IL117398A - Benzothiophene derivatives and pharmaceutical compositions containing them - Google Patents

Benzothiophene derivatives and pharmaceutical compositions containing them

Info

Publication number: IL117398A
Authority: IL; Israel
Prior art keywords: alkyl; rdurule; aryl; compounds; progestin
Prior art date: 1995-03-10

Application number

IL11739896A

Other languages

English (en)

Other versions

IL117398A0 (en

Original Assignee

Lilly Co Eli

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.)

1995-03-10

Filing date

1996-03-07

Publication date

2000-11-21

1996-03-07 Application filed by Lilly Co Eli filed Critical Lilly Co Eli

1996-07-23 Publication of IL117398A0 publication Critical patent/IL117398A0/xx

2000-11-21 Publication of IL117398A publication Critical patent/IL117398A/xx

Links

239000008194 pharmaceutical composition Substances 0.000 title abstract 2
FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical class C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title 1
125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical class C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 abstract 5
125000003118 aryl group Chemical group 0.000 abstract 5
150000001875 compounds Chemical class 0.000 abstract 5
125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 3
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
239000000262 estrogen Substances 0.000 abstract 3
229940011871 estrogen Drugs 0.000 abstract 3
239000000583 progesterone congener Substances 0.000 abstract 3
125000006729 (C2-C5) alkenyl group Chemical group 0.000 abstract 2
YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
XBQNZPDIRJPFAI-UHFFFAOYSA-N 3,3-dimethylpyrrolidine Chemical compound CC1(C)CCNC1 XBQNZPDIRJPFAI-UHFFFAOYSA-N 0.000 abstract 1
RDEHRKLSYJBKDV-UHFFFAOYSA-N 3,4-dimethylpyrrolidine Chemical compound CC1CNCC1C RDEHRKLSYJBKDV-UHFFFAOYSA-N 0.000 abstract 1
KYINPWAJIVTFBW-UHFFFAOYSA-N 3-methylpyrrolidine Chemical compound CC1CCNC1 KYINPWAJIVTFBW-UHFFFAOYSA-N 0.000 abstract 1
201000009273 Endometriosis Diseases 0.000 abstract 1
206010027304 Menopausal symptoms Diseases 0.000 abstract 1
206010028980 Neoplasm Diseases 0.000 abstract 1
208000001132 Osteoporosis Diseases 0.000 abstract 1
206010046798 Uterine leiomyoma Diseases 0.000 abstract 1
XYOVOXDWRFGKEX-UHFFFAOYSA-N azepine Chemical compound N1C=CC=CC=C1 XYOVOXDWRFGKEX-UHFFFAOYSA-N 0.000 abstract 1
201000011510 cancer Diseases 0.000 abstract 1
230000004663 cell proliferation Effects 0.000 abstract 1
HPXRVTGHNJAIIH-UHFFFAOYSA-N cyclohexanol Chemical group OC1CCCCC1 HPXRVTGHNJAIIH-UHFFFAOYSA-N 0.000 abstract 1
230000001419 dependent effect Effects 0.000 abstract 1
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
230000002526 effect on cardiovascular system Effects 0.000 abstract 1
125000001475 halogen functional group Chemical group 0.000 abstract 1
230000002401 inhibitory effect Effects 0.000 abstract 1
201000010260 leiomyoma Diseases 0.000 abstract 1
229960004296 megestrol acetate Drugs 0.000 abstract 1
RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 abstract 1
229910052757 nitrogen Inorganic materials 0.000 abstract 1
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
229940053934 norethindrone Drugs 0.000 abstract 1
VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 abstract 1
XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 abstract 1
230000001575 pathological effect Effects 0.000 abstract 1
230000001072 progestational effect Effects 0.000 abstract 1
229960003387 progesterone Drugs 0.000 abstract 1
239000000186 progesterone Substances 0.000 abstract 1
208000037803 restenosis Diseases 0.000 abstract 1
150000003839 salts Chemical class 0.000 abstract 1
210000000329 smooth muscle myocyte Anatomy 0.000 abstract 1
208000024891 symptom Diseases 0.000 abstract 1
208000010579 uterine corpus leiomyoma Diseases 0.000 abstract 1
201000007954 uterine fibroid Diseases 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Animal Behavior & Ethology (AREA)
Engineering & Computer Science (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Endocrinology (AREA)
Reproductive Health (AREA)
Urology & Nephrology (AREA)
Gynecology & Obstetrics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Steroid Compounds (AREA)

IL11739896A 1995-03-10 1996-03-07 Benzothiophene derivatives and pharmaceutical compositions containing them IL117398A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US08/402,415 US6395755B1 (en)	1995-03-10	1995-03-10	Benzothiophene pharmaceutical compounds

Publications (2)

Publication Number	Publication Date
IL117398A0 IL117398A0 (en)	1996-07-23
IL117398A true IL117398A (en)	2000-11-21

