DE68927861D1 - 11 beta-substituierte progesteron-analoge - Google Patents

11 beta-substituierte progesteron-analoge

Info

Publication number
DE68927861D1
DE68927861D1 DE68927861T DE68927861T DE68927861D1 DE 68927861 D1 DE68927861 D1 DE 68927861D1 DE 68927861 T DE68927861 T DE 68927861T DE 68927861 T DE68927861 T DE 68927861T DE 68927861 D1 DE68927861 D1 DE 68927861D1
Authority
DE
Germany
Prior art keywords
beta
alkynyl
alkenyl
alkyl
defined above
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 - Lifetime
Application number
DE68927861T
Other languages
English (en)
Other versions
DE68927861T2 (de
Inventor
C Edgar Cook
Mansukh C Wani
Yue-Wei Lee
Jerry R Reel
Douglas Rector
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Research Triangle Institute
Original Assignee
Research Triangle Institute
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Research Triangle Institute filed Critical Research Triangle Institute
Publication of DE68927861D1 publication Critical patent/DE68927861D1/de
Application granted granted Critical
Publication of DE68927861T2 publication Critical patent/DE68927861T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
    • C07J53/002—Carbocyclic rings fused
    • C07J53/004—3 membered carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0052—Nitrogen only at position 16(17)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Devices For Supply Of Signal Current (AREA)
  • Sub-Exchange Stations And Push- Button Telephones (AREA)
  • Control Of Eletrric Generators (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Light Receiving Elements (AREA)
  • Led Devices (AREA)
  • Junction Field-Effect Transistors (AREA)
  • Manufacture Of Tobacco Products (AREA)
  • Seasonings (AREA)
DE68927861T 1988-06-23 1989-06-23 11 beta-substituierte progesteron-analoge Expired - Lifetime DE68927861T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/210,503 US4954490A (en) 1988-06-23 1988-06-23 11 β-substituted progesterone analogs
PCT/US1989/002706 WO1989012448A1 (en) 1988-06-23 1989-06-23 11beta-SUBSTITUTED PROGESTERONE ANALOGS

Publications (2)

Publication Number Publication Date
DE68927861D1 true DE68927861D1 (de) 1997-04-17
DE68927861T2 DE68927861T2 (de) 1997-10-16

Family

ID=22783162

Family Applications (2)

Application Number Title Priority Date Filing Date
DE68927861T Expired - Lifetime DE68927861T2 (de) 1988-06-23 1989-06-23 11 beta-substituierte progesteron-analoge
DE122009000031C Active DE122009000031I2 (de) 1988-06-23 1989-06-23 11 beta-substituierte progesteron-analoge

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE122009000031C Active DE122009000031I2 (de) 1988-06-23 1989-06-23 11 beta-substituierte progesteron-analoge

Country Status (13)

Country Link
US (2) US4954490A (de)
EP (1) EP0422100B1 (de)
JP (1) JP2953725B2 (de)
KR (1) KR0161975B1 (de)
AT (1) ATE149839T1 (de)
AU (1) AU635211B2 (de)
CA (1) CA1338906C (de)
DE (2) DE68927861T2 (de)
DK (1) DK175760B1 (de)
LU (1) LU91575I2 (de)
NL (1) NL300392I2 (de)
NO (2) NO905546L (de)
WO (1) WO1989012448A1 (de)

Families Citing this family (89)

