CA2398018C - Gonadotropin-releasing hormone receptor antagonists and methods relating thereto - Google Patents
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto Download PDFInfo
- Publication number
- CA2398018C CA2398018C CA2398018A CA2398018A CA2398018C CA 2398018 C CA2398018 C CA 2398018C CA 2398018 A CA2398018 A CA 2398018A CA 2398018 A CA2398018 A CA 2398018A CA 2398018 C CA2398018 C CA 2398018C
- Authority
- CA
- Canada
- Prior art keywords
- compound
- 4alkyl
- ome
- substituted
- halogen
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/60—Three or more oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
- A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
- C07D409/04—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
- C07D409/06—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 only aliphatic carbon atoms
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D417/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D491/08—Bridged systems
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/08—Bridged 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
- C07D513/02—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 two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Immunology (AREA)
- Gynecology & Obstetrics (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Anesthesiology (AREA)
- Pregnancy & Childbirth (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17793300P | 2000-01-25 | 2000-01-25 | |
| US60/177,933 | 2000-01-25 | ||
| US23968300P | 2000-10-11 | 2000-10-11 | |
| US60/239,683 | 2000-10-11 | ||
| PCT/US2001/002740 WO2001055119A2 (en) | 2000-01-25 | 2001-01-25 | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2398018A1 CA2398018A1 (en) | 2001-08-02 |
| CA2398018C true CA2398018C (en) | 2011-10-18 |
Family
ID=26873790
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2398018A Expired - Fee Related CA2398018C (en) | 2000-01-25 | 2001-01-25 | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
Country Status (14)
| Country | Link |
|---|---|
| US (4) | US6608197B2 (https=) |
| EP (1) | EP1255738B1 (https=) |
| JP (1) | JP4931314B2 (https=) |
| KR (1) | KR100814269B1 (https=) |
| AT (1) | ATE548357T1 (https=) |
| AU (1) | AU767585B2 (https=) |
| CA (1) | CA2398018C (https=) |
| CY (1) | CY1112815T1 (https=) |
| DK (1) | DK1255738T3 (https=) |
| ES (1) | ES2383954T3 (https=) |
| MX (1) | MXPA02006848A (https=) |
| NO (1) | NO20023525L (https=) |
| PT (1) | PT1255738E (https=) |
| WO (1) | WO2001055119A2 (https=) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1255738E (pt) * | 2000-01-25 | 2012-06-19 | Neurocrine Biosciences Inc | Antagonistas do receptor da hormona de libertação da gonadotrofina e métodos relacionados com os mesmos |
| SE0100567D0 (sv) * | 2001-02-20 | 2001-02-20 | Astrazeneca Ab | Compounds |
| WO2003011293A2 (en) * | 2001-08-02 | 2003-02-13 | Neurocrine Biosciences, Inc. | Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists |
| JP2005505525A (ja) | 2001-08-02 | 2005-02-24 | ニューロクライン バイオサイエンシーズ, インコーポレイテッド | 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法 |
| EP1495768A4 (en) * | 2002-04-12 | 2007-12-05 | Takeda Pharmaceutical | MEANS FOR THE PREVENTION / TREATMENT OF HITZEWALLUNGEN |
| US7015226B2 (en) | 2003-07-07 | 2006-03-21 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
| CN100424078C (zh) * | 2003-07-07 | 2008-10-08 | 纽罗克里生物科学有限公司 | 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物 |
| ATE428427T1 (de) * | 2003-07-07 | 2009-05-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| KR20060041309A (ko) | 2003-08-13 | 2006-05-11 | 다케다 야쿠힌 고교 가부시키가이샤 | 4-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도 |
| CN102127057A (zh) * | 2004-03-15 | 2011-07-20 | 武田药品工业株式会社 | 二肽基肽酶抑制剂 |
| WO2005113516A1 (en) * | 2004-05-14 | 2005-12-01 | Neurocrine Biosciences, Inc. | Uracil-type gonadotropin-releasing hormone receptor antagonists and methods related thereto |
