ZA200407667B - Non-steroidal progesterone receptor modulators - Google Patents
Non-steroidal progesterone receptor modulators Download PDFInfo
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- ZA200407667B ZA200407667B ZA200407667A ZA200407667A ZA200407667B ZA 200407667 B ZA200407667 B ZA 200407667B ZA 200407667 A ZA200407667 A ZA 200407667A ZA 200407667 A ZA200407667 A ZA 200407667A ZA 200407667 B ZA200407667 B ZA 200407667B
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- South Africa
- Prior art keywords
- alkyl
- group
- halogen
- compound according
- optionally substituted
- Prior art date
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- 229940095745 sex hormone and modulator of the genital system progesterone receptor modulator Drugs 0.000 title description 3
- 125000000217 alkyl group Chemical group 0.000 claims description 77
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- 125000005843 halogen group Chemical group 0.000 claims description 20
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- 125000003342 alkenyl group Chemical group 0.000 claims description 16
- 125000000304 alkynyl group Chemical group 0.000 claims description 13
- 229910052760 oxygen Inorganic materials 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 11
- 229910052717 sulfur Inorganic materials 0.000 claims description 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 9
- 239000000203 mixture Substances 0.000 claims description 9
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- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical class C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 238000005984 hydrogenation reaction Methods 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 description 1
- 238000003402 intramolecular cyclocondensation reaction Methods 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 230000000938 luteal effect Effects 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 238000006396 nitration reaction Methods 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 238000007339 nucleophilic aromatic substitution reaction Methods 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 229910052763 palladium Inorganic materials 0.000 description 1
- 239000004031 partial agonist Substances 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 150000002989 phenols Chemical class 0.000 description 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 description 1
- CYQAYERJWZKYML-UHFFFAOYSA-N phosphorus pentasulfide Chemical compound S1P(S2)(=S)SP3(=S)SP1(=S)SP2(=S)S3 CYQAYERJWZKYML-UHFFFAOYSA-N 0.000 description 1
- 125000003367 polycyclic group Chemical group 0.000 description 1
- 229960003387 progesterone Drugs 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 238000005932 reductive alkylation reaction Methods 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 238000007127 saponification reaction Methods 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 239000012312 sodium hydride Substances 0.000 description 1
- 229910000104 sodium hydride Inorganic materials 0.000 description 1
- 239000012321 sodium triacetoxyborohydride Substances 0.000 description 1
- 239000003270 steroid hormone Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 238000006277 sulfonation reaction Methods 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- BNWCETAHAJSBFG-UHFFFAOYSA-N tert-butyl 2-bromoacetate Chemical compound CC(C)(C)OC(=O)CBr BNWCETAHAJSBFG-UHFFFAOYSA-N 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 150000003556 thioamides Chemical class 0.000 description 1
- 150000003568 thioethers Chemical class 0.000 description 1
- 150000003585 thioureas Chemical class 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
- 230000035897 transcription Effects 0.000 description 1
- QIWRFOJWQSSRJZ-UHFFFAOYSA-N tributyl(ethenyl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C=C QIWRFOJWQSSRJZ-UHFFFAOYSA-N 0.000 description 1
- PVFOMCVHYWHZJE-UHFFFAOYSA-N trichloroacetyl chloride Chemical compound ClC(=O)C(Cl)(Cl)Cl PVFOMCVHYWHZJE-UHFFFAOYSA-N 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- NMLXKNNXODLJIN-UHFFFAOYSA-M zinc;carbanide;chloride Chemical compound [CH3-].[Zn+]Cl NMLXKNNXODLJIN-UHFFFAOYSA-M 0.000 description 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
- C07D498/02—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
- C07D498/04—Ortho-condensed systems
-
- 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
-
- 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
- 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
-
- 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
-
- 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
- A61P5/36—Antigestagens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Hematology (AREA)
- Pregnancy & Childbirth (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02076350 | 2002-04-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200407667B true ZA200407667B (en) | 2006-07-26 |
Family
ID=28685924
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200407667A ZA200407667B (en) | 2002-04-04 | 2004-09-22 | Non-steroidal progesterone receptor modulators |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US7737136B2 (ja) |
