Pharmaceutical compositions, kits and methods comprising combinations of estrogen agonists/antagonists, estrogens and progestins

• US 7,030,157 B2
• Filed: 07/26/2002
• Issued: 04/18/2006
• Est. Priority Date: 07/31/2001
• Status: Expired due to Fees

• Current Assignee: Pfizer Inc.
• Original Assignee: Pfizer Inc.
• Inventors: Thompson, David D., Ke, HuaZhu
• Primary Examiner(s): HUI, SAN MING R
• Application Number:
  US10/206,587
• Publication Number:
  US 20030065017A1
• Time in Patent Office: 1,362 Days
• Field of Search: 514/482
• US Class Current: 514/482
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 5/30 Oestrogens

Abstract

The present invention relates to pharmaceutical compositions, kits and methods comprising combinations of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof and estrogens. The present invention also relates to pharmaceutical compositions, kits and methods comprising combinations of (−)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or nontoxic pharmacologically acceptable acid addition salts thereof, estrogens and progestins.

Claims

1. A method of enhancing libido in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

2. A method of enhancing libido in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.

3. A method of treating hypoactive sexual desire disorder in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amonut of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

4. A method of treating hypoactive sexual desire disorder in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.

5. A method of treating sexual arousal disorder in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

6. A method of treating sexual arousal disorder in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.

7. A method of treating dyspareunia in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amonut of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

8. A method of treating dyspareunia in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.

9. A method of increasing the frequency and intensity of orgasms in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

10. A method of increasing the frequency and intensity of orgasms in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.

11. A method of treating vaginismus in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof and an estrogen, provided said patient does not have vaginal atrophy.

12. A method of treating vaginismus in a patient, the method comprising administering to a patient in need thereof a therapeutically effective amount of (−

)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-naphthalene-2-ol or a pharmacologically acceptable acid addition salt thereof, an estrogen and a progestin, provided said patient does not have vaginal atrophy.