| EP1655288A1 (en) * | 2004-11-05 | 2006-05-10 | Institut Pasteur | Aryl pyrimidyl compounds, pharmaceutical compositions comprising them, their use as antimicrobial agents |
| GEP20135838B (en) | 2005-09-14 | 2013-06-10 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors usage at diabetes treatment |
| CN101360723A (zh) | 2005-09-16 | 2009-02-04 | 武田药品工业株式会社 | 制备嘧啶二酮衍生物的方法 |
| WO2007122634A2 (en) * | 2006-04-24 | 2007-11-01 | Jubilant Biosys Limited | Pyrimidinediones as tyrosine kinase inhibitors |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| PE20090044A1 (es) | 2007-04-06 | 2009-01-23 | Neurocrine Biosciences Inc | Antagonistas del receptor de la hormona liberadora de gonadotropina y procedimientos relacionados con los mismos |
| CL2008000986A1 (es) | 2007-04-06 | 2008-10-17 | Neurocrine Biosciences Inc | COMPUESTO DERIVADO DE HETEROCICLOS DE NITROGENO, AGONISTAS DEL RECEPTOR GnRH; COMPOSICION FARMACEUTICA QUE COMPRENDE A DICHO COMPUESTO; Y USO PARA TRATAR UNA AFECCION RELACIONADA CON LAS HORMONAS SEXUALES, ENDOMETRIOSIS, DISMENORREA, ENFERMEDAD DE OV |
| EP2147922B1 (en) * | 2007-04-18 | 2017-08-02 | Kissei Pharmaceutical Co., Ltd. | Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes |
| WO2008133128A1 (ja) * | 2007-04-18 | 2008-11-06 | Kissei Pharmaceutical Co., Ltd. | 縮合複素環誘導体、それを含有する医薬組成物及びその医薬用途 |
| US8765948B2 (en) * | 2007-11-07 | 2014-07-01 | Neurocrine Biosciences, Inc. | Processes for the preparation of uracil derivatives |
| DE102008030091B4 (de) * | 2008-06-25 | 2011-03-03 | Resprotect Gmbh | Uracilderivate und deren Verwendung |
| CA2736970A1 (en) * | 2008-09-12 | 2010-03-18 | Biolipox Ab | Pyrimidinone derivatives for use as medicaments |
| US9034850B2 (en) | 2009-11-20 | 2015-05-19 | Sk Chemicals Co., Ltd. | Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same |
| TW201130854A (en) | 2009-12-22 | 2011-09-16 | Bayer Schering Pharma Ag | Pyridinone derivatives and pharmaceutical compositions thereof |
| WO2012175514A1 (en) | 2011-06-21 | 2012-12-27 | Bayer Intellectual Property Gmbh | Pyridinone derivatives and pharmaceutical compositions thereof |
| US10881659B2 (en) | 2013-03-15 | 2021-01-05 | Abbvie Inc. | Methods of treating heavy menstrual bleeding |
| EP3600318A4 (en) * | 2017-03-31 | 2021-06-09 | Epizyme, Inc. | METHOD OF USING EHMT2 INHIBITORS |
| CN110621316B (zh) | 2017-04-21 | 2024-01-26 | Epizyme股份有限公司 | 用ehmt2抑制剂进行的组合疗法 |
| US20190054088A1 (en) | 2017-08-18 | 2019-02-21 | Abbvie Inc. | Pharmaceutical Formulations for Treating Endometriosis, Uterine Fibroids, Polycystic Ovary Syndrome or Adenomyosis |
| MX2020001877A (es) | 2017-08-18 | 2020-09-14 | Abbvie Inc | Formulaciones farmacéuticas para tratar la endometriosis, los fibromas uterinos, el síndrome de ovario poliquístico o la adenomiosis. |
| US12083227B2 (en) | 2017-08-18 | 2024-09-10 | Abbvie Inc. | Solid pharmaceutical formulations for treating endometriosis, uterine fibroids, polycystic ovary syndrome or adenomyosis |
| CN112261942A (zh) | 2018-04-19 | 2021-01-22 | 艾伯维公司 | 治疗重度月经出血的方法 |
| EP3826638A4 (en) | 2018-07-23 | 2022-04-06 | Abbvie Inc. | ELAGOLIX SODIUM COMPOSITIONS AND RELATED METHODS |
| PH12021551685A1 (en) | 2019-01-15 | 2022-05-16 | Lupin Inc | Deuterated elagolix-like compositions and methods |
| CN111333586A (zh) * | 2020-02-19 | 2020-06-26 | 诚达药业股份有限公司 | 一种含有6-甲基尿嘧啶结构化合物的制备方法 |
| CN111333587B (zh) * | 2020-04-11 | 2023-04-07 | 东莞市东阳光新药研发有限公司 | 取代的嘧啶-2,4(1h,3h)-二酮衍生物及其用途 |
| CN113527213B (zh) * | 2020-04-20 | 2023-01-03 | 上海英诺富成生物科技有限公司 | 促性激素释放激素受体拮抗剂及其用途 |
| CN117820248A (zh) * | 2021-04-14 | 2024-04-05 | 盐野义制药株式会社 | 具有病毒增殖抑制作用的三嗪衍生物及含有其的药物组合物 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2631625B1 (fr) * | 1988-05-17 | 1992-10-16 | Synthelabo | Derives de phenyl-6 piperazinylalkyl-3 1h,3h-pyrimidinedione-2,4, leur preparation et leur application en therapeutique |
