WO2002003976A3 - Combinations of bisphosphonates, estrogenic agents and optionally estrogens - Google Patents
Combinations of bisphosphonates, estrogenic agents and optionally estrogens Download PDFInfo
- Publication number
- WO2002003976A3 WO2002003976A3 PCT/US2001/020970 US0120970W WO0203976A3 WO 2002003976 A3 WO2002003976 A3 WO 2002003976A3 US 0120970 W US0120970 W US 0120970W WO 0203976 A3 WO0203976 A3 WO 0203976A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- alkyl
- ethers
- optionally
- bisphosphonates
- combinations
- Prior art date
Links
- 239000000262 estrogen Substances 0.000 title abstract 3
- 229940122361 Bisphosphonate Drugs 0.000 title abstract 2
- 150000004663 bisphosphonates Chemical class 0.000 title abstract 2
- 229940011871 estrogen Drugs 0.000 title abstract 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 2
- 150000002170 ethers Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical class 0.000 abstract 1
- 208000020084 Bone disease Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 239000008280 blood Substances 0.000 abstract 1
- 210000004369 blood Anatomy 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical class *C#N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- SMYMDRJWEFCCCI-UHFFFAOYSA-N trichloro(trichloromethoxy)methane Chemical compound ClC(Cl)(Cl)OC(Cl)(Cl)Cl SMYMDRJWEFCCCI-UHFFFAOYSA-N 0.000 abstract 1
- WZEOZJQLTRFNCU-UHFFFAOYSA-N trifluoro(trifluoromethoxy)methane Chemical compound FC(F)(F)OC(F)(F)F WZEOZJQLTRFNCU-UHFFFAOYSA-N 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical class FC(F)(F)* 0.000 abstract 1
Classifications
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
- A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/66—Phosphorus compounds
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
This invention comprises methods of treating bone disorders and lowering blood LDL levels comprising administration of a bisphosphonate, and compound of the formula (I) or (II), wherein Z is a moiety selected from the group of (a), (b), or (c); wherein: R1 is selected from H, OH or the C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety (1); R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof, and optionally an estrogen.
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01952365A EP1299093A2 (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
| AU2001273125A AU2001273125A1 (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
| JP2002508431A JP2004502730A (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optional estrogens |
| BR0112364-5A BR0112364A (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogens and optionally estrogens |
| MXPA02012897A MXPA02012897A (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optionally estrogens. |
| CA002415052A CA2415052A1 (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21618800P | 2000-07-06 | 2000-07-06 | |
| US21606900P | 2000-07-06 | 2000-07-06 | |
| US60/216,188 | 2000-07-06 | ||
| US60/216,069 | 2000-07-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2002003976A2 WO2002003976A2 (en) | 2002-01-17 |
| WO2002003976A3 true WO2002003976A3 (en) | 2003-01-03 |
Family
ID=26910620
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2001/020970 WO2002003976A2 (en) | 2000-07-06 | 2001-06-29 | Combinations of bisphosphonates, estrogenic agents and optionally estrogens |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1299093A2 (en) |
| JP (1) | JP2004502730A (en) |
| CN (1) | CN1450913A (en) |
| AU (1) | AU2001273125A1 (en) |
| BR (1) | BR0112364A (en) |
| CA (1) | CA2415052A1 (en) |
| MX (1) | MXPA02012897A (en) |
| WO (1) | WO2002003976A2 (en) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001271781A1 (en) * | 2000-07-06 | 2002-01-21 | Wyeth | Use of substituted indole compounds for treating sphincter incontinence |
| US6376486B1 (en) | 2000-07-06 | 2002-04-23 | American Home Products Corporation | Methods of inhibiting sphincter incontinence |
| US6455568B2 (en) | 2000-07-06 | 2002-09-24 | Wyeth | Combination therapy for inhibiting sphincter incontinence |
| EP1545206B1 (en) | 2002-07-24 | 2020-03-04 | Children's Hospital Medical Center | Compositions and products containing enantiomeric equol, and methods for their making |
| US8668914B2 (en) | 2002-07-24 | 2014-03-11 | Brigham Young University | Use of equol for treating skin diseases |
