Patent classifications
C07D495/18
OXA- IBOGAINE INSPIRED ANALOGUES FOR TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
The present invention provides a compound having the structure:
##STR00001## wherein D, E and F are each independently NR.sub.1, CR.sub.2R.sub.3 or CR.sub.6R.sub.7, wherein one of D, E and F is NR.sub.1 and the remaining two are CR.sub.2R.sub.3 or CR.sub.6R.sub.7, wherein R.sub.1 is H or -(alkyl), and wherein R.sub.2, R.sub.3, R.sub.6 and R.sub.7 are each independently H, -(alkyl), -(alkenyl), -(alkynyl), -cycloalkyl, -alkylcycloalkyl, -aryl, heteroaryl or -alkylaryl; X.sub.1 is C or N; X.sub.2 is O, S, N, NR.sub.14 or CR.sub.15, wherein R.sub.14 is H, -(alkyl) or -cycloalkyl, wherein R.sub.15 is H, -(alkyl) or -cycloalkyl, and wherein X.sub.2 is other than N when X.sub.1 is N; α and β represent a bond that is present or absent, and wherein either α or β is present, wherein when α is present, then X.sub.1 is C and X.sub.2 is O, S or NR.sub.14, or when β is present, then X.sub.1 is N and X.sub.2 is N or CR.sub.15; R.sub.4, R.sub.5, R.sub.8 and R.sub.9 are each independently H, -(alkyl), -(alkenyl), -(alkynyl), -cycloalkyl, -alkylcycloalkyl, -aryl, heteroaryl, -alkylaryl, —OH, —O(alkyl), —OAc, —S(alkyl), —NH.sub.2, —NH(alkyl), —N(alkyl).sub.2, —COOH, —CO.sub.2(alkyl), —CONH.sub.2, —CONH(alkyl), —CON(alkyl).sub.2 or —CN, wherein when D is NR.sub.1 then R.sub.4 and R.sub.5 are each independently H, -(alkyl), -(alkenyl), -(alkynyl), -cycloalkyl, -alkylcycloalkyl, -aryl, heteroaryl or -alkylaryl, wherein when F is NR.sub.1 then R.sub.8 and R.sub.9 are each independently H, -(alkyl), -(alkenyl), -(alkynyl), -cycloalkyl, -alkylcycloalkyl, -aryl, heteroaryl or -alkylaryl or R.sub.1 and R.sub.4 together form a —(CH.sub.2).sub.m—, wherein m represents an integer from 2 to 4; and R.sub.10, R.sub.11, R.sub.12 and R.sub.13 are each independently H, halogen, -(alkyl), -(alkenyl), -(alkynyl), -cycloalkyl, -(aryl), -(heteroaryl), —OH, —OAc, —O(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —SH, —S(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), —S-(heteroaryl), —NH.sub.2, —NH-(alkyl), —NH-(alkenyl), —NH-(alkynyl), —NH-(aryl), —NH-(heteroaryl), —CO.sub.2(alkyl), —CONH.sub.2, —CN, —CF.sub.3, —CF.sub.2H, —OCF.sub.3 or NO.sub.2 or R.sub.10 and R.sub.11 together form a —O(CH.sub.2)O— or R.sub.11 and R.sub.12 together form a —O(CH.sub.2)O— or R.sub.12 and R.sub.13 together form a —O(CH.sub.2)O—; wherein when X.sub.1 is C, X.sub.2 is NR.sub.14, and D is CR.sub.2R.sub.3, E is NR.sub.1, F is CR.sub.6R.sub.7, then (i) R.sub.14 and at least two of R.sub.10, R.sub.11, R.sub.12 and R.sub.13 are other than hydrogen, or (ii) one of R.sub.2, R.sub.3, R.sub.6 and R.sub.7 i
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
- Wilfried Braje ,
- George Doherty ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew Judd ,
- Aaron Kunzer ,
- Anthony Mastracchio ,
- Xiaohong Song ,
- Andrew Souers ,
- Gerard Sullivan ,
- Zhi-Fu Tao ,
- Chunqiu Lai ,
- Jesse Teske ,
- Michael Wendt ,
- Patrick Brady ,
- Xilu Wang ,
- Thomas Penning ,
- Yujia Dai ,
- Jane Gong ,
- Roberto Risi ,
- Yiyun Yu ,
- Guidong ZHU
The present disclosure provides for compounds of Formula (I)
##STR00001##
wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
- Wilfried Braje ,
- George Doherty ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew Judd ,
- Aaron Kunzer ,
- Anthony Mastracchio ,
- Xiaohong Song ,
- Andrew Souers ,
- Gerard Sullivan ,
- Zhi-Fu Tao ,
- Chunqiu Lai ,
- Jesse Teske ,
- Michael Wendt ,
- Patrick Brady ,
- Xilu Wang ,
- Thomas Penning ,
- Yujia Dai ,
- Jane Gong ,
- Roberto Risi ,
- Yiyun Yu ,
- Guidong ZHU
The present disclosure provides for compounds of Formula (I)
##STR00001##
wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
EPOXIDE FUNCTIONALIZED POLYAROMATIC FEEDSTOCK AND POLYMERS DERIVED THEREFROM
Epoxide functionalized polyaromatic feedstocks and processes for their preparation are described. The processes involve functionalizing polyaromatic hydrocarbon molecules and/or polyheterocyclic molecules present in petroleum or petrochemical streams with epoxide. The epoxide functionalized poly aromatic feedstock can be further treated so as to effect oligomerization or polymerization. The oligomers or polymers may be thermoplastic or thermoset materials and may find use in, for example, infrastructure applications, composites, fillers, fire retardants and 3-D printing materials.
EPOXIDE FUNCTIONALIZED POLYAROMATIC FEEDSTOCK AND POLYMERS DERIVED THEREFROM
Epoxide functionalized polyaromatic feedstocks and processes for their preparation are described. The processes involve functionalizing polyaromatic hydrocarbon molecules and/or polyheterocyclic molecules present in petroleum or petrochemical streams with epoxide. The epoxide functionalized poly aromatic feedstock can be further treated so as to effect oligomerization or polymerization. The oligomers or polymers may be thermoplastic or thermoset materials and may find use in, for example, infrastructure applications, composites, fillers, fire retardants and 3-D printing materials.
Heterocyclic Compounds And Their Use in Preventing or Treating Bacterial Infections
The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a β-lactamase inhibitor.
##STR00001##
Heterocyclic Compounds And Their Use in Preventing or Treating Bacterial Infections
The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a β-lactamase inhibitor.
##STR00001##
Heterocyclic Compounds And Their Use in Preventing or Treating Bacterial Infections
The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a β-lactamase inhibitor.
##STR00001##
Heterocyclic Compounds And Their Use in Preventing or Treating Bacterial Infections
The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a β-lactamase inhibitor.
##STR00001##
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
- Wilfried Braje ,
- George Doherty ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew Judd ,
- Aaron Kunzer ,
- Anthony Mastracchio ,
- Xiaohong Song ,
- Andrew Souers ,
- Gerard Sullivan ,
- Zhi-Fu Tao ,
- Chunqiu Lai ,
- Jesse Teske ,
- Michael Wendt ,
- Patrick Brady ,
- Xilu Wang ,
- Thomas Penning ,
- Yujia Dai ,
- Jane Gong ,
- Roberto Risi ,
- Yiyun Yu ,
- Guidong ZHU
The present disclosure provides for compounds of Formula (I)
##STR00001##
wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).