HUP0300419A2 - Ösztrogén agonista/antagonista metabolitok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents
Ösztrogén agonista/antagonista metabolitok, ezeket tartalmazó gyógyszerkészítmények és alkalmazásukInfo
- Publication number
- HUP0300419A2 HUP0300419A2 HU0300419A HUP0300419A HUP0300419A2 HU P0300419 A2 HUP0300419 A2 HU P0300419A2 HU 0300419 A HU0300419 A HU 0300419A HU P0300419 A HUP0300419 A HU P0300419A HU P0300419 A2 HUP0300419 A2 HU P0300419A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- general formula
- pyrrolidin
- formula
- pharmaceutical compositions
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229940011871 estrogen Drugs 0.000 title 1
- 239000000262 estrogen Substances 0.000 title 1
- 239000002207 metabolite Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- IAJILQKETJEXLJ-UHFFFAOYSA-N Galacturonsaeure Natural products O=CC(O)C(O)C(O)C(O)C(O)=O IAJILQKETJEXLJ-UHFFFAOYSA-N 0.000 abstract 2
- IAJILQKETJEXLJ-QTBDOELSSA-N aldehydo-D-glucuronic acid Chemical compound O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)C(O)=O IAJILQKETJEXLJ-QTBDOELSSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229940097043 glucuronic acid Drugs 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- -1 2-oxo-pyrrolidin-1-yl group Chemical group 0.000 abstract 1
- 238000004458 analytical method Methods 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
- C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- 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
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- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- 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
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
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- 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
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/12—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of acyclic carbon skeletons
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/12—Oxygen or sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Vascular Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
Abstract
A jelen találmány tárgyát olyan vegyületek képezik, amelyek a (-)-cisz-6-fenil-5-[4-(2-(pirrolidin-l-il-etoxi)-fenil]-5,6,7,8-tetrahidro- naftalin-2-ol (I) általános képletű metabolitjai. Atalálmány szerinti vegyületek analitikai vizsgálatokhoz standardkénthasználhatók; valamint kémiai anyagok további kémiai szintézise vagybioszintézise során intermedierként szolgálhatnak. A találmány továbbitárgyát betegségek kezelésére szolgáló gyógyszerészeti készítmények éseljárások képezik. Az (I) általános képletben az R1 jelentésepirrolidin-l-il- vagy 2-oxo-pirrolidin-l-il -csoport, az (a) általánosképletű csoport vagy az -NH(CH2)3C-OR6 általános képletű csoport; azR5 jelentése hidrogénatom, metilcsoport, glükuronsav, vagyszulfocsoport; az R2, az R3, az R4 és az R7 jelentése azonos vagykülönböző, és ezek a következők közül kerülhetnek ki: hidrogénatomvagy az OR5 általános képletű csoport; továbbá az R6 jelentésehidroxi-csoport, az -NHCH2COOH vagy az -NHCH2CH2SO3H képletű csoport,illetve glükuronsav. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26719800P | 2000-04-07 | 2000-04-07 | |
| PCT/IB2001/000427 WO2001077093A1 (en) | 2000-04-07 | 2001-03-19 | Estrogen agonist/antagonist metabolites |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0300419A2 true HUP0300419A2 (hu) | 2003-06-28 |
| HUP0300419A3 HUP0300419A3 (en) | 2005-07-28 |
Family
ID=23017734
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0300419A HUP0300419A3 (en) | 2000-04-07 | 2001-03-19 | Estrogen agonist/antagonist metabolites, pharmaceutical compositions containing them and their use |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US6455572B1 (hu) |
| EP (1) | EP1268453B1 (hu) |
| JP (1) | JP2004510693A (hu) |
| KR (1) | KR20020089434A (hu) |
| CN (1) | CN1209353C (hu) |
| AP (1) | AP2002002641A0 (hu) |
| AR (1) | AR035330A1 (hu) |
| AT (1) | ATE333450T1 (hu) |
| AU (2) | AU2001240985B2 (hu) |
