ES2041245T3 - Esteroides angioestaticos. - Google Patents

Esteroides angioestaticos.

Info

Publication number
ES2041245T3
ES2041245T3 ES198686906631T ES86906631T ES2041245T3 ES 2041245 T3 ES2041245 T3 ES 2041245T3 ES 198686906631 T ES198686906631 T ES 198686906631T ES 86906631 T ES86906631 T ES 86906631T ES 2041245 T3 ES2041245 T3 ES 2041245T3
Authority
ES
Spain
Prior art keywords
bond
alkyl
beta
integer
forms
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
ES198686906631T
Other languages
English (en)
Inventor
Paul A. Aristoff
Harvey I. Skulnick
Wendell Wierenga
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.)
Pharmacia and Upjohn Co
Original Assignee
Upjohn Co
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 Upjohn Co filed Critical Upjohn Co
Application granted granted Critical
Publication of ES2041245T3 publication Critical patent/ES2041245T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0061—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16
    • C07J5/0069—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • C07J7/005—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 substituted in position 16
    • C07J7/0055—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 substituted in position 16 by a saturated or unsaturated hydrocarbon group

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Esteroides angioestáticos. Uso de un compuesto de la fórmula I **fórmula** para la manufactura de un medicamento para uso en la inhibición de angiogénesis en un animal de sangre caliente, en que R1 es Beta-CH3 ó Beta-C2H5; R4 es H, CH3, Cl ó F; R6 es H ó CH3; R9 es H, OH, CH3, F ó =CH2; R10 es H, OH ó CH3; R13 es H, OH, = O, -O-PO(OH)2, ó -O-CO-(CH2)t COOH en que t es un número entero desde 2 a 6; R15 es= O ó H,OH; ------indica un enlace simple o doble a condición de que el enlace 16, 17 sea simple cuando R9 es = CH2 y que el enlace 4, 5 es simple cuando R13 es = O; R23 es OH, -O-CO-R11, -O-PO(OH)2 ó -O-CO-(CH2)t COOH, en que t es un número entero de 2 a 6; y R11 es -Y(CH2)rQ, -Y-(CH2)n-X-(CH2)m-SO3H ó -Y''-(CH2)p-X''-(CH2)q-NR16R17; en que Y es un enlace ó -O-; Y'' es un enlace, -O- o -S-; cada uno de X y X'' es un enlace, -CON(R18)-, -N(R18)CO-, -O-, -S-, -SO- ó -SO2-; R18 es H ó C1-4 alquilo; alguno de R16 y R17 es C1-4 alquilo ó C1-4 hidroxialquilo ó NR16 R17 es pirrolidino, piperidino, morfolino, tiomorfolino, piperazino ó N-(C1-4 alquilo) piperazino; y m, n, p, q y r son números enteros satisfaciendo: 1<m<5; 4<n<9; 2<p<9; 1<q<5; 2<r<9; m+n<10; p+q<10 (a condición de que 4<p+q<9 cuando X'' es un enlace) y Q es (1) -R19-CH2COOH, en que R19 es -S-, -SO-, -SO2, -SO2N(R20) ó -N(R20)SO2-; y R20 es H ó C1-4 alquilo; bajo la condición de que el número total de átomos de carbono en R20 y (CH2)r no sea mayor que 10; (2) -CO-COOH; (3) -CO-NH-CHR22-COOH, en que R22 es H, CH3, -CH2COOH, -CH2CH2-COOH, -CH2OH, -CH2SH, -CH2CH2SCH3 ó p-hidroxibencilo; (4) -CO-NCH3-CH2-COOH; (5) (2-carboxi-1-pirrolinil)carbonilo, ó (6) -NHCH2CONHCH2COOH; o una de sus sales mono o bis farmacéuticamente aceptables. (Reserva del art. 167.2 CPE)
ES198686906631T 1985-10-23 1986-10-16 Esteroides angioestaticos. Expired - Lifetime ES2041245T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US79056485A 1985-10-23 1985-10-23
US81186685A 1985-12-20 1985-12-20

Publications (1)

Publication Number Publication Date
ES2041245T3 true ES2041245T3 (es) 1993-11-16

Family

ID=27121047

Family Applications (1)

Application Number Title Priority Date Filing Date
ES198686906631T Expired - Lifetime ES2041245T3 (es) 1985-10-23 1986-10-16 Esteroides angioestaticos.

