Patent classifications
C07D277/22
Highly Selective Anti-Cancer Agents Targeting Non-Small Cell Lung Cancer and Other Forms of Cancer
Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
Analogs of proxisome proliferator activated receptor (PPAR) agonists and methods of using the same
Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.
Analogs of proxisome proliferator activated receptor (PPAR) agonists and methods of using the same
Peroxisome proliferator activated receptor (PPAR) compounds, and methods of using the same for treating bone fractures, treating osteoporosis and/or metabolic bone diseases, and inducing osteogenesis and/or chondrogenesis, are disclosed.
PHOTOCHROMIC AND ELECTROCHROMIC DIARYLCYCLOPENTENE DERIVATIVES AS OPTICAL FILTERS
A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R.sub.1 is independently selected from the group consisting of H, or halo; each R.sub.2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R.sub.2 together form CHCH and form part of a polymer backbone; each R.sub.3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R.sub.4 is aryl; and each R.sub.5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.
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PHOTOCHROMIC AND ELECTROCHROMIC DIARYLCYCLOPENTENE DERIVATIVES AS OPTICAL FILTERS
A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R.sub.1 is independently selected from the group consisting of H, or halo; each R.sub.2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R.sub.2 together form CHCH and form part of a polymer backbone; each R.sub.3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R.sub.4 is aryl; and each R.sub.5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.
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Highly selective anti-cancer agents targeting non-small cell lung cancer and other forms of cancer
Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
Highly selective anti-cancer agents targeting non-small cell lung cancer and other forms of cancer
Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
ANTI-CANCER COMPOUNDS AND CONJUGATES THEREOF
Disclosed are compounds based on dolastatins, drug-conjugates, methods of preparing drug-conjugates, and uses thereof. Also disclosed are pharmaceutical compositions and methods of treatment. The compounds and drug-conjugates disclosed herein can be used to treat diseases such as bladder cancer, breast cancer, colon cancer, rectal cancer, endometrial cancer, kidney cancer, lung cancer, melanoma, non-Hodgkin lymphoma, glioblastoma, pancreatic cancer, prostate cancer, and thyroid cancer.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC AND RELATED DISORDERS
The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.
COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC AND RELATED DISORDERS
The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.