AR071052A1 - Derivados de benzociclohepteno como estrogenos con actividad selectiva y composiciones farmaceuticas que los comprenden - Google Patents
Derivados de benzociclohepteno como estrogenos con actividad selectiva y composiciones farmaceuticas que los comprendenInfo
- Publication number
- AR071052A1 AR071052A1 ARP080104461A ARP080104461A AR071052A1 AR 071052 A1 AR071052 A1 AR 071052A1 AR P080104461 A ARP080104461 A AR P080104461A AR P080104461 A ARP080104461 A AR P080104461A AR 071052 A1 AR071052 A1 AR 071052A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- radical
- atom
- alkenyl
- perfluoro
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 9
- 125000000304 alkynyl group Chemical group 0.000 abstract 6
- 125000004429 atom Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- -1 perfluoro Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/23—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic, containing six-membered aromatic rings and other rings, with unsaturation outside the aromatic rings
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
- A61P5/30—Oestrogens
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C39/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring
- C07C39/12—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings
- C07C39/17—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a six-membered aromatic ring polycyclic with no unsaturation outside the aromatic rings containing other rings in addition to the six-membered aromatic rings, e.g. cyclohexylphenol
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C43/00—Ethers; Compounds having groups, groups or groups
- C07C43/02—Ethers
- C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
- C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
-
- 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
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
- C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Vascular Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
Reivindicacion 1: Compuestos caracterizados porque responden a la formula general (1) en la cual A es un resto de formula (2) en la cual X1 significa uno o más grupos en el anillo fenilo y representa en forma independiente en cada caso un halogeno, OH, radical alquilo C1-4, alquil C1-4-O, cicloalquil C3-6-O, acil C1-14-O, alquenilo C1-4, alquinilo C1-4, perfluoro(C1-4)alquilo, -CHO o CN, y X2 significa uno o más grupos en el anillo fenilo y representa en forma independiente en cada caso un H, halogeno, OH, radical alquilo C1-4, alquil C1-4-O, alquenilo C1-4, alquinilo C1-4, perfluoro(C1- 4)alquilo, -CHO o CN; R2 es un átomo de H, un radical alquilo C1-4, cicloalquilo C3-6 o acilo C1-14; R3 es un átomo de H o de F; R4 es un átomo de H, un radical alquilo C1-4, alquenilo C1-4, alquinilo C1-4, perfluoro(C1-4)alquilo, silil(C1-4)alquilo, un átomo de halogeno o un radical nitrilo; R5x y R5y significan independientemente entre sí un átomo de H, un alquilo C1-4, alquenilo C1-4, alquinilo C1-4, perfluoro(C1-4)alquilo, perfluoro(C1-4)alquenilo, alquil C1-4-O, arilo, heteroarilo o un grupo CN, o R5x y R5y juntos son un átomo de O, un átomo de S, un =CHZ en la cual Z significa un átomo de H, un radical alquilo C1-4, alquenilo C1-4, o R5x y R5y juntos son un radical alcanodiilo C2-4, alquenodiilo C2-6 o -OCH2- o R5y y R6 juntos representan una union, un radical alcanodiilo C1-4 o un alquenodiilo C2-6, y R5x tiene el significado dado precedentemente; R6 significa un átomo de H, un radical alquilo C1-4, alquenilo C1-4, alquinilo C1-4, perfluoro(C1- 4)alquilo o perfluoro(C1-4)alquenilo, o R6 y R5y juntos representan una union, un radical alcanodiilo C1-4o un alquenodiilo C2-6, y R5x tiene el significado dado precedentemente, o R6 y R7y juntos representan una union, un radical alcanodiilo C1-4 o un alquenodiilo C2-6, y R7x tiene el significado que se da más adelante; R7x y R7y representan independientemente entre sí un átomo de H, un radical alquilo C1-4, alquenilo C1-4, alquinilo C1-4, o R7x y R7y juntos representan un radical alcanodiilo C2-4, o alquenodiilo C2-6, o R7y y R6 juntos representan una union, un radical alcanodiilo C1-4 o un alquenodiilo C2-6, y R7x tiene el significado dado precedentemente. Reivindicacion 33: Composiciones farmacéuticas que comprenden al menos un compuesto de la formula general 1 de acuerdo con cualquiera de las reivindicaciones 1 a 32, caracterizadas porque cuando resulta apropiado se utilizan junto con excipientes y vehículos aceptables para uso farmacéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07075893A EP2048126A1 (de) | 2007-10-11 | 2007-10-11 | Benzocycloheptanderivate als selektiv wirksame Estrogene |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR071052A1 true AR071052A1 (es) | 2010-05-26 |
