Make Better Decisions - Finding and Evaluating Generic and Branded Drug Market Entry Opportunities

Get the Book: Make Better Decisions

Finding and Evaluating Generic and Branded Drug Market Entry Opportunities

PDF eBook: Just $10 Get Print Book on Amazon

Serving hundreds of leading biopharmaceutical companies globally:

Moodys
Cantor Fitzgerald
McKinsey
Deloitte
UBS
Medtronic

Generated: August 21, 2019

DrugPatentWatch Database Preview

Claims for Patent: 6,124,314

  Try a free trial


See Plans and Pricing

« Back to Dashboard

Summary for Patent: 6,124,314
Title: Osteoporosis compounds
Abstract:This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
Inventor(s): Cameron; Kimberly O. (East Lyme, CT), Lefker; Bruce A. (Gales Ferry, CT), Rosati; Robert L. (Stonington, CT)
Assignee: Pfizer Inc. (New York, NY)
Application Number:09/161,797
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,124,314
Patent Claims:1. A method of treating a vertebrate which presents with low bone mass comprising administering to said vertebrate a therapeutically effective amount of a compound of Formula II ##STR10## a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug, wherein:

A is ethylene, n-propylene, .alpha.-methylethylene, .beta.-methylethylene,

.alpha.,.alpha.-dimethylethylene, .beta.,.beta.-dimethylethylene or oxymethylene;

B is N or C(Q);

R is carboxy, (C.sub.1 -C.sub.10) alkoxycarbonyl, carbamoyl, mono-N- or di-N,N-(C.sub.1 -C.sub.4)alkyl-substituted carbamoyl or --COOY wherein Y is 1-succinimidoethyl, 1-pivaloyloxyethyl, 2-acetamidoethyl, diloweralkylaminoloweralkyl, or carbazoyl;

R.sup.1 is H, methyl, ethyl or propyl;

R.sup.2 is H or (C.sub.2 -C.sub.5) alkanoyl;

R.sup.3 is independently H or methyl;

R.sup.4 is H, (C.sub.1 -C.sub.4) alkyl, vinyl or 2,2,2-trifluoroethyl; or R.sup.4 and R.sup.1 are taken together to form a 5-9 membered carbocyclic ring;

R.sup.5, when B is C(Q), is formyl, acetyl, pivaloyl, propionyl, acryloyl, hydroxyacetyl, 3-hydroxypropionyl, hydroxymethyl, 1-hydroxyethyl, 1,2-dihydroxyethyl, 1,3-dihydroxypropyl or 1-hydroxyl-1-methylethyl;

R.sup.5, when B is N, is formyl, acetyl, propionyl, acryloyl, hydroxyacetyl, 2,2,2-trifluoroethyl or R.sup.6 SOy;

Z is methylene, ethylene, n-propylene, tetramethylene, vinylene or ethynylene;

Q is H, chloro, bromo, methyl, phenyl or substituted phenyl;

R.sup.6 is methyl, ethyl, propyl or isopropyl; and

y is 1 or 2.

2. A method of claim 1 wherein osteoporosis, osteotomy, childhood idiopathic bone loss or bone loss associated with periodontitis is treated.

3. A method of claim 2 wherein osteoporosis is treated in a human.

4. A method of claim 3 wherein glucocorticoid-induced osteoporosis, hyperthyroidism-induced osteoporosis, immobilization-induced osteoporosis, heparin-induced osteoporosis or immunosuppressive-induced osteoporosis is treated.

5. A method of claim 1 for augmenting or maintaining bone mass in a vertebrate comprising administering to said vertebrate a therapeutically effective amount of a compound of formula II, a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug.

6. A method of claim 5 wherein bone healing following facial reconstruction, maxillary reconstruction or mandibular reconstruction is treated, vertebral synostosis is induced or long bone extension is enhanced, the healing rate of a bone graft is enhanced or prosthetic ingrowth is enhanced.

