AR040783A1 - 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona - Google Patents
5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesteronaInfo
- Publication number
- AR040783A1 AR040783A1 AR20030102796A ARP030102796A AR040783A1 AR 040783 A1 AR040783 A1 AR 040783A1 AR 20030102796 A AR20030102796 A AR 20030102796A AR P030102796 A ARP030102796 A AR P030102796A AR 040783 A1 AR040783 A1 AR 040783A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- haloalkyl
- alkyl
- hydrogen
- heteroalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 102000003998 progesterone receptors Human genes 0.000 title abstract 2
- 108090000468 progesterone receptors Proteins 0.000 title abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 4
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 4
- 101100134922 Gallus gallus COR5 gene Proteins 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 1
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 abstract 1
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 abstract 1
- -1 C1- heteroalkyl 8 Chemical group 0.000 abstract 1
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/34—Gestagens
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/74—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
- G01N33/743—Steroid hormones
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Food Science & Technology (AREA)
- Analytical Chemistry (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physics & Mathematics (AREA)
- Cell Biology (AREA)
- Biochemistry (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Rheumatology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente se refiere a compuestos, composiciones farmacéuticas y métodos para modular procesos mediados por el receptor de la progesterona. También se proveen métodos para preparar tales compuestos y composiciones farmacéuticas. Reivindicación 1: Un compuesto de la fórmula (1) donde: R1 está seleccionado del grupo integrado por hidrógeno, alquilo C1-4, haloalquilo C1-4, heteroalquilo C1-4, COR5, CO2R5, SO2R5, y CONR5R6; R2 y R3 está seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, alquilo C1-6 y haloalquilo C1-6; o R2 y R3 forman juntos un anillo cicloalquilo de C3-12; R4 está seleccionado del grupo integrado por hidrógeno, F, Cl, Br, CN, OR5, alquilo C1-4, haloalquilo C1-4 y heteroalquilo C1-4; R5 y R6 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, alquilo C1-4, heteroalquilo C1-4 y haloalquilo C1-4; R7 a R9 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, F, Cl, Br, I, NO2, CN, OR5, NR5R6, SR5, COR5, CO2R5, CONR5R6, alquilo C1-8, heteroalquilo C1-8, haloalquilo C1-8, alquenilo C2-8 y alquinilo C2-8; R10 a R15 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, F, Cl, Br, OR5, alquilo C1-4, haloalquilo C1-4 y heteroalquilo C1-4; o R12 y R14 forman juntos un enlace, cuando Y es CR14R15; o eR12 y R14 forman juntos un enlace, cuando Z es CR14R15;Y y Z están seleccionados cada uno, de modo independiente, del grupo integrado por O, S, NR6 y CR14R15; n es 0, 1, 2 ó 3; o una sal o prodroga del mismos de aceptación farmacéutica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41814002P | 2002-10-11 | 2002-10-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040783A1 true AR040783A1 (es) | 2005-04-20 |
Family
ID=32094152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AR20030102796A AR040783A1 (es) | 2002-10-11 | 2003-08-04 | 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7084151B2 (es) |
| EP (1) | EP1558618A1 (es) |
| JP (1) | JP2006504736A (es) |
| AR (1) | AR040783A1 (es) |
| AU (1) | AU2003258047A1 (es) |
| CA (1) | CA2501833A1 (es) |
| MX (1) | MXPA05003800A (es) |
| WO (1) | WO2004033459A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6566372B1 (en) | 1999-08-27 | 2003-05-20 | Ligand Pharmaceuticals Incorporated | Bicyclic androgen and progesterone receptor modulator compounds and methods |
| US7026484B2 (en) * | 2001-02-23 | 2006-04-11 | Ligand Pharmaceuticals Incorporated | Tricyclic androgen receptor modulator compounds and methods |
