- SUBSTITUTED 1, 6-NAPHTHYRIDINE INHIBITORS OF CDK5
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Disclosed are compounds having structural formula I, and related salts and pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases and conditions such as kidney disease, kidney failure, kidney stones, or polycystic kidney disease, using the compounds of formula (I), and related salts and pharmaceutical compositions.
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Page/Page column 108-109
(2021/04/10)
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- C10-ALKYLENE SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF
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Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13- membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)
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- MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS
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The invention provides compounds of formula (I) or pharmaceutically acceptable salt thereof wherein ring A represents group A-I, A-II or A-III. Al represents -C(R4a)(R4a)-, -C(R4a)= -N(R4b)-, -N= -O- or -S-; A2 represents -C(R4c)(R4c)-, -C(R4c)= or -0-; A3 represents -C(R4c)(R4c)-, -C(R4c)= or -0-; A4 represents -C(R4a)(R4a)-, -C(R4a)= -N= -O- or -S-; A5 represents -C(R4a)(R4a)-, -C(R4a)= -N(R4b)-, -N= -O- or -S-; A6 represents -C(R4c)(R4c)- or -C(R4c)=; A7 represents -C(R4a)(R4a)-, -C(R4a)= -N= -O- or -S-; A8 represents -C(R4a)(R4a)-, -N(R4b)-, -O- or -S-; A9 represents -C(R4c)(R4c)- or -0-; A10 represents -C(R4c)(R4c)- or -0-; A11 represents -C(R4c)(R4c)- or -0-; A12 represents -C(R4a)(R4a)-, -O- or -S-; wherein group A-I, group A-II and group A-III de not contain adjacent oxygen atoms, adjacent oxygen and sulfur atoms or adjacent oxygen and nitrogen atoms or a moiety selected from the group consisting of N-C-N, N-C-S, S-C-S, O-C-N, O-C-O and O-C-S, wherein in each case the carbon atom in the N-C-N, N-C-S, S-C-S, O-C-N, O-C-O and O-C-S moiety is saturated; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a, R4b and R4c are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
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Page/Page column 74
(2019/05/02)
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- MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS
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The invention provides compounds of formula I or pharmaceutically acceptable salt thereof wherein Bl, B2, B3 and B4 represent independently C(R3); X represents -CH(R5)-, -C(R5)= or -(C=0)-, and wherein when X represents -CH(R5)- or -(C=0)- the dotted line represents a single bond, and when X represents -C(R5)= the dotted line represents a double bond; R1 represents independently at each occurrence methy, ethyl, methoxy or ethoxy; R2 represents halogen, cyano, hydroxyl, methyl, ethyl, methoxy, ethoxy, -N(R6a)(R6b) or -methylene- N(R6a)(R6b); R3 represents independently at each occurrence hydrogen, halogen, cyano or methyl; R4a represents methyl or ethyl; R4b represents halogen, Cl-C4alkyl, Cl-C4alkoxy or -0-Cl-C4alkylene-Cycle-Q; R5 represents hydrogen or methyl; R6a represents hydrogen or methyl; R6b represents hydrogen or methyl; Cycle-Q represents independently at each occurrence phenyl optionally substituted by 1 to 3 R7; R7 represents independently at each occurrence cyano, methyl, halomethyl, methoxy or halomethoxy; n is 1 or 2; and q is 0, 1 or 2; as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
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Page/Page column 24; 29
(2019/07/19)
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- MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS
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The invention provides compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof (I) wherein ring A represents group A-I or A- II (A-I, A-II) A1, A2, A3, A4 represent independently C(R4aa) or N, wherein no more than one of A1, A2, A3, and A4 represents N; A5 represents C(R4b) or N; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a and R4aa and R4b are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
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Page/Page column 122-123
(2018/02/03)
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- BENZOPIPERIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND HEMOGLOBINOPATHIES
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A compound of formula I: (I) wherein: n is 1 or 2; p is 0 or 1; R1a, R1b, R1c and R1d are independently selected from H, halo, C1-4 alkyl, C1-4 fluoroalkyl, C3-4 cycloalkyl, C1-4 alkyloxy, NH-C1-4 alkyl and cyano; R2a and R2b are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2c and R2d are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CH2OH; R2e is H or Me; R3a and R3b are independently selected from H and Me; R4 is either H or Me; R5 is either H or Me; R6a and R6b are independently selected from H and Me; A is either (IIa), where R7a is selected from N-linked N-containing C5-7 heterocycyl and (A); or (ii) (IIb), where X is selected from CH2, N H and O, one of R8a and R8b is selected from CI and ethoxy and the other of R8a and R8b is H.
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Page/Page column 55; 56
(2017/09/27)
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- COMPOUNDS AND THEIR USE TO TREAT HISTAMINE H3 RELATED DISORDERS
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The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, m, n, p, q, Q1, Q2, Q3, Q4, Q5, Q6, X1, X2, X3, X4, A1 and L1, are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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Page/Page column 61-62
(2013/03/26)
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- HETEROCYCLIC MGLU5 ANTAGONISTS
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Compounds (I) (R1 is an optionally substituted C1-C13 heteromonocyclic, heterobicyclic or heterotri cyclic group containing from 1 to 5 heteroatoms selected from N, O and S; R2 is H, an optionally substituted mo
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Page/Page column 60-61
(2011/04/18)
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- ETHER BENZYLIDENE PIPERIDINE 5-MEMBERED ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS
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The present invention relates to compounds of the Formula (I), and pharmaceutically acceptable salts thereof, and their use in the treatment of FAAH-mediated diseases or condition.
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Page/Page column 27
(2009/12/02)
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- ETHER BENZYLIDENE PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS
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The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.
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Page/Page column 27
(2009/12/02)
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- NOVEL HETEROCYCLIC DERIVATIVES AS M-GLU5 ANTAGONISTS
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This invention relates to novel heterocyclic compounds having selective affinity for the mGlu5 subtype of metabotropic receptors, pharmaceutical compositions thereof and uses for such compounds and compositions in the treatment of lower urinary tract diso
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Page/Page column 37-38
(2009/03/07)
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- BIARYL ETHER UREA COMPOUNDS
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The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity
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Page/Page column 37
(2008/12/04)
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