Claims for Patent: 10,239,891

Summary for Patent: 10,239,891

Title:	Compositions to detect remnant cancer cells
Abstract:	Disclosed are compounds, compositions and methods for detecting remnant cancer cells in a tissue sample.
Inventor(s):	Swiss; Gerald F. (Rancho Santa Fe, CA), Pariza; Richard J. (Newport Beach, CA), Moriarty; Robert M. (Michiana Shores, MI)
Assignee:	Indicator Systems International, Inc. (Newport Beach, CA)
Application Number:	15/595,920
Patent Claims:	1. A compound of formula I: ##STR00040## where: R and R.sup.1 are independently C.sub.2-C.sub.18 alkyl or cycloalkyl groups either or both optionally containing 1 to 8 heteroatoms selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O).sub.zH, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; and L is a linker of from 1 to 20 carbon atoms and 1 to 6 heteroatoms; selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O)H, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; and or pharmaceutically acceptable salts and/or solvates thereof. 2. A compound of formula II: ##STR00041## where: R and R.sup.1 are independently C.sub.2-C.sub.18 alkyl or cycloalkyl groups either or both optionally containing 1 to 8 heteroatoms selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O).sub.zH, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; and L is a linker of from 1 to 20 carbon atoms and 1 to 6 heteroatoms; selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O)H, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; and or pharmaceutically acceptable salts and/or solvates thereof. 3. A compound of formula III: ##STR00042## where: R and R.sup.1 are independently C.sub.2-C.sub.18 alkyl or cycloalkyl groups either or both optionally containing 1 to 8 heteroatoms selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O).sub.zH, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; R.sup.3 is hydrogen or C.sub.1-C.sub.6 alkyl; and L is a linker of from 1 to 20 carbon atoms and 1 to 6 heteroatoms; selected from the group consisting of oxygen, S(O).sub.x, >NR.sup.3, --OP(O).sub.yH, --OS(O).sub.zH, --C(O)--, amino, C.sub.1-C.sub.6 alkylamino, di(C.sub.1-C.sub.6 dialkyl)amino, --C(O)O--, --C(O)NR.sup.3--, --C(O)OH, --OH, and oxo wherein y and z are independently 1 or 2, and x is 0, 1 or 2; or a pharmaceutically acceptable salt and/or solvate thereof. 4. A pharmaceutical composition comprising a pharmaceutically acceptable inert diluent and a compound of formula I, II, or III. 5. The pharmaceutical composition of claim 4 wherein said composition is suitable for topical application onto a tissue sample. 6. The pharmaceutical composition of claim 5, wherein said composition comprises sterile water and optionally a water soluble or miscible co-solvent such as DMSO, ethanol, and octanol. 7. A compound, salts and solvates of formula selected from the group consisting of: ##STR00043## TABLE-US-00004 # R/R.sup.1 R.sup.2 L 1 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- H ##STR00044## 2 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- CH.sub.3 ##STR00045## 3 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ H --NHCH.sub.2CH.- sub.2CH.sub.2(OCH.sub.2CH.sub.2).sub.3CH.sub.2NHC(.dbd.S)NH-- CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- 4 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- H ##STR00046## 5 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- H ##STR00047## 6 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3CH.sub.2C(O)O-- H ##STR00048## 7 CH.sub.3O.sub.2C(CH.sub.2CH.sub.2O).sub.3C(O)(CH.sub.2CH.sub.2O).sub.3C(- O)O-- CH.sub.3O.sub.2C(CH.sub.2CH.sub.2O).sub.3C(O)(CH.sub.2CH.sub.2O).sub- .3C(O)O-- H ##STR00049## 8 CH.sub.3O(CH.sub.2CH.sub.2O).sub.2CH.sub.2C(O)O--/ CH.sub.3O(CH.sub.2CH.sub.2O).sub.2CH.sub.2C(O)O-- H ##STR00050## . 8. A compound, salts and solvates of formula selected from the group consisting of: ##STR00051## TABLE-US-00005 No. R/R.sup.1 L 9 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- ##STR00052## 10 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- ##STR00053## 11 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- ##STR00054## 12 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- ##STR00055## 13 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- ##STR00056## 14 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3CH.sub.2C(O)O-- ##STR00057## 15 CH.sub.3O.sub.2C(CH.sub.2CH.sub.2O).sub.3C(O)(CH.sub.2CH.sub.2O).sub.3C- (O)O-- ##STR00058## 16 CH.sub.3O(CH.sub.2CH.sub.2O).sub.4CH.sub.2CH.sub.2C(O)O--/ CH.sub.3O(CH.sub.2CH.sub.2O).sub.4CH.sub.2CH.sub.2C(O)O-- ##STR00059## . 9. A compound, salts and solvates of formula selected from the group consisting of: ##STR00060## TABLE-US-00006 Compound No. R/R.sup.1 L 17 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- --C(.dbd.S)NH-- 18 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- --CH.sub.2CH.sub.2C- H.sub.2NHC(.dbd.S)NH-- 19 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- --CH.sub.2NHC(.dbd.- S)NH-- 20 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O--/ CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- --CH.sub.2CH.sub.2N- HC(.dbd.S)NH-- 21 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)O-- --CH.sub.2CH.sub.2N- HC(.dbd.O)NH-- 22 CH.sub.3OCH.sub.2CH.sub.2OC(O)CH.sub.2CH.sub.2C(O)--/ CH.sub.3CH.sub.2C(O)-- --C(.dbd.S)NH-- 23 CH.sub.3O.sub.2C(CH.sub.2CH.sub.2O).sub.3C(O)(CH.sub.2CH.sub.2O).sub.3C- (O)-- --CH.sub.2NHC(.dbd.S)NH-- 24 CH.sub.3O(CH.sub.2CH.sub.2O).sub.4CH.sub.2CH.sub.2C(O)O--/ CH.sub.3O(CH.sub.2CH.sub.2O).sub.4CH.sub.2CH.sub.2C(O)O-- CH.sub.2NHC.dbd- .S)NH-- 25 ##STR00061## . --CH.sub.2CH.sub.2NHC(.dbd.S)NH--

Details for Patent 10,239,891

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2039-09-23