| DE20301728U1 (de) | 2002-10-11 | 2004-03-11 | Ligand Pharmaceuticals, Inc., San Diego | 5-substituierte 7,9-Difluor-5H-Chromeno(3,4-f) -Chinolin-Verbindungen als selektive Progesteronrezeptormodulator-Verbindungen |
| CA2501833A1 (en) | 2002-10-11 | 2004-04-22 | Ligand Pharmaceuticals Incorporated | 5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5h-chromeno[3,4-f]quinolines as selective progesterone receptor modulator compounds |
| AU2003258050A1 (en) * | 2002-10-11 | 2004-05-04 | Ligand Pharmaceuticals Incorporated | 5-cycloalkenyl 5h-chromeno(3,4-f)quinoline derivatives as selective progesterone receptor modulator compounds |
| MXPA06001751A (es) * | 2003-08-22 | 2006-05-12 | Ligand Pharm Inc | Derivados de 6-cicloamino-2-quinolinona como compuestos moduladores de receptor de androgeno. |
| EP2422800A3 (en) | 2006-03-07 | 2013-03-06 | Geeta Shroff | Compositions comprising human embryonic stem cells and their derivatives, methods of use, and methods of preparation |
| CA2710293A1 (en) * | 2007-12-20 | 2009-07-02 | Teva Women's Health, Inc. | Dosage regimens and pharmaceutical compositions and packages for emergency contraception |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5808139A (en) | 1992-04-21 | 1998-09-15 | Ligand Pharmaceuticals Incorporated | Non-steroid progesterone receptor agonist and antagonist and compounds and methods |
| US5506102A (en) | 1993-10-28 | 1996-04-09 | Ligand Pharmaceuticals Incorporated | Methods of using the A form of the progesterone receptor to screen for antagonists of steroid intracellar receptor-mediated transcription |
| US5688810A (en) | 1994-12-22 | 1997-11-18 | Ligand Pharmaceuticals Incorporated | Steroid receptor modulator compounds and methods |
| US6696459B1 (en) | 1994-12-22 | 2004-02-24 | Ligand Pharmaceuticals Inc. | Steroid receptor modulator compounds and methods |
| NZ300739A (en) * | 1994-12-22 | 2000-05-26 | Ligand Pharm Inc | Steroid receptor modulator compounds |
| JPH11209735A (ja) * | 1998-01-28 | 1999-08-03 | Dow Corning Toray Silicone Co Ltd | フイルム状シリコーンゴム接着剤及び接着方法 |
| US6506766B1 (en) | 1998-02-13 | 2003-01-14 | Abbott Laboratories | Glucocortiocoid-selective antinflammatory agents |
| US6380207B2 (en) | 1998-02-13 | 2002-04-30 | Abbott Laboratories | Glucocortiocoid-selective antiinflammatory agents |
| TR200003094T2 (tr) * | 1998-02-13 | 2001-01-22 | Abbott Laboratories | Glukokortikoid-seçimli enflamasyon önleyici maddeler. |
| US6001846A (en) | 1998-02-17 | 1999-12-14 | Ligand Pharmaceuticals Incorporated | Process for the preparation of 1,2-dihydroquinolines |
| US6093825A (en) | 1998-05-27 | 2000-07-25 | American Home Products | Methods for preparation of 1,2-dihydroquinolines |
| US6093826A (en) | 1998-06-08 | 2000-07-25 | Ligand Pharmaceuticals Incorporated | Process for the preparation of C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-f] quinolines |
| US6417214B1 (en) | 1999-05-04 | 2002-07-09 | Wyeth | 3,3-substituted indoline derivatives |
| US6355648B1 (en) | 1999-05-04 | 2002-03-12 | American Home Products Corporation | Thio-oxindole derivatives |
| US6329416B1 (en) | 1999-05-04 | 2001-12-11 | American Home Products Corporation | Combination regimens using 3,3-substituted indoline derivatives |
| US6358947B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Tetracyclic progesterone receptor modulator compounds and methods |
| AU4980100A (en) | 1999-05-04 | 2000-11-17 | American Home Products Corporation | Compositions containing benzimidazolones and progestogens |
| WO2000066560A1 (en) | 1999-05-04 | 2000-11-09 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| WO2000066592A1 (en) | 1999-05-04 | 2000-11-09 | American Home Products Corporation | Cyclic urea and cyclic amide derivatives |
| US6339098B1 (en) | 1999-05-04 | 2002-01-15 | American Home Products Corporation | 2,1-benzisothiazoline 2,2-dioxides |
| US6306851B1 (en) | 1999-05-04 | 2001-10-23 | American Home Products Corporation | Cyclocarbamate and cyclic amide derivatives |
| US6462032B1 (en) | 1999-05-04 | 2002-10-08 | Wyeth | Cyclic regimens utilizing indoline derivatives |