Family
ID=39167037
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080104461A AR071052A1 (es) | 2007-10-11 | 2008-10-14 | Derivados de benzociclohepteno como estrogenos con actividad selectiva y composiciones farmaceuticas que los comprenden |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20090099250A1 (es) |
| EP (2) | EP2048126A1 (es) |
| JP (1) | JP2011500538A (es) |
| AR (1) | AR071052A1 (es) |
| CA (1) | CA2700759A1 (es) |
| TW (1) | TW200927086A (es) |
| WO (1) | WO2009047343A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102010030538A1 (de) | 2010-06-25 | 2011-12-29 | Bayer Schering Pharma Aktiengesellschaft | 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| DE102011087987A1 (de) | 2011-12-08 | 2013-06-13 | Bayer Intellectual Property Gmbh | 6,7-Dihydro-5H-benzo[7]annulen-Derivate, Verfahren zu ihrer Herstellung, pharmazeutische Präparate die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| JOP20180012A1 (ar) * | 2012-08-07 | 2019-01-30 | Janssen Pharmaceutica Nv | عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد |
| WO2015017535A2 (en) * | 2013-08-02 | 2015-02-05 | Siemens Healthcare Diagnostics Inc. | Cell-based control and method |
| WO2015028409A1 (de) * | 2013-08-27 | 2015-03-05 | Bayer Pharma Aktiengesellschaft | 6,7-dihydro-5h-benzo[7]annulen-derivate, verfahren zu ihrer herstellung, pharmazeutische präparate die diese enthalten, sowie deren verwendung zur herstellung von arzneimitteln |
| HRP20211043T1 (hr) * | 2016-02-15 | 2021-10-01 | Sanofi | Derivati 6,7-dihidro-5h-benzo[7]anulena kao modulatori estrogenskih receptora |
| KR102477513B1 (ko) | 2016-11-17 | 2022-12-16 | 사노피 | 신규 치환된 n-(3-플루오로프로필)-피롤리딘 화합물, 그의 제조 방법 및 그의 치료 용도 |
| EP3434272A1 (en) | 2017-07-25 | 2019-01-30 | Sanofi | Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid |
| HUE059527T2 (hu) | 2018-09-07 | 2022-11-28 | Sanofi Sa | Eljárás metil-6-(2,4-diklórfenil)-5-[4-[(3S)-1-(3-fluorpropil)pirrolidin-3-il]oxifenil]-8,9 -dihidro-7H-benzo[7]annulén-2-karboxilát és sójának elõállítására |
| WO2020212543A1 (en) | 2019-04-18 | 2020-10-22 | Merck Patent Gmbh | Compounds for optically active devices |
| WO2021063967A1 (en) * | 2019-10-01 | 2021-04-08 | Sanofi | Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof |
| MX2022006990A (es) | 2019-12-09 | 2022-07-13 | Sanofi Sa | Forma cristalina de un derivado del acido 7h-benzo[7]anuleno-2-car boxilico. |
| TW202146007A (zh) | 2020-02-27 | 2021-12-16 | 法商賽諾菲公司 | 包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8813353D0 (en) | 1988-06-06 | 1988-07-13 | Ici Plc | Therapeutic product |
| DE19833786A1 (de) * | 1998-07-18 | 2000-01-20 | Schering Ag | Benzocycloheptene, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten, sowie deren Verwendung zur Herstellung von Arzneimitteln |
| WO2003000979A2 (en) | 2001-06-26 | 2003-01-03 | Traptek Llc | A treated yarn and methods for making same |
| PL374215A1 (en) * | 2001-08-11 | 2005-10-03 | Bristol-Myers Squibb Pharma Company | Selective estrogen receptor modulators |
| PL369464A1 (en) * | 2001-10-12 | 2005-04-18 | Schering Aktiengesellschaft | Synthesis of oxygen-substituted benzocycloheptenes, used as valuable intermediate products for producing tissue-selective oestrogens |
| CA2512000C (en) * | 2002-12-26 | 2011-08-09 | Eisai Co., Ltd. | Selective estrogen receptor modulator |
| US20060004087A1 (en) * | 2004-07-01 | 2006-01-05 | Wyeth | Tetracyclic compounds as estrogen ligands |
| ES2551086T3 (es) * | 2005-06-14 | 2015-11-16 | Baylor University | Análogos de combretastatina con actividad de unión a tubulina |
-
2007
- 2007-10-11 EP EP07075893A patent/EP2048126A1/de not_active Withdrawn
-
2008
- 2008-10-09 TW TW097139041A patent/TW200927086A/zh unknown
- 2008-10-10 CA CA2700759A patent/CA2700759A1/en not_active Abandoned
- 2008-10-10 JP JP2010528418A patent/JP2011500538A/ja active Pending
- 2008-10-10 WO PCT/EP2008/063664 patent/WO2009047343A1/en not_active Ceased
- 2008-10-10 US US12/249,056 patent/US20090099250A1/en not_active Abandoned
- 2008-10-10 EP EP08837938A patent/EP2200962A1/en not_active Withdrawn
- 2008-10-14 AR ARP080104461A patent/AR071052A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2009047343A1 (en) | 2009-04-16 |
| TW200927086A (en) | 2009-07-01 |
| JP2011500538A (ja) | 2011-01-06 |
| US20090099250A1 (en) | 2009-04-16 |
| CA2700759A1 (en) | 2009-04-16 |
| EP2200962A1 (en) | 2010-06-30 |
| EP2048126A1 (de) | 2009-04-15 |
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