CN1312147C - 作为选择性雌激素受体－β激动剂的取代的苯并吡喃类化合物 - Google Patents

作为选择性雌激素受体－β激动剂的取代的苯并吡喃类化合物 Download PDF

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Publication number
CN1312147C
CN1312147C CNB028229916A CN02822991A CN1312147C CN 1312147 C CN1312147 C CN 1312147C CN B028229916 A CNB028229916 A CN B028229916A CN 02822991 A CN02822991 A CN 02822991A CN 1312147 C CN1312147 C CN 1312147C
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CN
China
Prior art keywords
compound
preparation example
racemize
acceptable salt
solution
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Expired - Fee Related
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CNB028229916A
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English (en)
Chinese (zh)
Other versions
CN1589268A (zh
Inventor
J·A·多奇
V·G·克里斯南
C·W·卢加三世
B·L·纽保尔
B·H·诺尔曼
L·A·普菲菲尔
T·I·理查森
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of CN1589268A publication Critical patent/CN1589268A/zh
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Publication of CN1312147C publication Critical patent/CN1312147C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • 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
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/80—Dibenzopyrans; Hydrogenated dibenzopyrans
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/28—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D311/94—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 condensed with rings other than six-membered or with ring systems containing such rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
CNB028229916A 2001-11-19 2002-11-07 作为选择性雌激素受体－β激动剂的取代的苯并吡喃类化合物 Expired - Fee Related CN1312147C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US33276601P 2001-11-19 2001-11-19
US60/332,766 2001-11-19
US36362202P 2002-03-11 2002-03-11
US60/363,622 2002-03-11

Publications (2)

Publication Number Publication Date
CN1589268A CN1589268A (zh) 2005-03-02
CN1312147C true CN1312147C (zh) 2007-04-25

Family

ID=26988373

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028229916A Expired - Fee Related CN1312147C (zh) 2001-11-19 2002-11-07 作为选择性雌激素受体－β激动剂的取代的苯并吡喃类化合物

Country Status (23)

Country Link
US (1) US7217734B2 (enExample)
EP (1) EP1448544B1 (enExample)
JP (1) JP4381810B2 (enExample)
KR (1) KR100950616B1 (enExample)
CN (1) CN1312147C (enExample)
AT (1) ATE362471T1 (enExample)
AU (1) AU2002359283B2 (enExample)
CA (1) CA2467013C (enExample)
CY (1) CY1106726T1 (enExample)
DE (1) DE60220179T2 (enExample)
DK (1) DK1448544T3 (enExample)
EA (1) EA007382B1 (enExample)
EC (1) ECSP045113A (enExample)
ES (1) ES2286322T3 (enExample)
HR (1) HRP20040439A2 (enExample)
HU (1) HU229351B1 (enExample)
IL (3) IL161325A0 (enExample)
MX (1) MXPA04004703A (enExample)
NO (1) NO328563B1 (enExample)
NZ (1) NZ531850A (enExample)
PL (1) PL205733B1 (enExample)
PT (1) PT1448544E (enExample)
WO (1) WO2003044006A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7279499B2 (en) 2003-04-21 2007-10-09 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
EP1626974B1 (en) * 2003-04-21 2008-08-27 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
JP2008512458A (ja) 2004-09-07 2008-04-24 ワイス ６Ｈ−［１］ベンゾピラノ［４，３−ｂ］キノリン及びエストロゲン様物質としてのそれらの使用
ATE504582T1 (de) * 2004-10-18 2011-04-15 Lilly Co Eli Substituierte benzopyrane als selektive östrogenrezeptor-beta-agonisten
US20060166933A1 (en) * 2004-11-18 2006-07-27 Jain Nareshkumar F Novel 2H-chromene derivatives as selective estrogen receptor modulators
US8093302B2 (en) 2005-02-15 2012-01-10 Eli Lilly And Company Substituted tetralins as selective estrogen receptor-β agonists
US9604931B2 (en) 2007-01-22 2017-03-28 Gtx, Inc. Nuclear receptor binding agents
US9623021B2 (en) 2007-01-22 2017-04-18 Gtx, Inc. Nuclear receptor binding agents
US8063102B2 (en) 2009-03-13 2011-11-22 N.V. Organon Tetrahydronaphthalen-2-ol derivatives
TW201043595A (en) 2009-03-13 2010-12-16 Organon Nv Tetrahydronaphthalen-2-ol derivatives
CN105960236A (zh) 2013-12-05 2016-09-21 卡罗医药股份公司 用于治疗间皮瘤的雌激素受体β激动剂
JP6978420B2 (ja) 2015-09-17 2021-12-08 オハイオ・ステート・イノヴェーション・ファウンデーション カルボラン化合物及びその使用方法
WO2021183760A1 (en) * 2020-03-11 2021-09-16 Ohio State Innovation Foundation Methods of modulating t-cell activation using estrogen receptor beta (erβ) agonists