| EP (1) | EP1495030B1 (ja) |
| JP (1) | JP4418683B2 (ja) |
| KR (1) | KR100965173B1 (ja) |
| CN (1) | CN1279044C (ja) |
| AR (1) | AR039251A1 (ja) |
| AT (1) | ATE404567T1 (ja) |
| AU (1) | AU2003224161B2 (ja) |
| BR (1) | BR0308890A (ja) |
| CA (1) | CA2480940C (ja) |
| CY (1) | CY1108495T1 (ja) |
| DE (1) | DE60322867D1 (ja) |
| DK (1) | DK1495030T3 (ja) |
| EC (1) | ECSP045334A (ja) |
| ES (1) | ES2310654T3 (ja) |
| HK (1) | HK1070362A1 (ja) |
| HR (1) | HRP20040913A2 (ja) |
| IL (2) | IL164169A0 (ja) |
| IS (1) | IS7452A (ja) |
| MX (1) | MXPA04009709A (ja) |
| NO (1) | NO20044473L (ja) |
| NZ (1) | NZ535546A (ja) |
| PE (1) | PE20040350A1 (ja) |
| PL (1) | PL372846A1 (ja) |
| PT (1) | PT1495030E (ja) |
| RU (1) | RU2309155C2 (ja) |
| SI (1) | SI1495030T1 (ja) |
| TW (1) | TWI297685B (ja) |
| WO (1) | WO2003084963A1 (ja) |
| ZA (1) | ZA200407667B (ja) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI297685B (en) | 2002-04-04 | 2008-06-11 | Organon Nv | Non-steroidal progesterone receptor modulators |
| TWI370129B (en) * | 2005-02-14 | 2012-08-11 | Msd Oss Bv | Non steroidal glucocorticoid receptor modulators |
| TWI375676B (en) * | 2005-08-29 | 2012-11-01 | Msd Oss Bv | Non-steroidal glucocorticoid receptor modulators |
| NZ575276A (en) * | 2006-09-27 | 2011-07-29 | Organon Nv | Pyridooxazepine progesterone receptor modulators |
| US7989442B2 (en) | 2006-09-27 | 2011-08-02 | N.V. Organon | Progesterone receptor modulators |
| US8063037B2 (en) * | 2007-05-07 | 2011-11-22 | N. V. Organon | Progesterone receptor modulators |
| TW200914029A (en) * | 2007-05-07 | 2009-04-01 | Organon Nv | New progesterone receptor modulators |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7305811A (ja) | 1973-04-26 | 1974-10-29 | ||
| US4054572A (en) * | 1973-04-26 | 1977-10-18 | Akzona Incorporated | Hexahydro pyridine [1,2d] dibenza [b,f] (1,4)-diazepines |
| US4016161A (en) * | 1974-04-24 | 1977-04-05 | Akzona Incorporated | Amino-substituted 1,2,3,4,10,146-hexahydro-pyridino[1,2-a]dibenzo[c,f]azepines |
| ATE86484T1 (de) | 1987-08-08 | 1993-03-15 | Akzo Nv | Kontrazeptives implantat. |
| CA2026856A1 (en) | 1989-10-05 | 1991-04-06 | Mark G. Bock | 3-substituted-1,4-benzodiazepines useful as oxytocin |
| US5696127A (en) | 1994-12-22 | 1997-12-09 | Ligand Pharmaceuticals Incorporated | Steroid receptor modulator compounds and methods |
| IL123813A0 (en) | 1997-04-11 | 1998-10-30 | Akzo Nobel Nv | Drug delivery system for two or more active substances |
| TWI297685B (en) | 2002-04-04 | 2008-06-11 | Organon Nv | Non-steroidal progesterone receptor modulators |
| TWI370129B (en) | 2005-02-14 | 2012-08-11 | Msd Oss Bv | Non steroidal glucocorticoid receptor modulators |
| NZ575276A (en) | 2006-09-27 | 2011-07-29 | Organon Nv | Pyridooxazepine progesterone receptor modulators |
-
2003
- 2003-03-31 TW TW092107288A patent/TWI297685B/zh not_active IP Right Cessation
- 2003-04-01 MX MXPA04009709A patent/MXPA04009709A/es active IP Right Grant
- 2003-04-01 NZ NZ535546A patent/NZ535546A/en not_active IP Right Cessation
- 2003-04-01 BR BR0308890-1A patent/BR0308890A/pt not_active IP Right Cessation
- 2003-04-01 PT PT03720570T patent/PT1495030E/pt unknown
- 2003-04-01 DE DE60322867T patent/DE60322867D1/de not_active Expired - Lifetime
- 2003-04-01 AU AU2003224161A patent/AU2003224161B2/en not_active Ceased
- 2003-04-01 ES ES03720570T patent/ES2310654T3/es not_active Expired - Lifetime
- 2003-04-01 CA CA2480940A patent/CA2480940C/en not_active Expired - Fee Related
- 2003-04-01 AT AT03720570T patent/ATE404567T1/de active
- 2003-04-01 RU RU2004132215/04A patent/RU2309155C2/ru not_active IP Right Cessation
- 2003-04-01 EP EP03720570A patent/EP1495030B1/en not_active Expired - Lifetime
- 2003-04-01 US US10/510,275 patent/US7737136B2/en active Active
- 2003-04-01 CN CNB038099047A patent/CN1279044C/zh not_active Expired - Fee Related
- 2003-04-01 IL IL16416903A patent/IL164169A0/xx unknown
- 2003-04-01 SI SI200331416T patent/SI1495030T1/sl unknown
- 2003-04-01 JP JP2003582160A patent/JP4418683B2/ja not_active Expired - Fee Related
- 2003-04-01 WO PCT/EP2003/050085 patent/WO2003084963A1/en active IP Right Grant
- 2003-04-01 KR KR1020047015753A patent/KR100965173B1/ko not_active IP Right Cessation
- 2003-04-01 DK DK03720570T patent/DK1495030T3/da active
- 2003-04-01 PL PL03372846A patent/PL372846A1/xx not_active Application Discontinuation
- 2003-04-03 PE PE2003000343A patent/PE20040350A1/es not_active Application Discontinuation
- 2003-04-04 AR ARP030101176A patent/AR039251A1/es unknown
-
2004
- 2004-09-16 IS IS7452A patent/IS7452A/is unknown
- 2004-09-21 IL IL164169A patent/IL164169A/en not_active IP Right Cessation
- 2004-09-22 ZA ZA200407667A patent/ZA200407667B/en unknown
- 2004-10-01 EC EC2004005334A patent/ECSP045334A/es unknown
- 2004-10-04 HR HR20040913A patent/HRP20040913A2/xx not_active Application Discontinuation
- 2004-10-20 NO NO20044473A patent/NO20044473L/no not_active Application Discontinuation
-
2005
- 2005-04-11 HK HK05103033A patent/HK1070362A1/xx not_active IP Right Cessation
-
2008
- 2008-11-10 CY CY20081101280T patent/CY1108495T1/el unknown
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