Family

ID=23591799

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL11739896A IL117398A (en)	1995-03-10	1996-03-07	Benzothiophene derivatives and pharmaceutical compositions containing them

Country Status (16)

Country	Link
US (1)	US6395755B1 (de)
EP (2)	EP0953568B1 (de)
JP (1)	JPH11501930A (de)
AT (2)	ATE247100T1 (de)
AU (1)	AU697502B2 (de)
BR (1)	BR9607775A (de)
CA (1)	CA2214261A1 (de)
DE (2)	DE69609748T2 (de)
DK (1)	DK0731100T3 (de)
ES (2)	ES2148681T3 (de)
GR (1)	GR3034762T3 (de)
IL (1)	IL117398A (de)
PT (1)	PT731100E (de)
SI (1)	SI0731100T1 (de)
WO (1)	WO1996028155A1 (de)
ZA (1)	ZA961883B (de)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US6432982B1 (en) *	1996-02-21	2002-08-13	Eli Lilly And Company	Benzothiophenes, and formulations and methods using same
EP0801066A1 (de) *	1996-03-12	1997-10-15	Eli Lilly And Company	Heterozyklisch substituierte Benzothiophene und pharmazeutische Zusammensetzungen
CA2214072C (en) *	1996-08-29	2006-11-14	Eli Lilly And Company	Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods
CA2214196A1 (en) *	1996-09-26	1998-03-26	Eli Lilly And Company	Benzo[b]indeno[2,1-d]thiophene compounds, intermediates, processes, compositions and methods
CA2216592C (en) *	1996-10-24	2006-07-18	Brian Stephen Muehl	Benzothiophene compounds, intermediates, compositions, and methods
EP1401446B1 (de)	2001-05-22	2005-02-09	Eli Lilly And Company	Tetrahydrochinolin-derivate zur behandlung von krankheiten ausgelöst durch zu hohem oder zu niedrigem oestrogenspiegel
EP1395563B1 (de)	2001-05-22	2006-03-29	Eli Lilly And Company	2-substituierte 1,2,3,4-tetrahydrochinoline und derivate davon, zusammensetzungen und verfahren
CN1599606A (zh)	2001-07-31	2005-03-23	辉瑞产品公司	包含雌激素激动剂/拮抗剂、雌激素与孕激素组合的药物组合物、试剂盒和方法
ATE448215T1 (de) *	2004-01-22	2009-11-15	Lilly Co Eli	Selektive östrogen-rezeptor-modulatoren
GR1005694B (el) *	2005-06-08	2007-10-22	Αλεξης Μιχαηλ	Ιστοειδικα αντιοιστρογονα ειδικα για τον αλφα υποδοχεα των οιστρογονων

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE1300575B (de) *	1965-05-21	1969-08-07	Bristol Myers Co	Benzo[b]thiophene
US3947470A (en)	1974-06-20	1976-03-30	Smithkline Corporation	Substituted benzofurans and benzothiophenes
US4133814A (en) *	1975-10-28	1979-01-09	Eli Lilly And Company	2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
IT1154888B (it) *	1980-11-12	1987-01-21	Menarini Sas	Derivati del benzofurano 2-sostituiti e relativi metodi di preparazione
IL65379A0 (en) *	1981-04-03	1982-05-31	Lilly Co Eli	Process for preparing acylated benzothiophenes
GB2097788B (en) *	1981-04-03	1985-04-24	Lilly Co Eli	Benzothiophene compounds and process for preparing them
US4418068A (en) *	1981-04-03	1983-11-29	Eli Lilly And Company	Antiestrogenic and antiandrugenic benzothiophenes
US4380635A (en)	1981-04-03	1983-04-19	Eli Lilly And Company	Synthesis of acylated benzothiophenes
US4851554A (en)	1987-04-06	1989-07-25	University Of Tennessee Research Corporation	Certain 3-substituted 2-alkyl benzofuran derivatives
WO1989002893A1 (en) *	1987-09-30	1989-04-06	The University Of Tennessee Research Corporation	Certain 3-substituted 2-alkyl benzothiophene derivatives
US5395842A (en) *	1988-10-31	1995-03-07	Endorecherche Inc.	Anti-estrogenic compounds and compositions
FR2665444B1 (fr) *	1990-08-06	1992-11-27	Sanofi Sa	Derives d'amino-benzofuranne, benzothiophene ou indole, leur procede de preparation ainsi que les compositions les contenant.
DE4117512A1 (de) *	1991-05-25	1992-11-26	Schering Ag	2-phenylbenzo(b)furane und -thiophene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate
JP3157882B2 (ja) *	1991-11-15	2001-04-16	帝国臓器製薬株式会社	新規なベンゾチオフエン誘導体
TW366342B (en)	1992-07-28	1999-08-11	Lilly Co Eli	The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss
US5482949A (en)	1993-03-19	1996-01-09	Eli Lilly And Company	Sulfonate derivatives of 3-aroylbenzo[b]thiophenes
US6756388B1 (en) *	1993-10-12	2004-06-29	Pfizer Inc.	Benzothiophenes and related compounds as estrogen agonists
US5523309A (en) *	1995-03-10	1996-06-04	Eli Lilly And Company	Benzofuran pharmaceutical compounds