7. A method of claim 5 wherein a bone fracture is treated in a human.

8. A method for treating a vertebrate having a condition which presents with low bone mass comprising administering to said vertebrate

a. an amount of a compound of formula II ##STR11## a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug, wherein:

A is ethylene, n-propylene, .alpha.-methylethylene, .beta.-methylethylene, .alpha.,.alpha.-dimethylethylene, .beta.,.beta.-dimethylethylene or oxymethylene;

B is N or C(Q);

R is carboxy, (C.sub.1 -C.sub.10) alkoxycarbonyl, carbamoyl, mono-N- or di-N,N-(C.sub.1 -C.sub.4)alkyl-substituted carbamoyl or --COOY wherein Y is 1-succinimidoethyl, 1-pivaloyloxyethyl, 2-acetamidoethyl, diloweralkylaminoloweralkyl, or carbazoyl;

R.sup.1 is H, methyl, ethyl or propyl;

R.sup.2 is H or (C.sub.2 -C.sub.5) alkanoyl;

R.sup.3 is independently H or methyl;

R.sup.4 is H, (C.sub.1 -C.sub.4) alkyl, vinyl or 2,2,2-trifluoroethyl; or R.sup.4 and R.sup.1 are taken together to form a 5-9 membered carbocyclic ring;

R.sup.5, when B is C(Q), is formyl, acetyl, pivaloyl, propionyl, acryloyl, hydroxyacetyl, 3-hydroxypropionyl, hydroxymethyl, 1-hydroxyethyl, 1,2-dihydroxyethyl, 1,3-dihydroxypropyl or 1-hydroxyl-1-methylethyl;

R.sup.5, when B is N, is formyl, acetyl, propionyl, acryloyl, hydroxyacetyl, 2,2,2-trifluoroethyl or R.sup.6 SOy;

Z is methylene, ethylene, n-propylene, tetramethylene, vinylene or ethynylene;

Q is H, chloro, bromo, methyl, phenyl or substituted phenyl;

R.sup.6 is methyl, ethyl, propyl or isopropyl; and

y is 1 or 2; and

b. an amount of an anti-resorptive agent, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

9. A method of claim 8 wherein the anti-resorptive agent is droloxifene; raloxifene; tamoxifen; 4-hydroxy-tamoxifen; toremifene; centchroman; levormeloxifene; idoxifene; 6-(4-hydroxy-phenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-naphthalen-2-o l; {4-[2-(2-aza-bicyclo[2.2.1]hept-2-yl)-ethoxy]-phenyl}-[6-hydroxy-2-(4-hydr oxy-phenyl)-benzo[b]thiophen-3-yl]-methanone;

3-(4-(1,2-diphenyl-but-1-enyl)-phenyl)-acrylic acid;

2-(4-methoxy-phenyl)-3-[4-(2-piperidin-1-yl-ethoxy)-phenoxy]benzo[b]thiophe n-6-ol;

cis-6-(4-fluoro-phenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8tetra hydro-naphthalene-2-ol;

(-)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro -naphthalene-2-ol;

cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro-nap hthalene-2-ol;

cis-1-[6'-pyrrolodinoethoxy-3'-pyridyl]-2-phenyl-6-hydroxy-1,2,3,4-tetrahyd ronaphthalene;

1-(4'-pyrrolidinoethoxyphenyl)-2-(4"-fluorophenyl)-6-hydroxy-1,2,3,4-tetrah ydroisoquinoline;

cis-6-(4-hydroxyphenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetr ahydro-naphthalene-2-ol; or

1-(4'-pyrrolidinolethoxyphenyl)-2-phenyl-6-hydroxy-1,2,3,4-tetrahydroisoqui noline, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

10. A method of claim 9 wherein the anti-resorptive agent is tiludronic acid, zoledronic acid, alendronic acid, ibandronic acid, risedronic acid, etidronic acid, clodronic acid, and pamidronic acid, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

11. A method for treating a vertebrate which presents with low bone mass comprising administering to said vertebrate

a. an amount of a compound of formula II ##STR12## a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug, wherein:

A is ethylene, n-propylene, .alpha.-methylethylene, .beta.-methylethylene, .alpha.,.alpha.-dimethylethylene, .beta.,.beta.-dimethylethylene or oxymethylene;

B is N or C(Q);

R is carboxy, (C.sub.1 -C.sub.10) alkoxycarbonyl, carbamoyl, mono-N- or di-N,N-(C.sub.1 -C.sub.4)alkyl-substituted carbamoyl or --COOY wherein Y is 1-succinimidoethyl, 1-pivaloyloxyethyl, 2-acetamidoethyl, diloweralkylaminoloweralkyl, or carbazoyl;

R.sup.1 is H, methyl, ethyl or propyl;

R.sup.2 is H or (C.sub.2 -C.sub.5) alkanoyl;

R.sup.3 is independently H or methyl;

R.sup.4 is H, (C.sub.1 -C.sub.4) alkyl, vinyl or 2,2,2-trifluoroethyl; or R.sup.4 and R.sup.1 are taken together to form a 5-9 membered carbocyclic ring;

