Claims for Patent: 7,504,427

Summary for Patent: 7,504,427

Title:	Fluoroalkoxy-substituted 1,3-dihydro-isoindolyl compounds and their pharmaceutical uses
Abstract:	The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.
Inventor(s):	Muller; George W. (Bridgewater, NJ), Man; Hon-Wah (Princeton, NJ), Zhang; Weihong (Highland Park, NJ)
Assignee:	Celgene Corporation (Summit, NJ)
Application Number:	11/601,355
Patent Claims:	1. A pharmaceutical composition comprising a compound having the formula (I): ##STR00049## wherein: Y is --C(O)--, --CH.sub.2, --CH.sub.2C(O)--, --C(O)CH.sub.2--, or SO.sub.2; Z is --H, --C(O)R.sup.3, --(C.sub.0-1-alkyl)--SO.sub.2--(C.sub.1-4-alkyl), --C.sub.1-8-alkyl, --CH.sub.2OH, CH.sub.2(O)(C.sub.1-8-alkyl) or --CN; R.sub.1 and R.sub.2 are each independently --CHF.sub.2, --C.sub.1-8-alkyl, --C.sub.3-18-cycloalkyl, or --(C.sub.1-10-alkyl)(C.sub.3-18-cycloalkyl), and at least one of R.sub.1 and R.sub.2 is CHF.sub.2; R.sup.3 is --NR.sup.4R.sup.5, -alkyl, --OH, --O-alkyl, phenyl, benzyl, substituted phenyl, or substituted benzyl; R.sup.4 and R.sup.5 are each independently --H, --C.sub.1-8-alkyl, --OH, --OC(O)R.sup.6; R.sup.6 is --C.sub.1-8-alkyl, -amino(C.sub.1-8-alkyl), -phenyl, -benzyl, or -aryl; X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are each independent --H, -halogen, -nitro, --NH.sub.2, --CF.sub.3, --C.sub.1-6-alkyl, --(C.sub.0-4-alkyl)-(C.sub.3-6-cycloalkyl), (C.sub.0-4-alkyl)-NR.sup.7R.sup.8, (C.sub.0-4-alkyl)-N(H)C(O)--(R.sup.8), (C.sub.0-4-alkyl)-N(H)C(O)N(R.sup.7R.sup.8), (C.sub.0-4-alkyl)-N(H)C(O)O(R.sup.7R.sup.8), (C.sub.0-4-alkyl)-OR.sup.8, (C.sub.0-4-alkyl)-imidazolyl, (C.sub.0-4-alkyl)-pyrrolyl, (C.sub.0-4-alkyl)-oxadiazolyl, or (C.sub.0-4-alkyl)-triazolyl triazolyl or X.sub.1 and X.sub.2 or X.sub.2 and X.sub.3 or X.sub.3 and X.sub.4 are taken together with the atoms that join them to form a cycloalkyl or heterocycloalkyl ring of 3, 4, 5, 6 or 7 atoms; and R.sup.7 and R.sup.8 are each independently H, C.sub.1-9-alkyl, C.sub.3-6-cycloalkyl, (C.sub.1-6-alkyl)-(C.sub.3-6-cycloalkyl), (C.sub.1-6-alkyl)-N(R.sup.7R.sup.8), (C.sub.1-6-alkyl)-OR.sup.8, phenyl, benzyl, or aryl; or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, or prodrug thereof. 2. The pharmaceutical composition of claim 1 further comprising an additional therapeutic agent. 3. The pharmaceutical composition of claim 1, wherein the additional therapeutic agent is an anti-cancer agent. 4. The pharmaceutical composition of claim 3, wherein the anti-cancer agent is paclitaxel, cisplatin, tamoxifen, docetaxel, pirubicin, doxorubicin, irinotecan, leuprolide, bicalutamide, a goserlin implant, gemcitabine, sargramostim or steroids. 5. A method of treating cancer in a mammal which comprises administering to a patient in need of such treatment a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer, or prodrug thereof, wherein the cancer is a solid tumor or a blood-born tumor cancer selected from the group consisting of skin cancer, lymph node cancer, breast cancer, cervix cancer, uterus cancer, cancer of the gastrointestinal tract, lung cancer, ovarial cancer, prostate cancer, colon cancer, rectal cancer, mouth cancer, brain cancer, head and neck cancer, throat cancer, testinal cancer, kidney cancer, pancreas cancer, bone cancer, spleen cancer, liver cancer, bladder cancer, cancer of larynx, and cancer of nasal passages. 6. The method of claim 5, wherein the effective amount of a compound of formula (I) of claim 1 is from about 0.1 mg to about 300 mg per day, and wherein the compound is administered orally, parenterally, topically or mucosally. 7. The method of claim 6, wherein the effective amount is from about 1 mg to about 250 mg per day. 8. The method of claim 5, wherein the mammal is human.

Details for Patent 7,504,427

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Partner Therapeutics, Inc.	LEUKINE	sargramostim	For Injection	103362	03/05/1991		2022-12-30
Partner Therapeutics, Inc.	LEUKINE	sargramostim	Injection	103362	03/05/1991		2022-12-30