| US5140029A (en) | 1989-01-09 | 1992-08-18 | Janssen Pharmaceutica N.V. | 2-aminopyrimidinone derivatives |
| US5476855A (en) * | 1993-11-02 | 1995-12-19 | Mahmoud H. el Kouni | Enzyme inhibitors, their synthesis and methods for use |
| UY23948A1 (es) | 1995-02-08 | 2001-10-25 | Takeda Chemical Industries Ltd | Derivados de anillos condensados de tiofeno su producción y uso. |
| AU5844896A (en) | 1995-06-01 | 1996-12-18 | Takeda Chemical Industries Ltd. | Tricyclic diazepines useful as gnrh receptor antagonists |
| DK0748800T3 (da) * | 1995-06-09 | 2001-08-27 | Hoffmann La Roche | Pyrimidindion-, pyrimidintrion- og triazindionderivater som alfa-1-adrenergiske receptorantagonister |
| US5859014A (en) | 1995-06-09 | 1999-01-12 | Syntex (U.S.A.) Inc. | Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as α1 -adrenergic receptor antagonists |
| CA2229201A1 (en) | 1995-10-19 | 1997-04-24 | Satoshi Sasaki | Quinoline derivatives, their production and use |
| EP0862573A1 (en) | 1995-10-19 | 1998-09-09 | Takeda Chemical Industries, Ltd. | Thienopyridine derivatives as gonadotropin releasing hormone antagonists |
| PL327146A1 (en) | 1995-12-14 | 1998-11-23 | Merck & Co Inc | Antagonists of the gonadotrophin liberating hormone |
| US5780437A (en) | 1995-12-14 | 1998-07-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| SK77498A3 (en) | 1995-12-14 | 1999-01-11 | Merck & Co Inc | Nonpeptide derivatives, pharmaceutical composition containing them and their use |
| CA2240048A1 (en) | 1995-12-14 | 1997-06-19 | Mark Goulet | Antagonists of gonadotropin releasing hormone |
| CA2240115A1 (en) | 1995-12-14 | 1997-06-19 | Wallace T. Ashton | Antagonists of gonadotropin releasing hormone |
| US5849764A (en) | 1995-12-14 | 1998-12-15 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| JPH09286786A (ja) * | 1996-04-18 | 1997-11-04 | Nippon Paper Ind Co Ltd | ピリミジン誘導体及びその抗腫瘍剤としての用途 |
| WO1997044321A1 (en) | 1996-05-20 | 1997-11-27 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| CA2254974A1 (en) | 1996-05-20 | 1997-11-27 | Mark Goulet | Antagonists of gonadotropin releasing hormone |
| CA2254756A1 (en) | 1996-05-20 | 1997-11-27 | Mark Goulet | Antagonists of gonadotropin releasing hormone |
| US6150352A (en) | 1996-05-20 | 2000-11-21 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU729663B2 (en) | 1997-06-05 | 2001-02-08 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU7806998A (en) | 1997-06-05 | 1998-12-21 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| CA2292881A1 (en) | 1997-06-05 | 1998-12-10 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| WO1998055470A1 (en) | 1997-06-05 | 1998-12-10 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| US6313301B1 (en) | 1997-08-13 | 2001-11-06 | Takeda Chemical Industries, Ltd. | Thienopyridine derivatives, their intermediates and production thereof |
| US6194419B1 (en) | 1997-12-26 | 2001-02-27 | Takeda Chemical Industries, Ltd. | Nitrogen-containing heterocyclic compounds, their production and use |
| WO1999051232A1 (en) | 1998-04-02 | 1999-10-14 | Merck & Co., Inc. | Antagonists of gonadotropin releasing hormone |
| AU1345600A (en) * | 1998-11-12 | 2000-06-05 | Merck & Co., Inc. | Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists |
| CA2372044A1 (en) | 1999-05-14 | 2000-11-23 | Neurocrine Biosciences, Inc. | Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists |
| KR20010113969A (ko) | 1999-05-19 | 2001-12-28 | 추후보정 | 항응고제로서의 치환된 폴리시클릭 아릴 및 헤테로아릴우라실 |
| ES1043085Y (es) * | 1999-06-03 | 2001-02-01 | Nueva Ceramica Arb Sa | Teja planoconvexa |
| DE60022769T2 (de) | 1999-10-15 | 2006-07-06 | Neurocrine Biosciences, Inc., San Diego | Gonadotropin freisetzenden hormon rezeptor antagonisten und ihre verwandten verwendungen |
| PT1255738E (pt) * | 2000-01-25 | 2012-06-19 | Neurocrine Biosciences Inc | Antagonistas do receptor da hormona de libertação da gonadotrofina e métodos relacionados com os mesmos |
