Dihydropyridine derivatives |
| UA92007C2 (ru) | 2005-05-04 | 2010-09-27 | Н.В. Органон | Производные 4-фенил-5-оксо-1,4,5,6,7,8-гексагидрохинолина для лечения бесплодности |
| UA92008C2 (en) | 2005-05-04 | 2010-09-27 | Н.В. Органон | 4-PHENYL-5-OXO-l,4,5,6,7,8-HEXAHYDROQUINOLINE DERIVATIVES AS MEDICAMENTS FOR THE TREATMENT OF INFERTILITY |
-
2010
- 2010-07-16 TW TW099123483A patent/TW201116531A/zh unknown
- 2010-07-27 CA CA2769056A patent/CA2769056A1/en not_active Abandoned
- 2010-07-27 JP JP2012522143A patent/JP5723364B2/ja not_active Expired - Fee Related
- 2010-07-27 EP EP10737883.8A patent/EP2459560B1/en not_active Not-in-force
- 2010-07-27 ES ES10737883.8T patent/ES2548389T3/es active Active
- 2010-07-27 WO PCT/EP2010/060847 patent/WO2011012600A1/en not_active Ceased
- 2010-07-27 AU AU2010277620A patent/AU2010277620B2/en not_active Ceased
- 2010-07-28 AR ARP100102726A patent/AR077430A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP2459560A1 (en) | 2012-06-06 |
| CA2769056A1 (en) | 2011-02-03 |
| TW201116531A (en) | 2011-05-16 |
| EP2459560B1 (en) | 2015-08-19 |
| AU2010277620A8 (en) | 2012-01-19 |
| AU2010277620A1 (en) | 2012-01-12 |
| JP2013500307A (ja) | 2013-01-07 |
| JP5723364B2 (ja) | 2015-05-27 |
| WO2011012600A1 (en) | 2011-02-03 |
| ES2548389T3 (es) | 2015-10-16 |
| AU2010277620B2 (en) | 2014-09-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |