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1. 发明申请

WO2014145029A3 N-ACYL-N'-(PYRIDIN-2-YL) UREAS AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 审中-公开
公开(公告)号：WO2014145029A3
公开(公告)日：2014-09-18
申请号：PCT/US2014/029666
申请日：2014-03-14
申请人： DECIPHERA PHARMACEUTICALS, LLC , CALDWELL, Timothy Malcolm , SAMARAKOON, Thiwanka , VOGETI, Lakshminarayana , PATT, William C. , AHN, YuMi
发明人： CALDWELL, Timothy Malcolm , SAMARAKOON, Thiwanka , VOGETI, Lakshminarayana , PATT, William C. , AHN, YuMi , FLYNN, Daniel L. , KAUFMAN, Michael D.
IPC分类号： A61K31/4375
摘要： Described are compounds of Formula (I) which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-IR), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c- FMS, c-KIT, or PDGFR kinases.

2. 发明申请

WO2014145015A3 IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 审中-公开
公开(公告)号：WO2014145015A3
公开(公告)日：2014-09-18
申请号：PCT/US2014/029650
申请日：2014-03-14
申请人： DECIPHERA PHARMACEUTICALS, LLC , SAMARAKOON, Thiwanka , CALDWELL, Timothy, Malcolm , VOGETI, Lakshminarayana , AHN, YuMi , PATT, William, C. , YATES, Karen, M.
发明人： SAMARAKOON, Thiwanka , CALDWELL, Timothy, Malcolm , VOGETI, Lakshminarayana , AHN, YuMi , PATT, William, C. , YATES, Karen, M. , FLYNN, Daniel, L. , KAUFMAN, Michael, D.
IPC分类号： A61K31/4375
摘要： Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-IR), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c- FMS, c-KIT, or PDGFR kinases.

3. 发明申请

WO2006055525A2 PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：蛋白酪氨酸磷酸酶抑制剂及其使用方法
公开(公告)号：WO2006055525A2
公开(公告)日：2006-05-26
申请号：PCT/US2005041269
申请日：2005-11-15
申请人： CEPTYR INC , BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
发明人： BLASKOVICH MARK A , BAUGHMAN TED , LITTLE THOMAS , PATT WILLIAM , QABAR MAHER , SCHULTZ LAURI , HONG FENG , NAGULA GANGADHAR , GAGE JENNIFER LYNN , HOWBERT JAMES JEFFRY
IPC分类号： A61K31/675 , A61K31/66
CPC分类号： C07F9/6541 , C07F9/3808 , C07F9/4006 , C07F9/5721 , C07F9/5728 , C07F9/591 , C07F9/65517
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.
摘要翻译：本发明提供了可用于调节蛋白酪氨酸磷酸酶-1b（PTP1B）酶的生物学活性的式（I）和式（II）的化合物。本发明的化合物可用于治疗其中PTP1B酶是因子的疾病和/或病症。这些疾病和/或病症包括但不限于1型糖尿病，2型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖症，高脂血症，高甘油三酯血症，高胆固醇血症，低HDL水平，动脉粥样硬化，血管再狭窄，炎性肠病，胰腺炎，脂肪细胞瘤，脂肪细胞癌，脂肪肉瘤，血脂异常，癌症和神经变性疾病。

4. 发明申请

WO1997037985A1 NONPEPTIDE ENDOTHELIN ANTAGONISTS WITH INCREASED WATER SOLUBILITY 审中-公开
标题翻译：非特异性内皮素拮抗剂具有增加的水溶性
公开(公告)号：WO1997037985A1
公开(公告)日：1997-10-16
申请号：PCT/US1997003929
申请日：1997-03-12
申请人： WARNER-LAMBERT COMPANY , CHENG, Xue-Min , DOHERTY, Annette, Marian , PATT, William, Chester , REPINE, Joseph, Thomas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D307/60
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, male penile erectile dysfunction, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译：描述了内皮素（I）的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗动脉粥样硬化，再狭窄，雷诺氏现象，轻度或严重充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，男性阴茎勃起功能障碍，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，癌症恶性血管内皮瘤或前列腺癌，心肌梗死或缺血，急性或慢性肾功能衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素，败血症，出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生和内皮素水平升高。

5. 发明申请

WO2002064547A2 ISOPHTHALIC ACID DERIVATIVES AS MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：邻苯二甲酸衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2002064547A2
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000344
申请日：2002-02-04
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
发明人： BARVIAN, Nicole, Chantel , CONNOR, David, Thomas , DYER, Richard, Dennis , JOHNSON, Adam, Richard , PATT, William, Chester
IPC分类号： C07C235/60
CPC分类号： C07D213/30 , C07C69/80 , C07C69/90 , C07C69/92 , C07C229/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/78 , C07C235/60 , C07D285/14 , C07D317/54 , C40B50/14
摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula (I) wherein: R 1 , R 2 , and R 3 independently are hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , NR 4 R 5 , CN, or CF 3 ; E is independently O or S; A and B independently are OR 4 or NR 4 R 5 ; each R 4 and R 5 independently are H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, (CH 2 ) n aryl, (CH 2 ) n cycloalkyl, (CH 2 ) n heteroaryl, or R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.
摘要翻译：选择性MMP-13抑制剂是式（I）的间苯二甲酸衍生物，其中：R 1，R 2和R 4独立地选自： 3独立地为氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷氧基，C 2 -C 6链烯基，C 2 -C 6炔基，NO

6. 发明申请

WO2008033999A3 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开
标题翻译：激酶抑制剂用于治疗增殖性疾病
公开(公告)号：WO2008033999A3
公开(公告)日：2008-08-07
申请号：PCT/US2007078394
申请日：2007-09-13
申请人： DECIPHERA PHARMACEUTICALS LLC , FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , PATT WILLIAM C
发明人： FLYNN DANIEL L , PETILLO PETER A , KAUFMAN MICHAEL D , PATT WILLIAM C
IPC分类号： A61K31/54
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
摘要翻译：本发明涉及用于治疗各种疾病的新型激酶抑制剂和调节剂化合物。更具体地说，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法以及合成该化合物的方法。优选地，所述化合物可用于调节Raf激酶及其疾病多晶型物的激酶活性。本发明化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，结肠直肠癌，卵巢癌，乳头状甲状腺癌，非小细胞肺癌和间皮瘤。本发明化合物还可用于治疗类风湿性关节炎和视网膜病，包括糖尿病视网膜神经病和黄斑变性。

7. 发明申请

WO2006055525A3 PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2006055525A3
公开(公告)日：2006-05-26
申请号：PCT/US2005/041269
申请日：2005-11-15
申请人： CEPTYR, INC. , BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
发明人： BLASKOVICH, Mark A. , BAUGHMAN, Ted , LITTLE, Thomas , PATT, William , QABAR, Maher , SCHULTZ, Lauri , HONG, Feng , NAGULA, Gangadhar , GAGE, Jennifer Lynn , HOWBERT, James Jeffry
IPC分类号： A61K31/66 , C07F9/02
摘要： The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.

8. 发明申请

WO2002064571A1 PYRIMIDINE MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：哌嗪基金属蛋白酶抑制剂
公开(公告)号：WO2002064571A1
公开(公告)日：2002-08-22
申请号：PCT/IB2002/000190
申请日：2002-01-18
申请人： WARNER-LAMBERT COMPANY , BARVIAN, Nicole, Chantel , PATT, William, Chester
发明人： BARVIAN, Nicole, Chantel , PATT, William, Chester
IPC分类号： C07D239/28
CPC分类号： C07D239/28 , A61K31/505 , A61K31/513 , A61K31/5377 , A61K31/541 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R 2 is hydrogen, halo, hydroxy, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, NO 2 , NR 4 R 5 , CN, or CF 3 ; E is independently O or S; A and B independently are OR 4 or NR 4 R 5 ; R 4 and R 5 independently are H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, (CH2)n aryl, (CH 2 )n cycloalkyl, (CH2)n heteroaryl, or R 4 and R 5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6.
摘要翻译：选择性MMP-13抑制剂是式（I）的嘧啶衍生物或其药学上可接受的盐，其中R 2是氢，卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6烯基， C 6炔基，NO 2，NR 4 R 5，CN或CF 3; E独立地为O或S; A和B分别是OR 4或NR 4 R 5; R 4和R 5独立地是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，（CH 2）n芳基，（CH 2）n环烷基，（CH 2）n杂芳基或R 4 和R 5与它们所连接的氮原子一起形成含有3至8元环的碳原子并且任选地含有选自O，S或NH的杂原子，并且任选地被取代或未取代; n为0〜6。

9. 发明申请

WO1997037987A1 KETOACID ENDOTHELIN ANTAGONISTS 审中-公开
标题翻译： KETOACID内皮素拮抗剂
公开(公告)号：WO1997037987A1
公开(公告)日：1997-10-16
申请号：PCT/US1997003959
申请日：1997-03-12
申请人： WARNER-LAMBERT COMPANY , CHENG, Xue-Min , DOHERTY, Annette, Marian , HURLEY, Timothy, Robert , LOVDAHL, Michael, James , PATT, William, Chester , REPINE, Joseph, Thomas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D317/60
CPC分类号： C07C59/90 , C07D317/60
摘要： Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating acute respiratory distress syndrome (ARDS), atherosclerosis, restenosis, Raynaud's phenomenon, chronic obstructive pulmonary diseases, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, male penile erectile dysfunction, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels or endothelin.
摘要翻译：描述了内皮素I的新型非肽拮抗剂，以及其制备方法及其药物组合物，其可用于治疗急性呼吸窘迫综合征（ARDS），动脉粥样硬化，再狭窄，雷诺现象，慢性阻塞性肺疾病，轻度或严重充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，基本或恶性高血压，肺动脉高压，肺动脉高压旁路后，男性阴茎勃起功能障碍，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗塞或局部缺血，急性或慢性肾衰竭，肾脏缺血，放射性对照诱导的肾毒性，内毒素，败血症，出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生 sia和升高的水平或内皮素。

10. 发明申请

WO1997037986A1 ENDOTHELIN ANTAGONISTS WITH ETHER-LINKED GROUPS 审中-公开
标题翻译：具有以下连接组的内皮素拮抗剂
公开(公告)号：WO1997037986A1
公开(公告)日：1997-10-16
申请号：PCT/US1997003930
申请日：1997-03-12
申请人： WARNER-LAMBERT COMPANY , CHENG, Xue-Min , DOHERTY, Annette Marian , PATT, William, Chester , REPINE, Joseph, Thomas
发明人： WARNER-LAMBERT COMPANY
IPC分类号： C07D307/60
CPC分类号： C07D407/04 , C07D307/60
摘要： Novel nonpeptide endothelin antagonists with ether-linked groups are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, acute respiratory distress syndrome, chronic obstructive pulmonary diseases, male penile erectile dysfunction, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxicity, endotoxic, septic, hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.
摘要翻译：描述了具有醚连接基团的新型非肽内皮素拮抗剂，以及其制备方法及其药物组合物，其可用于治疗动脉粥样硬化，再狭窄，雷诺现象，轻度或严重充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，蛛网膜下腔出血，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，急性呼吸窘迫综合征，慢性阻塞性肺疾病，男性阴茎勃起功能障碍，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗塞或局部缺血，急性或慢性肾衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素，败血症，出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺超血浆和内皮素水平升高。

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