| JP4889944B2 (en) | 2002-10-29 | 2012-03-07 | コロラド ステート ユニバーシティー リサーチ ファウンデーション | Use of equol to treat androgen-mediated diseases |
| US8580846B2 (en) | 2002-10-29 | 2013-11-12 | Brigham Young University | Use of equol for ameliorating or preventing neuropsychiatric and neurodegenerative diseases or disorders |
| DK1790347T3 (en) | 2002-12-20 | 2015-01-19 | Hoffmann La Roche | Ibandronate high-dose-formulation |
| US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| NZ779654A (en) | 2015-10-01 | 2024-12-20 | Olema Pharmaceuticals Inc | Tetrahydro-1h-pyrido[3,4-b]indole anti-estrogenic drugs |
| HRP20221462T1 (en) | 2015-12-09 | 2023-01-20 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective estrogen receptor downregulators |
| CN109641874A (en) | 2016-05-10 | 2019-04-16 | C4医药公司 | C for target protein degradation3The glutarimide degron body of carbon connection |
| WO2017197051A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| ES2989988T3 (en) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Heterocyclic degronimers for the degradation of target proteins |
| ES2990061T3 (en) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Spirocyclic degronimers for the degradation of target proteins |
| CN109789143A (en) | 2016-07-01 | 2019-05-21 | G1治疗公司 | Antiproliferative based on pyrimidine |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| CN110177554B (en) | 2017-01-06 | 2023-06-02 | G1治疗公司 | Combination Therapies Used to Treat Cancer |
| CA3052810A1 (en) | 2017-02-10 | 2018-08-16 | G1 Therapeutics, Inc. | Benzothiophene estrogen receptor modulators |
| BR112019027967A2 (en) | 2017-06-29 | 2020-07-14 | G1 Therapeutics, Inc. | isolated crystalline form b, pharmaceutical composition, method for treating a disorder, method of a compound or composition, and, process for producing crystalline form b. |
| CN113453679A (en) | 2018-12-20 | 2021-09-28 | C4医药公司 | Targeted protein degradation |
| CN118344370A (en) | 2019-12-20 | 2024-07-16 | C4医药公司 | Isoindolinone and indazole compounds for EGFR degradation |
| CN115279370B (en) | 2020-03-05 | 2025-01-10 | C4医药公司 | Compounds for targeted degradation of BRD9 |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED RET DEGRADATION |
| CN119998285A (en) | 2022-08-03 | 2025-05-13 | 百时美施贵宝公司 | Compounds for modulating RET proteins |
| WO2024097980A1 (en) | 2022-11-04 | 2024-05-10 | Bristol-Myers Squibb Company | Ret-ldd protein inhibitors |
| WO2024097989A1 (en) | 2022-11-04 | 2024-05-10 | Bristol-Myers Squibb Company | Ret-ldd protein degraders |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999059581A1 (en) * | 1998-05-15 | 1999-11-25 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens |
| WO1999059969A1 (en) * | 1998-05-15 | 1999-11-25 | American Home Products Corporation | Compositions comprising 2-phenyl-indole compounds and estrogen formulations |
| WO1999063974A2 (en) * | 1998-06-11 | 1999-12-16 | Endorecherche, Inc. | Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues |
-
2001
- 2001-06-29 BR BR0112364-5A patent/BR0112364A/en not_active Application Discontinuation
- 2001-06-29 AU AU2001273125A patent/AU2001273125A1/en not_active Abandoned
- 2001-06-29 CN CN01815091A patent/CN1450913A/en active Pending
- 2001-06-29 EP EP01952365A patent/EP1299093A2/en not_active Withdrawn
- 2001-06-29 WO PCT/US2001/020970 patent/WO2002003976A2/en not_active Application Discontinuation
- 2001-06-29 MX MXPA02012897A patent/MXPA02012897A/en unknown
- 2001-06-29 CA CA002415052A patent/CA2415052A1/en not_active Abandoned
- 2001-06-29 JP JP2002508431A patent/JP2004502730A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999059581A1 (en) * | 1998-05-15 | 1999-11-25 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole in combination with estrogens |
| WO1999059969A1 (en) * | 1998-05-15 | 1999-11-25 | American Home Products Corporation | Compositions comprising 2-phenyl-indole compounds and estrogen formulations |
| WO1999063974A2 (en) * | 1998-06-11 | 1999-12-16 | Endorecherche, Inc. | Selective estrogen receptor modulator in combination with denydroepiandrosterone (dhea) or analogues |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2004502730A (en) | 2004-01-29 |
| MXPA02012897A (en) | 2003-10-24 |
| CA2415052A1 (en) | 2002-01-17 |
| AU2001273125A1 (en) | 2002-01-21 |
| EP1299093A2 (en) | 2003-04-09 |
| BR0112364A (en) | 2003-07-29 |
| CN1450913A (en) | 2003-10-22 |
| WO2002003976A2 (en) | 2002-01-17 |
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