| CN100424078C (zh) * | 2003-07-07 | 2008-10-08 | 纽罗克里生物科学有限公司 | 作为促性激素释放激素受体拮抗剂的嘧啶-2,4-二酮衍生物 |
| ATE428427T1 (de) * | 2003-07-07 | 2009-05-15 | Neurocrine Biosciences Inc | Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten |
| US7015226B2 (en) * | 2003-07-07 | 2006-03-21 | Neurocrine Biosciences, Inc. | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto |
-
2001
- 2001-01-25 PT PT01910362T patent/PT1255738E/pt unknown
- 2001-01-25 MX MXPA02006848A patent/MXPA02006848A/es active IP Right Grant
- 2001-01-25 JP JP2001555061A patent/JP4931314B2/ja not_active Expired - Lifetime
- 2001-01-25 KR KR1020027009582A patent/KR100814269B1/ko not_active Expired - Lifetime
- 2001-01-25 WO PCT/US2001/002740 patent/WO2001055119A2/en not_active Ceased
- 2001-01-25 AU AU37975/01A patent/AU767585B2/en not_active Expired
- 2001-01-25 EP EP01910362A patent/EP1255738B1/en not_active Expired - Lifetime
- 2001-01-25 US US09/771,107 patent/US6608197B2/en not_active Expired - Lifetime
- 2001-01-25 ES ES01910362T patent/ES2383954T3/es not_active Expired - Lifetime
- 2001-01-25 AT AT01910362T patent/ATE548357T1/de active
- 2001-01-25 CA CA2398018A patent/CA2398018C/en not_active Expired - Fee Related
- 2001-01-25 DK DK01910362.1T patent/DK1255738T3/da active
-
2002
- 2002-07-24 NO NO20023525A patent/NO20023525L/no not_active Application Discontinuation
-
2003
- 2003-02-06 US US10/361,144 patent/US6872728B2/en not_active Expired - Lifetime
-
2004
- 2004-12-17 US US11/016,551 patent/US7179815B2/en not_active Expired - Lifetime
-
2006
- 2006-09-11 US US11/520,022 patent/US7462625B2/en not_active Expired - Lifetime
-
2012
- 2012-06-01 CY CY20121100499T patent/CY1112815T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US6872728B2 (en) | 2005-03-29 |
| CA2398018A1 (en) | 2001-08-02 |
| ES2383954T3 (es) | 2012-06-27 |
| AU767585B2 (en) | 2003-11-20 |
| US20070208049A1 (en) | 2007-09-06 |
| WO2001055119A2 (en) | 2001-08-02 |
| JP4931314B2 (ja) | 2012-05-16 |
| US6608197B2 (en) | 2003-08-19 |
| JP2003520856A (ja) | 2003-07-08 |
| US7179815B2 (en) | 2007-02-20 |
| WO2001055119A3 (en) | 2002-02-14 |
| US7462625B2 (en) | 2008-12-09 |
| US20040048884A1 (en) | 2004-03-11 |
| NO20023525D0 (no) | 2002-07-24 |
| CY1112815T1 (el) | 2016-02-10 |
| KR100814269B1 (ko) | 2008-03-18 |
| HK1051042A1 (en) | 2003-07-18 |
| ATE548357T1 (de) | 2012-03-15 |
| US20050234082A1 (en) | 2005-10-20 |
| US20020132820A1 (en) | 2002-09-19 |
| AU3797501A (en) | 2001-08-07 |
| EP1255738A2 (en) | 2002-11-13 |
| MXPA02006848A (es) | 2002-12-13 |
| NO20023525L (no) | 2002-07-24 |
| KR20030012846A (ko) | 2003-02-12 |
| PT1255738E (pt) | 2012-06-19 |
| DK1255738T3 (da) | 2012-06-25 |
| EP1255738B1 (en) | 2012-03-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2398018C (en) | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto | |
| IL172833A (en) | Pyrimidine-2,4-dione derivatives and pharmaceutical compositions containing the same | |
| EP1220857B1 (en) | Gonadotropin releasing hormone receptor antagonists and their related methods of use | |
| EP1644342B1 (en) | Arylpyrimidines useful for the treatment of sex hormone-related conditions such as endometriosis, prostate cancer and the like | |
| CA2372044A1 (en) | Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists | |
| EP1414808A1 (en) | 1,2,4-triazin-3,5-diones as gonadotropin-releasing hormone receptor (gnrh) antagonists | |
| US6740656B2 (en) | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto | |
| AU2004200664B2 (en) | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto | |
| HK1051042B (en) | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto | |
| US6537998B1 (en) | Gonadotropin-releasing hormone receptor antagonists and methods relating thereto | |
| AU2002321864A1 (en) | 1,2,4-triazin-3,5-diones as gonadotropin-releasing hormone receptor (GNRH) antagonists |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20200127 |