* Cited by examiner, † Cited by third party
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DE3832303A1 (de) * 1988-09-20 1990-04-12 Schering Ag 11ss-phenyl-14ssh-steroide
ATE172469T1 (de) * 1989-08-04 1998-11-15 Schering Ag 11 beta-aryl-gona-4,9-dien-3-one
USRE34578E (en) * 1990-05-07 1994-04-05 Lubkin; Virginia Drugs for topical application of sex steroids in the treatment of dry eye syndrome, and methods of preparation and application
US5041434A (en) * 1991-08-17 1991-08-20 Virginia Lubkin Drugs for topical application of sex steroids in the treatment of dry eye syndrome, and methods of preparation and application
DE4042004A1 (de) * 1990-12-22 1992-06-25 Schering Ag 14(beta)-h-, 14- u. 15-en-11(beta)-aryl-4-estrene
US5407928A (en) * 1990-08-15 1995-04-18 Schering Aktiengesellschaft 11β-aryl-gona-4,9-dien-3-ones
CA2133966C (en) * 1992-04-21 1997-09-09 David A. Sullivan Ocular androgen therapy in sjogren's syndrome
US5536725A (en) * 1993-08-25 1996-07-16 Fmc Corporation Insecticidal substituted-2,4-diamino-5,6,7,8-tetrahydroquinazolines
US5780220A (en) * 1994-05-19 1998-07-14 Trustees Of The University Of Pennsylvania Methods and compositions for inhibiting HIV replication
US5639598A (en) * 1994-05-19 1997-06-17 The Trustees Of The University Of Pennsylvania Method and kit for identification of antiviral agents capable of abrogating HIV Vpr-Rip-1 binding interactions
EP0683172B1 (de) * 1994-05-19 1997-08-13 Akzo Nobel N.V. 11,21-Bisphenyl-19-nor-pregnan Derivate
US5929262A (en) * 1995-03-30 1999-07-27 The United States Of America As Represented By The Department Of Health And Human Services Method for preparing 17α-acetoxy-11β-(4-N, N-dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates
ES2152671T3 (es) * 1996-05-01 2001-02-01 Us Gov Health & Human Serv Derivados de progesterona sustituidos en posicion 21 como nuevos agentes antiprogestacionales.
US6900193B1 (en) * 1996-05-01 2005-05-31 The United States Of America As Represented By The Department Of Health And Human Services Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
WO1998005679A2 (en) * 1996-08-05 1998-02-12 Duke University Mixed agonists of the progesterone receptor and assays therefor
US6090798A (en) * 1997-12-19 2000-07-18 Alcon Laboratories, Inc. Treatment of GLC1A glaucoma with glucocorticoid antagonists
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US5962444A (en) * 1998-05-29 1999-10-05 Research Triangle Institute 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6262042B1 (en) * 1998-05-29 2001-07-17 Research Triangle Institute 17β-amino and hydroxylamino-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6172052B1 (en) * 1998-12-04 2001-01-09 Research Triangle Institute 17β-acyl-17α-propynyl-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
US6740645B1 (en) * 1999-09-03 2004-05-25 Research Triangle Institute 17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties
AU4584901A (en) * 2000-03-17 2001-10-15 Us Gov Health & Human Serv Structural modification of 19-norprogesterone i: 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
ATE437853T1 (de) * 2001-02-14 2009-08-15 Karobio Ab Glucocorticoid-rezeptoren-modulatoren
ES2212912B1 (es) * 2003-01-22 2005-10-01 Crystal Pharma, S.A. Procedimiento para la obtencion de 17alfa-acetoxi-11beta-(4-n,n-dimetilaminofenil)-19-norpregna-4,9-dien-3,20-diona.
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US20060247452A1 (en) * 2004-01-21 2006-11-02 Guisasola Luis Octavio S Method for obtaining 17sg(a)-acetoxy-11$g(b)-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione
JP5017109B2 (ja) * 2004-07-09 2012-09-05 ザ・ポピュレイション・カウンシル，インコーポレイテッド プロゲステロン受容体モジュレーターを含有する徐放性組成物
EP1862468A1 (de) * 2006-06-02 2007-12-05 Bayer Schering Pharma Aktiengesellschaft Kristallines 11beta-(4-Acetylphenyl)-20,20,21,21,21-pentafluor-17-hydroxy-19-nor-17alpha-pregna-4,9-dien-3-on