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999002512A1 (en) * 1997-07-09 1999-01-21 Novo Nordisk A/S Dl-2,3-diaryl-2h-1-benzopyrans
WO2001064665A1 (en) * 2000-03-01 2001-09-07 Akzo Nobel N.V. Chroman derivatives as estrogenic compounds

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3901926A (en) * 1973-04-02 1975-08-26 Abbott Lab Alkylphenyl benzopyrans
EP0935000A3 (en) 1995-09-08 1999-09-08 Karo Bio Ab Orphan receptor
US6593322B1 (en) 1999-03-17 2003-07-15 Signal Pharmaceuticals, Inc. Compounds and methods for modulation of estrogen receptors
JP2003521468A (ja) 1999-03-17 2003-07-15 シグナル ファーマシューティカルズ， インコーポレイテッド エストロゲンレセプタを変調させるための化合物及び方法
TR200102992T2 (tr) 1999-04-16 2004-12-21 Astrazeneca Ab ß östrojen reseptörü ligandları.
CA2396059A1 (en) 1999-12-30 2001-07-12 Signal Pharmaceuticals, Inc. Compounds and methods for modulation of estrogen receptors
ES2293986T3 (es) 2000-03-27 2008-04-01 N.V. Organon Compuestos no esteroides tetraciclicos para tratamientos relacionados con el estrogeno.
GB2361642A (en) 2000-10-24 2001-10-31 Karobio Ab Estrogen receptor beta (ERbeta) agonists for use in cancer treatment
UA83620C2 (ru) 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
TWI306450B (en) 2001-12-13 2009-02-21 Wyeth Corp Substituted phenyl naphthalenes as estrogenic agents
US6630508B1 (en) * 2002-02-11 2003-10-07 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor β agonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999002512A1 (en) * 1997-07-09 1999-01-21 Novo Nordisk A/S Dl-2,3-diaryl-2h-1-benzopyrans
WO2001064665A1 (en) * 2000-03-01 2001-09-07 Akzo Nobel N.V. Chroman derivatives as estrogenic compounds

Also Published As

Publication number Publication date
PL205733B1 (pl) 2010-05-31
NO20042583L (no) 2004-06-18
NO328563B1 (no) 2010-03-22
KR20040063963A (ko) 2004-07-15
US7217734B2 (en) 2007-05-15
HK1068349A1 (en) 2005-04-29
AU2002359283B2 (en) 2007-06-21
MXPA04004703A (es) 2004-08-19
PL374510A1 (en) 2005-10-31
JP4381810B2 (ja) 2009-12-09
DE60220179D1 (de) 2007-06-28
ES2286322T3 (es) 2007-12-01
IL161325A (en) 2008-07-08
IL161325A0 (en) 2004-09-27
HRP20040439A2 (en) 2005-04-30
CN1589268A (zh) 2005-03-02
US20040249167A1 (en) 2004-12-09
EA200400695A1 (ru) 2004-12-30
CY1106726T1 (el) 2012-05-23
IL185867A0 (en) 2008-01-06
KR100950616B1 (ko) 2010-04-01
EP1448544B1 (en) 2007-05-16
AU2002359283A1 (en) 2003-06-10
JP2005513027A (ja) 2005-05-12
NZ531850A (en) 2007-01-26
PT1448544E (pt) 2007-08-10
HUP0402628A2 (hu) 2005-04-28
HU229351B1 (en) 2013-11-28
EA007382B1 (ru) 2006-10-27
ECSP045113A (es) 2004-07-23
EP1448544A1 (en) 2004-08-25
CA2467013C (en) 2010-08-10
ATE362471T1 (de) 2007-06-15
CA2467013A1 (en) 2003-05-30
IL185867A (en) 2009-09-22
DE60220179T2 (de) 2008-02-07
WO2003044006A1 (en) 2003-05-30
DK1448544T3 (da) 2007-10-08
AU2002359283B8 (en) 2003-06-10

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CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20070425

Termination date: 20151107

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