| BG (1) | BG107137A (hu) |
| BR (1) | BR0109838A (hu) |
| CA (1) | CA2405070A1 (hu) |
| CR (1) | CR6766A (hu) |
| CZ (1) | CZ20023223A3 (hu) |
| DE (1) | DE60121557T2 (hu) |
| DK (1) | DK1268453T3 (hu) |
| EA (1) | EA004866B1 (hu) |
| EE (1) | EE200200580A (hu) |
| ES (1) | ES2266169T3 (hu) |
| HK (1) | HK1052511B (hu) |
| HR (1) | HRP20020802A2 (hu) |
| HU (1) | HUP0300419A3 (hu) |
| IL (1) | IL152082A0 (hu) |
| IS (1) | IS6549A (hu) |
| MA (1) | MA26890A1 (hu) |
| MX (1) | MXPA02009940A (hu) |
| NO (1) | NO20024767L (hu) |
| OA (1) | OA12325A (hu) |
| PA (1) | PA8514901A1 (hu) |
| PE (1) | PE20011183A1 (hu) |
| PL (1) | PL358593A1 (hu) |
| PT (1) | PT1268453E (hu) |
| SK (1) | SK14092002A3 (hu) |
| TN (1) | TNSN01052A1 (hu) |
| TR (1) | TR200202310T2 (hu) |
| UY (1) | UY26656A1 (hu) |
| WO (1) | WO2001077093A1 (hu) |
| ZA (1) | ZA200207995B (hu) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5631365A (en) | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
| US7001926B2 (en) | 2000-03-10 | 2006-02-21 | Oxigene, Inc. | Tubulin binding agents and corresponding prodrug constructs |
| US7091240B2 (en) | 2000-03-10 | 2006-08-15 | Oxigene, Inc. | Tubulin binding ligands and corresponding prodrug constructs |
| CZ20002567A3 (cs) * | 2000-07-11 | 2001-12-12 | Léčiva, A.S. | Tableta vyrobitelná přímým tabletováním, obsahující aktivní látku kyselinu 4-amino-1-hydroxybutyliden-1,1-bisfosfonovou, a způsob její výroby |
| EP1192945A3 (en) * | 2000-09-21 | 2004-03-03 | Pfizer Products Inc. | Use of an estrogen agonist/antagonist for treating osteoarthritis |
| AU781168B2 (en) * | 2001-01-26 | 2005-05-12 | Pfizer Products Inc. | Method of treating certain cancers using an estrogen agonist/antagonist |
| US7479504B2 (en) * | 2002-01-18 | 2009-01-20 | Merck & Co., Inc. | Edg receptor agonists |
| AU2003208516A1 (en) * | 2002-03-14 | 2003-09-22 | Warner-Lambert Company Llc | Method for characterizing metabolites using hydrogen/deuterium exchange |
| US20050095241A1 (en) * | 2003-08-26 | 2005-05-05 | Vadlamudi Ratna K. | Estrogen receptor modulators and uses thereof |
| US7456214B2 (en) | 2004-05-03 | 2008-11-25 | Baylor University | Chromene-containing compounds with anti-tubulin and vascular targeting activity |
| AU2012200714B2 (en) * | 2004-08-13 | 2014-04-17 | Wyeth Llc | Tanaproget derivatives, metabolites, and uses thereof |
| PT1778710E (pt) * | 2004-08-13 | 2012-04-12 | Wyeth Llc | Derivados de tanaproget, metabolitos e suas utilizações |
| WO2006136944A1 (en) * | 2005-06-22 | 2006-12-28 | Pfizer Products Inc. | Stereoselective hydrogenation process for preparing cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-2-methoxy-5,6,7,8-tetrahydronaphthalene hydrochloride |
| US7902147B2 (en) | 2007-11-05 | 2011-03-08 | Duke University | Chronic lymphocytic leukemia prognosis and treatment |
| TW201043595A (en) * | 2009-03-13 | 2010-12-16 | Organon Nv | Tetrahydronaphthalen-2-ol derivatives |
| US9845291B2 (en) | 2014-12-18 | 2017-12-19 | Genentech, Inc. | Estrogen receptor modulators and uses thereof |
| WO2017168174A1 (en) | 2016-04-02 | 2017-10-05 | N4 Pharma Uk Limited | New pharmaceutical forms of sildenafil |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3522319A (en) * | 1964-01-23 | 1970-07-28 | Ciba Geigy Corp | Phenol substituted tetrahydronaphthalenes useful as estrogenics |
| US5552412A (en) | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
| UA51676C2 (uk) | 1995-11-02 | 2002-12-16 | Пфайзер Інк. | (-)цис-6(s)-феніл-5(r)[4-(2-піролідин-1-ілетокси)феніл]-5,6,7,8-тетрагідронафталін-2-ол d-тартрат, спосіб його одержання, спосіб лікування захворювань, що піддаються лікуванню агоністами естрогену, та фармацевтична композиція |
| IL120266A (en) | 1996-02-28 | 2005-05-17 | Pfizer | Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions |
| TW442286B (en) | 1996-02-28 | 2001-06-23 | Pfizer | New therapeutic uses of estrogen agonists |
| US6358951B1 (en) | 1998-08-21 | 2002-03-19 | Pfizer Inc. | Growth hormone secretagogues |
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