| US6380235B1 (en) | 1999-05-04 | 2002-04-30 | American Home Products Corporation | Benzimidazolones and analogues |
| US6358948B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| US6369056B1 (en) | 1999-05-04 | 2002-04-09 | American Home Products Corporation | Cyclic urea and cyclic amide derivatives |
| AU4501800A (en) | 1999-05-04 | 2000-11-17 | American Home Products Corporation | Tetracyclic progesterone receptor modulator compounds and methods |
| EP1173210B1 (en) | 1999-05-04 | 2004-09-15 | Wyeth | Contraceptive compositions containing antiprogestinic and progestinic |
| US6407101B1 (en) | 1999-05-04 | 2002-06-18 | American Home Products Corporation | Cyanopyrroles |
| US6391907B1 (en) | 1999-05-04 | 2002-05-21 | American Home Products Corporation | Indoline derivatives |
| US6423699B1 (en) | 1999-05-04 | 2002-07-23 | American Home Products Corporation | Combination therapies using benzimidazolones |
| US6319912B1 (en) | 1999-05-04 | 2001-11-20 | American Home Products Corporation | Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides |
| US6498154B1 (en) | 1999-05-04 | 2002-12-24 | Wyeth | Cyclic regimens using quinazolinone and benzoxazine derivatives |
| US6444668B1 (en) | 1999-05-04 | 2002-09-03 | Wyeth | Combination regimens using progesterone receptor modulators |
| US6509334B1 (en) | 1999-05-04 | 2003-01-21 | American Home Products Corporation | Cyclocarbamate derivatives as progesterone receptor modulators |
| US6380178B1 (en) | 1999-05-04 | 2002-04-30 | American Home Products Corporation | Cyclic regimens using cyclocarbamate and cyclic amide derivatives |
| US6399593B1 (en) | 1999-05-04 | 2002-06-04 | Wyeth | Cyclic regimens using cyclic urea and cyclic amide derivatives |
| US6566372B1 (en) | 1999-08-27 | 2003-05-20 | Ligand Pharmaceuticals Incorporated | Bicyclic androgen and progesterone receptor modulator compounds and methods |
| US6172241B1 (en) | 1999-10-15 | 2001-01-09 | Ligand Pharmaceuticals Incorporated | Process for the preparation of 1,2-dihydroquinolines |
| UA73119C2 (en) | 2000-04-19 | 2005-06-15 | American Home Products Corpoir | Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors |
| CA2501833A1 (en) * | 2002-10-11 | 2004-04-22 | Ligand Pharmaceuticals Incorporated | 5-(1',1'-cycloalkyl/alkenyl)methylidene 1,2-dihydro-5h-chromeno[3,4-f]quinolines as selective progesterone receptor modulator compounds |
| AU2003258050A1 (en) | 2002-10-11 | 2004-05-04 | Ligand Pharmaceuticals Incorporated | 5-cycloalkenyl 5h-chromeno(3,4-f)quinoline derivatives as selective progesterone receptor modulator compounds |
| DE20301728U1 (de) | 2002-10-11 | 2004-03-11 | Ligand Pharmaceuticals, Inc., San Diego | 5-substituierte 7,9-Difluor-5H-Chromeno(3,4-f) -Chinolin-Verbindungen als selektive Progesteronrezeptormodulator-Verbindungen |
-
2003
- 2003-08-04 CA CA002501833A patent/CA2501833A1/en not_active Abandoned
- 2003-08-04 WO PCT/US2003/024416 patent/WO2004033459A1/en not_active Ceased
- 2003-08-04 JP JP2004543231A patent/JP2006504736A/ja active Pending
- 2003-08-04 AR AR20030102796A patent/AR040783A1/es not_active Application Discontinuation
- 2003-08-04 EP EP03808050A patent/EP1558618A1/en not_active Withdrawn
- 2003-08-04 MX MXPA05003800A patent/MXPA05003800A/es unknown
- 2003-08-04 AU AU2003258047A patent/AU2003258047A1/en not_active Abandoned
- 2003-10-10 US US10/684,227 patent/US7084151B2/en not_active Expired - Lifetime
-
2006
- 2006-06-02 US US11/445,844 patent/US20060223839A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004033459A1 (en) | 2004-04-22 |
| US7084151B2 (en) | 2006-08-01 |
| JP2006504736A (ja) | 2006-02-09 |
| AU2003258047A1 (en) | 2004-05-04 |
| EP1558618A1 (en) | 2005-08-03 |
| US20060223839A1 (en) | 2006-10-05 |
| US20040147530A1 (en) | 2004-07-29 |
| MXPA05003800A (es) | 2005-06-08 |
| CA2501833A1 (en) | 2004-04-22 |
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Legal Events
| Date | Code | Title | Description |
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| FA | Abandonment or withdrawal |