WO2001049673A2 - Compounds and methods for modulation of estrogen receptors - Google Patents
Compounds and methods for modulation of estrogen receptors Download PDFInfo
- Publication number
- WO2001049673A2 WO2001049673A2 PCT/US2000/035671 US0035671W WO0149673A2 WO 2001049673 A2 WO2001049673 A2 WO 2001049673A2 US 0035671 W US0035671 W US 0035671W WO 0149673 A2 WO0149673 A2 WO 0149673A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- compound
- animal
- effective amount
- bone
- cancer
- 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.)
- Ceased
Links
- 0 *c(cc1)ccc1C(C(Oc1c2)=O)=C(c(cc3)ccc3OCCN3CCCCC3)c1ccc2O Chemical compound *c(cc1)ccc1C(C(Oc1c2)=O)=C(c(cc3)ccc3OCCN3CCCCC3)c1ccc2O 0.000 description 1
- GUFYHGPNYOBLAR-UHFFFAOYSA-N CN1C(CCOc(cc2)ccc2C(c(ccc(O)c2)c2O2)=C(c(cc3)ccc3Cl)C2=O)CCC1 Chemical compound CN1C(CCOc(cc2)ccc2C(c(ccc(O)c2)c2O2)=C(c(cc3)ccc3Cl)C2=O)CCC1 GUFYHGPNYOBLAR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/06—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
- C07D311/08—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
- C07D311/16—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK00990966T DK1246814T3 (da) | 1999-12-30 | 2000-12-29 | Forbindelser og fremgangsmåder til modulation af östrogenreceptorer |
| KR1020027008569A KR20020075388A (ko) | 1999-12-30 | 2000-12-29 | 에스트로겐 수용체의 조절 화합물 및 조절 방법 |
| DE60018215T DE60018215T2 (de) | 1999-12-30 | 2000-12-29 | Verbindungen und verfahren zur modulation von estrogen rezeptoren |
| JP2001550213A JP2003519219A (ja) | 1999-12-30 | 2000-12-29 | エストロゲン受容体をモジュレートするための化合物および方法 |
| HK04101233.1A HK1058521B (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
| AU30771/01A AU781282B2 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
| CA002396059A CA2396059A1 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
| IL15046300A IL150463A0 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
| EP00990966A EP1246814B1 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
| AT00990966T ATE289300T1 (de) | 1999-12-30 | 2000-12-29 | Verbindungen und verfahren zur modulation von estrogen rezeptoren |
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47577699A | 1999-12-30 | 1999-12-30 | |
| US09/475,776 | 1999-12-30 | ||
| US09/492,939 US6291456B1 (en) | 1998-12-30 | 2000-01-27 | Compounds and methods for modulation of estrogen receptors |
| US09/492,939 | 2000-01-27 | ||
| US09/611,156 US6331562B1 (en) | 1998-12-30 | 2000-07-06 | Compounds and methods for modulation of estrogen receptors |
| US09/611,156 | 2000-07-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2001049673A2 true WO2001049673A2 (en) | 2001-07-12 |
| WO2001049673A3 WO2001049673A3 (en) | 2001-12-06 |
Family
ID=27413348
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2000/035671 Ceased WO2001049673A2 (en) | 1999-12-30 | 2000-12-29 | Compounds and methods for modulation of estrogen receptors |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1246814B1 (enExample) |
| JP (1) | JP2003519219A (enExample) |
| KR (1) | KR20020075388A (enExample) |
| CN (1) | CN1281598C (enExample) |
| AT (1) | ATE289300T1 (enExample) |
| AU (1) | AU781282B2 (enExample) |
| CA (1) | CA2396059A1 (enExample) |
| DE (1) | DE60018215T2 (enExample) |
| DK (1) | DK1246814T3 (enExample) |
| ES (1) | ES2238034T3 (enExample) |
| IL (1) | IL150463A0 (enExample) |
| PT (1) | PT1246814E (enExample) |
| WO (1) | WO2001049673A2 (enExample) |
Cited By (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1281710A1 (en) * | 2001-08-03 | 2003-02-05 | CHIESI FARMACEUTICI S.p.A. | 2H-1-benzopyran derivatives, processes for their preparation and pharmaceutical compositions thereof |
| EP1120114A3 (en) * | 2000-01-12 | 2003-08-20 | Pfizer Products Inc. | Compositions and methods for treating conditions responsive to estrogen |
| WO2003089422A1 (en) * | 2002-04-19 | 2003-10-30 | Signal Pharmaceuticals, Inc. | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| WO2004101544A1 (en) * | 2003-05-14 | 2004-11-25 | Warner-Lambert Company Llc | Benzyl sulfonamide derivatives as androgen receptor antagonists |