Country Status (9)

Country Link
EP (2) EP0245357B1 (es)
JP (1) JP2545522B2 (es)
AT (1) ATE66002T1 (es)
DE (1) DE3680788D1 (es)
ES (1) ES2041245T3 (es)
GR (1) GR3002675T3 (es)
HK (1) HK129594A (es)
SG (1) SG99594G (es)
WO (1) WO1987002672A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4876250A (en) * 1988-10-31 1989-10-24 Alcon Laboratories, Inc. Methods for controlling ocular hypertension with angiostatic steroids
US5407926A (en) * 1987-12-29 1995-04-18 Alcon Laboratories, Inc. Ophthalmic composition
AU657690B2 (en) * 1990-06-11 1995-03-23 Alcon Laboratories, Inc. Steroids which inhibit angiogenesis
US5972922A (en) * 1990-06-11 1999-10-26 Alcon Laboratories, Inc. Steroids which inhibit angiogenesis
EP1236470A3 (en) * 1991-11-22 2004-09-01 Alcon Laboratories, Inc. Angiostatic steroids
US5929111A (en) * 1996-12-18 1999-07-27 Alcon Laboratories, Inc. A-seco steroids effective at treating ophthalmic pathological neovascularization and controlling intraocular pressure
US6596703B1 (en) 1997-07-11 2003-07-22 Jagotec Ag Promotion of wound healing utilizing steroids having reduced deteriorous systemic side effects typical of glucocorticoids, mineralocorticoids and sex steroids
US6011023A (en) * 1997-08-27 2000-01-04 Alcon Laboratories, Inc. Angiostatic steroids
BR122020006408B1 (pt) 2013-03-29 2021-09-28 The Johns Hopkins University Dose unitária de unidades formadoras de colônia de c. novyi, composição farmacêutica e uso de c. novyi nt para tratar ou atenuar um efeito de um tumor sólido presente em um ser humano
WO2015191602A2 (en) 2014-06-09 2015-12-17 Biomed Valley Discoveries, Inc. Combination therapies targeting tumor-associated stroma or tumor cells
ES2830044T3 (es) 2015-01-30 2021-06-02 Biomed Valley Discoveries Inc Malonato de C21H22C12N4O2 cristalino
US9676746B2 (en) 2015-01-30 2017-06-13 Biomed Valley Discoveries, Inc. Crystalline forms of C21H22Cl2N4O2

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2868783A (en) * 1958-04-14 1959-01-13 Upjohn Co 11-oxygenated-17alpha, 21-dihydroxy-4-pregnen-20-ones and the 21-esters thereof
US3098085A (en) * 1958-07-04 1963-07-16 Ciba Geigy Corp Process for the manufacture of 16alpha-methyl-allopregnanes substituted in the 21-position
US3083199A (en) * 1961-01-11 1963-03-26 Farmaceutici Italia delta3-5alpha-steroids and 3alpha-hydroxy-5alpha-steroids and the preparation thereof
US3045033A (en) * 1961-05-10 1962-07-17 Schering Corp Water soluble cyclophosphate esters of steroids and process for preparing same
US3402173A (en) 1965-03-19 1968-09-17 Syntex Corp 18-lower alkyl pregnanes and derivatives
US3780177A (en) 1967-06-16 1973-12-18 Warner Lambert Co 17-butyrate,21-ester derivatives of 6alpha,9alpha-difluoroprednisolone,compositions and use
DE2257132C3 (de) * 1972-11-18 1982-05-13 Schering Ag, 1000 Berlin Und 4619 Bergkamen Verfahren zur Reduktion von 3-Ketosteroiden
US3980778A (en) 1973-10-25 1976-09-14 The Upjohn Company Anti-inflammatory steroid
EP0001737B1 (de) * 1977-10-26 1981-01-07 Schering Aktiengesellschaft 17-Alpha-(3-Jodbenzoyloxy)-9-Alpha-chlor-4-pregnen-3.20-dione, deren D-Homo-analoga und Verfahren zu ihrer Herstellung
US4318853A (en) * 1980-01-31 1982-03-09 The Upjohn Company 9β,11β-Epoxy-5β-corticoids
ZA817929B (en) 1980-12-22 1982-10-27 Upjohn Co 5alpha-and 5beta-androstane-17beta-carboxylates
US4456602A (en) * 1982-08-23 1984-06-26 The Upjohn Company Amine containing ester prodrugs of corticosteroids
US4443440A (en) * 1982-08-30 1984-04-17 The Upjohn Company Amine containing ester prodrugs of corticosteroids
US4469689A (en) * 1983-03-30 1984-09-04 The Upjohn Company Sulfonate containing ester prodrugs of corticosteroids
US4588718A (en) * 1984-03-28 1986-05-13 The Upjohn Company Carboxy containing ester prodrugs of corticosteroids
CA1310009C (en) * 1984-03-28 1992-11-10 John Mark Braughler Ester prodrugs of steroids

Also Published As

Publication number Publication date
EP0245357B1 (en) 1991-08-07
DE3680788D1 (de) 1991-09-12
EP0245357A1 (en) 1987-11-19
HK129594A (en) 1994-11-25
WO1987002672A1 (en) 1987-05-07
SG99594G (en) 1994-10-28
ATE66002T1 (de) 1991-08-15
EP0221705A1 (en) 1987-05-13
GR3002675T3 (en) 1993-01-25
JPS63501292A (ja) 1988-05-19
JP2545522B2 (ja) 1996-10-23

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