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EP2148681B1 (de) * 2007-04-20 2016-03-16 PregLem S.A. Selektive progesteronmodulatoren zur behandlung von uteriner blutung
HU228636B1 (en) * 2007-06-27 2013-04-29 Richter Gedeon Nyrt Industrial method for the synthesis of 17-acetoxy-11betha-4[-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
EP2532350A1 (de) 2007-10-17 2012-12-12 Laboratoire HRA Pharma Pharmazeutische Kombinationen mit einem Glucocorticoid Rezeptorantagonist und einem Cortisol Synthasehemmer zur Behandlung des Cushing-Syndroms
US8299050B2 (en) 2008-01-29 2012-10-30 Laboratoire Hra-Pharma Method for treating uterine fibroids
US8512745B2 (en) * 2008-12-08 2013-08-20 Laboratoire Hra Pharma Ulipristal acetate tablets
CA2757496A1 (en) 2009-04-14 2010-10-21 Andre Ulmann Method for on-demand contraception
DE102009034368A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-acyloxyalkylenphenyl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034366A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-methylenoxyalkylenaryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034367A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-benzyliden-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
DE102009034362A1 (de) 2009-07-20 2011-01-27 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-aryl-Derivate, Verfahren zu ihrer Herstellung und ihre Verwendung zur Behandlung von Krankheiten
DE102009034526A1 (de) 2009-07-21 2011-02-10 Bayer Schering Pharma Aktiengesellschaft 17-Hydroxy-17-pentafluorethyl-estra-4,9(10)-dien-11-ethinylphenyl-Derivate, Verfahren zu deren Herstellung und deren Verwendung zur Behandlung von Krankheiten
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US8426392B2 (en) 2009-12-09 2013-04-23 Laboratoire Hra-Pharma Method for providing emergency contraception
WO2011091892A1 (en) 2010-02-01 2011-08-04 Ulmann Andre A method for late post coital contraception using ulipristal acetate
WO2011091890A1 (en) 2010-02-01 2011-08-04 Laboratoire Hra-Pharma A method for post coital contraception in overweight for obese female subjects using ulipristal acetate
DE102010007722A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
DE102010007719A1 (de) 2010-02-10 2011-08-11 Bayer Schering Pharma Aktiengesellschaft, 13353 Progesteronrezeptorantagonisten
CN102906103A (zh) * 2010-03-22 2013-01-30 利普生物药剂公司 用于抗孕酮的非毒性递送的组合物和方法
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CN102344478B (zh) * 2011-07-22 2013-08-07 上海希迈医药科技有限公司 一种17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的结晶物及其制备方法
CN104628806A (zh) * 2012-01-19 2015-05-20 华润紫竹药业有限公司 甾体化合物及其制备方法和用途
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JP6322623B2 (ja) 2012-05-25 2018-05-09 ラボラトワール・アシュエールア−ファルマＬａｂｏｒａｔｏｉｒｅ Ｈｒａ−Ｐｈａｒｍａ 乳房腫瘍の予防および処置のための酢酸ウリプリスタル
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CN103073612B (zh) * 2013-02-04 2015-11-04 山东大学 醋酸乌利司他关键中间体的制备方法
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US5073548A (en) 1991-12-17
NO905546D0 (no) 1990-12-21
KR900701820A (ko) 1990-12-04
ATE149839T1 (de) 1997-03-15
DE122009000031I1 (de) 2009-11-05
WO1989012448A1 (en) 1989-12-28
EP0422100B1 (de) 1997-03-12
JPH03505582A (ja) 1991-12-05
NO905546L (no) 1990-12-21
DE122009000031I2 (de) 2011-06-16
CA1338906C (en) 1997-02-11
DK175760B1 (da) 2005-02-14
LU91575I2 (fr) 2009-08-03
EP0422100A1 (de) 1991-04-17
NO2009014I1 (no) 2009-07-06
AU635211B2 (en) 1993-03-18
JP2953725B2 (ja) 1999-09-27
NO178264C (de) 1996-02-21
AU3850689A (en) 1990-01-12
DK305390D0 (da) 1990-12-21
KR0161975B1 (ko) 1998-11-16
US4954490A (en) 1990-09-04
NO178264B (de) 1995-11-13
NO2009014I2 (no) 2009-12-28
DK305390A (da) 1990-12-21
DE68927861T2 (de) 1997-10-16
EP0422100A4 (de) 1994-04-27
NL300392I2 (nl) 2009-10-01
NL300392I1 (nl) 2009-08-03

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