| EP1460969A4 (en) * | 2001-11-29 | 2005-08-17 | Gtx Inc | PREVENTION AND TREATMENT OF OSTEOPOROSIS INDUCED BY THE DEPRIVATION OF ANDROGEN |
| US7091235B2 (en) | 2002-10-15 | 2006-08-15 | Signal Pharmaceuticals, Llc | Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer |
| EP1450812A4 (en) * | 2001-10-03 | 2007-03-28 | Signal Pharm Inc | USE OF BENZOPYRANOES FOR THE TREATMENT OR PREVENTION OF A PRIMARY BRAIN CARCINOMA OR A BRAIN METASTASE |
| US7217734B2 (en) | 2001-11-19 | 2007-05-15 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| US7279499B2 (en) | 2003-04-21 | 2007-10-09 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| WO2008002490A3 (en) * | 2006-06-23 | 2008-06-26 | Radius Health Inc | Treatment of vasomotor symptoms with selective estrogen receptor modulators |
| AU2005202072B2 (en) * | 2001-11-29 | 2008-10-23 | Gtx, Inc. | Prevention and treatment of androgen-deprivation induced conditions |
| US7442812B2 (en) | 2003-04-21 | 2008-10-28 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| US7524866B2 (en) | 2001-11-29 | 2009-04-28 | Gtx, Inc. | Prevention and treatment of androgen—deprivation induced osteoporosis |
| US7674783B2 (en) * | 2002-11-22 | 2010-03-09 | Dimera Inc. | Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease |
| CN105801544A (zh) * | 2016-04-18 | 2016-07-27 | 中国药科大学 | 3-芳基-4-芳香胺-香豆素衍生物及其制备方法和医药用途 |
| CN105801543A (zh) * | 2016-04-18 | 2016-07-27 | 中国药科大学 | 4-芳香胺-香豆素衍生物及其制备方法和医药用途 |
| US9555014B2 (en) | 2010-05-12 | 2017-01-31 | Radius Health, Inc. | Therapeutic regimens |
| US9920044B2 (en) | 2010-09-28 | 2018-03-20 | Radius Pharmaceuticals, Inc. | Selective androgen receptor modulators |
| US10071066B2 (en) | 2014-03-28 | 2018-09-11 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| US10385008B2 (en) | 2017-01-05 | 2019-08-20 | Radius Pharmaceuticals, Inc. | Polymorphic forms of RAD1901-2HCL |
| US10420734B2 (en) | 2014-03-28 | 2019-09-24 | Duke University | Method of treating cancer using selective estrogen receptor modulators |
| US11771682B2 (en) | 2016-06-22 | 2023-10-03 | Ellipses Pharma Ltd. | AR+ breast cancer treatment methods |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1177787A3 (en) * | 2000-07-28 | 2003-09-10 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating cataracts |
| WO2005028472A1 (en) * | 2003-09-15 | 2005-03-31 | Signal Pharmaceuticals, Llc | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| CA2595472A1 (en) * | 2005-01-21 | 2006-07-27 | Janssen Pharmaceutica N.V. | Novel coumarin derivatives as ion channel openers |
| CN106492204A (zh) * | 2016-12-27 | 2017-03-15 | 郑州郑先医药科技有限公司 | 一种治疗白内障的药物组合物 |
| CN106727637A (zh) * | 2016-12-27 | 2017-05-31 | 郑州郑先医药科技有限公司 | 一种治疗白内障的西药组合物及其用途 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5883118A (en) * | 1996-01-11 | 1999-03-16 | Nova Nordisk A/S | Prostatic carcinoma |
| US5726202A (en) * | 1996-01-11 | 1998-03-10 | Novo Nordisk A/S | Benign prostatic hypertrophy |
| IL124882A0 (en) * | 1996-01-11 | 1999-01-26 | Novo Nordisk As | Use of 3, 4-diphenyl chromans for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of menopausal symptoms |
| ATE248157T1 (de) * | 1998-12-30 | 2003-09-15 | Signal Pharm Inc | Verbindungen und verfahren zur modulation von estrogen rezeptoren |
-
2000
- 2000-12-29 AU AU30771/01A patent/AU781282B2/en not_active Ceased
- 2000-12-29 ES ES00990966T patent/ES2238034T3/es not_active Expired - Lifetime
- 2000-12-29 CN CNB008192227A patent/CN1281598C/zh not_active Expired - Fee Related
- 2000-12-29 CA CA002396059A patent/CA2396059A1/en not_active Abandoned
- 2000-12-29 IL IL15046300A patent/IL150463A0/xx unknown
- 2000-12-29 DE DE60018215T patent/DE60018215T2/de not_active Expired - Fee Related
- 2000-12-29 WO PCT/US2000/035671 patent/WO2001049673A2/en not_active Ceased
- 2000-12-29 EP EP00990966A patent/EP1246814B1/en not_active Expired - Lifetime