1995
- 1995-03-10 US US08/402,415 patent/US6395755B1/en not_active Expired - Fee Related
1996
- 1996-03-06 DK DK96301534T patent/DK0731100T3/da active
- 1996-03-06 DE DE69609748T patent/DE69609748T2/de not_active Expired - Fee Related
- 1996-03-06 SI SI9630256T patent/SI0731100T1/xx unknown
- 1996-03-06 PT PT96301534T patent/PT731100E/pt unknown
- 1996-03-06 DE DE69629500T patent/DE69629500T2/de not_active Expired - Fee Related
- 1996-03-06 ES ES96301534T patent/ES2148681T3/es not_active Expired - Lifetime
- 1996-03-06 EP EP99202800A patent/EP0953568B1/de not_active Expired - Lifetime
- 1996-03-06 AT AT99202800T patent/ATE247100T1/de not_active IP Right Cessation
- 1996-03-06 ES ES99202800T patent/ES2205702T3/es not_active Expired - Lifetime
- 1996-03-06 AT AT96301534T patent/ATE195519T1/de not_active IP Right Cessation
- 1996-03-06 EP EP96301534A patent/EP0731100B1/de not_active Expired - Lifetime
- 1996-03-07 IL IL11739896A patent/IL117398A/xx not_active IP Right Cessation
- 1996-03-07 WO PCT/US1996/003164 patent/WO1996028155A1/en not_active Ceased
- 1996-03-07 BR BR9607775A patent/BR9607775A/pt not_active Application Discontinuation
- 1996-03-07 AU AU53048/96A patent/AU697502B2/en not_active Ceased
- 1996-03-07 ZA ZA9601883A patent/ZA961883B/xx unknown
- 1996-03-07 JP JP8527729A patent/JPH11501930A/ja active Pending
- 1996-03-07 CA CA002214261A patent/CA2214261A1/en not_active Abandoned
2000
- 2000-11-07 GR GR20000402451T patent/GR3034762T3/el not_active IP Right Cessation

Also Published As

Publication number	Publication date
EP0731100A1 (de)	1996-09-11
DE69609748T2 (de)	2001-04-12
US6395755B1 (en)	2002-05-28
IL117398A0 (en)	1996-07-23
JPH11501930A (ja)	1999-02-16
CA2214261A1 (en)	1996-09-19
ES2148681T3 (es)	2000-10-16
MX9706737A (es)	1997-11-29
SI0731100T1 (en)	2001-02-28
EP0953568A1 (de)	1999-11-03
GR3034762T3 (en)	2001-02-28
DE69629500T2 (de)	2004-07-01
AU5304896A (en)	1996-10-02
PT731100E (pt)	2001-01-31
DE69629500D1 (de)	2003-09-18
ATE195519T1 (de)	2000-09-15
DK0731100T3 (da)	2000-09-18
DE69609748D1 (de)	2000-09-21
WO1996028155A1 (en)	1996-09-19
BR9607775A (pt)	1998-07-07
ZA961883B (en)	1997-09-08
EP0731100B1 (de)	2000-08-16
ES2205702T3 (es)	2004-05-01
AU697502B2 (en)	1998-10-08
EP0953568B1 (de)	2003-08-13
ATE247100T1 (de)	2003-08-15

Legal Events

Date	Code	Title
2001-04-30	FF	Patent granted
2001-07-24	KB	Patent renewed
2006-12-07	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
CA2228997A1 (en)	1997-02-27	Benzothiophene compounds
MY132075A (en)	2007-09-28	Naphthyl compounds, intermediates, processes, compositions, and methods
AU692690B2 (en)	1998-06-11	Novel benzofuran pharmaceutical compounds useful for alleviating the symptoms of post menopausal syndrome
SI0731100T1 (en)	2001-02-28	Benzothiophene pharmaceutical compounds
IE46092L (en)	1978-05-26	Esters of the androstane and oestrane series
PL324816A1 (en)	1998-06-22	Naphtylic and dihydronaphtylic intermediatew compounds, compounds, agents and associated compounds
EP0774966A4 (de)	1998-01-07	Benzofuranverbindungen, präparate und verfahren
MX9706741A (es)	1997-11-29	Compuestos farmaceuticos novedosos de naftilo.
NZ334184A (en)	2000-04-28	Naphthyl compounds, intermediates, compositions for the prevention of bone loss or bone resorption and lower cholesterol
EP0827959A3 (de)	1998-03-18	Benzo[B]thiophenverbindungen,Zwischenprodukte,Verfahren,Zusammensetzungen und Methode
NO973470L (no)	1997-07-28	Fremgangsmåte for minsking av serumkalsiumnivåer