R.sup.5, when B is C(Q), is formyl, acetyl, pivaloyl, propionyl, acryloyl, hydroxyacetyl, 3-hydroxypropionyl, hydroxymethyl, 1-hydroxyethyl, 1,2-dihydroxyethyl, 1,3-dihydroxypropyl or 1-hydroxyl-1-methylethyl;

R.sup.5, when B is N, is formyl, acetyl, propionyl, acryloyl, hydroxyacetyl, 2,2,2-trifluoroethyl or R.sup.6 SOy;

Z is methylene, ethylene, n-propylene, tetramethylene, vinylene or ethynylene;

Q is H, chloro, bromo, methyl, phenyl or substituted phenyl;

R.sup.6 is methyl, ethyl, propyl or isopropyl; and

y is 1 or 2; and

b. an amount of a bone anabolic agent, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

12. A method of claim 11 wherein said anabolic agent in component b is IGF-1, a bone morphogenetic protein (BMP), a prostaglandin, a prostaglandin agonist/antagonist, sodium fluoride, parathyroid hormone (PTH), an active fragment of parathyroid hormone, a growth hormone or a growth hormone secretagogue, a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug.

13. A method of claim 8 for augmenting and maintaining bone mass in a vertebrate comprising administering to said vertebrate

a. an amount of said compound of formula II, a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug; and

b. an amount of an anti-resorptive agent, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

14. A method of claim 13 wherein the anti-resorptive agent is droloxifene; raloxifene; tamoxifen; 4-hydroxy-tamoxifen; toremifene; centchroman; levormeloxifene; idoxifene; 6-(4-hydroxy-phenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-naphthalen-2-o l; {4-[2-(2-aza-bicyclo[2.2.1]hept-2-yl)-ethoxy]-phenyl}-[6-hydroxy-2-(4-hydr oxy-phenyl)-benzo[b]thiophen-3-yl]-methanone;

3-(4-(1,2-diphenyl-but-1-enyl)-phenyl)-acrylic acid;

2-(4-methoxy-phenyl)-3-[4-(2-piperidin-1-yl-ethoxy)-phenoxy]-benzo[b]thioph en-6-ol;

cis-6-(4-fluoro-phenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetr ahydronaphthalene-2-ol;

(-)-cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydro naphthalene-2-ol;

cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaph thalene-2-ol;

cis-1-[6'-pyrrolodinoethoxy-3'-pyridyl]-2-phenyl-6-hydroxy-1,2,3,4-tetrahyd ronaphthalene;

1-(4'-pyrrolidinoethoxyphenyl)-2-(4"-fluorophenyl)-6-hydroxy-1,2,3,4-tetrah ydroisoquinoline;

cis-6-(4-hydroxyphenyl)-5-[4-(2-piperidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetr ahydro-naphthalene-2-ol; or

1-(4'-pyrrolidinolethoxyphenyl)-2-phenyl-6-hydroxy-1,2,3,4-tetrahydroisoqui noline, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

15. A method of claim 14 wherein the anti-resorptive agent is tiludronic acid, zoledronic acid, alendronic acid, ibandronic acid, risedronic acid, etidronic acid, clodronic acid, and pamidronic acid, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

16. A method of claim 11 for augmenting and maintaining bone mass in a vertebrate comprising administering to said vertebrate

a. an amount of a compound of formula II, a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug; and

b. an amount of a bone anabolic agent, a prodrug thereof or a pharmaceutically acceptable salt of said agent or said prodrug.

17. A method of claim 16 wherein said anabolic agent in component b is IGF-1, a bone morphogenetic protein (BMP), a prostaglandin, a prostaglandin agonist/antagonist, sodium fluoride, parathyroid hormone (PTH), an active fragment of parathyroid hormone, a growth hormone or a growth hormone secretagogue, a prodrug thereof or a pharmaceutically acceptable salt of said compound or said prodrug.

Details for Patent 6,124,314

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 001 2015-01-23   Try a Free Trial Pfizer Inc. (New York, NY) 2017-10-10 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 002 2015-01-23   Try a Free Trial Pfizer Inc. (New York, NY) 2017-10-10 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 003 2015-01-23   Try a Free Trial Pfizer Inc. (New York, NY) 2017-10-10 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 004 2015-01-23   Try a Free Trial Pfizer Inc. (New York, NY) 2017-10-10 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

Subscribe to access the full database, or try a Free Trial

Make Better Decisions: Try a trial or see plans & pricing

Serving hundreds of leading biopharmaceutical companies globally:

US Department of Justice
Moodys
Baxter
Mallinckrodt
Deloitte
McKinsey

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.