- 2000-12-29 PT PT00990966T patent/PT1246814E/pt unknown
- 2000-12-29 AT AT00990966T patent/ATE289300T1/de not_active IP Right Cessation
- 2000-12-29 JP JP2001550213A patent/JP2003519219A/ja active Pending
- 2000-12-29 DK DK00990966T patent/DK1246814T3/da active
- 2000-12-29 KR KR1020027008569A patent/KR20020075388A/ko not_active Abandoned
Cited By (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1120114A3 (en) * | 2000-01-12 | 2003-08-20 | Pfizer Products Inc. | Compositions and methods for treating conditions responsive to estrogen |
| EP1281710A1 (en) * | 2001-08-03 | 2003-02-05 | CHIESI FARMACEUTICI S.p.A. | 2H-1-benzopyran derivatives, processes for their preparation and pharmaceutical compositions thereof |
| EP1450812A4 (en) * | 2001-10-03 | 2007-03-28 | Signal Pharm Inc | USE OF BENZOPYRANOES FOR THE TREATMENT OR PREVENTION OF A PRIMARY BRAIN CARCINOMA OR A BRAIN METASTASE |
| US7217734B2 (en) | 2001-11-19 | 2007-05-15 | Eli Lilly And Company | Substituted benzopyrans as selective estrogen receptor-beta agonists |
| EP2098247A3 (en) * | 2001-11-29 | 2010-05-26 | GTX, Inc. | Prevention and treatment of androgen-deprivation induced loss of BMD or bone fractures |
| US7524866B2 (en) | 2001-11-29 | 2009-04-28 | Gtx, Inc. | Prevention and treatment of androgen—deprivation induced osteoporosis |
| EP1460969A4 (en) * | 2001-11-29 | 2005-08-17 | Gtx Inc | PREVENTION AND TREATMENT OF OSTEOPOROSIS INDUCED BY THE DEPRIVATION OF ANDROGEN |
| EP1574212A1 (en) * | 2001-11-29 | 2005-09-14 | GTX Inc. | Prevention and treatment of androgen-deprivation induced hot flashes, decreased lean muscle mass, loss of libido or erectile dysfunction |
| EP1666033A1 (en) * | 2001-11-29 | 2006-06-07 | GTX, Inc. | Prevention and treatment of androgen-deprivation induced osteoporosis |
| AU2005202072B2 (en) * | 2001-11-29 | 2008-10-23 | Gtx, Inc. | Prevention and treatment of androgen-deprivation induced conditions |
| AU2002356928B2 (en) * | 2001-11-29 | 2008-04-17 | Gtx Inc. | Prevention and treatment of androgen-deprivation induced osteoporosis |
| AU2003239155B2 (en) * | 2002-04-19 | 2008-12-04 | Novartis Ag | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| JP2006504629A (ja) * | 2002-04-19 | 2006-02-09 | シグナル ファーマシューティカルズ,エルエルシー | ベンゾピラノン化合物、その組成物およびそれを使用する治療方法 |
| WO2003089422A1 (en) * | 2002-04-19 | 2003-10-30 | Signal Pharmaceuticals, Inc. | Benzopyranone compounds, compositions thereof, and methods of treatment therewith |
| CN100436440C (zh) * | 2002-04-19 | 2008-11-26 | 信号药品公司 | 苯并吡喃酮化合物、其组合物以及其治疗方法 |
| EP1556374A4 (en) * | 2002-10-15 | 2007-12-19 | Signal Pharm Inc | BENZOPYRANONE COMPOUNDS, COMPOSITIONS THEREOF AND METHOD FOR TREATING OR PREVENTION OF CANCER |
| US7358274B2 (en) | 2002-10-15 | 2008-04-15 | Signal Pharmaceuticals, Llc | Methods for treating or preventing cancer using Benzopyranone Compounds |
| US7091235B2 (en) | 2002-10-15 | 2006-08-15 | Signal Pharmaceuticals, Llc | Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer |
| US7589119B2 (en) | 2002-10-15 | 2009-09-15 | Signal Pharmaceutical, Llc | Methods for treating or preventing metastatic cancer using benzopyranone compounds |
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Also Published As
| Publication number | Publication date |
|---|---|
| DE60018215D1 (de) | 2005-03-24 |
| CN1437591A (zh) | 2003-08-20 |
| CN1281598C (zh) | 2006-10-25 |
| DK1246814T3 (da) | 2005-05-30 |
| IL150463A0 (en) | 2002-12-01 |
| EP1246814B1 (en) | 2005-02-16 |
| EP1246814A2 (en) | 2002-10-09 |
| AU3077101A (en) | 2001-07-16 |
| AU781282B2 (en) | 2005-05-12 |
| WO2001049673A3 (en) | 2001-12-06 |
| HK1058521A1 (en) | 2004-05-21 |
| ATE289300T1 (de) | 2005-03-15 |
| ES2238034T3 (es) | 2005-08-16 |
| KR20020075388A (ko) | 2002-10-04 |
| CA2396059A1 (en) | 2001-07-12 |
| DE60018215T2 (de) | 2006-02-09 |
| JP2003519219A (ja) | 2003-06-17 |
| PT1246814E (pt) | 2005-07-29 |
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